CN1480128A - Preparation of transparent, cryptomorphic external remedy - Google Patents
Preparation of transparent, cryptomorphic external remedy Download PDFInfo
- Publication number
- CN1480128A CN1480128A CNA031497721A CN03149772A CN1480128A CN 1480128 A CN1480128 A CN 1480128A CN A031497721 A CNA031497721 A CN A031497721A CN 03149772 A CN03149772 A CN 03149772A CN 1480128 A CN1480128 A CN 1480128A
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- liniment
- gel
- mixture
- weight
- active component
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- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000011505 plaster Substances 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 239000013558 reference substance Substances 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 206010040872 skin infection Diseases 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 229920002994 synthetic fiber Polymers 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 201000003875 tinea corporis Diseases 0.000 description 1
- 201000004647 tinea pedis Diseases 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 229960002117 triamcinolone acetonide Drugs 0.000 description 1
- YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 description 1
- 229940070384 ventolin Drugs 0.000 description 1
- 210000002268 wool Anatomy 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
An externally-applied transparent medicine for treating dermatopathy and taking care of skin health contains active medicinal components, filming material (plasticizer and bioadhesive. Its advantages are good adhesion to skin, high rubbing resistance, good air permeability and isolation, and long acting.
Description
Technical field of the present invention
The present invention relates to a kind of transparent, cryptomorphic external medicine preparation---liniment, it has good adhesiveness, wear-resisting wiping and hidden property, particularly a kind of transparent, stealthy gel liniment that comprises effective active component of this topical administration carrier, be used for the treatment of dermatosis, be used for aspects such as health and beauty.
Background technology of the present invention
External medicine preparation can be widely used in fields such as treating skin disease, wound, pain relieving, health and beauty.
Skin infection is common by the caused infectious disease of pathogenic microorganism in people's daily life, has certain infectiousness, as tinea, herpes or the like.Dermopathic healing is avoided self cross infection except reasonable use medicine, prolong drug action time is the key factor that can not be ignored.
Non-infectious dermatosis and skin trauma in Drug therapy, also need ill skin is carried out special protection, as psoriasis and wound, should avoid the friction of skin and locker room, prevent the deterioration of the state of an illness and increase patient's misery.
Externally-used pain-relieving or health care plaster, owing to some the viscose composition that contains causes user allergy, or some breakage, young tender position can't administration.
In above-mentioned treatment and using, all need a kind of safe, non-stimulated, can play with outside good isolation effect, reduce the new formulation of drug loss, prolong drug curative effect, this new formulation also needs to have certain practicality simultaneously, and good adhesiveness, transparent hidden property are promptly arranged.All there are certain shortcoming in external medicine preparation such as preparations such as powder agent, spray, solution, lotion, unguentum, gel, membrane and patch commonly used at present, for example medicine is to the inefficiency of lesions position transmission, can not prevent patient's self cross infection, when patient's normal activity, cause drug loss owing to rubbing, the misery that perhaps adds the heavy patient because of friction is easy to pollute medicated clothing, bedding of patient etc.; And the patch with backing layer may produce allergy even ulcer phenomenon owing to the breathability difference; Wiping not attractive in appearance when membrane is used for exposure portion, not wear-resisting, and these problems of being brought by dosage form also may cause patient's compliance to reduce, thus further reduce therapeutic effect.Therefore, need a kind of topical formulations easy to clean to obtain more effective treatment.
Membrane or the liniment made with macromolecular material appearred in recent years, for example US 5,888,494 A disclose a kind of liniment that contains opioid with filmogen preparation commonly used, but be inconvenient to carry, and this liniment only comprises filmogen commonly used, does not solve film caducous problem and stealthy problem when being subjected to rubbing that liniment forms.The not relevant report that can overcome external preparation above-mentioned defective, that contain required active component in the prior art, thus need a kind of novel, wear-resisting wiping, preparation of not having above-mentioned defective, so that a more effective topical administration system can be provided.
Description of the invention
The objective of the invention is to provide a kind of evident in efficacy, easy to use, market prospect is wide and do not have external preparation---the stealthy liniment of above-mentioned defective.
Though in the prior art relevant for the report of making liniment with macromolecular material, but the present invention finds surprisingly, film former and a kind of bioadhesive polymer are mixed in certain proportion, can obtain a kind of liniment with unexpected effect, this liniment is a gel, in that be coated on the skin can be dry voluntarily after 2-5 minute, form uniform, water white stealthy film and begin to discharge medicine.Its formed this thin film has good cohesive, contractility and wearability, be not in the situation that will deliberately be removed, and it can continue closely to stick on and reaches on the skin about 24 hours.In addition, this liniment can be used for the skin affected part of Any shape and size; This thin film also has good permeability, has the good compatibility with skin, and the patient is in use without any sense of discomfort, and also imperceptible have foreign body to exist; And because this film is water white, so can clearly observe the progression of disease situation in affected part; In case need stop treatment, the formed film of this liniment can be removed from skin easily.Thereby film former and bioadhesive polymer are not used in combination the instruction that obtains after application, can to obtain to have the gelatinous external liniment of good adhesiveness, breathability, water white stealthy film in the prior art.
The formed film of this liniment can also effectively absorb the exudate in affected part, reduces sense of discomfort and can reduce transudate to make the affected part that the danger of ulcer take place.Simultaneously; the formed film of liniment of the present invention can also be protected the skin of lesions position effectively; make it to avoid external pollution and friction stimulation; avoid cross infection; and can keep being capped the moisture of position skin in right amount; thereby soften cuticle increases medicine to the infiltration of skin than the depths focus.
The objective of the invention is to provide a kind of film former of active component, some and external liniment of bioadhesive polymer of comprising, this liniment also preferably comprises the volatile solvent, and can randomly comprise external preparation such as plasticizer, cutaneous permeable agent, antiseptic additive commonly used.
The definition of used among the present invention " bioadhesion " refer to biological or synthetic material adhesion on the skin and/or mucosa of biology, thereby this material can be retained the more normal time thereon.The definition of " bioadhesive polymer " refers to the material with bioadhesive among the present invention.The definition of " stealthy film " refers to a kind of water white film among the present invention.
The present composition contains and accounts for composition total weight 2% to 30% weight, the film former of preferred 5%-15% weight.Employed film former is commonly usedly in the prior art to have an excellent biological compatibility, nontoxic, non-stimulated in the present composition, filmogen with pliability, hygroscopicity and water solublity or fat-soluble characteristics, optional from polyvinyl alcohol (PVA), ethylene-vinyl acetate copolymer (EVA), Pioloform, polyvinyl acetal, methacrylate-methacrylic acid copolymer, hydroxypropyl cellulose, hypromellose, polyvidone or their mixture.The polyvinyl alcohol of preferred various models (PVA) as PVA04-88,04-86,05-88,17-88 or its mixture, more preferably is PVA04-86, PVA17-88 or their mixture.Used various filmogens for example PVA can obtain by commercial sources.
The present composition contains and accounts for composition total weight 0.5%-10% weight, preferred 0.5%-5% weight, the particularly bioadhesive polymer of 0.5-3% weight.Employed bioadhesive polymer is optional from polyacrylic acid, polymethylacrylic acid, cellulose derivative such as carboxymethyl cellulose, methylcellulose, polyvinylpyrrolidone, tragcanth, sodium alginate, HPMC or their mixture in the present composition.Preferred biological safety is good, the polyacrylic acid crosslinked resin that adhesiveness is good.Polyacrylic acid crosslinked resin is a kind of acrylic acid crosslinked resin, the copolymer of particularly poly-alkyl sucrose or poly-alkyl tetramethylolmethane and acrylic crosslinking polymer, carbomer (Carbopol) for example, the present invention can use the carbomer of various models, as carbomer 934,940,910 or its mixture, preferred carbomer 934 and 940.Used various biological adhesives can obtain by commercial sources, and for example carbomer can have been bought with the title of Carbopol from BF Goodrich company.
The present composition preferably contains and accounts for composition total weight 5%-30% weight, the volatile solvent of preferred 10%-30% weight.Employed volatile solvent has for example ethanol, acetone, ethyl acetate, isopropyl alcohol, cyclohexane extraction or their mixture, preferred alcohol, acetone or its mixture in the present composition.
The present composition preferably contains and accounts for composition total weight 1%-20% weight, the plasticizer of preferred 2%-10% weight.Employed plasticizer has for example glycerol, propylene glycol, dibutyl phthalate or its mixture in the present composition, preferably glycerine, propylene glycol or its mixture, be the mixture of glycerol and propylene glycol more preferably, for example it is with 0.5: 1-1: the mixture that 3 ratio forms.
Compositions of the present invention can also randomly comprise antiseptic and/or cutaneous permeable agent, suitable antiseptic has for example methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben, sorbitol, hydroxy benzoate, propyl parabene, a phenyl methylcarbamate or one or more mixture wherein; Suitable cutaneous permeable agent has for example azone, dimethyl sulfoxide, carbamide, propylene glycol or its mixture, preferred dimethyl sulfoxide, azone, propylene glycol, with and composition thereof.The content of antiseptic is about 0.001%-0.5% weight of said composition gross weight.The content of cutaneous permeable agent is about 0.1%-40% weight of said composition gross weight.
Can also comprise adjuvant commonly used in the pharmaceutical preparation prior aries such as pH regulator agent, correctives in the preparation of the present invention so that preparation of the present invention has pleasant fragrance and suitable character such as pH value, the selection of these materials and interpolation are known in all being to those skilled in the art, wherein said pH regulator agent such as sodium hydroxide solution, triethanolamine etc.
Liniment of the present invention can comprise the various dermatosis that are used for the treatment of, analgesic drug product, the active component of aesthetic health care etc., wherein said dermatosis is antibacterial or the caused dermatosis of fungal infection for example, used active component is that the prior art kind is commonly used, for example can be the azole (imidazoles and triazole) of antibiotic as the treatment fungal infection, propylamine, sulfo-amino methyl ester class, the thebaine class, pyrrones, miazines or the like or their mixture, clotrimazole for example, miconazole, ketoconazole, econazole, bifonazole, terbinafine or their mixture, preferred bifonazole and terbinafine.Said active component can also be the tretinoin medicines of for example treating psoriasis, acne: tretinoin, isotretinoin; Hormone such as steroid 17-hydroxy-11-dehydrocorticosterone: triamcinolone acetonide, dexamethasone, Mo Tamisong etc.; Antiviral drugs is as phthiobuzone, ribavirin, acyclovir or their mixture; Anti-inflammatory analgesic class material is as ibuprofen and derivant, diclofenac sodium, naproxen or their mixture.Active component of the present invention can be selected as required by those skilled in the art, can use one or more active component.As required active component and application dose thereof are selected will be apparent to those skilled in the art, can change according to the factors such as the order of severity of treatment disease, this variation also within the scope of the invention.
The amount of contained active component can be selected with reference to clinical dosage commonly used as required in the preparation of the present invention, the amount of active component can selected in very wide scope according to many factors, the character of wherein said factor such as selected active component, the disease of being treated, the application purpose of preparation etc., this selection is known to those skilled in the art, as a reference, the quantity of active component can be 0.0001% to 10% weight of composition weight, preferred 0.005% to 5% weight, the antifungal drug that for example can contain 0.5-10% weight, or the antiviral drugs of 0.1-10% weight.
In one embodiment of the invention, the content of active component is the 1-10% weight of composition total weight in this liniment, the content of filmogen is the 2%-30% weight of composition total weight, and the content of bioadhesive polymer is the 0.5%-10% of composition total weight.In preferred embodiments, the content of filmogen is the 5%-15% weight of composition total weight, and the content of bioadhesive polymer is the 0.5%-5% weight of composition total weight.In another preferred embodiment, the content of active component is 1% weight of composition total weight in this liniment, the content of filmogen is the 10%-15% weight of composition total weight, and the content of bioadhesive polymer is the 0.5%-3% weight of composition total weight.
In embodiment preferred of the present invention, this liniment also contains the plasticizer of the 5%-20% weight that accounts for composition total weight.
In one embodiment of the invention, this liniment contains antiseptic that accounts for composition total weight 0.001%-0.5% weight and/or the cutaneous permeable agent that accounts for composition total weight 0.1%-40% weight.
The present invention also provides a kind of method for preparing described liniment, and it comprises the steps:
(1) filmogen is added water-soluble expanding, place the back of spending the night and in 90 ℃ water-bath, heat swelling, make gel;
(2) bioadhesive polymer is added water-soluble expanding, placement is spent the night, and makes gel;
(3) take by weighing in the active component adding ethanol of requirement, make suspension, add immediately through supersound process
Go in the gel of (1), stir so that its homodisperse;
(4) gel with (2) adds in the gel of (3), stirs rapidly, and mix homogeneously is transferred pH to 4-7,
Obtain transparent or white gels;
This gel is carried out packing with the flexible pipe of required specification to get final product.
The present invention also provides the method for the described liniment of another kind of preparation, and it comprises the steps:
(1) filmogen is added water-soluble expanding, place the back of spending the night and in 90 ℃ water-bath, heat swelling, make gel;
(2) bioadhesive polymer is added water-soluble expanding, placement is spent the night, and makes gel;
(3) take by weighing in the active component adding ethanol of requirement, make suspension, add immediately through supersound process
Go in the gel of (1), stir so that its homodisperse;
(4) in the gel of (3), add plasticizer, mix homogeneously;
(5) gel with (2) adds in the gel of (4), stirs rapidly, and mix homogeneously is transferred pH to 4-7,
Obtain transparent or white gels;
This gel is carried out packing with the flexible pipe of required specification to get final product.
The present invention also provides a kind of method for preparing described liniment, and it comprises the steps:
(2) filmogen is added water-soluble expanding, place the back of spending the night and in 90 ℃ water-bath, heat swelling, make gel;
(3) bioadhesive polymer is added water-soluble expanding, placement is spent the night, and makes gel;
(4) antiseptic is dissolved in the ethanol, gained solution is joined in the gel of (1) mix homogeneously;
(5) take by weighing in the active component adding ethanol of requirement, make suspension, add immediately through supersound process
Go in the gel of (3), stir so that its homodisperse;
(6) in the gel of (4), add plasticizer and/or cutaneous permeable agent, mix homogeneously;
(6) gel with (2) adds in the gel of (5), stirs rapidly, and mix homogeneously is transferred pH to 4-7,
Obtain transparent or white gels;
This gel is carried out packing with the flexible pipe of required specification to get final product.
When using the liniment of the milky gel form of gained evenly is applied in the affected part and gets final product, it is a drying and forming-film after 2-5 minute.
The gained liniment can be preserved with the medicinal flexible pipe packing of different size.
Liniment of the present invention can be used for dermatosis, for example all kinds of tinea, herpes etc.; Fields such as externally applied analgetic, wound, health and beauty.
Now the present invention is further detailed with the following examples.
Embodiment
Embodiment 1
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | Quantity % weight |
| ????PVA04-86 | ????6.7 |
| ????PVA17-88 | ????6.7 |
| Acritamer 940 | ????1 |
| Glycerol | ????3.3 |
| Propylene glycol | ????5 |
| Azone | ????2 |
| Ethyl hydroxybenzoate | ????0.1 |
| Ethanol | ????13 |
| 10% sodium hydroxide | ????1ml |
| Water | ????61.2 |
| Amount to | ????100 |
This liniment can form water white thin film after 2-5 minute, the film forming good toughness of institute's shape has been difficult for the limit, and rub resistance can peel off when specially removing.
The antifungal drug that adds 1%-5% respectively as bifonazole, terbinafine, miconazole nitrate, clotrimazole, is made the antifungal haptogen.
Try out for respectively 10 tinea pedis, tinea corporis patient bifonazole, terbinafine, after medication 1-2 week, the hypertrophy cutin of affected skin has clear improvement with chapping, and 4 weeks were almost recovered.Said preparation has played good focus buffer action, and its hidden property does not affect the appearance simultaneously, has avoided cross infection again, has prolonged the action time of medicine.
Embodiment 2
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | % weight |
| ????PVA05-88 | ????10 |
| Acritamer 940 | ????1 |
| Glycerol | ????3.3 |
| Propylene glycol | ????1 |
| Azone | ????2 |
| Nipagin | ????0.16 |
| Propyl parabene, | ????0.017 |
| Between phenyl methylcarbamate | ????0.086 |
| Ethanol | ????13 |
| Triethanolamine | In right amount, to pH6 |
| Water | ????65.3 |
| Amount to | ????100 |
This liniment can form water white thin film after 2-5 minute, the film forming good toughness of institute's shape has been difficult for the limit, and rub resistance can peel off when specially removing.
By required different purposes, add different types of active medicine, it is carried out packing with flexible pipe.
Embodiment 3
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | % weight |
| ????PVA04-86 | ????5 |
| Carbomer 934 | ????3 |
| Glycerol | ????3 |
| Propylene glycol | ????5 |
| Dimethyl sulfoxide | ????0.6 |
| Carbamide | ????10 |
| Methyl hydroxybenzoate | ????0.1 |
| Propylparaben | ????0.1 |
| 95% ethanol | ????20 |
| Water | In right amount |
By required different purposes, add different types of active medicine, it is carried out packing with flexible pipe.
Obtain having the liniment of above-mentioned character.
Embodiment 4
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | % weight |
| ????PVA04-86 | ????4 |
| ????PVA17-88 | ????4 |
| Carbomer 934 | ????2 |
| Glycerol | ????6 |
| Dimethyl sulfoxide | ????0.4 |
| Parachlorometaxylenol | ????0.05 |
| Triethanolamine | In right amount, to pH6 |
| Ethanol | ????20 |
| Water | In right amount |
Obtain having the liniment of above-mentioned character.Embodiment 5
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | % weight |
| Terbinafine | ????5 |
| ????PVA17-88 | ????5 |
| Acritamer 940 | ????1 |
| Glycerol | ????6 |
| Dimethyl sulfoxide | ????0.4 |
| Ethyl hydroxybenzoate | ????0.1 |
| Triethanolamine | In right amount to pH6 |
| Ethanol | ????26 |
| Water | In right amount |
Obtain having the liniment of above-mentioned character.According to different demands, add required medicine.
Embodiment 6
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
Composition % weight
Bifonazole 1
PVA04-86????????????????1.25
PVA17-88????????????????3.75
Acritamer 940 3
Dimethyl sulfoxide 0.4
Carbamide 5
Sorbic acid 0.2
Triethanolamine is in right amount to pH6
Ethanol 30
Water is an amount of
Obtain having the liniment of above-mentioned character.
Embodiment 7
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | % weight |
| Phthiobuzone | ????1 |
| ????PVA04-86 | ????11.25 |
| ????PVA17-88 | ????3.75 |
| Acritamer 940 | ????2 |
| Dimethyl sulfoxide | ????0.4 |
| Ethyl hydroxybenzoate | ????0.1 |
| Ethanol | ????20 |
| Acetone | ????10 |
| Water | In right amount |
Obtain having the liniment of above-mentioned character.
Embodiment 8
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
Composition % weight
Tretinoin 0.025
PVA124??????????????????10
Acritamer 940 1.5
Dimethyl sulfoxide 0.5
Carbamide 10
Sorbic acid 0.2
Sodium hydroxide is an amount of, to pH6
Ethanol 30
Water is an amount of
Be used for the treatment of psoriasis, can avoid the friction of medicated clothing and diseased region, improve curative effect.Embodiment 9
Prepare a kind of liniment of the present invention by following prescription according to above-mentioned corresponding method.
| Composition | % weight |
| Terbinafine | ????1 |
| ????PVA05-88 | ????3.75 |
| ????PVA17-88 | ????1.25 |
| Acritamer 940 | ????3 |
| Glycerol | ????3.3 |
| Propylene glycol | ????1 |
| Azone | ????2 |
| Nipagin | ????0.16 |
| Propyl parabene, | ????0.017 |
| Ethanol | ????30 |
| Triethanolamine | In right amount, transfer pH to 6 |
| Water | In right amount |
This liniment can form water white thin film after 2-5 minute, the film forming good toughness of institute's shape has been difficult for the limit, and rub resistance can peel off when specially removing.
Embodiment 10
Skin irritation Journal of Sex Research 1. test objectives of stealthy film:
The irritant reaction situation that is produced behind observer's rabbit skin contact test sample.2. test material:
2.1 test sample:
Stealthy film, lot number is 200300311.Main component comprises: carbomer, and glycerol, propylene glycol, PVA, azone, Nipagin ester, ethanol, etc.
2.2 reference substance: medical ventolin.2.3 animal:
Animal strain: new zealand rabbit.
Body weight: 2.0～3.0kg.
Sex: male, totally 6.
Animal identification: adopt thorn to dye overbit identification.
Animal grouping: animal is divided into 2 groups at random, stealthy film and vaseline matched group, 3 every group.3. dosage:
Respectively be coated with 1g stealthy film, vaseline, continuous 7 day to rabbit every day.4. route of administration: skin coating.5. test method:
24hr takes off tame rabbit back vertebra diamond wool with electric clipper the about 50cm of every lateral area before the administration
2" ten " notched cut is done with the sterile surgical cutter by the damaged skin district at epidermis.Respectively the stealthy film of 1g, vaseline 1g are applied to 2 groups, once a day, continuous 7 days.Respectively at removal be subjected to behind the reagent thing 1,24,48,72hr observes and smears recovery situation and the time that the position has or not situation such as erythema and edema and above-mentioned variation.6. observation index:
Local excitation reaction: perusal skin erythema and edema.7. evaluation of result:
Table 1 scoring is pressed in the skin irritation reaction, calculates mean scores, and＜0.5 is nonirritant.
Table 1 skin irritation reaction scoring
The irritant reaction score value
Erythema
No erythema 0
Inadequate visible 1
Moderate erythema 2
Edema
No edema 0
Inadequate visible 1
The cutaneous protuberance profile is known 28. results:
Observe animal skin change intact skin irritant test mean scores every day during the administration:
Blank group: 0.042
Stealthy film group: 0.208
Damaged skin irritant test mean scores:
Blank group: 0
Stealthy film group: 0.3759. conclusion:
Complete and the damaged skin of rabbit contacts vaseline repeatedly, and behind the stealthy film, intact skin stimulus intensity mean scores is respectively 0.042,0.208, and the damaged skin mean scores is respectively 0,0.375.Stealthy film is to rabbit skin nonirritant.
Claims (35)
1. an external preparation composition is characterized in that it comprises the active component of effective drug level, filmogen, bioadhesive polymer.
2. preparation as claimed in claim 1 is characterized in that it is the gel liniment, in that be coated on the skin just can be dry voluntarily after 2-5 minute, form the stealthy film of uniform, water white, wear-resisting wiping and begins to discharge medicine.
3. liniment as claimed in claim 1 or 2 is characterized in that wherein the content of filmogen is the 2%-30% weight of composition total weight, and the content of bioadhesive polymer is the 0.5%-10% weight of composition total weight.
4. liniment as claimed in claim 3, the content that it is characterized in that filmogen are the 5%-15% weight of composition total weight, and the content of bioadhesive polymer is the 0.5%-5% weight of composition total weight.
5. as any described preparation of claim in front, it is characterized in that wherein said filmogen is selected from the group of the polyvinyl alcohol (PVA) that comprises various models, ethylene-vinyl acetate copolymer (EVA), Pioloform, polyvinyl acetal, methacrylate-methacrylic acid copolymer, hydroxypropyl cellulose, hypromellose, polyvidone; And/or said bioadhesive polymer is selected from copolymer, cellulose derivative such as carboxymethyl cellulose, methylcellulose, tragcanth, sodium alginate, HPMC or their mixture of poly-alkyl sucrose or poly-alkyl tetramethylolmethane and acrylic crosslinking polymer.
6. liniment as claimed in claim 5 is characterized in that wherein said filmogen is selected from polyvinyl alcohol or its mixture of various models; And/or said bioadhesive polymer is selected from carbomer 934,940,910 or its mixture.
7. liniment as claimed in claim 6 is characterized in that wherein said filmogen is selected from PVA04-86, PVA05-88, PVA17-88 or its mixture; And/or said bioadhesive polymer is selected from Acritamer 940.
8. liniment as claimed in claim 1 or 2 is characterized in that wherein containing the volatile solvent that accounts for composition total weight 5%-30% weight.
9. liniment as claimed in claim 8 is characterized in that wherein contained volatile solvent is selected from ethanol, acetone, ethyl acetate, isopropyl alcohol, cyclohexane extraction or their mixture.
10. liniment as claimed in claim 1 or 2 is characterized in that it contains the plasticizer that accounts for composition total weight 5%-20%.
11. compositions as claimed in claim 10 is characterized in that wherein said plasticizer is selected from glycerol, propylene glycol, dibutyl phthalate or their mixture.
12. liniment as claimed in claim 1 or 2 is characterized in that it also comprises antiseptic and/or Percutaneous absorption enhancer.
13. liniment as claimed in claim 12 is characterized in that wherein containing the antiseptic that accounts for composition total weight 0.001%-0.5% weight and/or accounts for the cutaneous permeable agent of coating combination gross weight 0.1%-40% weight.
14. liniment as claimed in claim 13, wherein antiseptic is selected from and comprises methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben, sorbic acid, hydroxy benzoate, propyl parabene, a phenyl methylcarbamate or one or more mixture wherein.
15., it is characterized in that wherein said cutaneous permeable agent is selected from azone, dimethyl sulfoxide, carbamide, propylene glycol or their mixture as any described liniment of claim 13-14.
16., but it is characterized in that wherein said active component is selected from the active component of external used medicine as any described liniment of claim in front.
17. liniment as claimed in claim 16, it is characterized in that comprise effective drug level active component be antibiotic.
18. antibiotic as claimed in claim 17 refers to antifungal drug.
19. liniment as claimed in claim 18 is characterized in that wherein said active component is selected from azole (imidazoles and triazole), propylamine, sulfo-amino methyl ester class, thebaine class, pyrrones, pyrimidine active component or their mixture that the treatment dermatosis is used.
20. liniment as claimed in claim 19 is characterized in that wherein said active component is selected from clotrimazole, miconazole, ketoconazole, econazole, bifonazole, terbinafine or their mixture.
21. as antifungal agent substrate concentration as described in the claim 20 is 0.5-10%.
22. liniment as claimed in claim 16, it is characterized in that comprise effective drug level active component be hormone.
23. hormone as claimed in claim 22 refers to the steroid 17-hydroxy-11-dehydrocorticosterone.
24., comprise dexamethasone, fluocinolone acetonide, Mo Tamisong or their mixture as steroid 17-hydroxy-11-dehydrocorticosterone as described in the claim 23.
25. liniment as claimed in claim 16, it is characterized in that comprise effective drug level active component be the retinoid material.
26. retinoid active component as claimed in claim 25 comprises tretinoin and isotretinoin.
27. liniment as claimed in claim 16, it is characterized in that comprise effective drug level active component be antiviral class material.
28., comprise phthiobuzone, ribavirin, acyclovir or their mixture as antiviral drugs as described in the claim 27.
29. as antiviral drug concentration in the liniment as described in the claim 28 is 0.1-10%.
30. liniment as claimed in claim 16, it is characterized in that comprise effective drug level active component be anti-inflammatory analgesic class material.
31., comprise ibuprofen and derivant thereof, diclofenac sodium, naproxen or their mixture as anti-inflammatory analgesic class medicine as described in the claim 30.
32. one kind prepares the method for liniment as claimed in claim 1 or 2, it is characterized in that it comprises following steps:
(1) filmogen is added water-soluble expanding, place the back of spending the night and in 90 ℃ water-bath, heat swelling, make gel;
(2) bioadhesive polymer is added water-soluble expanding, placement is spent the night, and makes gel;
(3) take by weighing in the active medicine adding ethanol of requirement, make suspension, add immediately through supersound process
Go in the gel of (1), stir so that its homodisperse;
(4) gel with (2) adds in the gel of (3), stirs rapidly, and mix homogeneously is transferred pH to 4-7,
Obtain transparent or white gels.
33. one kind prepares the method for liniment as claimed in claim 1 or 2, it is characterized in that it comprises following steps:
(1) filmogen is added water-soluble expanding, place the back of spending the night and in 90 ℃ water-bath, heat swelling, make gel;
(2) bioadhesive polymer is added water-soluble expanding, placement is spent the night, and makes gel;
(3) take by weighing in the active medicine adding ethanol of requirement, make suspension, add immediately through supersound process
Go in the gel of (1), stir so that its homodisperse;
(4) in the gel of (3), add plasticizer, mix homogeneously;
(5) gel with (2) adds in the gel of (4), stirs rapidly, and mix homogeneously is transferred pH to 4-7,
Obtain transparent or white gels.
34. a method for preparing as liniment as described in the claim 19 is characterized in that it comprises following steps:
(1) filmogen is added water-soluble expanding, place the back of spending the night and in 90 ℃ water-bath, heat swelling, make gel;
(2) bioadhesive polymer is added water-soluble expanding, placement is spent the night, and makes gel;
(3) antiseptic is dissolved in the ethanol, gained solution is joined in the gel of (1) mix homogeneously;
(4) take by weighing in the active medicine adding ethanol of requirement, make suspension, add immediately through supersound process
Go in the gel of (3), stir so that its homodisperse;
(5) in the gel of (4), add plasticizer and/or cutaneous permeable agent, mix homogeneously;
(6) gel with (2) adds in the gel of (5), stirs rapidly, and mix homogeneously is transferred pH to 4-7,
Obtain transparent or white gels.
35. a method for preparing as liniment as described in the claim 19 is characterized in that it comprises following steps:
(1) filmogen adds water-soluble expanding, and places the back of spending the night and heat swelling in 90 ℃ water-bath, makes gel;
(2) bioadhesive polymer is added water-soluble expanding, placement is spent the night, and makes gel;
(3) antiseptic is dissolved in the ethanol, gained solution is joined in the gel of (1) mix homogeneously;
(4) take by weighing in the active medicine adding ethanol of requirement,, join (3) immediately through supersound process
Gel in, stir so that its homodisperse;
(5) in the gel of (4), add plasticizer and/or cutaneous permeable agent, mix homogeneously;
(6) gel with (2) adds in the gel of (5), stirs rapidly, and mix homogeneously is transferred pH extremely
4-7 obtains transparent or white gels.
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031497721A CN1480128A (en) | 2003-08-06 | 2003-08-06 | Preparation of transparent, cryptomorphic external remedy |
| CN 200410039087 CN1286459C (en) | 2003-08-06 | 2004-02-02 | Transparaent and disappearing external medicine preparation containing benzotolazo |
| CNB2004100377305A CN1316965C (en) | 2003-08-06 | 2004-05-10 | A transparent and invisible external drug delivery carrier |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031497721A CN1480128A (en) | 2003-08-06 | 2003-08-06 | Preparation of transparent, cryptomorphic external remedy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1480128A true CN1480128A (en) | 2004-03-10 |
Family
ID=34156367
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031497721A Pending CN1480128A (en) | 2003-08-06 | 2003-08-06 | Preparation of transparent, cryptomorphic external remedy |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1480128A (en) |
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101879283A (en) * | 2010-06-13 | 2010-11-10 | 中国人民解放军第三军医大学 | A novel spray film preparation for skin trauma and its preparation method |
| CN102258455A (en) * | 2010-05-28 | 2011-11-30 | 上海市计划生育科学研究所 | A kind of steroid hormone coating agent and preparation method thereof |
| CN102614520A (en) * | 2012-04-24 | 2012-08-01 | 杨定乾 | Composite matrix of water-soluble film coating agent |
| CN105853344A (en) * | 2015-02-09 | 2016-08-17 | 晶化生技医药股份有限公司 | Film-forming gel composition |
| CN105963242A (en) * | 2007-06-11 | 2016-09-28 | 优势医疗公司 | Drug delivery system for the prevention of cerebral vasospasm |
| CN106109473A (en) * | 2016-08-31 | 2016-11-16 | 孙华燕 | A kind of compound vitamin A acid liniment |
| CN106474093A (en) * | 2015-08-27 | 2017-03-08 | 重庆华邦制药有限公司 | Desonide liniment and preparation method thereof |
| CN107184505A (en) * | 2017-05-05 | 2017-09-22 | 浙江省海洋开发研究院 | A kind of natural anti-oxidation face cream and preparation method thereof |
| CN108853103A (en) * | 2018-06-15 | 2018-11-23 | 王建涛 | A kind of antimycotic skin composition containing fukinanolide |
| EP3346998A4 (en) * | 2015-08-17 | 2019-08-28 | Sidmak Laboratories (India) PVT. Ltd. | TOPIC FILM DELIVERY SYSTEM |
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- 2003-08-06 CN CNA031497721A patent/CN1480128A/en active Pending
Cited By (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105963242A (en) * | 2007-06-11 | 2016-09-28 | 优势医疗公司 | Drug delivery system for the prevention of cerebral vasospasm |
| CN102258455B (en) * | 2010-05-28 | 2014-09-17 | 上海市计划生育科学研究所 | A kind of steroid hormone coating agent and preparation method thereof |
| CN102258455A (en) * | 2010-05-28 | 2011-11-30 | 上海市计划生育科学研究所 | A kind of steroid hormone coating agent and preparation method thereof |
| CN101879283B (en) * | 2010-06-13 | 2013-01-02 | 中国人民解放军第三军医大学 | Novel membrane spraying preparation for skin trauma and preparation method |
| CN101879283A (en) * | 2010-06-13 | 2010-11-10 | 中国人民解放军第三军医大学 | A novel spray film preparation for skin trauma and its preparation method |
| CN102614520A (en) * | 2012-04-24 | 2012-08-01 | 杨定乾 | Composite matrix of water-soluble film coating agent |
| CN105853344A (en) * | 2015-02-09 | 2016-08-17 | 晶化生技医药股份有限公司 | Film-forming gel composition |
| CN105853344B (en) * | 2015-02-09 | 2020-06-23 | 晶化生技医药股份有限公司 | Film-forming gel compositions |
| EP3346998A4 (en) * | 2015-08-17 | 2019-08-28 | Sidmak Laboratories (India) PVT. Ltd. | TOPIC FILM DELIVERY SYSTEM |
| CN106474093A (en) * | 2015-08-27 | 2017-03-08 | 重庆华邦制药有限公司 | Desonide liniment and preparation method thereof |
| CN106109473A (en) * | 2016-08-31 | 2016-11-16 | 孙华燕 | A kind of compound vitamin A acid liniment |
| CN107184505A (en) * | 2017-05-05 | 2017-09-22 | 浙江省海洋开发研究院 | A kind of natural anti-oxidation face cream and preparation method thereof |
| CN108853103A (en) * | 2018-06-15 | 2018-11-23 | 王建涛 | A kind of antimycotic skin composition containing fukinanolide |
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