CN105560248A - Pharmaceutical composition for treating fungal infection and preparing method and application thereof - Google Patents
Pharmaceutical composition for treating fungal infection and preparing method and application thereof Download PDFInfo
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- CN105560248A CN105560248A CN201610076763.3A CN201610076763A CN105560248A CN 105560248 A CN105560248 A CN 105560248A CN 201610076763 A CN201610076763 A CN 201610076763A CN 105560248 A CN105560248 A CN 105560248A
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- pharmaceutical composition
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- dopamine
- uracil
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 35
- 206010017533 Fungal infection Diseases 0.000 title claims abstract description 9
- 208000031888 Mycoses Diseases 0.000 title claims abstract description 9
- 238000000034 method Methods 0.000 title abstract description 4
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims abstract description 32
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims abstract description 32
- ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims abstract description 28
- 238000002360 preparation method Methods 0.000 claims abstract description 21
- 239000004471 Glycine Substances 0.000 claims abstract description 16
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims abstract description 16
- 229960003638 dopamine Drugs 0.000 claims abstract description 16
- 239000003814 drug Substances 0.000 claims abstract description 14
- 239000002674 ointment Substances 0.000 claims abstract description 14
- 229940035893 uracil Drugs 0.000 claims abstract description 14
- 239000007788 liquid Substances 0.000 claims abstract description 13
- 201000004647 tinea pedis Diseases 0.000 claims description 19
- 206010067197 Tinea manuum Diseases 0.000 claims description 18
- 210000002683 foot Anatomy 0.000 claims description 16
- 239000000470 constituent Substances 0.000 claims description 6
- 239000002671 adjuvant Substances 0.000 claims description 4
- BTGMTHBOODBMHN-SUHMBNCMSA-N N-[3-[1-[[(3S)-2-hydroxy-5-oxooxolan-3-yl]carbamoyl]cyclopropyl]-2,4-dioxo-1-propan-2-ylpyrimidin-5-yl]-2-methyl-4-(naphthalen-2-ylamino)benzamide Chemical group CC(C)n1cc(NC(=O)c2ccc(Nc3ccc4ccccc4c3)cc2C)c(=O)n(c1=O)C1(CC1)C(=O)N[C@H]1CC(=O)OC1O BTGMTHBOODBMHN-SUHMBNCMSA-N 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 229940079593 drug Drugs 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 5
- 208000002474 Tinea Diseases 0.000 abstract description 4
- 241000130764 Tinea Species 0.000 abstract description 3
- 231100000331 toxic Toxicity 0.000 abstract 1
- 230000002588 toxic effect Effects 0.000 abstract 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 15
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 15
- 239000000499 gel Substances 0.000 description 14
- 239000008215 water for injection Substances 0.000 description 13
- 239000012467 final product Substances 0.000 description 6
- 210000003491 skin Anatomy 0.000 description 5
- 238000003756 stirring Methods 0.000 description 5
- 230000001225 therapeutic effect Effects 0.000 description 5
- 238000004140 cleaning Methods 0.000 description 4
- 230000003203 everyday effect Effects 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 238000004806 packaging method and process Methods 0.000 description 4
- 230000001954 sterilising effect Effects 0.000 description 4
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 3
- 241000233866 Fungi Species 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 208000003251 Pruritus Diseases 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 229920002125 Sokalan® Polymers 0.000 description 3
- 239000003429 antifungal agent Substances 0.000 description 3
- 229960001631 carbomer Drugs 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 230000002538 fungal effect Effects 0.000 description 3
- 238000011084 recovery Methods 0.000 description 3
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 3
- 235000010234 sodium benzoate Nutrition 0.000 description 3
- 239000004299 sodium benzoate Substances 0.000 description 3
- 239000003981 vehicle Substances 0.000 description 3
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 2
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- 241000894006 Bacteria Species 0.000 description 2
- 229920000742 Cotton Polymers 0.000 description 2
- 206010048768 Dermatosis Diseases 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 2
- BYBLEWFAAKGYCD-UHFFFAOYSA-N Miconazole Chemical compound ClC1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 BYBLEWFAAKGYCD-UHFFFAOYSA-N 0.000 description 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 2
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 2
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 description 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 2
- 239000006071 cream Substances 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 239000008273 gelatin Substances 0.000 description 2
- 229920000159 gelatin Polymers 0.000 description 2
- 235000019322 gelatine Nutrition 0.000 description 2
- 235000011852 gelatine desserts Nutrition 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 231100000957 no side effect Toxicity 0.000 description 2
- 238000010422 painting Methods 0.000 description 2
- 230000000306 recurrent effect Effects 0.000 description 2
- 208000017520 skin disease Diseases 0.000 description 2
- 239000000661 sodium alginate Substances 0.000 description 2
- 235000010413 sodium alginate Nutrition 0.000 description 2
- 229940005550 sodium alginate Drugs 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- 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 description 1
- MCCACAIVAXEFAL-UHFFFAOYSA-N 1-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]imidazole;nitric acid Chemical compound O[N+]([O-])=O.ClC1=CC(Cl)=CC=C1COC(C=1C(=CC(Cl)=CC=1)Cl)CN1C=NC=C1 MCCACAIVAXEFAL-UHFFFAOYSA-N 0.000 description 1
- XSROMLOMDFTVMJ-UHFFFAOYSA-O 1h-imidazol-1-ium;nitrate Chemical compound [O-][N+]([O-])=O.[NH2+]1C=CN=C1 XSROMLOMDFTVMJ-UHFFFAOYSA-O 0.000 description 1
- CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 description 1
- 239000005711 Benzoic acid Substances 0.000 description 1
- 206010005913 Body tinea Diseases 0.000 description 1
- 239000002126 C01EB10 - Adenosine Substances 0.000 description 1
- 241000222122 Candida albicans Species 0.000 description 1
- 208000003322 Coinfection Diseases 0.000 description 1
- 206010013700 Drug hypersensitivity Diseases 0.000 description 1
- 201000000297 Erysipelas Diseases 0.000 description 1
- 206010019851 Hepatotoxicity Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 241001299895 Microsporum ferrugineum Species 0.000 description 1
- 241000893976 Nannizzia gypsea Species 0.000 description 1
- -1 Nipagin ester Chemical class 0.000 description 1
- 206010067482 No adverse event Diseases 0.000 description 1
- 206010040844 Skin exfoliation Diseases 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 1
- 206010042566 Superinfection Diseases 0.000 description 1
- 206010043866 Tinea capitis Diseases 0.000 description 1
- 201000010618 Tinea cruris Diseases 0.000 description 1
- 241000223238 Trichophyton Species 0.000 description 1
- 241000893966 Trichophyton verrucosum Species 0.000 description 1
- 241001480050 Trichophyton violaceum Species 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 229960005305 adenosine Drugs 0.000 description 1
- 229940121375 antifungal agent Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- 229940095731 candida albicans Drugs 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 229960004022 clotrimazole Drugs 0.000 description 1
- VNFPBHJOKIVQEB-UHFFFAOYSA-N clotrimazole Chemical compound ClC1=CC=CC=C1C(N1C=NC=C1)(C=1C=CC=CC=1)C1=CC=CC=C1 VNFPBHJOKIVQEB-UHFFFAOYSA-N 0.000 description 1
- 238000010960 commercial process Methods 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 230000035618 desquamation Effects 0.000 description 1
- 238000007598 dipping method Methods 0.000 description 1
- 201000005311 drug allergy Diseases 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 230000003628 erosive effect Effects 0.000 description 1
- 230000007717 exclusion Effects 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 238000011010 flushing procedure Methods 0.000 description 1
- 208000024386 fungal infectious disease Diseases 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 229940075507 glyceryl monostearate Drugs 0.000 description 1
- 230000007686 hepatotoxicity Effects 0.000 description 1
- 231100000304 hepatotoxicity Toxicity 0.000 description 1
- 229960003444 immunosuppressant agent Drugs 0.000 description 1
- 230000001861 immunosuppressant effect Effects 0.000 description 1
- 239000003018 immunosuppressive agent Substances 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000003780 keratinization Effects 0.000 description 1
- 229960004125 ketoconazole Drugs 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 206010025226 lymphangitis Diseases 0.000 description 1
- 229960002509 miconazole Drugs 0.000 description 1
- 229960005040 miconazole nitrate Drugs 0.000 description 1
- 238000000386 microscopy Methods 0.000 description 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 230000001717 pathogenic effect Effects 0.000 description 1
- 230000036285 pathological change Effects 0.000 description 1
- 231100000915 pathological change Toxicity 0.000 description 1
- 235000010241 potassium sorbate Nutrition 0.000 description 1
- 239000004302 potassium sorbate Substances 0.000 description 1
- 229940069338 potassium sorbate Drugs 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 201000003875 tinea corporis Diseases 0.000 description 1
- 229940055035 trichophyton verrucosum Drugs 0.000 description 1
- 230000002747 voluntary effect Effects 0.000 description 1
- 239000003871 white petrolatum Substances 0.000 description 1
Classifications
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- 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
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/42—Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
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- 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
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
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- A—HUMAN NECESSITIES
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
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- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
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- Engineering & Computer Science (AREA)
- Inorganic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dermatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Emergency Medicine (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides a pharmaceutical composition for treating fungal infection and a preparing method and application thereof. The pharmaceutical composition is prepared from, by weight, 15-40 parts of serine, 20-45 parts of glycine, 10-35 parts of uracil and 1-20 parts of dopamine. The invention further provides the application of the pharmaceutical composition in preparing drugs for treating tinea of feet and hands. The pharmaceutical composition is a liquid preparation, gel or ointment. The total effective rate of the pharmaceutical composition on tinea of feet and hands can reach 100%, no toxic or side effect is caused, and no relapse is caused.
Description
Technical field
The invention belongs to field of medicaments, particularly a kind of pharmaceutical composition for the treatment of fungal infection and its preparation method and application.
Background technology
Shallow epidermis skin fungal infectious disease occupies very high ratio in dermatosis, general easy recurrence, and comparatively refractory more, belongs to one of refractory skin.Cutaneous fungal infection disease common clinically comprises the tinea manuum, tinea pedis, tinea cruris, tinea corporis, tinea capitis etc.Its symptom is mainly manifested in the moist flushing of local skin, erosion, dipping turn white or play phlysis, skin pruritus unbearably, scratch after often cause erysipelas and lymphangitis etc. because of secondary infection, easy keratinization desquamation after dry, to chap.Can be contagious, easily recur.What cause cutaneous fungal infection mainly contains trichophyton, alpha fungus, trichophyton gypseum, Trichophyton violaceum, chaff shape fish-scale tinea bacterium, ascospore bacterium, acrothesium floccosum, Candida albicans, Sabouraudites lanosus, Microsporum ferrugineum and Trichophyton verrucosum etc.
Topical antifungal agents concrete at present relates generally to medicinal external emulsifiable paste or the cream such as clotrimazole, miconazole, ketoconazole.But the general toleration of above-mentioned azole drug is good, but especially long-term or heavy dose of medication may cause the untoward reaction etc. of side effect of digestive tract, hepatotoxicity, central nervous system in the treatment.In addition, all there is pruritus problem in most of fungal infection, and part also with inflammation, makes patient medication interdependence very poor, and causes superinfection.Therefore, the antifungal drug researching and developing a kind of better efficacy seems particularly important.
Summary of the invention
Tinea manus and pedis is the dermatosis that pathogenic skin filamentous fungi causes at brothers position.Can be divided into the tinea manuum, tinea pedis according to its site of pathological change, the traditional Chinese medical science claims the tinea manuum to be " fungal infection of hand and foot ", and tinea pedis is commonly called as " tinea pedis ".Tinea manus and pedis is clinical common refractory skin, patient illness part pruritus, pain, oozes out, peels, and this sick treatment is more difficult, has the feature of recurrent exerbation.
For above-mentioned technical problem, the invention provides a kind of pharmaceutical composition for the treatment of tinea manus and pedis and preparation method thereof.
Constituent and the content thereof of pharmaceutical composition of the present invention comprise with parts by weight: serine 15 ~ 40 parts, glycine 20 ~ 45 parts, uracil 10 ~ 35 parts, dopamine 1 ~ 20 part.
Further, constituent and the content thereof of described pharmaceutical composition comprise with parts by weight: serine 30 ~ 40 parts, glycine 30 ~ 38 parts, uracil 16 ~ 23 parts, dopamine 8 ~ 15 parts.
Further, constituent and the content thereof of described pharmaceutical composition comprise with parts by weight: serine 35 parts, glycine 35 parts, uracil 20 parts, dopamine 10 parts.
Pharmaceutical composition of the present invention is carved when needed and is added pharmaceutically acceptable adjuvant.
Present invention also offers the application of described pharmaceutical composition in preparation treatment tinea manus and pedis medicine.
The dosage form of described medicine can be liquid preparation, gel or unguentum.
Beneficial effect of the present invention is embodied in: (1) pharmaceutical composition of the present invention has obvious inhibitory action to the scratchiness in tinea manus and pedis symptom; (2) pharmaceutical composition of the present invention is prepared into liquid preparation or gel or unguentum all can not affect its concrete curative effect to tinea manus and pedis; (3) pharmaceutical composition of the present invention has no side effect, and does not recur after drug withdrawal; (4) pharmaceutical composition of the present invention total effective rate on the therapeutic effect of tinea manus and pedis can reach 100%.
Detailed description of the invention
Following examples are used for the present invention is described, but are not restriction the present invention scopes required for protection.
The present invention's adenosine used, dopamine are purchased in Shanghai ten thousand boundary Bioisystech Co., Ltd.
The present invention's uracil used is purchased in Qilu Tianhe Huishi Pharmacy Co., Ltd..
Serine of the present invention and glycine are purchased in Tianjin TianAn Medicine Industry Co., Ltd.
The adjuvant that the present invention is used and medicine commercially can be purchased.
embodiment 1 liquid preparation
Take serine 35g, glycine 35g, uracil 20g, the potassium sorbate of dopamine 10g and 2.5g injects water to 1000ml, stirs, adjust ph 6.5 ~ 7.5, filters, embedding, 115 DEG C of sterilizing 30min, and packaging, to obtain final product.
embodiment 2 gel
Take the serine 35g of recipe quantity, glycine 35g, uracil 20g, dopamine 10g, after appropriate water for injection stirring and dissolving, then adds containing 5g carbomer, in the gel-type vehicle of propylene glycol 90g, Nipagin ester 0.3g and appropriate water for injection, prepare according to the conventional method of gel, add sodium hydroxide, stirring and being neutralized to pH value is 5.5 ~ 7.5, add water for injection to 1000g, 115 DEG C of sterilizing 30min, packaging, obtains gel.
embodiment 3 unguentum
Take the serine 35g of recipe quantity, glycine 35g, uracil 20g, dopamine 10g, add appropriate water for injection to dissolve, add again in the substrate of sodium carboxymethyl cellulose 120g, glycerol 110g, sodium benzoate 2.5g and appropriate water for injection, according to the customary preparation methods of unguentum, make unguentum.
embodiment 4 liquid preparation
Take the serine 15g of recipe quantity, glycine 45g, uracil 10g, dopamine 15g, after mix homogeneously, add 80ml glycerol and 2g sodium benzoate, add water for injection to 1000ml, stir, adjust ph 6.5 ~ 7.5, filter, filtrate embedding, 115 DEG C of sterilizing 30min, packaging, to obtain final product.
embodiment 5 unguentum
Take the serine 15g of recipe quantity, glycine 20g, uracil 10g, dopamine 1g, after mix homogeneously, add appropriate water for injection and dissolve, and then join in the substrate containing 90g white vaseline, 11g glyceryl monostearate, 60g stearic acid, 0.5g benzoic acid and appropriate water for injection, the method preparation preparing unguentum conveniently, to obtain final product.
embodiment 6 gel
Take the serine 40g of recipe quantity, glycine 38g, uracil 23g, dopamine 15g, after mix homogeneously, dissolve in appropriate water for injection, then the solution dissolved slowly is joined containing carbomer 7g, triethanolamine 5g, gelatin 8g, sodium alginate 10g, in the gel-type vehicle of glycerol 90g and appropriate water for injection, prepare according to the customary preparation methods of gel, to obtain final product.
embodiment 7 liquid preparation
Take the serine 40g of recipe quantity, glycine 45g, uracil 35g, dopamine 2 0g, after mix homogeneously, adds appropriate water for injection and dissolves, add 100ml glycerol and 2.5g sodium benzoate again, stir, inject water to 1000ml, adjust ph 6.5 ~ 7.5, filter, embedding, 115 DEG C of sterilizing 30min, packaging, to obtain final product.
embodiment 8 gel
Take the serine 30g of recipe quantity, glycine 30g, uracil 16g, dopamine 8g, dissolve in appropriate water for injection, then slowly join containing carbomer 8g, triethanolamine 5g, gelatin 3g, sodium alginate 14g, in the gel-type vehicle of glycerol 150g and appropriate water for injection, prepare according to the customary preparation methods of gel, to obtain final product.
Pharmaceutical composition described in above-described embodiment, after adding pharmaceutically acceptable adjuvant, can make gel, liquid preparation, unguentum, directly smears or be sprayed at affected part during use, and these adopt existing commercial process all can realize.By experiment the curative effect of pharmaceutical composition of the present invention will be described below.
the application of experimental example 1 pharmaceutical composition of the present invention in treatment tinea manus and pedis
The liquid preparation of the contrast embodiment of the present invention 1, the gel of embodiment 2, the unguentum of embodiment 3 carries out effect assessment to the effectiveness of tinea manus and pedis patient and safety.
1. data 2:
Collect qualified tinea manus and pedis patient 200 example, age 18-65 year, the course of disease 1 month-10 years, wherein man 112 example, female 88 example.Random point matched group, treatment a group, treatment b group, treatment c group, often organizes 50 routine patients.There is not significant difference, P>0.05 in four groups of sexes, age, courses of disease, has comparability.
2. inclusion criteria:
(1) in age 16-70 year, men and women does not limit;
(2) patient of tinea manus and pedis is diagnosed as through clinical and mycology microscopy;
(3) patient of this experiment of voluntary participation.
3. exclusion standard:
(1) gestation and women breast-feeding their children;
(2) to 1% imidazolium nitrate health emulsifiable paste or or drug allergy person of the present invention;
Oral or 1 week interior local topical antifungal drug person in (3) 1 months;
(4) immunosuppressant person and diabetics is used.
4. Therapeutic Method:
Matched group: 1% Miconazole Nitrate Cream (trade name: daktarin, Xian-Janssen Pharmaceutical Ltd. produces) is smeared in affected part, and after cleaning affected part every day, outer painting is also gently rubbed, 3 times/day;
Treatment a group: the liquid preparation that the present invention obtains according to embodiment 1 is smeared in affected part, after cleaning affected part every day, dips liquid medicine painting with Cotton Gossypii, can stay between webs by the Cotton Gossypii being moistened with medicinal liquid, 3 times/day;
Treatment b group: the gel that the present invention obtains according to embodiment 2 is smeared in affected part, after cleaning affected part every day, gets described gel uniform application affected part, 3 times/day;
Treatment c group: the unguentum that the present invention obtains according to embodiment 3 is smeared in affected part, after cleaning affected part every day, gets described unguentum uniform application affected part, 3 times/day.
Above 4 groups of equal administrations 3 weeks, stop observation post administration 1 week.
5. efficacy determination:
Recovery from illness: erythra disappears completely, gargalesthesia disappears, negative fungal examination;
Effective: deflorescence >=60%, gargalesthesia obviously alleviates, negative fungal examination;
Effective: deflorescence 20% ~ 60%, gargalesthesia alleviates, negative fungal examination or the positive;
Invalid: deflorescence <20% or the state of an illness continue to increase the weight of, gargalesthesia is the same or aggravate, and fungus microscope examination is positive;
Total effective rate=(recovery from illness+effective+effectively)/case load × 100%.
6. statistical method: the present invention adopts SPSS13.0 statistics software to process the result that the present invention is last.
7. result
React after the patient medication of three treatment groups: use the gargalesthesia of pharmaceutical composition of the present invention to tinea manus and pedis to have obvious inhibitory action, therapeutic effect is good.In experimentation, patient has no adverse reaction appearance; In 1 week that observes after treatment is finished, in 3 treatment groups, not there is recurrent cases, in matched group, have 8 people's recurrences.Treatment a group total effective rate is 98%, and treatment b group total effective rate is 100%, and treatment c group total effective rate is 98%, and matched group total effective rate is 84%, specifically in table 1:
Recovery from illness | Effective | Effectively | Invalid | Total effective (%) | |
Matched group | 12 | 11 | 19 | 8 | 84 |
Treatment a group | 26 | 17 | 6 | 1 | 98 |
Treatment b group | 23 | 19 | 8 | 0 | 100 |
Treatment c group | 25 | 16 | 8 | 1 | 98 |
The total effective rate of 3 treatment groups has statistical significance compared with matched group, p<0.05, the total effective rate of 3 treatment groups compares each other, no difference of science of statistics, p>0.05, result is known thus, pharmaceutical composition of the present invention is used for the preparation of liquid preparation, gel, unguentum, can not affect the therapeutic effect of described pharmaceutical composition to tinea manus and pedis.
To sum up, pharmaceutical composition of the present invention is obviously better than matched group for the therapeutic effect of tinea manus and pedis, and compared to the treatment of Western medicine, pharmaceutical composition of the present invention has no side effect, and therapeutic effect total effective rate can reach 100%, and without recurrence.
Claims (6)
1. treat a pharmaceutical composition for fungal infection, it is characterized in that, constituent and the content thereof of described pharmaceutical composition comprise with parts by weight: serine 15 ~ 40 parts, glycine 20 ~ 45 parts, uracil 10 ~ 35 parts, dopamine 1 ~ 20 part.
2. pharmaceutical composition according to claim 1, is characterized in that, constituent and the content thereof of described pharmaceutical composition comprise with parts by weight: serine 30 ~ 40 parts, glycine 30 ~ 38 parts, uracil 16 ~ 23 parts, dopamine 8 ~ 15 parts.
3. pharmaceutical composition according to claim 1, is characterized in that, constituent and the content thereof of described pharmaceutical composition comprise with parts by weight: serine 35 parts, glycine 35 parts, uracil 20 parts, dopamine 10 parts.
4. the pharmaceutical composition according to claims 1 to 3 any one, is characterized in that, described pharmaceutical composition can add pharmaceutically acceptable adjuvant when needed.
5. the application of the pharmaceutical composition described in a Claims 1 to 4 any one in preparation treatment tinea manus and pedis medicine.
6. application according to claim 5, is characterized in that, the dosage form of described medicine can be liquid preparation, gel or unguentum.
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CN114272246A (en) * | 2021-12-14 | 2022-04-05 | 暨南大学 | Application of uracil in preparing anti-infective medicine |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1771930A (en) * | 2005-10-19 | 2006-05-17 | 浙江杭康海洋生物药业有限公司 | Externally applied compound amino acid prepn for promoting wound healing and its prepn and application |
CN104623037A (en) * | 2015-02-14 | 2015-05-20 | 淄博夸克医药技术有限公司 | Medicine for treating tinea manus and pedis |
-
2016
- 2016-02-04 CN CN201610076763.3A patent/CN105560248A/en active Pending
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1771930A (en) * | 2005-10-19 | 2006-05-17 | 浙江杭康海洋生物药业有限公司 | Externally applied compound amino acid prepn for promoting wound healing and its prepn and application |
CN104623037A (en) * | 2015-02-14 | 2015-05-20 | 淄博夸克医药技术有限公司 | Medicine for treating tinea manus and pedis |
Non-Patent Citations (1)
Title |
---|
马元龙 等: "12种氨基酸对五种致病性真菌生长及形态变化的观察", 《中国皮肤性病学杂志》 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN114272246A (en) * | 2021-12-14 | 2022-04-05 | 暨南大学 | Application of uracil in preparing anti-infective medicine |
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