HK1186683B - Ophthalmic composition for contact lens - Google Patents

Description

Ophthalmic composition for contact lens

Technical Field

The present invention relates to contact lens compositions that can inhibit bacterial attachment to contact lenses. The invention also relates to methods of inhibiting bacterial attachment to contact lenses. The invention further relates to methods for inhibiting lipid adhesion to contact lenses.

Background

In recent years, the number of people wearing contact lenses has increased. It is necessary to maintain as clean a contact lens as possible for direct contact with the ocular mucosa; therefore, during use, it is important to reduce the attachment of foreign matter such as bacteria. Although many normal (indigenous) bacteria on the conjunctiva are non-pathogenic bacteria; however, bacteria excessively adhere to the contact lens so that extracellular substances and the like secreted by the adhered bacteria form a biofilm on the surface of the contact lens. Biofilms may risk becoming a hotbed for pathogenic microorganisms, increasing the risk of microbial infection.

Contact lenses carrying an antibacterial substance have been reported as a known technique for inhibiting adhesion of bacteria to contact lenses (patent documents 1 and 2). However, from the viewpoint of formulation design of ophthalmic compositions for contact lenses such as eye drops, eye washes, and contact lens care solutions, techniques for inhibiting adhesion of bacteria to contact lenses have not been sufficiently studied.

Polyoxyethylene castor oil is generally used in ophthalmic compositions as a nonionic surfactant to assist dissolution of compounding ingredients (see patent document 3) and is one of effective solubilizing agents.

In order to impart a cooling sensation during administration, terpenoids are used in ophthalmic compositions (see patent document 4).

However, no effect of polyoxyethylated castor oil or terpenoids on bacterial attachment to contact lenses was found; naturally, the effect of the combined use of polyoxyethylated castor oil and terpenoids on bacterial adhesion to contact lenses was also not found.

CITATION LIST

Patent document

Patent document 1: JP2003-248200A

Patent document 2: JP2009-533081A

Patent document 3: JP2005-298448A

Patent document 4: JP2004-315517A

Disclosure of Invention

Problems to be solved by the invention

It is an object of the present invention to provide an ophthalmic composition for a contact lens, which is capable of inhibiting the adhesion of bacteria to the contact lens.

Means for solving the problems

The present inventors have conducted intensive studies in order to solve the above problems. As a result, they have surprisingly found that in an ophthalmic composition for a contact lens comprising a terpenoid together with a polyoxyethylene castor oil, adhesion of bacteria to the contact lens is effectively inhibited. Through further studies by the present inventors, it was unexpectedly found that the combined use of a polyoxyethylene castor oil and a terpenoid compound can inhibit lipid adsorption to a contact lens.

Further studies based on these findings led to the completion of the present invention.

The present invention provides ophthalmic compositions according to the following embodiments.

Item 1 to 1, an ophthalmic composition for a contact lens, comprising (a) a polyoxyethylene castor oil and (B) a terpenoid compound.

Item 1 to 2, the ophthalmic composition for a contact lens according to item 1 to 1, wherein the content of component (a) is 0.01 to 3w/v% relative to the total amount of the ophthalmic composition for a contact lens.

Item 1 to 3, the ophthalmic composition for a contact lens according to item 1 to 1 or 1 to 2, wherein the polyoxyethylene castor oil is a polyoxyethylene castor oil in which an average addition mole number of ethylene oxide is 3 to 60 (for example, polyoxyethylene castor oil 3, polyoxyethylene castor oil 10, polyoxyethylene castor oil 20, polyoxyethylene castor oil 35, polyoxyethylene castor oil 40, polyoxyethylene castor oil 50, and polyoxyethylene castor oil 60).

Item 1 to 4, the ophthalmic composition for a contact lens according to any one of items 1 to 3, wherein component (B) is at least one selected from the group consisting of menthol, camphor, geraniol, borneol and cineole. Item 1 to 5, the ophthalmic composition for a contact lens according to any one of items 1 to 4, wherein the content of component (B) is 0.0001 to 1w/v% with respect to the total amount of the ophthalmic composition for a contact lens.

Item 1 to 6, the ophthalmic composition for a contact lens according to one of items 1 to 5, wherein the total amount of the component (B) is 0.01 to 1,000 parts by weight per 100 parts by weight of the total amount of the component (A).

The ophthalmic composition for a contact lens according to any one of items 1 to 7, which further comprises a buffer.

The ophthalmic composition for a contact lens according to items 1 to 8, wherein the buffer is a boric acid buffer.

Item 1 to 9, the ophthalmic composition for a contact lens according to item 1 to 7 or 1 to 8, wherein the content of the buffer is 0.01 to 10w/v% relative to the total amount of the ophthalmic composition for a contact lens.

The ophthalmic composition for a contact lens according to any one of items 1 to 10, which further comprises a nonionic surfactant other than a polyoxyethylene castor oil.

Item 1 to 11, the ophthalmic composition for a contact lens according to item 1 to 10, wherein the nonionic surfactant other than polyoxyethylene castor oil is at least one selected from the group consisting of a polyoxyethylene sorbitan fatty acid ester, a polyoxyethylene hydrogenated castor oil, and a polyoxyethylene polyoxypropylene block copolymer. Item 1 to 12, the ophthalmic composition for a contact lens according to item 1 to 10 or 1 to 11, wherein the content of the nonionic surfactant other than the polyoxyethylene castor oil is 0.001 to 3w/v% with respect to the total amount of the ophthalmic composition for a contact lens.

The ophthalmic composition for a contact lens according to any one of items 1 to 13, which is an eye drop for a contact lens, according to any one of items 1 to 12.

The ophthalmic composition for a contact lens according to any one of items 1 to 14, which is an eye wash for a contact lens, according to any one of items 1 to 12.

The ophthalmic composition for a contact lens according to any one of items 1 to 15, which is a solution for a contact lens.

The ophthalmic composition for a contact lens according to any one of items 1 to 16, which is a contact lens care solution.

The ophthalmic composition for contact lenses according to any one of items 1 to 17, which is a disinfecting, cleaning and preserving solution for contact lenses.

The ophthalmic composition for a contact lens according to any one of items 1 to 18, 1 to 17, wherein the contact lens is a hard contact lens.

The ophthalmic composition for a contact lens according to any one of items 1 to 19, items 1 to 17, wherein the contact lens is an oxygen permeable hard contact lens.

The ophthalmic composition for a contact lens according to any one of items 1 to 20, 1 to 17, wherein the contact lens is a soft contact lens.

The ophthalmic composition for a contact lens according to any one of items 1 to 21, 1 to 17, wherein the contact lens is a silicone hydrogel contact lens.

According to the following embodiments, the present invention provides a method of inhibiting adhesion of bacteria to a contact lens, a method of imparting an effect of inhibiting adhesion of bacteria to a contact lens, a method of inhibiting adsorption of lipids to a contact lens, a method of imparting an effect of inhibiting adsorption of lipids to a contact lens, and a method of producing an ophthalmic composition for a contact lens.

Item 2, a method for inhibiting bacterial attachment to a contact lens, comprising contacting a contact lens with an ophthalmic composition for a contact lens comprising (a) a polyoxyethylene castor oil and (B) a terpenoid.

Item 3, a method for imparting an effect of inhibiting bacterial adhesion to a contact lens to an ophthalmic composition for a contact lens, comprising adding (a) a polyoxyethylene castor oil and (B) a terpenoid to the ophthalmic composition for a contact lens.

Item 4, a method for inhibiting lipid adsorption to a contact lens, which comprises contacting a contact lens with an ophthalmic composition for a contact lens comprising (a) a polyoxyethylene castor oil and (B) a terpenoid.

Item 5, a method for imparting an effect of inhibiting lipid adsorption to a contact lens to an ophthalmic composition for a contact lens, which comprises adding (a) a polyoxyethylene castor oil and (B) a terpenoid to the ophthalmic composition for a contact lens.

Item 6, a method for producing an ophthalmic composition for contact lenses having an effect of inhibiting bacterial adhesion and/or an effect of inhibiting lipid adsorption to contact lenses, which comprises adding (a) a polyoxyethylene castor oil and (B) a terpenoid compound to a carrier selected from the group consisting of water and hydrous ethanol.

Item 7, the method according to any one of items 2 to 6, wherein the polyoxyethylene castor oil is a polyoxyethylene castor oil having an average addition mole number of ethylene oxide of 3 to 60 (for example, polyoxyethylene castor oil 3, polyoxyethylene castor oil 10, polyoxyethylene castor oil 20, polyoxyethylene castor oil 35, polyoxyethylene castor oil 40, polyoxyethylene castor oil 50, and polyoxyethylene castor oil 60).

Item 8, the method according to any one of items 2 to 7, wherein component (B) is at least one selected from the group consisting of menthol, camphor, geraniol, borneol and cineole.

Item 9, the method according to any one of items 2 to 8, wherein the content of component (B) in the ophthalmic composition for contact lens is 0.0001 to 1w/v% with respect to the total amount of the ophthalmic composition for contact lens.

Item 10, the method according to any one of items 2 to 9, wherein the total amount of the component (B) is 0.01 to 1,000 parts by weight per 100 parts by weight of the total amount of the component (a).

Item 11, the method of any one of items 2 to 10, wherein the ophthalmic composition for a contact lens further comprises a buffer.

Item 12, the method of item 11, wherein the buffer is a boric acid buffer.

Item 13, the method according to item 11 or 12, wherein the amount of buffer in the ophthalmic composition for contact lens is 0.01 to 10w/v% relative to the total amount of the ophthalmic composition for contact lens.

Item 14, the method of any of items 2 to 13, wherein the composition further comprises a nonionic surfactant other than a polyoxyethylated castor oil.

Item 15, the method according to item 14, wherein the nonionic surfactant other than the polyoxyethylene castor oil is at least one selected from the group consisting of a polyoxyethylene sorbitan fatty acid ester, a polyoxyethylene hydrogenated castor oil, and a polyoxyethylene polyoxypropylene block copolymer.

Item 16, the method according to item 14 or 15, wherein the content of the nonionic surfactant other than the polyoxyethylene castor oil in the ophthalmic composition for contact lens is 0.001 to 3w/v% with respect to the total amount of the ophthalmic composition for contact lens.

The method according to any one of items 2 to 16, wherein the ophthalmic composition for a contact lens is an eye drop for a contact lens.

Item 18, the method of any one of items 2 to 16, wherein the ophthalmic composition for a contact lens is an eyewash for a contact lens.

Item 19, the method according to any one of items 2 to 16, wherein the ophthalmic composition for a contact lens is a contact lens wearing solution.

Item 20, the method of any one of items 2 to 16, wherein the ophthalmic composition for a contact lens is a contact lens care solution.

Item 21, the method according to any one of items 2 to 16, wherein the ophthalmic composition for contact lenses is a disinfecting, cleaning and preserving solution for contact lenses.

The method of any of claims 2-21, wherein the contact lens is a hard contact lens.

Item 23, the method of any one of items 2 to 21, wherein the contact lens is an oxygen permeable hard contact lens.

The method of any of claims 2-21, wherein the contact lens is a soft contact lens.

The method of any of claims 2-21, wherein the contact lens is a silicone hydrogel contact lens.

ADVANTAGEOUS EFFECTS OF INVENTION

According to the present invention, the combined use of the polyoxyethylene castor oil and the terpenoid compound can inhibit bacterial adhesion to the contact lens, reducing the risk of bacterial infectious diseases caused by wearing the contact lens. Further, the combined use inhibits the formation of a biofilm formed by extracellular substances or the like secreted from the bacteria; and/or attachment of pathogenic microorganisms produced on biofilms. That is, the present invention can reduce the risk of disease infection by pathogenic microorganisms caused by wearing contact lenses. Accordingly, the present invention provides ophthalmic compositions for contact lenses that allow contact lenses to be used in a safer manner.

The combined use of the polyoxyethylene castor oil and the terpenoid compound can inhibit adsorption of lipids (e.g., lipids derived from in vivo secretions, cosmetics, and the like) to the contact lens and reduce lipid deposits on the lens caused by wearing the contact lens. In addition, the combined use thereof further inhibits discomfort such as blurred vision or a feeling of foreign bodies due to lipid deposits, and development of microorganisms caused by lipid deposits. Accordingly, the present invention provides ophthalmic compositions for contact lenses that allow contact lenses to be used in a safer or more comfortable manner.

Detailed Description

In the present specification, the unit "%" of the content ratio represents w/v%, which is the same as g/100 mL.

In the present specification, the abbreviation "POE" means polyoxyethylene unless otherwise specified.

In the present specification, the abbreviation "POP" means polyoxypropylene unless otherwise specified.

In this specification, unless otherwise indicated, the abbreviation "SCL" refers to soft contact lenses.

1. Ophthalmic composition for contact lens

The ophthalmic composition for a contact lens of the present invention comprises a polyoxyethylene castor oil (hereinafter sometimes referred to as component (a)).

The polyoxyethylene castor oil is a known compound obtained by addition polymerization of ethylene oxide with castor oil, and several polyoxyethylene castor oils different in the average addition mole number of ethylene oxide are known. The average addition mole number of ethylene oxide in the polyoxyethylene castor oil is not particularly limited; however, it is, for example, 3 to 60. Specific examples thereof include polyoxyethylene castor oil 3, polyoxyethylene castor oil 10, polyoxyethylene castor oil 20, polyoxyethylene castor oil 35, polyoxyethylene castor oil 40, polyoxyethylene castor oil 50, and polyoxyethylene castor oil 60.

These polyoxyethylene castor oils may be used alone or in combination of two or more; preferably in a combination of two or more. Note that the polyoxyethylene castor oil used in the present invention is a compound different from and distinguishable from polyoxyethylene hydrogenated castor oil obtained by addition polymerization of ethylene oxide with hydrogenated castor oil.

The content of the component (a) in the ophthalmic composition for contact lenses of the present invention is suitably determined depending on the kind of the component (a), the kind of the component (B) to be used in combination with the component (a), the formulation form of the ophthalmic composition, and the like. For example, the total amount of component (A) is 0.01 to 3w/v%, preferably 0.02 to 2w/v%, more preferably 0.05 to 1w/v%, even more preferably 0.2 to 0.6w/v%, relative to the total amount of the ophthalmic composition for contact lenses.

The above content of component (a) advantageously further increases the effect of inhibiting the adhesion of bacteria to the contact lens, and increases the effect of inhibiting the adsorption of lipids to the contact lens.

The ophthalmic composition of the present invention contains a terpenoid compound (referred to as component (B)) in addition to component (a). Such combined use of components (a) and (B) can significantly inhibit bacterial attachment to the contact lens. The combined use of components (a) and (B) may also significantly inhibit lipid adsorption to the contact lens.

The terpenoid compound used as the component (B) is not particularly limited as long as it is pharmacologically (pharmaceutically) or physiologically acceptable in the medical field. Examples of terpenoids include menthol, camphor, borneol, geraniol, eucalyptol, citronellol, menthone, carvone, anethole, eugenol, limonene, linalool, linear acetate (linear acetate), and derivatives thereof. These compounds may be in the d, l or dl form. An essential oil containing the above compound can be used as the terpenoid in the present invention. Examples of such essential oils include eucalyptus oil, bergamot oil, peppermint oil (peppermint oil), mentha piperita oil (cool mint oil), spearmint oil (spearmint oil), peppermint oil (mint oil), fennel oil, cinnamon oil, rose oil, and the like. For example, when cineole is used as the terpenoid, eucalyptus oil may be used as the source of cineole. These terpenoids may be used alone or in combination of two or more.

Of these components (B), menthol, camphor, geraniol, borneol, eucalyptol and the like advantageously further improve the effect of inhibiting the adhesion of bacteria to the contact lens, and/or the effect of inhibiting the adsorption of lipids to the contact lens. Preferred examples of the essential oil containing the above components include eucalyptus oil, mentha piperita oil, peppermint oil, camphor oil and the like. More preferred are menthol, camphor, geraniol, borneol and cineole, and even more preferred are l-menthol, d-camphor, dl-camphor, d-borneol and cineole.

In order to further increase the inhibitory effect of bacteria adhesion to a contact lens and/or the inhibitory effect of lipid adsorption to a contact lens, the content of component (B) in the ophthalmic composition for contact lens of the present invention is 0.0001 to 1w/v%, preferably 0.001 to 0.1w/v%, more preferably 0.003 to 0.06w/v%, particularly preferably 0.003 to 0.02w/v%, relative to the total amount of the ophthalmic composition for contact lens. When an essential oil containing terpenoids is used as component (B), the total amount of terpenoids in the essential oil to be added is determined to satisfy the above content.

The ratio of component (B) to component (a) in the ophthalmic composition of the present invention is not particularly limited as long as the above content is satisfied. In order to more improve the inhibitory effect of bacteria adhesion to a contact lens and/or the inhibitory effect of lipid adsorption to a contact lens, it is desirable to satisfy the ratio so that the total amount of component (B) is 0.01 to 1,000 parts by weight, preferably 0.1 to 500 parts by weight, more preferably 0.5 to 100 parts by weight, even more preferably 0.5 to 80 parts by weight, particularly preferably 0.5 to 50 parts by weight, and most preferably 1 to 25 parts by weight, per 100 parts by weight of the total amount of component (a).

The ophthalmic compositions for contact lenses of the invention preferably include a buffering agent that can adjust the pH of the ophthalmic compositions of the invention. The buffer that can be contained in the ophthalmic composition for a contact lens of the present invention is not particularly limited as long as it is a pharmacologically (pharmaceutically) or physiologically acceptable buffer in the field of medicine. Examples of such buffers include boric acid buffers, phosphoric acid buffers, carbonic acid buffers, citric acid buffers, acetic acid buffers, aspartic acid and aspartate, and the like. These buffers may be used in combination. Examples of boric acid buffers include boric acid or borates such as alkali metal borates and alkaline earth metal borates. Examples of phosphoric acid buffers include phosphoric acid or phosphates such as alkali metal phosphates and alkaline earth metal phosphates. Examples of carbonic acid buffers include carbonic acid or carbonates such as alkali metal carbonates and alkaline earth metal carbonates. Examples of citric acid buffers include citric acid or alkali metal citrates, and alkaline earth metal citrates, and the like. As the boric acid buffer or phosphoric acid buffer, boric acid hydrate or phosphoric acid hydrate may also be used. More specifically, examples of the boric acid buffer include boric acid or a salt thereof (sodium borate, potassium tetraborate, potassium metaborate, ammonium borate, borax, etc.); examples of the phosphoric acid buffer include phosphoric acid or a salt thereof (disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, trisodium phosphate, dipotassium phosphate, calcium monohydrogen phosphate, calcium dihydrogen phosphate, etc.); examples of the carbonic acid buffer include carbonic acid or salts thereof (sodium bicarbonate, sodium carbonate, ammonium carbonate, potassium carbonate, calcium carbonate, potassium bicarbonate, magnesium carbonate, etc.); examples of the citric acid buffer include citric acid or salts thereof (sodium citrate, potassium citrate, calcium citrate, sodium dihydrogen citrate, disodium citrate, etc.); and examples of the acetic acid buffer include acetic acid or a salt thereof (ammonium acetate, potassium acetate, calcium acetate, sodium acetate, etc.) and aspartic acid or a salt thereof (sodium aspartate, magnesium aspartate, potassium aspartate, etc.). Among the buffers, a boric acid buffer (especially a combination of boric acid and borax) is preferred.

When the ophthalmic composition for a contact lens of the present invention includes a buffer, the content of the buffer cannot be determined uniformly, and varies depending on the kind of the buffer used, the kinds and contents of other components, the formulation form of the ophthalmic composition for a contact lens, and the like. For example, the total amount of the buffer is 0.01 to 10w/v%, preferably 0.05 to 5w/v%, more preferably 0.1 to 2.5w/v%, even more preferably 0.1 to 1w/v%, relative to the total amount of the ophthalmic composition for contact lenses.

The ophthalmic composition for a contact lens of the present invention further comprises a surfactant other than polyoxyethylene castor oil. Such a surfactant is not particularly limited as long as it is pharmacologically (pharmaceutically) or physiologically acceptable in the medical field. The surfactant may be a nonionic surfactant, an amphoteric surfactant, an anionic surfactant, or a cationic surfactant.

Specific examples of the nonionic surfactant that may be contained in the ophthalmic composition for a contact lens of the present invention include POE sorbitan fatty acid esters such as POE (20) sorbitan monolaurate (polysorbate 20), POE (20) sorbitan monopalmitate (polysorbate 40), POE (20) sorbitan monostearate (polysorbate 60), POE (20) sorbitan tristearate (polysorbate 65) and POE (20) sorbitan monooleate (polysorbate 80); POE hydrogenated castor oil such as POE (60) hydrogenated castor oil (polyoxyethylene hydrogenated castor oil 60); POE alkyl ethers such as POE (9) lauryl ether; POE-POP alkyl ethers such as POE (20) POP (4) cetyl ether; polyoxyethylene-polyoxypropylene block copolymers such as POE (196) POP (67) glycol (poloxamer 407 and pluronic F127), and POE (200) POP (70) glycol. In the above-listed compounds, POE means polyoxyethylene, POP means polyoxypropylene, and each number in parentheses indicates the number of moles added. In addition, specific examples of the amphoteric surfactant which may be contained in the ophthalmic composition for a contact lens of the present invention include alkyldiaminoethylglycine or a salt thereof (e.g., hydrochloride).

In addition, specific examples of the cationic surfactant that may be contained in the ophthalmic composition for a contact lens of the present invention include benzalkonium chloride (benzalkonium chloride), benzethonium chloride, and the like.

Specific examples of anionic surfactants that may be included in the ophthalmic composition for a contact lens of the present invention include alkylbenzenesulfonates, alkylsulfates, polyoxyethylene alkylsulfates, aliphatic α -sulfomethyl esters, α -olefin sulfonic acids, and the like. Nonionic surfactants are preferred, and POE sorbitan fatty acid esters, POE hydrogenated castor oil, and POE-POP block copolymers are more preferred. Polysorbate 80, polyoxyethylene hydrogenated castor oil 60 and poloxamer 407 are particularly preferred.

Among these surfactants, nonionic surfactants are preferable.

In the ophthalmic composition for a contact lens of the present invention, the surfactant may be used alone or in combination of two or more.

When the ophthalmic composition for a contact lens of the present invention includes a surfactant, the content of the surfactant may be appropriately determined according to the kind of the surfactant, the kinds and contents of other components, the formulation form of the ophthalmic composition for a contact lens, and the like. As an example of the content of the surfactant, the total amount of the surfactant is 0.001 to 3w/v%, preferably 0.01 to 2w/v%, more preferably 0.05 to 1w/v%, particularly preferably 0.1 to 1w/v%, relative to the total amount of the ophthalmic composition for contact lens.

The ophthalmic composition for a contact lens of the present invention may further include a tonicity agent. The tonicity agent that may be contained in the ophthalmic composition for contact lens of the present invention is not particularly limited as long as it is pharmacologically (pharmaceutically) or physiologically acceptable in the medical field. Examples of tonicity agents include disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate, sodium hydrogen sulfite, sodium sulfite, potassium chloride, calcium chloride, sodium chloride, magnesium chloride, potassium acetate, sodium bicarbonate, sodium carbonate, sodium thiosulfate, magnesium sulfate, glycerin, propylene glycol and the like. Of these tonicity agents, preferable examples include glycerin, propylene glycol, sodium chloride, potassium chloride, calcium chloride and magnesium chloride, more preferable examples include sodium chloride and glycerin, and particularly preferable examples include sodium chloride. These tonicity agents may be used alone or in combination of two or more.

When the ophthalmic composition for a contact lens of the present invention includes a tonicity agent, the content of the tonicity agent cannot be limited, and varies depending on the kind of the tonicity agent used. For example, the total amount of tonicity agent is 0.01 to 10w/v%, preferably 0.05 to 5w/v%, more preferably 0.1 to 3w/v% with respect to the total amount of the ophthalmic composition for contact lenses.

The pH of the ophthalmic composition for a contact lens of the present invention is not particularly limited as long as it is within a pharmacologically (pharmaceutically) or physiologically acceptable range in the field of medicine. The pH of the ophthalmic composition for a contact lens of the present invention is, for example, in the range of 4.0 to 9.5, preferably 5.0 to 9.0, more preferably 6.2 to 8.5, even more preferably 6.5 to 8, and particularly preferably about 6.5 to 7.5.

The osmotic pressure of the ophthalmic composition for a contact lens of the present invention is not particularly limited as long as it is within a range acceptable to the human body. The osmotic pressure ratio of the ophthalmic composition for a contact lens of the present invention is preferably 0.5 to 5.0, more preferably 0.6 to 3.0, and particularly preferably 0.7 to 2.0. The osmotic pressure can be adjusted according to a method known in the art of the present invention using inorganic salts, polyols, sugar alcohols and/or sugars, and the like. The osmotic pressure ratio was a ratio of the osmotic pressure based on the sample of the japanese pharmacopoeia revised at the fifteenth time to 286mOsm (osmotic pressure of a 0.9w/v% sodium chloride aqueous solution). The osmotic pressure can be measured with reference to an osmotic pressure measurement method (freezing point depression method) described in japanese pharmacopoeia. To obtain a standard solution for osmotic pressure ratio measurement (0.9w/v% sodium chloride solution), sodium chloride (standard reagent according to japanese pharmacopoeia) is dried at 500 to 650 ℃ for 40 to 50 minutes, and then allowed to cool in a drying agent (silica gel). 0.900g of the resultant was precisely measured, and then the resultant was dissolved in purified water, thereby accurately preparing 100mL of the solution. Alternatively, a commercially available standard solution for determination of osmotic pressure ratio (0.9w/v% aqueous sodium chloride solution) may be used.

The ophthalmic composition for a contact lens of the present invention may include, in addition to the above components, pharmacologically active components or biologically active components in combination in appropriate amounts as long as the effects of the present invention are obtained. This component is not particularly limited, and examples thereof include effective components in ophthalmic medicines described in Standards for application for the Manufacture (Import) of Non-description Drugs2000(Ippanyou Iyakuhin Seizou (yunyu) Syounin Kizyun2000) edited by Yakuji Shinsa kenkyyukai. Specific examples of the components for ophthalmic drugs include the following components.

Antihistamines such as isoprinine, diphenhydramine hydrochloride, chloroaniline maleate, ketotifen fumarate, and pemirolast potassium.

Decongestants such as tetrahydrozoline hydrochloride, naphazoline sulfate, epinephrine hydrochloride, ephedrine hydrochloride, and methamphetamine hydrochloride.

Disinfectants such as cetylpyridinium, algaecide, benzethonium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate and polyhexamethylene biguanide hydrochloride.

Vitamins such as flavin adenine dinucleotide sodium, cyanocobalamin, retinol acetate, retinol palmitate, pyridoxine hydrochloride, panthenol, calcium pantothenate and tocopheryl acetate.

Amino acids such as potassium aspartate and magnesium aspartate.

Anti-inflammatory agents such as dipotassium glycyrrhizinate, pranoprofen, allantoin, azulene, sodium azulene sulfonate, guaiazulene, berberine hydrochloride, berberine sulfate, lysozyme chloride and licorice.

Others such as cromolyn sodium, sodium chondroitin sulfate, sodium hyaluronate, sulfamethoxazole and sulfamethoxazole sodium.

In addition, various additives may be appropriately selected by a conventional method according to the use, the form of the preparation, and the like, as long as the effect of the present invention is obtained, and added to the ophthalmic composition for contact lens of the present invention. The additives may be used alone or in combination in appropriate amounts. Examples of the additives include those described in the Japanese pharmaceutic Excipients Directory (Japan Pharmaceutical Excipients Directory)2007 (edited by the Japan International pharmaceutic Excipients Council Japan). Representative components include the following additives.

Carrier: for example, aqueous carriers such as water, aqueous ethanol.

Sugar: such as cyclodextrin.

Sugar alcohol: such as xylitol, sorbitol and mannitol. These may be in the d-, l-or dl-form.

Preservatives, disinfectants and antimicrobials: for example, alkyldiaminoethylglycine hydrochloride, sodium benzoate, ethanol, algaecide, benzethonium chloride, chlorhexidine gluconate, chlorobutanol, sorbic acid, potassium sorbate, sodium dehydroacetate, methyl paraben, ethyl paraben, propyl paraben, butyl paraben, hydroxyquinoline sulfate, phenethyl alcohol, benzyl alcohol and Glokill (trade name, Rhodia).

The ophthalmic composition for a contact lens of the present invention can be prepared by a method comprising adding desired amounts of each of component (a) and component (B) and other components if necessary to a carrier in such a manner that these components have desired concentrations. For example, eye drops, contact lens wearing solutions, eye washes, or contact lens care solutions are prepared by dissolving or suspending the above components in purified water, adjusting pH and osmotic pressure to predetermined levels, and subjecting these to sterilization treatment by filtration sterilization or the like. With respect to the dissolution of the components (a) and (B) and the dissolution of the component having high hydrophobicity, a component having an auxiliary dissolution effect such as a surfactant may be added in advance; the mixture is then stirred, after which purified water is added thereto, and subsequently dissolved or suspended.

The dosage form of the ophthalmic composition for contact lens of the present invention is not particularly limited as long as it can be used in the field of ophthalmology. Examples of the dosage form include liquid, paste, and the like. Of these, a liquid is preferable. When the ophthalmic composition for a contact lens of the present invention is in a liquid state, pharmacologically (pharmaceutically) or physiologically acceptable water in the medical field can be used as the aqueous carrier. Examples of the water include distilled water, purified water, sterile purified water, water for injection, distilled water for injection, and the like. These definitions are based on the japanese pharmacopoeia revised at the fifteenth time.

The ophthalmic composition for contact lens of the present invention is not limited in formulation form as long as it is used in the field of ophthalmology. Examples thereof include eye drops for contact lenses (examples of the eye drops include eye drops that can be used while wearing contact lenses), eye washes for contact lenses (examples of the eye washes include those that can be used while wearing contact lenses including eye washes), contact lens wearing liquids, contact lens care liquids (disinfectant liquid for contact lenses, storage liquid for contact lenses, cleaning and storage liquid for contact lenses, and disinfecting, cleaning and storage liquid for contact lenses (multipurpose solution), and the like). Among these, eye drops for contact lenses are particularly preferable as the formulation form of the ophthalmic composition for contact lenses of the present invention.

In the present invention, examples of the contact lens include soft contact lenses, non-aqueous soft contact lenses, hard contact lenses, oxygen permeable hard contact lenses, vision correction contact lenses and non-vision correction contact lenses, and other various types of contact lenses.

In general, a soft contact lens may refer to a hydrated soft contact lens (a lens having a water content of 10% or more according to a vision correction contact lens standard (hereinafter, referred to as a contact lens standard) (Notification No.349of the Ministry of Welfare in2001) (hereinafter, referred to as a hydrated soft contact lens)); however, in the present specification, soft contact lenses include those containing no water (lenses made of a material having a water content of less than 10% and high flexibility according to the contact lens standard) in addition to the above-mentioned soft contact lenses.

Soft contact lenses include both ionic contact lenses and nonionic contact lenses, as well as both contact lenses having a low water content (water content: less than 50%) and contact lenses having a high water content (water content: 50% or more). That is, examples of soft contact lenses include those according to groups I-IV of the SCL classification of the U.S. food and drug administration.

Soft contact lenses include both silicone hydrogel contact lenses (hereinafter SHCL) and non-silicone hydrogel contact lenses (soft contact lenses other than silicone hydrogel lenses). Silicone hydrogel contact lenses include both ionic silicone hydrogel contact lenses and nonionic silicone hydrogel contact lenses.

In particular, bacterial adhesion to contact lenses is likely to occur in soft contact lenses (particularly, hydrated soft contact lenses), and it is strongly desired to inhibit bacterial adhesion to soft contact lenses. Accordingly, as a formulation form of the ophthalmic composition for contact lenses of the present invention, an ophthalmic composition for contact lenses is preferable as an ophthalmic composition for soft contact lenses (that is, a suitable lens is a soft contact lens, particularly, a water-containing soft contact lens).

Examples of soft contact lenses include those comprising, as constituent materials, polymers comprising one or more monomers selected from the group consisting of 2-hydroxyethyl methacrylate (HEMA), 2, 3-dihydroxypropyl methacrylate (i.e., glycerol methacrylate), N-vinyl pyrrolidone, methacrylic acid and its sodium salt, polyvinyl alcohol, N-butyl methacrylate, and N-butyl acrylate as polymeric components.

Furthermore, bacterial attachment and/or lipid adsorption are particularly prone to occur on silicone hydrogel lenses; therefore, it is strongly desired to inhibit bacterial attachment and/or lipid adsorption on silicone hydrogel lenses.

Accordingly, ophthalmic compositions for contact lenses whose target lens is a silicone hydrogel lens are particularly preferred.

In general, hard contact lenses may refer to oxygen-impermeable hard contact lenses; however, in this specification, unless otherwise stated, hard contact lenses include oxygen permeable hard contact lenses in addition to oxygen permeable hard contact lenses.

Examples of hard contact lenses include those comprising, as constituent materials, polymers comprising one or more monomers selected from the group consisting of methyl methacrylate, cellulose acetate butyrate, tris (trimethylsiloxy) silylpropyl methacrylate, pentamethyldisiloxypropyl methacrylate, trifluoroethyl methacrylate, hexafluoroisopropyl methacrylate, and perfluorooctyl ethyl methacrylate as polymeric components.

The "water content" of a contact lens refers to the weight proportion of water contained in the lens relative to the weight of the entire lens.

As the container for containing the ophthalmic composition for a contact lens of the present invention, a container that can be generally used for containing the ophthalmic composition for a contact lens can be used. The container may be made of glass or plastic. When a plastic container is used to contain the ophthalmic composition for a contact lens of the present invention, examples of the constituent material of the plastic container include, but are not limited to, polyethylene naphthalate, polyarylate, polyethylene terephthalate, polypropylene, polyethylene, polyimide, copolymers thereof, and mixtures of two or more thereof. Examples of the copolymer include those containing other polyester units and imide units in addition to any of ethylene 2, 6-naphthalate units, arylate units, ethylene terephthalate units, propylene units, ethylene units, and imide units as a main component. A particularly preferred example thereof is polyethylene terephthalate.

The ophthalmic composition for contact lenses of the present invention inhibits bacterial adhesion to contact lenses, and prevents bacterial infectious diseases of the ocular mucosa. Therefore, the ophthalmic composition for contact lenses of the present invention can be used for preventing bacterial infectious diseases of the ocular mucosa. The ophthalmic composition for contact lenses of the present invention can inhibit lipid adsorption to contact lenses, thereby inhibiting blurred vision and a feeling of foreign bodies due to lipid deposits on contact lenses. Thus, the ophthalmic compositions of the present invention can be used to reduce discomfort during contact lens wear. The lipid inhibited from adsorption is preferably one derived from an in vivo secretion or a cosmetic. Examples of the lipid include simple lipids such as fats and oils (triacylglycerol), waxes (fatty acid esters of higher alcohols), sterol esters, fatty acid esters of vitamins; complex lipids such as glycerophospholipids, sphingophospholipids, glyceroglycolipids, glycosphingolipids, lipids with C-P bonds and sulpholipids; and derivatized lipids such as steroids (e.g., cholesterol), fatty acids, higher alcohols, fat soluble vitamins, and hydrocarbons. In particular, derivatized lipids are preferred, with cholesterol being most preferred.

The ophthalmic composition for a contact lens of the present invention can be used in the same manner as in the conventional ophthalmic composition for a contact lens, depending on the use of the composition and the form of preparation.

Specifically, for example, when the ophthalmic composition for a contact lens of the present invention is used as eye drops for a contact lens, the eye may be dropped during or before wearing the contact lens as with conventional eye drops. When the ophthalmic composition for a contact lens of the present invention is used as an eyewash for a contact lens, the eye may be washed with the ophthalmic composition during or before wearing the contact lens as with a conventional eyewash.

Alternatively, when the ophthalmic composition for contact lenses of the present invention is used as a multi-purpose solution, the contact lenses may be washed, rinsed, and then stored using the ophthalmic composition of the present invention, as with conventional multi-purpose solutions.

During this use period, the contact lens is brought into contact with the ophthalmic composition for a contact lens of the present invention.

2. Method for inhibiting adhesion of bacteria to contact lens, and method for imparting effect of inhibiting adhesion of bacteria to contact lens to ophthalmic composition for contact lens

As described above, the combined use of components (A) and (B) can inhibit bacterial attachment to the contact lens.

Accordingly, from a different perspective, the present invention provides a method of inhibiting bacterial attachment to a contact lens, the method comprising contacting an ophthalmic composition for a contact lens comprising (a) a polyoxyethylene castor oil and (B) a terpenoid with a contact lens.

The present invention also provides a method for imparting an effect of inhibiting bacterial adhesion to a contact lens to an ophthalmic composition for a contact lens, the method comprising adding (a) a polyoxyethylene castor oil and (B) a terpenoid to the ophthalmic composition for a contact lens.

In these methods, the kinds of the component (A) and the component (B), the contents and the ratio thereof, the kinds and the contents of the components other than those described above, the preparation form of the ophthalmic composition for contact lens, the kind of contact lens, the container, the method of embodiment, and the like are used in the same manner as in the above-mentioned "ophthalmic composition for contact lens" section 1.

In particular, these methods are suitably applicable to soft contact lenses, in particular those belonging to group IV. The method is also suitably applicable to silicone hydrogel lenses.

3. Method of inhibiting lipid adsorption to contact lenses and imparting contact lensesMethod for reducing the effect of lipid adsorption to contact lenses with ophthalmic compositions

As described above, the combined use of components (A) and (B) can inhibit bacterial attachment to the contact lens.

Thus, from a different perspective, the present invention provides a method of inhibiting lipid adsorption to a contact lens, the method comprising contacting an ophthalmic composition for a contact lens comprising (a) a polyoxyethylene castor oil and (B) a terpenoid with a contact lens.

The present invention further provides a method for imparting an ophthalmic composition for a contact lens with an effect of inhibiting lipid adsorption to a contact lens, which comprises adding (a) a polyoxyethylene castor oil and (B) a terpenoid to the ophthalmic composition for a contact lens.

In these methods, the types of the component (A) and the component (B), the contents and the ratio thereof, the types and the contents of the components other than those described above, the preparation form of the ophthalmic composition for contact lens, the type of contact lens, the container, the method of application, and the like are the same as or determined in accordance with the above-mentioned "ophthalmic composition for contact lens 1".

In particular, these methods are suitably applicable to hard contact lenses. The method is also suitably applicable to silicone hydrogel lenses.

Examples

The present invention is explained in detail below based on examples; however, the present invention is not limited to these examples.

Experimental example 1: experiment for measuring bacterial adherence to contact lenses (1)

Experimental liquids (examples 1-1 and 1-2, and comparative examples 1-1 to 1-4) having the formulations shown in table 1 were prepared by standard methods, and these liquids were used to evaluate the adhesion of bacteria (Pseudomonas aeruginosa (ATCC9027)) to Soft Contact Lenses (SCLs) (classified according to the us food and drug administration of SCL: group IV; main material: "etafilcon a"). In preparing the test solutions, borax (hereinafter the same) was added in an amount such that the pH of each test solution became 7.

Each lens was immersed in 5mL of sterilized physiological saline for 4 hours or more (lens pretreatment). 1mL of each assay was placed individually in a single well of a 24-well multi-well plate. The water on the surface of each lens was allowed to drain gently at the edge of the plate and the lens was placed in each well. Saline was used as a control (n = 3). After 24 hours, the water from each lens was gently drained at the edge of the plate, and the lenses were placed in a chamber containing 5mL of Pseudomonas aeruginosa liquid (10)⁷To 10⁸CFU/mL) (suspended in physiological saline) in each well of a 12-well multiwell plate. The lenses were stored at room temperature for 30 minutes. Subsequently, each lens was placed in each well of a 6-well plate containing 5mL of physiological saline per well using forceps, and the plate was shaken for one minute. The lenses were transferred to each Spitz tube containing 5mL of additional saline, sonicated (38kHz) for 3 minutes, and then stirred with a tube mixer for one minute. Thereby, bacteria attached to each SCL are removed to form an attached bacterial liquid.

Each of the obtained adherent bacteria solutions was diluted to a concentration suitable for measurement, inoculated in soybean casein digest agar medium (SCDLP agar medium) with lecithin and polysorbate 80, and cultured overnight at 33 ℃. Thereafter, the number of observed colonies was counted, and corrected by the dilution ratio to determine the number of cells (viable cell number) attached to each lens. The inhibition (%) of bacterial adhesion relative to the number of adhered cells obtained using the experimental solution of comparative example 1-1 (control) was calculated according to the following formula.

Mathematical formula 1

Bacterial adhesion inhibition (%) = {1- (number of adhered cells in each test solution/number of adhered cells in each test solution of comparative example 1-1) } × 100

Table 1 shows the results obtained. The use of polyoxyethylene castor oil alone (comparative examples 1-2 and 1-3) tends to show an equal or lower bacterial adhesion inhibition rate (i.e., increased bacterial adhesion) relative to or compared with the control (comparative example 1-1), and does not show a bacterial adhesion inhibition effect. Further, menthol alone (comparative examples 1 to 4) showed little effect of inhibiting bacterial adhesion. In contrast, the combined use of the polyoxyethylene castor oil and menthol (examples 1-1 and 1-2) unexpectedly showed an enhanced excellent bacterial adhesion inhibiting effect as compared with the use of menthol alone.

TABLE 1

Unit (w/v%)

Experimental example 2: experiment for measuring bacterial adherence to contact lenses (2)

Experiments for measuring bacterial adhesion were performed in the same manner as in experimental example 1 using the experimental liquids shown in table 1 (comparative example 1-1) and table 2 (examples 1-3 and 1-4 and comparative examples 1-5 and 1-6). The inhibition rate (%) of bacterial adhesion with respect to the number of adhered cells obtained using the experimental solution of comparative example 1-1 (control) was calculated.

Table 2 shows the results obtained. Compared with the control (comparative example 1-1), camphor alone (comparative example 1-5) or borneol alone (comparative example 1-6) showed little effect of inhibiting bacterial adhesion or showed a more decreased rate of inhibiting bacterial adhesion (increased bacterial adhesion). In contrast, the combined use of the polyoxyethylene castor oil and camphor or borneol (examples 1 to 3 or 1 to 4) unexpectedly showed an excellent bacterial adhesion-inhibiting effect.

TABLE 2

Unit (w/v%)

Reference experiment example 1: experiment for measuring bacterial adherence to contact lenses (3)

Experiments for measuring bacterial adhesion were performed in the same manner as in experimental example 1 using the experimental liquids shown in table 1 (comparative example 1-1) and table 3 (reference examples 1-1 to 1-3). The inhibition rate (%) of bacterial adhesion with respect to the number of adhered cells obtained using the experimental solution of comparative example 1-1 (control) was calculated.

Table 3 shows the results obtained. Although the use of polyoxyethylene hydrogenated castor oil alone (reference example 1-1) showed the bacterial adhesion inhibiting effect, the use of polyoxyethylene hydrogenated castor oil in combination with menthol (reference example 1-2) and the use of polyoxyethylene hydrogenated castor oil in combination with camphor (reference example 1-3) showed more increased bacterial adhesion to contact lenses than reference example 1-1. This indicates that, unlike polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, which is a nonionic surfactant like polyoxyethylene castor oil, does not show an increased bacterial adhesion inhibitory effect when used in combination with terpenoids.

TABLE 3

Unit (w/v%)

The results surprisingly show that, although terpenoids do not always show a bacterial adhesion inhibiting effect and polyoxyethylene castor oil does not show a bacterial adhesion inhibiting effect, the combined use of terpenoids and polyoxyethylene castor oil shows an excellent bacterial adhesion inhibiting effect.

This effect is not obtained when polyoxyethylene hydrogenated castor oil is used instead of polyoxyethylene castor oil.

Experimental example 3: experiment (1) measuring adsorption of lipid to PMMA

The experimental liquids shown in Table 4 (examples 2-1 and 2-2 and comparative examples 2-1 to 2-4) were used to evaluate lipid adsorption to hard contact lenses. As the hard contact lens, a sheet obtained by uniformly cutting a polymethyl methacrylate (PMMA) resin, which is a material of the hard contact lens, into a circular shape is used.

mu.L of each experimental solution (examples 2-1 and 2-2 and comparative examples 2-1 to 2-4) was placed individually in each well of a 24-well microplate, and a piece of PMMA was immersed in each well, followed by shaking at 34 ℃ for 24 hours. After shaking was complete, each PMMA pellet was rinsed in approximately 200mL of physiological saline and transferred to a 24-well microplate containing 1,000 μ L of fluorescent lipid solution per well. Then, shaking was again carried out at 34 ℃ for 24 hours. After 24 hours, the PMMA, which had been subjected to the shaking treatment, was transferred to a plate containing 1mL of another physiological saline, and the fluorescence intensity (excitation wavelength: 485nm, fluorescence wavelength: 538nm) of each well was measured using a fluorescence plate reader. As a fluorescent lipid solution, 4mL2% polysorbate was added to a 500. mu.L mixture of chloroform solution (1mg/mL) and methanol containing fluorescently labeled Lipids (cholesterol, 25-NBD- (powder); non-cholesterol, 25- { N- [ (7-nitro-2, 1, 3-benzoxadiazol-4-yl) -methyl ] amino } -27; both produced by Avanti Polar Lipids, Co., Ltd.) in a 1:4 volume ratio. Stirring was carried out and physiological saline (0.9w/v% sodium chloride) was added to the mixture. Thus, a total of 20mL of the mixture was used.

The lipid adsorption inhibition ratio of each experimental solution with respect to the lipid adsorption amount of the control (comparative example 2-1) was calculated according to the following formula.

Mathematical formula 2

Lipid adsorption inhibition (%) = {1- (fluorescence intensity of each experimental solution/fluorescence intensity of comparative example 2-1) } × 100

Table 4 shows the results. The polyoxyethylene castor oil alone (comparative examples 2-2 and 2-3) showed almost the same or slightly higher lipid adhesion-inhibiting effect as compared with the control (comparative example 2-1); and menthol alone (comparative examples 2-4) significantly reduced the rate of lipid adhesion inhibition (i.e., increased lipid adhesion). In contrast, the combined use of the polyoxyethylene castor oil and menthol (example 2-1 or 2-2) unexpectedly showed an excellent lipid adsorption-inhibiting effect.

TABLE 4

Unit (w/v%)

Reference experiment example 2: measurement of experiment for inhibiting adsorption of lipid to PMMA (2)

Experiments for measuring inhibition of lipid adsorption were performed in the same manner as in experimental example 3 using the experimental liquids shown in table 4 (comparative example 2-1) and table 5 (reference examples 2-1 and 2-2). The lipid adsorption inhibition (%) relative to the lipid adsorption amount of the control (comparative example 2-1) was calculated.

Table 5 shows the results obtained. Although polyoxyethylene hydrogenated castor oil alone (reference example 2-1) showed a lipid adsorption-inhibiting effect, the combined use of polyoxyethylene hydrogenated castor oil and menthol (reference example 2-2) had more lipid adsorption to the contact lens than reference 2-1. This indicates that polyoxyethylene hydrogenated castor oil, which is a nonionic surfactant like polyoxyethylene castor oil, does not show an enhanced lipid adsorption-inhibiting effect when used in combination with terpenoids.

TABLE 5

Unit (w/v%)

	Reference example 2-1	Reference examples 2 to 2
			Polyoxyethylene hydrogenated castor oil 60	0.5	0.5
l-menthol	-	0.015
			Boric acid	0.2	0.2
Borax	Proper amount of	Proper amount of
			Purified water	Balance of	Balance of
Total amount of	100mL	100mL
			pH	7	7
Lipid adsorption inhibition (%)	17.4	10.0

The results surprisingly show that although polyoxyethylene castor oil shows little lipid adhesion inhibiting effect and terpenoid shows increased lipid adhesion, the combined use of polyoxyethylene castor oil and terpenoid shows excellent lipid adhesion inhibiting effect. In contrast, the use of a terpenoid in combination with a polyoxyethylene hydrogenated castor oil used instead of the polyoxyethylene castor oil more reduces the lipid adhesion-inhibiting effect.

Experimental example 4: experiment for measuring bacterial adhesion to contact lens (4)

The experimental solutions shown in tables 6 and 7 (examples 3a-1 to 3a-4 and 3b-1 to 3b-4 and comparative examples 3a and 3b) were prepared according to standard methods. Using these liquids, an experiment for measuring bacterial adhesion to a contact lens was performed in the same manner as in experimental example 1.

Tables 6 and 7 show the results. Examples 3a-1 to 3a-4, which further comprise one or two materials selected from menthol, geraniol and eucalyptus oil in addition to the polyoxyethylene castor oil 10, show significantly higher bacteria attachment inhibiting effects than comparative example 3a, which comprises the polyoxyethylene castor oil 10 alone. Similarly, examples 3b-1 to 3b-5 comprising menthol, geraniol and eucalyptus oil showed significantly higher bacteria attachment inhibiting effects than comparative example 3b comprising polyoxyethylene castor oil 35 alone. As the eucalyptus oil, a product having a eucalyptol content of 80w/v% or more according to the Japanese pharmacopoeia revised at the fifteenth time was used.

The results show that the combined use of a polyoxyethylene castor oil and a terpenoid in an ophthalmic composition for a contact lens shows a remarkably high bacterial adhesion-inhibiting effect.

TABLE 6

Unit (w/v%)

	Comparative example 3a	Example 3a-1	Example 3a-2	Examples 3a to 3	Examples 3a to 4
						Polyoxyethylene Castor oil 10	0.05	0.05	0.05	0.05	0.05
l-menthol	-	0.005	-	-	0.005
						Geraniol	-	-	0.005	-	-
Eucalyptus oil	-	-	-	0.005	0.005
						Polyoxyethylene hydrogenated castor oil 60	0.05	0.05	0.05	0.05	0.05
Boric acid	0.2	0.2	0.2	0.2	0.2
						Borax	Proper amount of	Proper amount of	Proper amount of	Proper amount of	Proper amount of
Purified water (mL)	Balance of	Balance of	Balance of	Balance of	Balance of
						pH	7	7	7	7	7
Bacterial adhesion inhibition (%)	-	13.8	25.9	36.1	26.3

TABLE 7

Unit (w/v%)

Experimental example 5: experiment for measuring bacterial adherence to contact lens (5)

The experimental solutions shown in the following table (examples 3c-1 and 3c-2 and comparative examples 3c-1 and 3c-2) were prepared according to standard methods. Using these test liquids, a test for measuring bacterial adhesion to a contact lens was performed in the same manner as in experimental example 1.

Table 8 shows the results. Example 3c-1, which contained menthol, geraniol, and eucalyptus oil in addition to the polyoxyethylene castor oil 10, showed a significantly higher bacterial adhesion inhibiting effect than comparative example 3c-1, which contained the polyoxyethylene castor oil 10 alone. Similarly, example 3c-2 containing menthol and geraniol in addition to the polyoxyethylene castor oil 10 and the polyoxyethylene castor oil 35 showed a significantly higher bacterial adhesion inhibition effect than comparative example 3c-2 containing only the polyoxyethylene castor oil 10 and the polyoxyethylene castor oil 35.

The results show that the combined use of a polyoxyethylene castor oil and a terpenoid in an ophthalmic composition for a contact lens shows a remarkably high bacterial adhesion-inhibiting effect.

TABLE 8

Unit (w/v%)

Preparation examples

Eye drops for contact lenses (formulation examples 1 to 7), eye washes for contact lenses (formulation example 8), contact lens wearing solutions (formulation example 9), and multi-purpose solutions for contact lenses (formulation example 10) were prepared by standard methods according to the formulations shown in table 9.

The unit of osmotic pressure is mOsm (milliosmoles).

TABLE 9

Claims (21)

1. An ophthalmic composition for a contact lens comprising component a: polyoxyethylene castor oil, and component B: at least one terpenoid selected from the group consisting of menthol, camphor and borneol.

2. The ophthalmic composition for a contact lens according to claim 1, wherein the total content of component B is 0.01 to 1,000 parts by weight per 100 parts by weight of the total amount of component a.

3. The ophthalmic composition for a contact lens according to claim 1, wherein the polyoxyethylene castor oil is a polyoxyethylene castor oil having an average addition mole number of ethylene oxide of 3 to 60.

4. The ophthalmic composition for a contact lens according to claim 1, further comprising a buffer.

5. The ophthalmic composition for a contact lens according to claim 4, wherein the buffer is a boric acid buffer.

6. The ophthalmic composition for a contact lens according to claim 1, further comprising a nonionic surfactant other than a polyoxyethylene castor oil.

7. The ophthalmic composition for a contact lens according to claim 6, wherein the nonionic surfactant other than polyoxyethylene castor oil is at least one selected from the group consisting of polyoxyethylene sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, and polyoxyethylene polyoxypropylene block copolymer.

8. The ophthalmic composition for a contact lens according to claim 2, wherein the polyoxyethylene castor oil is a polyoxyethylene castor oil having an average addition mole number of ethylene oxide of 3 to 60.

9. The ophthalmic composition for a contact lens according to claim 2, further comprising a buffer.

10. The ophthalmic composition for a contact lens according to claim 9, wherein the buffer is a boric acid buffer.

11. The ophthalmic composition for a contact lens according to claim 2, further comprising a nonionic surfactant other than a polyoxyethylene castor oil.

12. The ophthalmic composition for a contact lens according to claim 11, wherein the nonionic surfactant other than polyoxyethylene castor oil is at least one selected from the group consisting of polyoxyethylene sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, and polyoxyethylene polyoxypropylene block copolymer.

13. The ophthalmic composition for a contact lens according to claim 8, further comprising a nonionic surfactant other than a polyoxyethylene castor oil.

14. The ophthalmic composition for a contact lens according to claim 13, further comprising a buffer, and the buffer is a boric acid buffer, and the nonionic surfactant other than polyoxyethylene castor oil is at least one selected from the group consisting of polyoxyethylene sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, and polyoxyethylene polyoxypropylene block copolymer.

15. A method of inhibiting bacterial attachment to a contact lens comprising contacting an ophthalmic composition for a contact lens comprising component a: polyoxyethylene castor oil, and component B: at least one terpenoid selected from the group consisting of menthol, camphor and borneol.

16. The method according to claim 15, wherein the total content of component B is 0.01 to 1,000 parts by weight per 100 parts by weight of the total amount of component a.

17. The method according to claim 15, wherein the polyoxyethylene castor oil is a polyoxyethylene castor oil in which an average addition mole number of ethylene oxide is 3 to 60.

18. The method according to claim 15, said ophthalmic composition further comprising a buffering agent.

19. The method of claim 18, wherein the buffer is a boric acid buffer.

20. The method according to claim 15, said composition further comprising a nonionic surfactant other than a polyoxyethylated castor oil.

21. The method according to claim 20, wherein the nonionic surfactant other than the polyoxyethylene castor oil is at least one selected from the group consisting of polyoxyethylene sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, and polyoxyethylene polyoxypropylene block copolymer.