CN105456182A - Topical cream for treating fungal infection and production method thereof - Google Patents
Topical cream for treating fungal infection and production method thereof Download PDFInfo
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- CN105456182A CN105456182A CN201510892966.5A CN201510892966A CN105456182A CN 105456182 A CN105456182 A CN 105456182A CN 201510892966 A CN201510892966 A CN 201510892966A CN 105456182 A CN105456182 A CN 105456182A
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- fungal infection
- agent
- skin
- emulsifiable paste
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- 206010017533 Fungal infection Diseases 0.000 title claims abstract description 28
- 208000031888 Mycoses Diseases 0.000 title claims abstract description 28
- 238000004519 manufacturing process Methods 0.000 title claims abstract description 7
- 229940100611 topical cream Drugs 0.000 title abstract 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 29
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims abstract description 18
- XMAYWYJOQHXEEK-OZXSUGGESA-N (2R,4S)-ketoconazole Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2C=NC=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 XMAYWYJOQHXEEK-OZXSUGGESA-N 0.000 claims abstract description 16
- 229960004125 ketoconazole Drugs 0.000 claims abstract description 16
- CBGUOGMQLZIXBE-XGQKBEPLSA-N clobetasol propionate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CCl)(OC(=O)CC)[C@@]1(C)C[C@@H]2O CBGUOGMQLZIXBE-XGQKBEPLSA-N 0.000 claims abstract description 15
- 229960004703 clobetasol propionate Drugs 0.000 claims abstract description 15
- 238000002360 preparation method Methods 0.000 claims abstract description 14
- 239000003755 preservative agent Substances 0.000 claims abstract description 13
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical compound CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 claims abstract description 12
- 239000003963 antioxidant agent Substances 0.000 claims abstract description 11
- 230000003078 antioxidant effect Effects 0.000 claims abstract description 11
- 235000006708 antioxidants Nutrition 0.000 claims abstract description 11
- 235000021355 Stearic acid Nutrition 0.000 claims abstract description 10
- 229940101006 anhydrous sodium sulfite Drugs 0.000 claims abstract description 10
- 229940082500 cetostearyl alcohol Drugs 0.000 claims abstract description 10
- 239000003995 emulsifying agent Substances 0.000 claims abstract description 10
- 229940057995 liquid paraffin Drugs 0.000 claims abstract description 10
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims abstract description 10
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims abstract description 10
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims abstract description 10
- 239000008213 purified water Substances 0.000 claims abstract description 10
- GEHJYWRUCIMESM-UHFFFAOYSA-L sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 claims abstract description 10
- 239000008117 stearic acid Substances 0.000 claims abstract description 10
- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 claims abstract description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 10
- 229930003427 Vitamin E Natural products 0.000 claims abstract description 9
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims abstract description 9
- 235000019165 vitamin E Nutrition 0.000 claims abstract description 9
- 229940046009 vitamin E Drugs 0.000 claims abstract description 9
- 239000011709 vitamin E Substances 0.000 claims abstract description 9
- 239000003961 penetration enhancing agent Substances 0.000 claims abstract description 7
- 229960004274 stearic acid Drugs 0.000 claims abstract description 6
- 239000002562 thickening agent Substances 0.000 claims abstract description 6
- 238000003756 stirring Methods 0.000 claims description 25
- 239000012071 phase Substances 0.000 claims description 17
- 239000008346 aqueous phase Substances 0.000 claims description 15
- 238000011282 treatment Methods 0.000 claims description 14
- 108010019657 polymyxin drug combination nystatin neomycin dimethicone acetarsol Proteins 0.000 claims description 13
- 238000010438 heat treatment Methods 0.000 claims description 10
- 230000002421 anti-septic effect Effects 0.000 claims description 6
- 230000001804 emulsifying effect Effects 0.000 claims description 5
- 238000002844 melting Methods 0.000 claims description 5
- 230000008018 melting Effects 0.000 claims description 5
- 239000000080 wetting agent Substances 0.000 claims description 4
- 239000003814 drug Substances 0.000 abstract description 16
- 206010070834 Sensitisation Diseases 0.000 abstract description 5
- 230000008313 sensitization Effects 0.000 abstract description 5
- 239000004909 Moisturizer Substances 0.000 abstract description 4
- 230000001333 moisturizer Effects 0.000 abstract description 4
- 230000035699 permeability Effects 0.000 abstract description 4
- 230000000638 stimulation Effects 0.000 abstract description 3
- 230000002335 preservative effect Effects 0.000 abstract 2
- 230000003247 decreasing effect Effects 0.000 abstract 1
- 239000000686 essence Substances 0.000 abstract 1
- PGBHMTALBVVCIT-VCIWKGPPSA-N framycetin Chemical compound N[C@@H]1[C@@H](O)[C@H](O)[C@H](CN)O[C@@H]1O[C@H]1[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](N)C[C@@H](N)[C@@H]2O)O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CN)O2)N)O[C@@H]1CO PGBHMTALBVVCIT-VCIWKGPPSA-N 0.000 abstract 1
- 230000002538 fungal effect Effects 0.000 abstract 1
- 235000011187 glycerol Nutrition 0.000 abstract 1
- 229940053050 neomycin sulfate Drugs 0.000 abstract 1
- 210000003491 skin Anatomy 0.000 description 19
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 8
- 230000000694 effects Effects 0.000 description 8
- 238000012360 testing method Methods 0.000 description 6
- 229940079593 drug Drugs 0.000 description 5
- 206010005913 Body tinea Diseases 0.000 description 4
- 208000002474 Tinea Diseases 0.000 description 4
- 201000010618 Tinea cruris Diseases 0.000 description 4
- 239000011248 coating agent Substances 0.000 description 4
- 238000000576 coating method Methods 0.000 description 4
- 150000002632 lipids Chemical class 0.000 description 4
- 201000003875 tinea corporis Diseases 0.000 description 4
- 230000000844 anti-bacterial effect Effects 0.000 description 3
- 230000003110 anti-inflammatory effect Effects 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 239000003906 humectant Substances 0.000 description 3
- 239000002674 ointment Substances 0.000 description 3
- 229930003231 vitamin Natural products 0.000 description 3
- 239000011782 vitamin Substances 0.000 description 3
- 229940088594 vitamin Drugs 0.000 description 3
- 235000013343 vitamin Nutrition 0.000 description 3
- 150000003722 vitamin derivatives Chemical class 0.000 description 3
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 2
- 208000003322 Coinfection Diseases 0.000 description 2
- 206010048768 Dermatosis Diseases 0.000 description 2
- 241000233866 Fungi Species 0.000 description 2
- 201000004681 Psoriasis Diseases 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- 208000007712 Tinea Versicolor Diseases 0.000 description 2
- 206010067197 Tinea manuum Diseases 0.000 description 2
- 206010056131 Tinea versicolour Diseases 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 239000003429 antifungal agent Substances 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 238000011443 conventional therapy Methods 0.000 description 2
- 239000003246 corticosteroid Substances 0.000 description 2
- 239000002537 cosmetic Substances 0.000 description 2
- 230000003203 everyday effect Effects 0.000 description 2
- 210000002683 foot Anatomy 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 230000014759 maintenance of location Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 2
- 239000013558 reference substance Substances 0.000 description 2
- 208000017520 skin disease Diseases 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 201000004647 tinea pedis Diseases 0.000 description 2
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 206010015150 Erythema Diseases 0.000 description 1
- 102000011782 Keratins Human genes 0.000 description 1
- 108010076876 Keratins Proteins 0.000 description 1
- 102000004895 Lipoproteins Human genes 0.000 description 1
- 108090001030 Lipoproteins Proteins 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 125000003275 alpha amino acid group Chemical group 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 230000003064 anti-oxidating effect Effects 0.000 description 1
- 230000001139 anti-pruritic effect Effects 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 239000003908 antipruritic agent Substances 0.000 description 1
- OJHAHQJRQIOCFK-UHFFFAOYSA-N azane;chloroform;methanol Chemical compound N.OC.ClC(Cl)Cl OJHAHQJRQIOCFK-UHFFFAOYSA-N 0.000 description 1
- 244000052616 bacterial pathogen Species 0.000 description 1
- 230000017531 blood circulation Effects 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 210000000736 corneocyte Anatomy 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 230000000593 degrading effect Effects 0.000 description 1
- 231100000223 dermal penetration Toxicity 0.000 description 1
- 230000002500 effect on skin Effects 0.000 description 1
- 231100000321 erythema Toxicity 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 244000053095 fungal pathogen Species 0.000 description 1
- 238000004817 gas chromatography Methods 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 229920002674 hyaluronan Polymers 0.000 description 1
- 229960003160 hyaluronic acid Drugs 0.000 description 1
- 230000008595 infiltration Effects 0.000 description 1
- 238000001764 infiltration Methods 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 230000002427 irreversible effect Effects 0.000 description 1
- 210000002510 keratinocyte Anatomy 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 239000013521 mastic Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- GBMDVOWEEQVZKZ-UHFFFAOYSA-N methanol;hydrate Chemical compound O.OC GBMDVOWEEQVZKZ-UHFFFAOYSA-N 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- YTJSFYQNRXLOIC-UHFFFAOYSA-N octadecylsilane Chemical compound CCCCCCCCCCCCCCCCCC[SiH3] YTJSFYQNRXLOIC-UHFFFAOYSA-N 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 230000001835 salubrious effect Effects 0.000 description 1
- 231100000241 scar Toxicity 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 210000004927 skin cell Anatomy 0.000 description 1
- 206010040882 skin lesion Diseases 0.000 description 1
- 231100000444 skin lesion Toxicity 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 210000000434 stratum corneum Anatomy 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 238000004809 thin layer chromatography Methods 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/7036—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Molecular Biology (AREA)
- Dermatology (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a topical cream for treating fungal infection and a production method thereof. The topical cream for treating the fungal infection is prepared from ketoconazole, clobetasol propionate, neomycin sulfate, a thickening agent, a moisturizer, a penetration enhancer, an antioxidant, a preservative, an emulsifier, essence and purified water; the thickening agent is prepared from stearic acid, cetostearyl alcohol and liquid paraffin; the moisturizer is prepared from glycerin and a natural moisturizer; azone is adopted as the penetration enhancer; vitamin E is adopted as the antioxidant; anhydrous sodium sulfite is adopted as the preservative. The topical cream for treating the fungal infection has the advantages that the permeability in the skin is good, fungal residues under the skin layer can be effectively decreased, stimulation and sensitization possibility of the skin are lowered, the medicine applying comfort of the skin is effectively improved, relapse is not prone to occur, and the topical cream is an effective preparation for treating the fungal infection.
Description
Technical field
The present invention relates to a kind of medicinal external emulsifiable paste pharmaceutical composition and preparation method thereof, particularly a kind of medicinal external emulsifiable paste and production method thereof for the treatment of fungal infection.
Background technology
Dermatosis is one of the commonly encountered diseases, frequently-occurring disease that affect human health, wherein in the majority with fungal infection type.Along with Antibiotics medicine extensively, is in large quantities used, cause the drug resistance of pathogenic bacterium to improve constantly, secondary infection and mixed infection constantly occur, and make Disease cannot obtain desirable therapeutic effect.At present, although the medicine for the treatment of fungal infection is many, most drug permeability is in skin not good, medicine only with skin surface contact, cause the pathogenic fungi below cortex to exist residual, easily recur.In order to the shelf life of prolong drug, the antiseptic that in the pharmaceutical composition of existing treatment fungal infection, usual interpolation is conventional and antioxidant, the interpolation of these components may produce the possibility of stimulation and sensitization, the sense of discomfort after increase skin coating to skin.
Summary of the invention
The object of the invention is to overcome the deficiencies in the prior art, a kind of good penetrability is in skin provided, the fungus that can effectively reduce below cortex remains, the excitement and the sensitization that reduce skin may simultaneously, effectively improve skin coating comfort, not easily recur, there is medicinal external emulsifiable paste and the production method thereof of the treatment fungal infection of Preferred effects.
In order to achieve the above object, a kind of medicinal external emulsifiable paste for the treatment of fungal infection of the present invention, is made up of the component of following percentage by weight:
Ketoconazole 0.5-2%
Clobetasol propionate 0.02-0.03%
Polygynax 0.5-1.0%
Thickening agent 16-32%
Wetting agent 10-20%
Transdermal penetration enhancer 0.5-1.0%
Antioxidant 0.2-0.5%
Antiseptic 0.4-1.0%
Emulsifying agent 4-8%
Essence 0.2-0.5%
Purified water surplus
Wherein, described thickening agent is stearic acid, cetostearyl alcohol and liquid Paraffin;
Described wetting agent is glycerol and natural moisture preserving agent;
Described transdermal penetration enhancer is azone;
Described antioxidant is vitamin E;
Described antiseptic is anhydrous sodium sulfite.
As preferably, a kind of medicinal external emulsifiable paste for the treatment of fungal infection of the present invention, is made up of the component of following percentage by weight:
Ketoconazole 1.0-1.5%
Clobetasol propionate 0.025-0.028%
Polygynax 0.65-0.85%
Stearic acid 5-10%
Cetostearyl alcohol 3-7%
Liquid Paraffin 8-15%
Glycerol 5-10%
Natural moisture preserving agent 5-10%
Azone 0.5-1.0%
Vitamin E 0.1-0.2%
Anhydrous sodium sulfite 0.4-0.6%
Emulsifying agent 4-8%
Essence 0.2-0.5%
Purified water surplus
Natural moisture preserving agent is amino acid humectant, and be a kind of efficient moisture-retention agent of amphoteric ion type, effect is identical with hyaluronic acid, can safety for cosmetics and washing series products in.Because amino acid humectant is pure natural structural material, so amino acid humectant a kind ofly absorbs fast, active high new moisturizer.There is high biological compatibility, very easily water-soluble, very heat-resisting, acidproof and alkaline-resisting and applied widely, skin histology can be entered by rapid permeability, improve the moisture holding capacity of skin, the vigor of activated cell, give skin gloss and salubrious effect of moistening.In addition sun-proof in addition, the effect of antiinflammatory.
Azone is the fabulous dermal osmosis accelerator of osmosis in medicine and cosmetic industry, obvious transdermal is all had to help the effect of oozing to oleophylic, hydrophilic medicament and active component, keratodermatitis and lipid are interacted, reduce the phase inversion temperature of active substance to lipid in horny layer gap, add mobility, diffusional resistance in horny layer of medicine or active additive is reduced, therefore plays and very strong shortly ooze effect.
Vitamin E has antioxidation, can strengthen capillary of skin resistance, and maintains normal permeability, improves blood circulation.It can enter Skin Cell and carry out free radical resisting chain reaction, can prevent skin keratin.Also be medicine for external use (can pass through skin to be absorbed) and the oral medicine of locality wound simultaneously, all can prevent scar.
The medicinal external emulsifiable paste for the treatment of fungal infection of the present invention adopts ketoconazole, clobetasol propionate, polygynax and mastic adjuvant scientific allocation to form, be applied in patient skin surface, by medicines such as clobetasol propionate, ketoconazole, polygynax, reach rapid antiinflammatory, antipruritic, antibacterial and bactericidal action; Simultaneously by adding natural moisture preserving agent, having antiinflammatory concurrently and improving the effect of moisture of skin retentivity; Add azone, play very strong skin and urge to ooze effect, make medicine effectively infiltrate into below cortex, reduce fungus and remain, prevent recurrence; Adopt vitamin E as antioxidant, safely, stable, non-stimulated, reduce the stimulation of skin and the possible of sensitization while preventing compositions from degrading, the combination of antioxidant and antiseptic is compared with employing single variety antioxidant, and can reduce stimulates and can the consumption of sensitization antioxidant and concentration.And, not containing dimethyl sulfoxide in the present invention, dimethyl sulfoxide uses one of dermal penetration enhancer the earliest, dimethyl sulfoxide can make the degeneration of skin keratinocytes internal protein, the ordered arrangement of lipid between corneocyte can be destroyed, Stratum corneum lipids, lipoprotein can be sloughed, strengthen the osmosis of medicine, but when using high-concentration dimethyl sulfoxide, skin can be made to produce erythema, blister and irreversible damage.The present invention, by the synergism of each component, improves the comfort of skin coating, makes patient can obtain desirable therapeutic effect while deep layer sterilization.
Another object of the present invention is to provide a kind of production method for the treatment of the medicinal external emulsifiable paste of fungal infection, comprise the steps:
1, oil phase preparation: take stearic acid, cetostearyl alcohol, liquid Paraffin put a vessel in heating, stirring, make it melting; Add vitamin E and azone, stir, make it to be uniformly dissolved; Add ketoconazole, clobetasol propionate that precision takes again, limit edged stirs, and slowly makes it to dissolve, is incubated at 78-82 DEG C, obtained oil phase;
2, aqueous phase preparation: purified water is placed in another container, add glycerol, natural moisture preserving agent, anhydrous sodium sulfite, emulsifying agent and the accurate polygynax taken, heating, stirring, make it to be uniformly dissolved, and is incubated at 78-82 DEG C, obtained aqueous phase;
3, emulsifying: slowly joined in oil phase by aqueous phase while hot, add essence, lowers the temperature gradually after constantly stirring 20-50min by same direction, to white fine and smooth paste, is cooled to 20-40 DEG C, obtains emulsifiable paste.
This preparation technology flow process is reasonable, does not destroy the chemical constitution of various raw material and infiltration auxiliary addition agent, and is easy to operation.
Detailed description of the invention
Embodiment 1
(1) oil phase preparation: take stearic acid 100g, cetostearyl alcohol 70g, liquid Paraffin 150g puts a vessel in heating, stirring, make it melting; Add vitamin E2 g, azone 10g, stir, make it to be uniformly dissolved; Add ketoconazole 20g, clobetasol propionate 0.3g that precision takes again, limit edged stirs, and slowly makes it to dissolve, is incubated at 78 DEG C, obtained oil phase;
(2) aqueous phase preparation: purified water 418g is placed in another container, add glycerol 65g, natural moisture preserving agent 65g, anhydrous sodium sulfite 4.7g, emulsifying agent 80g and the accurate polygynax 10g taken, heating, stirring, make it to be uniformly dissolved, be incubated at 78 DEG C, obtained aqueous phase;
(3) emulsifying: slowly joined in oil phase by aqueous phase while hot, adds essence 5g, lowers the temperature gradually after constantly stirring 50min by same direction, to white fine and smooth paste, is cooled to 20 DEG C, obtained 1000g emulsifiable paste.
Embodiment 2
(1) oil phase preparation: take stearic acid 50g, cetostearyl alcohol 30g, liquid Paraffin 80g puts a vessel in heating, stirring, make it melting; Add vitamin e1 .8g, azone 5g, stir, make it to be uniformly dissolved; Add ketoconazole 5g, clobetasol propionate 0.2g that precision takes again, limit edged stirs, and slowly makes it to dissolve, is incubated at 82 DEG C, obtained oil phase;
(2) aqueous phase preparation: purified water 627g is placed in another container, add glycerol 50g, natural moisture preserving agent 100g, anhydrous sodium sulfite 4g, emulsifying agent 40g and the accurate polygynax 5g taken, heating, stirring, make it to be uniformly dissolved, be incubated at 82 DEG C, obtained aqueous phase;
(3) emulsifying: slowly joined in oil phase by aqueous phase while hot, adds essence 2g, lowers the temperature gradually after constantly stirring 20min by same direction, to white fine and smooth paste, is cooled to 40 DEG C, obtained 1000g emulsifiable paste.
Embodiment 3
(1) oil phase preparation: take stearic acid 67.5g, cetostearyl alcohol 55g, liquid Paraffin 100g puts a vessel in heating, stirring, make it melting; Add vitamin e1 g, azone 9g, stir, make it to be uniformly dissolved; Add ketoconazole 10g, clobetasol propionate 0.25g that precision takes again, limit edged stirs, and slowly makes it to dissolve, is incubated at 80 DEG C, obtained oil phase;
(2) aqueous phase preparation: purified water 539.5g is placed in another container, add glycerol 100g, natural moisture preserving agent 50g, anhydrous sodium sulfite 6g, emulsifying agent 50g and the accurate polygynax 8.75g taken, heating, stirring, make it to be uniformly dissolved, be incubated at 80 DEG C, obtained aqueous phase;
(3) emulsifying: slowly joined in oil phase by aqueous phase while hot, adds essence 3g, lowers the temperature gradually after constantly stirring 30min by same direction, to white fine and smooth paste, is cooled to 35 DEG C, obtained 1000g emulsifiable paste.
Adopt the ketoconazole in gas chromatography discriminating emulsifiable paste and clobetasol propionate, the retention time of need testing solution two main peak is consistent with the retention time of reference substance solution two main peak.Adopting thin layer chromatography, take chloroform as solvent, with methanol-chloroform-ammonia (13.5mol/L) (60:20:40) for developing solvent, differentiates the polygynax in emulsifiable paste; In trial target chromatograph, on the position corresponding to polygynax reference substance chromatograph, the speckle of display same color.
Adopt the content of ketoconazole and clobetasol propionate in high effective liquid chromatography for measuring emulsifiable paste; Be filler with octadecylsilane chemically bonded silica, with methanol-water (74:26) for mobile phase, determined wavelength is 239nm, and number of theoretical plate ketoconazole peak calculates and is not less than 2000, and ketoconazole peak and the peak-to-peak separating degree of clobetasol propionate are greater than 2.0.
Result of use is tested:
Case selection: totally 200 routine outpatients, wherein tinea corporis and cruris 68 example, tinea manus and pedis 64 example, tinea versicolor 46 example, psoriasis vulgaris 44 example.
Administrated method: be applied to skin lesion place outside the medicinal external emulsifiable paste of the present invention being treated fungal infection, and repeatedly rub gently repeatedly, every day 2 times.Tinea corporis and cruris and tinea versicolor continuous use 1 week; Tinea manus and pedis is used in conjunction 2 weeks; Psoriasis is used in conjunction 4 weeks, weekly further consultation 1 time.Treatments period does not use other antifungal drug and corticosteroid medication.
Result: the medicinal external emulsifiable paste that the present invention treats fungal infection treats 4 kinds of dermatosis observed results
As seen from the above table, the medicinal external emulsifiable paste that the present invention treats fungal infection has good antibacterial action to mycotic infection of superficial part.
Result of use contrast test:
Tinea corporis and cruris patient is divided into two groups at random, test group the present invention treats the medicinal external emulsifiable paste of fungal infection, the contrast groups ointment affected part of exterior coating of conventional therapy fungal infection, apply ointment every day 2 times, continuous treatment 1 week, treatments period does not use other antifungal drug and corticosteroid medication, and observes the recurrence of two groups of patients symptomatic after a week.
Result: the present invention treats the medicinal external emulsifiable paste of fungal infection and the Contrast on effect of conventional therapy fungal infection ointment
As seen from the above table, test group total effective rate is 100%, and contrast groups total effective rate is 91%, two groups of cure rates and effective percentage difference highly significant (P < 0.01); Test group relapse rate is 2.0%, and contrast groups relapse rate is 18.0%, and the relapse rate using medicinal external emulsifiable paste of the present invention to treat tinea corporis and cruris significantly reduces.
The medicinal external emulsifiable paste that the present invention treats fungal infection forms according to scientific compatibility, proves through test, the functional component in emulsifiable paste can hypersynchronous to cortex, to treatment fungal infection Be very effective, be treat the effective preparation of fungal infection.
Claims (3)
1. treat a medicinal external emulsifiable paste for fungal infection, it is characterized in that: be made up of the component of following percentage by weight:
Ketoconazole 0.5-2%
Clobetasol propionate 0.02-0.03%
Polygynax 0.5-1.0%
Thickening agent 16-32%
Wetting agent 10-20%
Transdermal penetration enhancer 0.5-1.0%
Antioxidant 0.2-0.5%
Antiseptic 0.4-1.0%
Emulsifying agent 4-8%
Essence 0.2-0.5%
Purified water surplus
Wherein, described thickening agent is stearic acid, cetostearyl alcohol and liquid Paraffin;
Described wetting agent is glycerol and natural moisture preserving agent;
Described transdermal penetration enhancer is azone;
Described antioxidant is vitamin E;
Described antiseptic is anhydrous sodium sulfite.
2. a kind of medicinal external emulsifiable paste for the treatment of fungal infection according to claim 1, is characterized in that: be made up of the component of following percentage by weight:
Ketoconazole 1.0-1.5%
Clobetasol propionate 0.025-0.028%
Polygynax 0.65-0.85%
Stearic acid 5-10%
Cetostearyl alcohol 3-7%
Liquid Paraffin 8-15%
Glycerol 5-10%
Natural moisture preserving agent 5-10%
Azone 0.5-1.0%
Vitamin E 0.1-0.2%
Anhydrous sodium sulfite 0.4-0.6%
Emulsifying agent 4-8%
Essence 0.2-0.5%
Purified water surplus.
3. treat a production method for the medicinal external emulsifiable paste of fungal infection, it is characterized in that: comprise the steps:
(1) oil phase preparation: take stearic acid, cetostearyl alcohol, liquid Paraffin put a vessel in heating, stirring, make it melting; Add vitamin E and azone, stir, make it to be uniformly dissolved; Add ketoconazole, clobetasol propionate that precision takes again, limit edged stirs, and slowly makes it to dissolve, is incubated at 78-82 DEG C, obtained oil phase;
(2) aqueous phase preparation: purified water is placed in another container, add glycerol, natural moisture preserving agent, anhydrous sodium sulfite, emulsifying agent and the accurate polygynax taken, heating, stirring, make it to be uniformly dissolved, and is incubated at 78-82 DEG C, obtained aqueous phase;
(3) emulsifying: slowly joined in oil phase by aqueous phase while hot, add essence, lowers the temperature gradually after constantly stirring 20-50min by same direction, to white fine and smooth paste, is cooled to 20-40 DEG C, obtains emulsifiable paste.
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| CN201510892966.5A CN105456182A (en) | 2015-12-08 | 2015-12-08 | Topical cream for treating fungal infection and production method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106937955A (en) * | 2017-03-31 | 2017-07-11 | 天津迈拓思生物科技有限公司 | A kind of compound preparation for treating psoriasis |
| CN107441127A (en) * | 2017-09-01 | 2017-12-08 | 骆凌翔 | The compound effacement emulsion of suppression oxygen orientation medicine transdermal chronic disease one again |
| CN114159376A (en) * | 2020-09-10 | 2022-03-11 | 九江学院 | Liquiritigenin emulsifying ointment and preparation method and application thereof |
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| CN1130065A (en) * | 1995-10-23 | 1996-09-04 | 滇虹天然药物厂 | Compound ketoconazole external-use preparation |
| CN101015553A (en) * | 2007-03-06 | 2007-08-15 | 杨文龙 | Medicinal composition for treating skin superficial fungal infection and preparation process thereof |
| CN101712912A (en) * | 2009-11-25 | 2010-05-26 | 南顺商标有限公司 | Skin-care detergent containing vitamin E and amino acid humectant |
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| CN1130065A (en) * | 1995-10-23 | 1996-09-04 | 滇虹天然药物厂 | Compound ketoconazole external-use preparation |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106937955A (en) * | 2017-03-31 | 2017-07-11 | 天津迈拓思生物科技有限公司 | A kind of compound preparation for treating psoriasis |
| CN107441127A (en) * | 2017-09-01 | 2017-12-08 | 骆凌翔 | The compound effacement emulsion of suppression oxygen orientation medicine transdermal chronic disease one again |
| CN114159376A (en) * | 2020-09-10 | 2022-03-11 | 九江学院 | Liquiritigenin emulsifying ointment and preparation method and application thereof |
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Address after: Tongxiang City, Jiaxing City, Zhejiang province 314500 Economic Development Zone Foreign Investment Zone Applicant after: Zhejiang Ding Tai pharmaceutical Limited by Share Ltd Address before: Tongxiang City, Jiaxing City, Zhejiang province 314500 Economic Development Zone Foreign Investment Zone Applicant before: Zhenjiang Dingtai Pharmaceutical Co., Ltd. |
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