HK1189488A - Topical formulations for the treatment of papillary tubercles, nail diseases and nail care - Google Patents
Topical formulations for the treatment of papillary tubercles, nail diseases and nail care Download PDFInfo
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Description
The present application is a divisional application of Chinese patent application 200510105663.0 entitled "topical formulation for warts, nail diseases, and nail care," filed on 29/9/2005 by Heiyou, Switzerland.
Technical Field
The present invention relates to an anhydrous topical product for the treatment of warts, nail diseases and nail care comprising one or more active ingredients, as a carrier, one or more of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid or undecylenic acid C1-C4Alkyl esters, optionally with physiologically compatible auxiliaries.
The invention also relates to a method for preparing such formulations and to the use thereof.
Background
Warts (Verruca) are caused by viruses, in particular papilloma polyoma vacuolating viruses (Papovaviruses), and are mostly benign hyperplasias of the dermal papilla tissue under the aggregating horny skin called keratin and are not easily penetrated. At least 50 different cutaneous hyper-proliferations are classified as warts and are caused by more than 100 wart viruses, i.e. papilloma viruses. In particular, linear warts are present, which appear as elongated hyperplasias on the face, neck or eyelids. Planar warts appear on the face, back of the hand, neck, or chest. These warts may spread by scratching or shaving. In addition, there are so-called drusen, which are very similar in shape to cauliflower, and appear on the head or neck, or periungual warts, which appear on fingers and hands, and often also appear around the nails. In addition, the more troublesome and troublesome warts that appear on the sole of the foot, called spinous warts, are extremely difficult to treat. The local treatment of wart, nail disease and nail care has no side effect and low treatment cost. The main problem in the removal of warts and the use of topical formulations for nail treatment and nail care is how to allow sufficient amounts of active ingredients and adjuvants to penetrate through the stratum corneum of warts or nails into the deep tissues to be treated in order to remove pathogenic bacteria below the stratum corneum, such as: viral and fungal infections. The existing pathogenic bacteria can be treated by general methods and their symptoms can be eliminated by direct topical treatment. In most cases, however, symptoms may recur after treatment is discontinued. It is known that warts can be treated by some natural methods, but success cannot be truly guaranteed because skin and stratum corneum penetration remains a problem.
Methods have been proposed for improving the therapeutic results by direct topical application of active ingredients, which are used together with so-called carriers, i.e. substances which, in addition to increasing the solubility of the active ingredient, have good permeability through the stratum corneum and the nails and have the ability to transport the active ingredient through the nail tissue. For example: the medicament for the treatment of onychomycosis described in EP-A-0503988 comprises, in addition to the antimycotic active ingredient and the aqueous medium in which the antimycotic agent is at least partially dissolved, at least one hydrophilic substance which promotes the penetration of the antimycotic agent into the nail. In addition to a wide variety of compounds, ethyl lactate is also described as a permeation-promoting substance. The formulations described in EP-A-0503988 are suitable only for cA limited amount of active ingredient, since they only partially dissolve the active ingredient. Furthermore, from the point of view of the water content in the formulation, when hydrolyzable compounds (e.g., ethyl lactate) are used as permeation-promoting substances, stable formulations cannot be prepared because these compounds decompose by hydrolysis during storage.
There is no satisfactory product for topical treatment of nail disease or for topical nail care which contains a carrier which ensures long-term delivery of the desired amount of active ingredient through the cuticle and nail into the nail bed and base.
Disclosure of Invention
Accordingly, the present invention has been made to solve the problems associated with the removal of warts, the topical treatment of nail diseases, and the topical maintenance of nails, and to provide a pharmaceutical and cosmetic care product that can be used for a long period of time.
Accordingly, the present invention has been made to solve the problems associated with the removal of warts, the topical treatment of nail diseases, and the topical maintenance of nails, and to provide a pharmaceutical and cosmetic care product that can be used for a long period of time.
An anhydrous topical product for treating warts, treating nail disease and caring nails in accordance with the present invention comprises the following:
a) one or more active ingredients selected from the group consisting of,
b) c of one or more of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid or undecylenic acid as a carrier1-C4Alkyl esters, and
c) optionally, physiologically compatible adjuvants.
In one embodiment, the topical product is characterized in that it comprises ethyl esters of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid or undecylenic acid as carrier.
In another embodiment, the topical product comprises as the carrier an isopropyl ester of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid, or undecylenic acid.
In one embodiment, the topical product is characterized in that it comprises ethyl lactate as the carrier.
A particularly important product for eliminating warts is a formulation comprising thuja oil.
In one embodiment, the topical product comprises as the active ingredient one or more substances selected from the group consisting of: synthetic or natural antimycotic agents, antibiotics, antibacterials, corticosteroids and trophoblasts.
In another embodiment, the topical product is characterized by comprising one or more of the antimycotic active ingredients selected from the group consisting of: (±) -cis-2, 6-dimethyl-4- [ 2-methyl-3- (p-tert-amyl-phenyl) propyl ] morpholine (amoolfin), Amphotericin (Amphotericin), 6-cyclohexyl-1-hydroxy-4-methyl-2 (1H) -pyridinone (cyclopiropirox), bis-phenyl- (2-chlorophenyl) -1-imidazolylmethane (clotrimazole), l- [2- (2, 4-dichlorophenyl) -2- (4-chlorobenzoyloxy) -ethyl ] -imidazole (econazole (Econazol)), 2, 4-difluoro- α, α -bis (1H-l,2, 4-triazol-l-ylmethyl) benzyl alcohol (fluconazole (Fluconazol)), (viny;) 5-fluorocytosine (Fluctysin)), 7-chloro-trimethoxy-methylspiro- [ benzofuran-cyclohexene ] -dione (Griseofulvin), l- [2, 4-dichloro-beta- (2, 6-dichlorobenzyloxy) -phenethyl ] -imidazole (isoconazole (Isoconazole)), (+ -) -l-sec-butyl-4- {4- [4- (4- { [ (2R, 4S) -2- (2, 4-dichlorophenyl) -2- (1,2, 4-triazol-1-ylmethyl) -1, 3-dioxolan-4-yl ] methoxy } phenyl) -1-piperazinyl ] phenyl } -4, 5-dihydro-1, 2, 4-triazol-5-one (itraconazole)), (±) cis-l-acetyl-4- {4- ([2- (2, 4-dichlorophenyl) -2- (1H-imidazol-l-ylmethyl) -l, 3-dioxolan-4-yl ] methoxy) phenyl } piperazine (ketoconazole (Ketoconazol)), l- [2, 4-dichloro- β - (2, 4-dichlorophenylmethyloxy) -phenethyl ] -imidazole (miconazole (Miconazol)), (E) -N-cinnamyl-N-methyl-1-naphthylmethylamine (Naftifin)), Nystatin (Nystatin), (E) - (6, 6-dimethyl-2-hepten-4-ynyl) -N-methyl-1-naphthylmethylamine (terbinafine (Terbinafin)), 1- [2- { (2-chloro-3-thienyl) methoxy } -2- (2, 4-dichlorophenyl) ethyl ] -1H-imidazole (tioconazole (Tioconazol)), O-2-naphthyl-N-methyl-N- (3-tolyl) -thiocarbamate (tolnafat), α - (2, 4-difluorophenyl) -5-fluoro- β -methyl- α - (1H-1,2, 4-triazol-1-ylmethyl) -4-pyrimidineethanol (voriconazole).
In one embodiment, the topical product is characterized in that it comprises one or more ingredients selected from the group consisting of: tea tree essential oil, lavender oil, thuja oil, neem extract and ABC oil.
In one embodiment, the topical product is characterized in that it comprises one or more of the antibiotic active ingredients selected from the group consisting of: alpha-amino-4-hydroxybenzyl penicillin (Amoxicillin), D- (-) -alpha-aminobenzyl penicillin (Ampicillin), 3-dimethyl-7-oxo-6-phenylacetamido-4-thia-1-azabicyclo- [3.2.0] -heptane-2-carboxylic acid (benzylpenicillin), benzylpenicillin-benzathine, 3-chloro-7-D (2-phenylglycinylamino) -cephalosporanic acid (Cefaclor), 7 beta- [ D-2-amino- (4-hydroxy-phenyl) -acetylamino ] -3-methyl-cephalosporanic acid (Cefadroxil), Cefadroxil (Cefadroxil)), (Ampicillin (ampicilin), and the like, Aminophenyl-acetamido-methyl-cephalosporanic acid (cephalexin), D (-) -p-2-dichloroacetamido-1- (4-nitrophenyl) -1, 3-propanediol (Chloramphenicol, 1-cyclopropyl-6-fluoro-1, 4-dihydro-4-oxo-7- (1-piperazinyl) -3-quinolinecarboxylic acid (Ciprofloxacin)), (Z) - (2R,5R) -3- (2-hydroxyethylidene) -7-oxo-4-oxa-1-azabicyclo [3.2.0] heptane-2-carboxylic acid (Clavulanic acid)), 7-chloro-7-deoxy-lincomycin (Clindamycin)), alpha-hydroxy-2-methyl-cephalosporanic acid (Ciprofloxacin)), alpha-hydroxy-4-oxa-1-azabicyclo [3.2.0] heptane-2-carboxylic acid (Clavulanic acid)), beta-7-chloro-7-deoxy-lincomycin, 6-deoxy-5-hydroxytetracycline (doxycycline), 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7- (l-piperazinyl) -l, 8-naphthyridine-3-carboxylic acid (Enoxacin), erythromycin, 3- (2-chloro-6-fluorophenyl) -5-methyl-4-isoxazolyl-penicillin (Flucloxacillin), Kanamycin (Kanamycin), Lincomycin (Lincomycin), 7-dimethylamino-6-deoxy-6-demethyltetracycline (minocycline), 6- (2-ethoxy-1-naphthamido) -penicillin (nafcillin)), l-ethyl-l, 4-dihydro-7-methyl-4-oxo-l, 8-naphthyridine-3-carboxylic acid (nalidixic acid), Neomycin (Neomycin), l-ethyl-6-fluoro-l, 4-dihydro-4-oxo-7- (l-piperazinyl) -3-quinolinecarboxylic acid (Norfloxacin), (±) -9-fluoro-2, 3-dihydro-3-methyl-10- (4-methyl-1-piperazinyl) -7-oxo-7H-pyrido [ l,2,3-de ] [ l,4] benzoxazine-6-carboxylic acid (Ofloxacin)),), 6- (5-methyl-3-phenyl-4-isoxazolecarboxamido) penicillanic acid (mexazolecillin (Oxacillin)), 6-phenoxyacetylamino-penicillanic acid (phenoxymethylpenicillin) and 4-dimethylamino-octahydro-pentahydroxy-1, 11-dioxo-6-methyl-naphthonaphthalene-2-urea (tetracycline).
In another embodiment, the topical product is characterized in that it comprises one or more of the antimicrobial active ingredients selected from the group consisting of: alkyl benzyl dimethyl ammonium chloride (benzalkonium chloride), N-benzyl-N, N-dimethyl-2- {2- [ p- (1,1,3, 3-tetramethyl butyl) -phenoxy]-ethoxy } -ethylammonium hydroxide (benzethonium chloride), cetyltrimethylammonium hydroxide (Cetrimonium bromide), 1' -hexamethylene-bis- [5- (p-chlorophenyl) -bis-biguanide](Chlorhexidin), N1,N1-decamethylene-bis- (4-aminomethylquinaldinium hydroxide) (clonidine (Dequalinium chloride)), N- (4-chlorophenyl) -N' - (3, 4-dichlorophenyl) urea (triclocarban), 5-chloro-2- (2, 4-dichlorophenoxy) phenol (Triclosan).
In one embodiment, the topical product is characterized in that it comprises one or more of said corticosteroid active ingredients selected from the group consisting of: 9 α -chloro-16 β -methylhydrogenprednisone (Beclomethason), 9-fluoro-l 1 β,17, 21-trihydroxy-16 β -methyl-1, 4-pregnadiene-3, 20-dione (betamethasone), 21-chloro-9-fluoro-11 β, 17-dihydroxy-16 β -methyl-1, 4-pregnadiene-3, 20-dione (clobetamethasone), 17, 21-dihydroxy-pregna-4-ene-3, 11, 20-trione (Cortisone), 11 β,16 α,17 α, 21-tetrahydroxy-1, 4-pregnadiene-3, 20-dione-16, 17-propanone acetal (propyloxyphenone (desonide)), and their use in preparing medicaments, 9-fluoro-l 1 β -17, 21-trihydroxy-16 α -methylpregna-l, 4-diene-3, 20-dione (dexamethasone (dexamethoson)), 9 α,11 β -dichloro-6 α -fluoro-21-hydroxy-16 α,17 α - (isopropylidenedioxy) -pregna-1, 4-diene-3, 20-dione (fluocinonide), 6 α,9 α -difluoro-16 α,17 α -isopropylidenedioxy-corticosterone (fluocinonide)), 6 α,9 α -difluoro-16 α,17 α -isopropylidenedioxy-corticosterone-acetate (fluocinonide)), 6 α -fluoro-11 β, 21-dihydroxy-6 α, 17-isopropylidenedioxy-4-pregnene-3, 20-dione (Fludoraxycortid), 3- (2-chloroethoxy) -9 alpha-fluoro-6-formyl-11 beta, 21-dihydroxy-16 alpha, 17 alpha-isopropylidenedioxy-3, 5-diene-20-one (Formocotal), 21-chloro-9 alpha-fluoro-11 beta-hydroxy-16 alpha, 17 alpha-isopropylidenedioxy-4-pregnene-3, 20-dione (Halcinonide), 17 alpha-hydroxycorticosterone (hydrocortisone), 11 beta, 17, 21-trihydroxy-6 alpha-methyl-1, 4-pregnene-3, 20-diketones (methylprednisolone), 11 β,17, 21-trihydroxy-pregna-1, 4-diene-3, 20-dione (prednisolone (Prednisolon)), 17 α, 21-dihydroxy-pregna-1, 4-diene-3, 11, 20-trione (prednisone (Prednison)), 9-fluoro-16 α -hydroxyhydroprednisolone (triamcinolone), acetonifluorprednisolone-16 α,17 α -acetonide (triamcinonide)).
In one embodiment, the topical product is characterized in that it comprises the trophoblast and anabolic substance L-proline.
In one embodiment, the topical product is characterized in that it comprises the L-proline in combination with one or more nutritive and anabolic substances selected from the group consisting of amino acids, vitamins and minerals.
In another embodiment, said topical product is characterized in that it comprises said L-proline in combination with one or more compounds selected from the group consisting of: lysine, cysteine, gelatin, biotin, panthenol in combination with inorganic or organic calcium, magnesium or zinc compounds as nutrients and anabolic substances.
In one embodiment, the topical product is characterized in that it comprises one or more adjuvants selected from the group consisting of: terpene or terpene-containing oil, alcohol, ketone, fatty acid ester, polyethylene glycol, surfactant, urea, antioxidant and complexing agent.
In another embodiment, the topical product is characterized in that it comprises 0.01 to 20% by weight of one or more active ingredients, 1 to 99.99% by weight of the C of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid or undecylenic acid1-C4Alkyl esters, with from 0 to 98.99% by weight of auxiliaries.
In one embodiment, a method of making the topical product is characterized by uniformly mixing one or more of the C of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid, or undecylenic acid1-C4-alkyl ester and optionally one or more auxiliary agents, then adding one or more active ingredients to the mixture with stirring, optionally dissolving with heating, and continuing stirring until a homogeneous solution is formed.
In another embodiment, a method of preparing said topical product is characterized in that said topical product is prepared by adding other physiologically compatible formulating auxiliaries to said solution.
The invention also relates to the use of said topical product for the preparation of a medicament for the treatment, prevention, post-treatment or supportive treatment of warts, nail diseases and periungual diseases.
The invention further relates to the use of said topical product for nail care.
The invention also further relates to the use of said topical product for the preparation of a medicament for the treatment of fungal infections of hooves, claws and claws of pets and livestock.
Accordingly, the present invention has been made to solve the problems associated with the removal of warts, the topical treatment of nail diseases, and the topical maintenance of nails, and to provide a pharmaceutical and cosmetic care product that can be used for a long period of time.
An anhydrous topical product for treating warts, treating nail disease and caring nails in accordance with the present invention comprises the following:
a) one or more active ingredients selected from the group consisting of,
b) c of one or more of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid or undecylenic acid as a carrier1-C4Alkyl esters, and
c) optionally, physiologically compatible adjuvants.
The anhydrous topical products of the present invention can employ as active ingredients substantially all synthetic and natural substances that can treat warts, nails, and periungual diseases. Nourishing and anabolic substances effective in caring nail can also be used as active ingredients.
Suitable active ingredients that may be included in the products according to the invention are antimycotics (including those of synthetic and natural origin), antibiotics, antibacterials, corticosteroids, trophoblasts and anabolics, and combinations thereof. Specific examples of such active ingredients are:
antimycotic agents and their physiologically compatible salts, such as, for example: (±) -cis-2, 6-dimethyl-4- [ 2-methyl-3- (p-tert-amyl-phenyl) propyl ] morpholine (amoolfin), Amphotericin (Amphotericin), 6-cyclohexyl-1-hydroxy-4-methyl-2 (1H) -pyridinone (cyclopiropirox), bis-phenyl- (2-chlorophenyl) -1-imidazolylmethane (clotrimazole), l- [2- (2, 4-dichlorophenyl) -2- (4-chlorobenzoyloxy) -ethyl ] -imidazole (econazole (Econazol)), 2, 4-difluoro- α, α -bis (1H-l,2, 4-triazol-l-ylmethyl) benzyl alcohol (fluconazole (Fluconazol)), (viny;) 5-fluorocytosine (Fluctysin)), 7-chloro-trimethoxy-methylspiro- [ benzofuran-cyclohexene ] -dione (Griseofulvin), l- [2, 4-dichloro-beta- (2, 6-dichlorobenzyloxy) -phenethyl ] -imidazole (isoconazole (Isoconazole)), (+ -) -l-sec-butyl-4- {4- [4- (4- { [ (2R, 4S) -2- (2, 4-dichlorophenyl) -2- (1,2, 4-triazol-1-ylmethyl) -1, 3-dioxolan-4-yl ] methoxy } phenyl) -1-piperazinyl ] phenyl } -4, 5-dihydro-1, 2, 4-triazol-5-one (itraconazole)), (±) cis-l-acetyl-4- {4- ([2- (2, 4-dichlorophenyl) -2- (1H-imidazol-l-ylmethyl) -l, 3-dioxolan-4-yl ] methoxy) phenyl } piperazine (ketoconazole)), l- [2, 4-dichloro- β - (2, 4-dichlorophenylmethyloxy) -phenethyl ] -imidazole (miconazole)), (E) -N-cinnamyl-N-methyl-1-naphthylmethylamine (Naftifin)), Nystatin (Nystatin), (E) -N- (6, 6-dimethyl-2-hepten-4-ynyl) -N-methyl-1-naphthylmethylamine (terbinafine (Terbinafin)), 1[2- { (2-chloro-3-thienyl) methoxy } -2- (2, 4-dichlorophenyl) ethyl ] -1H-imidazole (tioconazole (Tioconazol)), O-2-naphthyl-N-methyl-N- (3-tolyl) -thiocarbamate (tolnafat), α - (2, 4-difluorophenyl) -5-fluoro- β -methyl- α - (1H-1,2, 4-triazol-1-ylmethyl) -4-pyrimidineethanol (voriconazole).
Natural antimycotics such as, for example: aromatic essential oil and plant extract.
Antibiotics and their physiologically compatible salts, such as, for example: alpha-amino-4-hydroxybenzyl penicillin (Amoxicillin), D- (-) -alpha-aminobenzyl penicillin (Ampicillin), 3-dimethyl-7-oxo-6-phenylacetamido-4-thia-1-azabicyclo- [3.2.0] -heptane-2-carboxylic acid (benzyl penicillin (Ampicillin)), benzyl penicillin-benzathine (benzathine), 3-chloro-7-D (2-phenylglycinylamino) -cephalo-nic acid (Cefaclor), 7 beta- [ D-2-amino- (4-hydroxy-phenyl) -acetamido ] -3-methyl-cephalo-nic acid (Cefadroxil)), (Cefaclor), Aminophenyl-acetamido-methyl-cephalosporanic acid (cephalexin), D (-) -p-2-dichloroacetamido-1- (4-nitrophenyl) -1, 3-propanediol (Chloramphenicol, 1-cyclopropyl-6-fluoro-1, 4-dihydro-4-oxo-7- (1-piperazinyl) -3-quinolinecarboxylic acid (Ciprofloxacin)), (Z) - (2R,5R) -3- (2-hydroxyethylidene) -7-oxo-4-oxa-1-azabicyclo [3.2.0] heptane-2-carboxylic acid (Clavulanic acid)), 7-chloro-7-deoxy-lincomycin (Clindamycin)), alpha-hydroxy-2-methyl-cephalosporanic acid (Ciprofloxacin)), alpha-hydroxy-4-oxa-1-azabicyclo [3.2.0] heptane-2-carboxylic acid (Clavulanic acid)), beta-7-chloro-7-deoxy-lincomycin, 6-deoxy-5-hydroxytetracycline (doxycycline), 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7- (l-piperazinyl) -l, 8-naphthyridine-3-carboxylic acid (Enoxacin), erythromycin, 3- (2-chloro-6-fluorophenyl) -5-methyl-4-isoxazolyl-penicillin (flucloxacin), Kanamycin (Kanamycin), Lincomycin (Lincomycin), 7-dimethylamino-6-deoxy-6-demethyltetracycline (minocycline), 6- (2-ethoxy-1-naphthamido) -penicillin (Nafcillin), l-ethyl-l, 4-dihydro-7-methyl-4-oxo-l, 8-naphthyridine-3-carboxylic acid (Nalidixic acid), Neomycin (Neomycin), l-ethyl-6-fluoro-l, 4-dihydro-4-oxo-7- (l-piperazinyl) -3-quinolinecarboxylic acid (Norfloxacin), (±) -9-fluoro-2, 3-dihydro-3-methyl-10- (4-methyl-1-piperazinyl) -7-oxo-7H-pyrido [ l,2,3-de ] [ l,4] benzoxazine-6-carboxylic acid (Ofloxacin)),), 6- (5-methyl-3-phenyl-4-isoxazolecarboxamido) penicillanic acid (mexazolecillin (oxacilin)), 6-phenoxyacetamido-penicillanic acid (phenoxymethylpenicillin), 4-dimethylamino-octahydro-pentahydroxy-1, 11-dioxo-6-methyl-naphthonaphthalene-2-urea (tetracycline).
Antibacterial agents, such as, for example: alkyl benzyl dimethyl ammonium chloride (Benzalkonium chloride), N-benzyl-N, N-dimethyl-2- {2- [ p- (1,1,3, 3-tetramethylbutyl) -phenoxy]-ethoxy } -ethylammonium hydroxide (benzethonium chloride), cetyltrimethylammonium hydroxide (Cetrimonium bromide), 1' -hexamethylene-bis- [5- (p-chlorophenyl) -bis-guanidide](Chlorhexidin), N1,N1Decamethylene-bis- (4-aminomethylquinaldinium hydroxide) (captopril (Dequalinium chloride)), N- (4-chlorophenyl) -N' - (3, 4-dichlorophenyl) urea (triclocarban (T)riclocarbane)), 5-chloro-2- (2, 4-dichlorophenoxy) phenol (Triclosan).
The salts with which corticosteroids are physiologically compatible, such as, for example: 9 α -chloro-16 β -methylhydrogenprednisone (Beclomethason), 9-fluoro-l 1 β,17, 21-trihydroxy-16 β -methyl-1, 4-pregnadiene-3, 20-dione (betamethasone), 21-chloro-9-fluoro-11 β, 17-dihydroxy-16 β -methyl-1, 4-pregnadiene-3, 20-dione (clobetamethasone), 17, 21-dihydroxy-pregna-4-ene-3, 11, 20-trione (Cortisone), 11 β,16 α,17 α, 21-tetrahydroxy-1, 4-pregnadiene-3, 20-dione-16, 17-propanone acetal (propyloxyphenone (desonide)), and their use in preparing medicaments, 9-fluoro-l 1 β -17, 21-trihydroxy-16 α -methylpregna-l, 4-diene-3, 20-dione (dexamethasone (dexamethoson)), 9 α,11 β -dichloro-6 α -fluoro-21-hydroxy-16 α,17 α - (isopropylidenedioxy) -pregna-1, 4-diene-3, 20-dione (fluocinonide), 6 α,9 α -difluoro-16 α,17 α -isopropylidenedioxy-corticosterone (fluocinonide)), 6 α,9 α -difluoro-16 α,17 α -isopropylidenedioxy-corticosterone-acetate (fluocinonide)), 6 α -fluoro-11 β, 21-dihydroxy-6 α, 17-isopropylidenedioxy-4-pregnene-3, 20-dione (Fludoraxycortid), 3- (2-chloroethoxy) -9 alpha-fluoro-6-formyl-11 beta, 21-dihydroxy-16 alpha, 17 alpha-isopropylidenedioxy-3, 5-diene-20-one (Formocotal), 21-chloro-9 alpha-fluoro-11 beta-hydroxy-16 alpha, 17 alpha-isopropylidenedioxy-4-pregnene-3, 20-dione (Halcinonide), 17 alpha-hydroxycorticosterone (hydrocortisone), 11 beta, 17, 21-trihydroxy-6 alpha-methyl-1, 4-pregnene-3, 20-diketones (methylprednisolone), 11 β,17, 21-trihydroxy-pregna-1, 4-diene-3, 20-dione (prednisolone (Prednisolon)), 17 α, 21-dihydroxy-pregna-1, 4-diene-3, 11, 20-trione (prednisone (Prednison)), 9-fluoro-16 α -hydroxyhydroprednisolone (triamcinolone), acetonifluorprednisolone-16 α,17 α -acetonide (triamcinonide)).
Trophoblasts and anabolics, such as 2-pyrrolidinecarboxylic acid (L-proline). Preferred antimycotic agents according to the invention are bis-phenyl- (2-chlorophenyl) -l-imidazolylmethane (clotrimazole), 1- [2, 4-dichloro- β - (2, 6-dichlorophenylmethyloxy) -phenethyl ] -imidazole (isoconazole)), 2, 4-difluoro- α, α -bis (1H-l,2, 4-triazol-l-ylmethyl) benzyl alcohol (fluconazole (Fluconazol)), (±) -l-sec-butyl-4- {4- [4- (4- { [ (2R, 4S) -2- (2, 4-dichlorophenyl) -2- (l,2, 4-triazol-1-ylmethyl) -1, 3-dioxolan-4-yl ] methoxy } phenyl) -1-piperazinyl ] phenyl } -4, 5-dihydro-l, 2, 4-triazol-5-one (itraconazole)), (±) cis-1-acetyl-4- {4- ([2- (2, 4-dichlorophenyl) -2- (1H-imidazol-1-ylmethyl) -1, 3-dioxolan-4-yl ] methoxy) phenyl } piperazine (ketoconazole (Ketoconazol)), 1- [2, 4-dichloro- β - (2, 4-dichlorobenzyloxy) -phenethyl ] -imidazole (miconazole (Miconazol)), (E) -N- (6, 6-dimethyl-2-hepten-4-ynyl) -N-methyl-1-naphthylmethylamine (terbinafine (Terbinafin)), α - (2, 4-difluorophenyl) -5-fluoro- β -methyl- α - (1H-l,2, 4-triazol-l-ylmethyl) -4-pyrimidineethanol (voriconazole).
Preferred antimycotic agents according to the invention are bis-phenyl- (2-chlorophenyl) -1-imidazolylmethane (clotrimazole)), 1- [2, 4-dichloro- β - (2, 6-dichlorobenzyloxy) -phenethyl ] -imidazole (isoconazole)), (±) -1-sec-butyl-4- {4- [4- (4- { [ (2R, 4S) -2- (2, 4-dichlorophenyl) -2- (l,2, 4-triazol-l-ylmethyl) -1, 3-dioxolan-4-yl ] methoxy } phenyl) -1-piperazinyl ] phenyl } -4, 5-dihydro-l, 2, 4-triazol-5-one (itraconazole), (±) cis-l-acetyl-4- {4- ([2- (2, 4-dichlorophenyl) -2- (1H-imidazol-l-ylmethyl) -1, 3-dioxolan-4-yl ] methoxy) phenyl } piperazine (ketoconazole)).
Preferred natural antimycotic agents are tea tree oil (Melaleuca alternifolia), lavender oil (Lavandula officinalis chaix) and Neem extract (Azadirachta indica). These natural antimycotic agents may be used alone as active ingredients or in combination with other various such active ingredients. Preferred active ingredient combinations are lavender oil, tea tree oil and neem extract, and especially thuja oil for the elimination of warts. Preferred antibacterial agents are, for example: 1, 1' -hexamethylene-bis- [5- (p-chlorophenyl) -biguanide ] (chlorhexidine).
Preferred corticosteroids are 11 β,16 α,17 α, 21-tetrahydroxy-1, 4-pregnadiene-3, 20-dione-16, 17-propanone acetal (prednisolone (desonide)), 9 α,11 β -dichloro-6 α -fluoro-21-hydroxy-16 α,17 α - (isopropylidenedioxy) -pregna-1, 4-diene-3, 20-dione (flulone (fluocinonide)), 6 α,9 α -difluoro-16 α,17 α -isopropylidenedioxy-corticosterone-acetate (fluocinonide)), 6 α -fluoro-11 β, 21-dihydroxy-6 α, 17-isopropylidenedioxy-4-pregnene-3, 20-dione (fludroxycrit), 3- (2-chloroethoxy) -9 α -fluoro-6-formyl-11 β, 21-dihydroxy-16 α,17 α -isopropylidenedioxy-3, 5-dien-20-one (Formocortal), 21-chloro-9 α -fluoro-11 β -hydroxy-16 α,17 α -isopropylidenedioxy-4-pregnene-3, 20-dione (halcinonide), hydroxolone-16 α,17 α -acetonide (triamcinolone acetonide)).
Examples of specific combinations of active ingredients are:
a corticosteroid in combination with an antimycotic, antibiotic or antibacterial agent. Preferred combinations are for example: (±) cis-l-acetyl-4- {4- ([2- (2, 4-dichlorophenyl) -2- (1H-imidazol-l-ylmethyl) -l, 3-dioxolan-4-yl ] methoxy) phenyl } -piperazine (ketoconazole) in combination with 11 β,16 α,17 α, 21-tetrahydroxy-1, 4-pregnadiene-3, 20-dione-16, 17-propanone acetal (Desonid)).
A combination of a synthetic anti-fungal agent and a natural anti-fungal agent. A preferred combination is bis-phenyl- (2-chloro-phenyl) -l-imidazolylmethane (Clotrimazol) in combination with tea tree essential oil.
Combinations of various natural anti-fungal agents. A preferred combination is a combination of lavender Oil, tea tree essential Oil, neem extract (Azadirachta indica) and ABC Oil (Australian Blue Cypress Oil) and Thuja occidentalis Oil.
2-pyrrolidinecarboxylic acid (L-proline) in combination with one or more other nutritive and anabolic substances selected from the group consisting of: amino acids, vitamins and minerals.
Preferred combinations of 2-pyrrolidinecarboxylic acid (L-proline) and one or more nutritive and anabolic substances are (S) -2, 6-diaminohexanoic acid (lysine), (R) -2-amino-3-mercaptopropionic acid (cysteine), gelatin, cis-2- (4-carboxybutyl) -3, 4-ureidotetrahydrothiophene (biotin), (±)2, 4-dihydroxy-N- (3-hydroxypropyl) -3, 3-dimethylbutyric acid (panthenol), D (+) -2, 4-dihydroxy-N- (3-hydroxypropyl) -3, 3-dimethylbutyric acid (panthenol) in combination with an inorganic or organic calcium, magnesium or zinc compound.
L-proline is an anabolic substance particularly suitable for nail anabolism and nail care. L-proline is currently the only component of nail care products that is optional, as an active ingredient comprising cA sulfur-containing amino acid or cA derivative of cA sulfur-containing amino acid (EP-A-0534810).
The above-mentioned substances are hereinafter represented by the corresponding names indicated by the above-mentioned parenthesized names.
C as a vehicle1-C4Alkyl esters include methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, and tert-butyl esters. Polybasic acids: in the esters of malic acid, citric acid and tartaric acid, the ester group contains C1-C4The alkyl groups may be identical or different. The polybasic acids mentioned above may be esterified from all carboxylate groups or from some carboxylate groups. Except for malic acid and tartaric acid di-C1-C4Besides alkyl esters, the corresponding malic acid and monoalkyl tartrate esters can also be used. C of suitable citric acid1-C4Alkyl esters are the corresponding mono-, di-and trialkyl esters. The preferred ester is ethyl ester. Other preferred esters are isopropyl esters. The preferred single compound is ethyl lactate. Other preferred single compounds are diethyl malate and diisopropyl malate.
The topical products of the present invention are formulated with one or more active ingredients in addition to one or more of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid, or mixtures thereof as a carrierC of undecylenic acid1-C4Besides the alkyl esters, physiologically compatible auxiliaries may also be present. Suitable auxiliaries are, for example: terpene or terpene-containing oil, alcohol, ketone, fatty acid ester, polyethylene glycol, surfactant, urea, antioxidant and complexing agent.
Suitable terpenes are acyclic, monocyclic and bicyclic terpenes and oils containing such terpenes. Examples of acyclic terpenes are acyclic terpene hydrocarbons, such as, for example: myrcene, acyclic terpene alcohols, such as, for example: citronellol and geraniol, and acyclic terpene aldehydes and ketones, such as, for example: citral, alpha-ionone and beta-ionone. Examples of monocyclic terpenes are monocyclic terpene hydrocarbons such as, for example: alpha-terpine, gamma-terpine and limonene, monocyclic terpene alcohols, such as, for example: thymol, menthol, eucalyptol and carvacrol, and monocyclic terpene ketones, such as, for example: menthone and carvone. Examples of bicyclic terpenes are carane terpenes such as, for example: carone, pinane terpenes such as, for example: alpha-pinene and beta-pinene, and bornane terpenes, such as, for example: camphor and borneol. Particularly suitable terpenes are monocyclic terpene alcohols, such as, for example: thymol and menthol. Examples of suitable terpene-containing oils are peppermint oil, myristyl oil, geranium oil, rose essential oil, thuja oil, and balm oil. Particularly suitable oils are peppermint oil, lavender oil and lily oil. As mentioned above, Thuja occidentalis oil is particularly suitable for eliminating warts.
Suitable alcohols are branched or unbranched alcohols having 1 to 3 hydroxyl groups and 2 to 6 carbon atoms, where the hydroxyl groups may be partially or completely etherified or esterified. Particularly suitable alcohols are ethanol, 1-propanol, 2-propanol (isopropanol), 1, 2-propanediol (propylene glycol), 2-phenylethanol (phenylethanol), 1-butanol (butanol), ethylene glycol monomethyl ether (methoxyethanol), ethylene glycol monophenyl ether (phenoxyethanol), 1,2, 3-trihydroxypropane (glycerol), ethyl acetate, butyl acetate, diacetin (diacetin) and triacetin (triacetin).
Examples of suitable ketones are acetone and methyl ethyl ketone (2-butanone).
The fatty acid esters are esters of saturated and unsaturated, branched and unbranched fatty acids having from 8 to 21 carbon atoms, the alcohol component of which comprises branched and unbranched alcohols having from 1 to 6 carbon atoms. Particularly suitable fatty acid esters are isopropyl tridecanoate, isopropyl myristate (isopropyl myristate), methyl pentadecanoate and glycerol mono-9-octadecenoate (glycerol monooleate).
Suitable polyethylene glycols are, for example: polyethylene glycol 400.
Suitable surfactants are, for example: a nonionic surfactant component. Particularly suitable surfactants are partial fatty acid esters of sorbitan (Span), partial fatty acid esters of polyoxyethylene sorbitan (Tween), fatty acid esters of polyoxyethylene (Myrj) and fatty alcohol ethers of polyoxyethylene (Brij).
Suitable antioxidants are, for example: butylated Hydroxytoluene (BHT), butyl-4-methoxyphenol (BHA), tocopherol and ascorbic acid.
Suitable complexing agents are, for example: ethylenediaminetetraacetic acid (EDTA) and disodium ethylenediaminetetraacetate (Na)2-ETDA)。
Topical products according to the invention may be presented, for example: solutions, tinctures, lotions, gels, ointments, creams and pastes. The preferred topical administration form is a solution.
The invention also relates to a process for the preparation of the topical product according to the invention, characterized in that ethyl lactate is homogeneously mixed with one or more adjuvants, and then one or more active ingredients are added to the mixture with stirring, optionally with heating (up to 80 ℃), and stirring is continued until a homogeneous solution is obtained. The resulting solution is preferably used directly for topical application. However, the solution may also be converted into another form for topical administration by adding other physiologically compatible formulation auxiliaries, using known dissolving, mixing and suspending methods.
The topical products of the present invention are preferably used in the form of a solution. Preferred topical products according to the invention comprise:
0.01 to 20% by weight of one or more active ingredients,
1 to 99.99 wt.% of one or more C's of lactic acid, malic acid, tartaric acid or citric acid1-C4Alkyl esters with
0 to 98.99% by weight of one or more physiologically compatible auxiliaries.
The invention also relates to the use of the topical products according to the invention for the treatment, prophylaxis, aftertreatment or supportive treatment of warts, nail diseases and periungual diseases, and for nail care. In addition, the invention relates to the use of the product according to the invention for the treatment of fungal infections of hooves, claws and claws of domestic animals and pets.
For example, topical products containing antimycotics are suitable for the following diseases:
-the treatment, prevention and aftertreatment of onychomycosis caused by dermatophytes, yeasts or moulds or mixed infections,
-the treatment, prevention and aftertreatment of ungual fungal infections in psoriasis, diabetes or AIDS patients,
supportive treatment of periungual nail infections such as, for example: candida (Candidaparonychium).
For example, topical products containing antibiotics are suitable for diseases such as:
supportive treatment and/or prevention of bacterially induced nail-and periungual infections.
For example, topical products containing antimicrobial agents are suitable for use in, for example, the following conditions:
-treatment and prevention of nail and periungual infections caused by non-specific or unidentified pathogenic bacteria.
Topical products, for example containing corticosteroids or combinations of corticosteroids with antimycotics, antibiotics or antibacterials, are suitable for diseases such as:
-the treatment, prevention, post-treatment or supportive treatment of warts, nail-psoriasis or other inflamed nail-and periungual diseases.
The topical pharmaceutical product of the present invention is suitable for treating warts, finger and toe nail diseases and periungual diseases, and can treat hoof, claw and claw diseases of pets and livestock. The frequency of administration of the pharmaceutical product depends on the extent and location of the disease. Usually 1 to 3 applications per day are sufficient. The solution can be applied directly to the affected part of the nail, or to the hoof, claw or claw, and if desired, to the skin surrounding the affected part. The therapy should be continued for about 2 weeks after the symptoms have been eliminated to prevent recurrence.
The topical cosmetic products according to the invention comprising one or more nourishing and anabolic substances are suitable for caring nails, such as, for example: atrophy of nails of fingers and toes. Nail atrophy includes, for example: brittle, cracked and thin nails, and blotchy spots or streaky white spots. The formulation is applied to the unaesthetic nail and may be applied to the surrounding skin as desired. The frequency of administration of the formulation varies depending on the extent and location of atrophy. Generally, 1-2 applications per day are sufficient.
The topical product of the present invention has the advantage that it allows the active ingredient to enter the affected area of the nail within a few days and to act on the nail bed and nail roots. Treatment of nail diseases is usually completed after about 2 to 3 months, by a more rapid onset of action and its improved penetration. In this way it is clear that patient compliance is improved as it greatly shortens the long treatment time required for other procedures. On the affected part of the skin, especially the periungual skin, the healing process and maintenance effect are faster, because the active ingredients can be fully and rapidly infiltrated into the skin. Nail care is typically performed for one month. The nail care product can be used for a long time if the healthy nail is to be maintained.
Detailed Description
The following examples illustrate the invention:
example 1:
urea was added to 20 ml of ethyl lactate with stirring, and dissolved in a 100 ml flask by heating (about 50 ℃ C.). Clotrimazole (Clotrimazol) was added to the above solution with stirring, followed by addition of ethyl lactate to 100 ml. Stirring was continued until a homogeneous solution was formed.
Example 2:
2.0 percent of thuja occidentalis oil
98.0 percent of ethyl lactate
Example 3:
2.0 percent of thuja occidentalis oil
Tea tree essential oil 1.0%
2.0 percent of lactic acid
95.0 percent of ethyl lactate
Example 4:
2.0 percent of thuja occidentalis oil
2.0 percent of salicylic acid
96.0 percent of malic acid ethyl ester
Example 5:
ciclopirox olamine 8.0%
(Ciclopiroxolamin)
92.0 percent of ethyl lactate
Example 6:
ethanol 5.0%
Undecylenic acid 10.0%
85.0 percent of methyl citrate
Example 7:
2.0 percent of lavender oil
Undecylenic acid 10.0%
88.0 percent of ethyl lactate
Example 8:
urea was added to 20 ml of ethyl lactate with stirring, and dissolved in a 100 ml flask by heating (about 50 ℃ C.). Clotrimazole (Clotrimazol) and tea tree essential oil were added to the above solution with stirring, followed by addition of ethyl lactate to 100 ml. Stirring was continued until a homogeneous solution was formed.
Example 9:
all the materials were weighed into a beaker and stirred until a homogeneous solution was formed.
Example 10:
the mixture was stirred until a homogeneous solution formed.
Example 11:
proline-solution 1.5%
L-proline 1.5 g
Propylene glycol 65.0 g
Ethyl lactate 33.5 g
L-proline was added to propylene glycol with stirring and dissolved by heating. Finally, ethyl lactate is added, and stirring is continued until a uniform solution is formed.
Example 12:
l-proline 2.0 g
Diethyl malate 93.0 g
Isopropanol 5.0 g
L-proline was added to diethyl malate with stirring and stirring was continued until complete dissolution.
Example 13:
the following table shows the compositions according to the invention using 50.0 g each of the hydroxycarboxylic acids-C according to the invention1-C4Alkyl esters as carrier and 1.0 g each of active ingredient. The composition is prepared by adding the active ingredient to the hydroxycarboxylic acid ester with stirring at room temperature or slightly elevated temperature (about 30 ℃ to 50 ℃). Depending on the active ingredient, a ready-to-use solution is formed after stirring for 1 to 5 hours.
| Active ingredient | Esters of hydroxycarboxylic acids |
| Clotrimazole (Clotrimazol) | Lactic acid ethyl ester |
| Isoconazole (Isoconazol) | Lactic acid ethyl ester |
| Ketoconazole (Ketoconazol) | Lactic acid ethyl ester |
| Itraconazole (Itraconazol) | Lactic acid ethyl ester |
| Clotrimazole (Clotrimazol) | Citric acid triethyl ester |
| Isoconazole (Isoconazol) | Citric acid triethyl ester |
| Ketoconazole (Ketoconazol) | Citric acid triethyl ester |
| Itraconazole (Itraconazol) | Citric acid triethyl ester |
| Clotrimazole (Clotrimazol) | Diisopropyl malate |
| Isoconazole (Isoconazol) | Diisopropyl malate |
| Ketoconazole (Ketoconazol) | Diisopropyl malate |
| Itraconazole (Itraconazol) | Diisopropyl malate |
Example 14:
the following table shows further compositions according to the invention, using 88.0 g each of hydroxycarboxylic acids-C according to the invention1-C4-alkyl esters as a carrier and 12.0 g of active ingredient combination consisting of 5 g lavender oil, 5 g tea tree essential oil and 2 g neem extract. The compositions are prepared by adding the active ingredient to the individual hydroxycarboxylic acid esters employed with stirring at room temperature. The resulting composition is ready for use.
Claims (19)
1. Use of a topical product for the manufacture of a medicament for the treatment of warts, wherein said topical product comprises
a) One or more active ingredients selected from the group consisting of,
b) c of one or more of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid or undecylenic acid as a carrier1-C4-an alkyl ester, and
c) optionally, physiologically compatible adjuvants.
2. Use according to claim 1, characterized in that said topical product comprises said carrier selected from the group consisting of ethyl esters of lactic, malic, tartaric, citric, undecanoic or undecylenic acid.
3. Use according to claim 1, wherein said topical product comprises said carrier selected from the group consisting of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid, and isopropyl esters of undecylenic acid.
4. Use according to claim 1 or 2, characterized in that the carrier comprised by the topical product is ethyl lactate.
5. Use according to any one of claims 1 to 3, characterized in that the carrier comprised by the topical product is methyl undecanoate or methyl undecylenate.
6. Use according to any one of claims 1 to 3, wherein the topical product comprises diethyl malate as the carrier.
7. Use as claimed in claim 1, characterized in that said topical product comprises as said active ingredient one or more substances selected from the group consisting of: synthetic or natural antimycotic agents, antibiotics, antibacterials, corticosteroids and trophoblasts.
8. The use as claimed in claim 1, characterized in that said topical product comprises one or more of said antimycotic active ingredients selected from the group consisting of: (±) -cis-2, 6-dimethyl-4- [ 2-methyl-3- (p-tert-amyl-phenyl) propyl ] morpholine (amoolfin), Amphotericin (Amphotericin), 6-cyclohexyl-1-hydroxy-4-methyl-2 (1H) -pyridinone (cyclopiropirox), bis-phenyl- (2-chlorophenyl) -1-imidazolylmethane (clotrimazole), l- [2- (2, 4-dichlorophenyl) -2- (4-chlorobenzoyloxy) -ethyl ] -imidazole (econazole (Econazol)), 2, 4-difluoro- α, α -bis (1H-l,2, 4-triazol-l-ylmethyl) benzyl alcohol (fluconazole (Fluconazol)), (viny;) 5-fluorocytosine (Fluctysin)), 7-chloro-trimethoxy-methylspiro- [ benzofuran-cyclohexene ] -dione (Griseofulvin), l- [2, 4-dichloro-beta- (2, 6-dichlorobenzyloxy) -phenethyl ] -imidazole (isoconazole (Isoconazole)), (+ -) -l-sec-butyl-4- {4- [4- (4- { [ (2R, 4S) -2- (2, 4-dichlorophenyl) -2- (1,2, 4-triazol-1-ylmethyl) -1, 3-dioxolan-4-yl ] methoxy } phenyl) -1-piperazinyl ] phenyl } -4, 5-dihydro-1, 2, 4-triazol-5-one (itraconazole)), (±) cis-l-acetyl-4- {4- ([2- (2, 4-dichlorophenyl) -2- (1H-imidazol-l-ylmethyl) -l, 3-dioxolan-4-yl ] methoxy) phenyl } piperazine (ketoconazole (Ketoconazol)), l- [2, 4-dichloro- β - (2, 4-dichlorophenylmethyloxy) -phenethyl ] -imidazole (miconazole (Miconazol)), (E) -N-cinnamyl-N-methyl-1-naphthylmethylamine (Naftifin)), Nystatin (Nystatin), (E) - (6, 6-dimethyl-2-hepten-4-ynyl) -N-methyl-1-naphthylmethylamine (terbinafine (Terbinafin)), 1- [2- { (2-chloro-3-thienyl) methoxy } -2- (2, 4-dichlorophenyl) ethyl ] -1H-imidazole (tioconazole (Tioconazol)), O-2-naphthyl-N-methyl-N- (3-tolyl) -thiocarbamate (tolnafat), α - (2, 4-difluorophenyl) -5-fluoro- β -methyl- α - (1H-1,2, 4-triazol-1-ylmethyl) -4-pyrimidineethanol (voriconazole).
9. The use as claimed in claim 1, characterized in that said topical product comprises one or more ingredients selected from: tea tree essential oil, lavender oil, thuja oil, neem extract and ABC oil.
10. Use as claimed in claim 1, characterized in that said topical product comprises one or more of said antibacterial or said antimycotic active ingredients selected from the group consisting of thuja oil and ABC oil.
11. Use according to claim 1, wherein said topical product comprises one or more of said antibiotic active ingredients selected from the group consisting of: alpha-amino-4-hydroxybenzyl penicillin (Amoxicillin), D- (-) -alpha-aminobenzyl penicillin (Ampicillin), 3-dimethyl-7-oxo-6-phenylacetamido-4-thia-1-azabicyclo- [3.2.0] -heptane-2-carboxylic acid (benzylpenicillin), benzylpenicillin-benzathine, 3-chloro-7-D (2-phenylglycinylamino) -cephalosporanic acid (Cefaclor), 7 beta- [ D-2-amino- (4-hydroxy-phenyl) -acetylamino ] -3-methyl-cephalosporanic acid (Cefadroxil), Cefadroxil (Cefadroxil)), (Ampicillin (ampicilin), and the like, Aminophenyl-acetamido-methyl-cephalosporanic acid (cephalexin), D (-) -p-2-dichloroacetamido-1- (4-nitrophenyl) -1, 3-propanediol (Chloramphenicol, 1-cyclopropyl-6-fluoro-1, 4-dihydro-4-oxo-7- (1-piperazinyl) -3-quinolinecarboxylic acid (Ciprofloxacin)), (Z) - (2R,5R) -3- (2-hydroxyethylidene) -7-oxo-4-oxa-1-azabicyclo [3.2.0] heptane-2-carboxylic acid (Clavulanic acid)), 7-chloro-7-deoxy-lincomycin (Clindamycin)), alpha-hydroxy-2-methyl-cephalosporanic acid (Ciprofloxacin)), alpha-hydroxy-4-oxa-1-azabicyclo [3.2.0] heptane-2-carboxylic acid (Clavulanic acid)), beta-7-chloro-7-deoxy-lincomycin, 6-deoxy-5-hydroxytetracycline (doxycycline), 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7- (l-piperazinyl) -l, 8-naphthyridine-3-carboxylic acid (Enoxacin), erythromycin, 3- (2-chloro-6-fluorophenyl) -5-methyl-4-isoxazolyl-penicillin (Flucloxacillin), Kanamycin (Kanamycin), Lincomycin (Lincomycin), 7-dimethylamino-6-deoxy-6-demethyltetracycline (minocycline), 6- (2-ethoxy-1-naphthamido) -penicillin (nafcillin)), l-ethyl-l, 4-dihydro-7-methyl-4-oxo-l, 8-naphthyridine-3-carboxylic acid (nalidixic acid), Neomycin (Neomycin), l-ethyl-6-fluoro-l, 4-dihydro-4-oxo-7- (l-piperazinyl) -3-quinolinecarboxylic acid (Norfloxacin), (±) -9-fluoro-2, 3-dihydro-3-methyl-10- (4-methyl-1-piperazinyl) -7-oxo-7H-pyrido [ l,2,3-de ] [ l,4] benzoxazine-6-carboxylic acid (Ofloxacin)),), 6- (5-methyl-3-phenyl-4-isoxazolecarboxamido) penicillanic acid (mexazolecillin (Oxacillin)), 6-phenoxyacetylamino-penicillanic acid (phenoxymethylpenicillin) and 4-dimethylamino-octahydro-pentahydroxy-1, 11-dioxo-6-methyl-naphthonaphthalene-2-urea (tetracycline).
12. Use as claimed in claim 1, characterized in that said topical product comprises one or more of said antibacterial active ingredients selected from the group consisting of: alkyl benzyl dimethyl ammonium chloride (benzalkonium chloride), N-benzyl-N, N-dimethyl-2- {2- [ p- (1,1,3, 3-tetramethyl butyl) -phenoxy]-ethoxy } -ethylammonium hydroxide (benzethonium chloride), cetyltrimethylammonium hydroxide (Cetrimonium bromide), 1' -hexamethylene-bis- [5- (p-chlorophenyl) -bis-biguanide](Chlorhexidin), N1,N1-decamethylene-bis- (4-aminomethylquinaldinium hydroxide) (clonidine (Dequalinium chloride)), N- (4-chlorophenyl) -N' - (3, 4-dichlorophenyl) urea (triclocarban), 5-chloro-2- (2, 4-dichlorophenoxy) phenol (Triclosan).
13. Use according to claim 1, wherein the topical product comprises one or more of said corticosteroid active ingredients selected from the group consisting of: 9 α -chloro-16 β -methylhydrogenprednisone (Beclomethason), 9-fluoro-l 1 β,17, 21-trihydroxy-16 β -methyl-1, 4-pregnadiene-3, 20-dione (betamethasone), 21-chloro-9-fluoro-11 β, 17-dihydroxy-16 β -methyl-1, 4-pregnadiene-3, 20-dione (clobetamethasone), 17, 21-dihydroxy-pregna-4-ene-3, 11, 20-trione (Cortisone), 11 β,16 α,17 α, 21-tetrahydroxy-1, 4-pregnadiene-3, 20-dione-16, 17-propanone acetal (propyloxyphenone (desonide)), and their use in preparing medicaments, 9-fluoro-l 1 β -17, 21-trihydroxy-16 α -methylpregna-l, 4-diene-3, 20-dione (dexamethasone (dexamethoson)), 9 α,11 β -dichloro-6 α -fluoro-21-hydroxy-16 α,17 α - (isopropylidenedioxy) -pregna-1, 4-diene-3, 20-dione (fluocinonide), 6 α,9 α -difluoro-16 α,17 α -isopropylidenedioxy-corticosterone (fluocinonide)), 6 α,9 α -difluoro-16 α,17 α -isopropylidenedioxy-corticosterone-acetate (fluocinonide)), 6 α -fluoro-11 β, 21-dihydroxy-6 α, 17-isopropylidenedioxy-4-pregnene-3, 20-dione (Fludoraxycortid), 3- (2-chloroethoxy) -9 alpha-fluoro-6-formyl-11 beta, 21-dihydroxy-16 alpha, 17 alpha-isopropylidenedioxy-3, 5-diene-20-one (Formocotal), 21-chloro-9 alpha-fluoro-11 beta-hydroxy-16 alpha, 17 alpha-isopropylidenedioxy-4-pregnene-3, 20-dione (Halcinonide), 17 alpha-hydroxycorticosterone (hydrocortisone), 11 beta, 17, 21-trihydroxy-6 alpha-methyl-1, 4-pregnene-3, 20-diketones (methylprednisolone), 11 β,17, 21-trihydroxy-pregna-1, 4-diene-3, 20-dione (prednisolone (Prednisolon)), 17 α, 21-dihydroxy-pregna-1, 4-diene-3, 11, 20-trione (prednisone (Prednison)), 9-fluoro-16 α -hydroxyhydroprednisolone (triamcinolone), acetonifluorprednisolone-16 α,17 α -acetonide (triamcinonide)).
14. The use as claimed in claim 1, characterized in that said topical product comprises the substance L-proline, a nutrient and an anabolic substance.
15. The use as claimed in claim 1, characterized in that said topical product comprises said L-proline in combination with one or more nutritive and anabolic substances selected from the group consisting of amino acids, vitamins and minerals.
16. Use as claimed in claim 1, characterized in that said topical product comprises said L-proline in combination with one or more substances selected from: lysine, cysteine, gelatin, biotin, panthenol in combination with inorganic or organic calcium, magnesium or zinc compounds as nutrients and anabolic substances.
17. The use as claimed in claim 1, characterized in that the topical product comprises one or more adjuvants selected from the group consisting of: terpene or terpene-containing oil, alcohol, ketone, fatty acid ester, polyethylene glycol, surfactant, urea, antioxidant and complexing agent.
18. Use according to claim 1, characterized in that the topical product comprises 0.01 to 20% by weight of one or more active ingredients, 1 to 99.99% by weight of the C of lactic acid, malic acid, tartaric acid, citric acid, undecanoic acid or undecylenic acid1-C4Alkyl esters, with from 0 to 98.99% by weight of auxiliaries.
19. Use of the topical product in the use of claim 1 in the manufacture of a medicament for the treatment of hoof, claw and claw mold infections in pets and livestock.
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HK1189488A true HK1189488A (en) | 2014-06-13 |
Family
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