CN1518985A - A group of medication compsn. for treating acne - Google Patents
A group of medication compsn. for treating acne Download PDFInfo
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- CN1518985A CN1518985A CNA03115154XA CN03115154A CN1518985A CN 1518985 A CN1518985 A CN 1518985A CN A03115154X A CNA03115154X A CN A03115154XA CN 03115154 A CN03115154 A CN 03115154A CN 1518985 A CN1518985 A CN 1518985A
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Abstract
A composite medicine for treating acne is prepared from Adapalin, antibiotic and/or cortin or azelein acid or cimetidine or benzoyl peroxide or tanshinone IIA or metronidazole or tinidazole, and excipient. Its advantage is high curative effect.
Description
Technical field
The drug regimen that the present invention relates to have medical application is more specifically said so and is contained the pharmaceutical composition that is used for the treatment of acne that adapalene and antibiotics and/or 17-hydroxy-11-dehydrocorticosterone are formed.
Background technology
Acne is commonly called as acne, is a kind of common hair follicle, the chronic inflammatory diseases of sebaceous gland.Its pathogenic factor has several factors, and it is generally acknowledged that main cause has: the adolescence androgen secretion increases, and causes the sebaceous gland enlargement, and smegma increases, and makes hair follicle, sebaceous gland conduit keratinization thromboembolism, and sebum deposits and forms fat bolt, i.e. acne in hair follicle.Under anaerobic environment, anaerobe such as propionibacterium acnes are bred in a large number, produce fat dissolving enzyme, separate sebum and produce free acid, hair follicle stimulating causes inflammation, and causes the follicular wall damage to be broken, make the sebum of alluvial enter intradermal, thereby cause the hair follicle inflammatory reaction of varying degree on every side.In addition, dyshormonia, greasiness polysaccharide and zest diet, high temperature and some chemical factor also have certain effect to the generation of acne and development.
Adapalene is a kind flavol chemical compound, for third generation retinoid medicine, has acne dissolving, antiproliferative and antiinflammatory action.Its mechanism of action is optionally in conjunction with retinoic acid nuclear receptor γ (RAR γ), directly regulates the final differentiation of epithelial cells, does not act on Cytoplasm retinoic acid conjugated protein (CRABP), more fast and effeciently acts on the keratinization adjustment process.By regulating the differentiation of follicular epithelium cell, reduce the formation of micropowder thorn and bring into play the effect of treatment acne.Adapalene chemical name: 6-[3-(1-adamantyl)-4-methoxyphenyl]-the 2-naphthoic acid (6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid), chemical structural formula:
Because the occurrence factor of acne is many-sided, the means of clinical drug therapy also are many-sided.The main at present medicine that uses has the external folk prescription or the compound preparation of antibiotic, retinoid medicine, estrogen, 17-hydroxy-11-dehydrocorticosterone, trace element and antifungal drug etc.At different symptoms and paathogenic factor, to unite the component of using different mechanism of action and constitute compound preparation, effect is better than single preparations of ephedrine.
The purpose of this invention is to provide one group of pharmaceutical composition that is used for the treatment of acne.All the other form for excipient said composition by adapalene and antibiotics and/or 17-hydroxy-11-dehydrocorticosterone, and the antibiotics of said composition indication is the medicine of anaerobe resistants such as erythromycin, chloromycetin, clindamycin, clindamycin phosphate and metronidazole, tinidazole.Form the compound external-use preparation when adapalene and antibiotics and comprise gel, cream, ointment, liniment and solution etc.
The pharmaceutical composition (percentage by weight) of treatment acne contains 0.01%-1% adapalene and antibiotics and/or 17-hydroxy-11-dehydrocorticosterone or Azelaic Acid or cimetidine or benzoyl peroxide or tanshinone or metronidazole or tinidazole, and all the other are excipient.
The content (percentage by weight) of adapalene composition is 0.01%-1% when preparing above-mentioned various external preparation, and optimum content is 0.1%.
Adapalene and following arbitrary topical antibiotic that is usually used in treating acne, be erythromycin, chloromycetin, clindamycin, clindamycin phosphate, and the medicine of anaerobe resistants such as metronidazole, tinidazole is formed the compound external-use preparation, be gel, cream, ointment, liniment and solution etc., be used for the part and be coated with the acne of liniment for treatment with anaerobic infection.In compound gel, cream, ointment, liniment and solution that one of adapalene and said medicine are formed, the concentration of adapalene is 0.01%-1%, and optium concentration is 0.1%.Correspondingly, erythromycin is during as the compound recipe composition, and its concentration is 1%-10%, and the best is 2% or 3%; Chloromycetin is during as the compound recipe composition, and its concentration is 1%-5%, and the best is 2%; Clindamycin hydrochloride is during as the compound recipe composition, and its concentration is 0.1%-5%, and the best is 1%; Clindamycin phosphate is during as the compound recipe composition, and its concentration is 0.1%-5%, and the best is 1%; Metronidazole is during as the compound recipe composition, and its concentration is 0.1%-5%, and the best is 1% or 2%; Tinidazole is during as the compound recipe composition, and its concentration is 0.1%-5%, and the best is 1% or 1.5%.
Form the compound external-use preparation when adapalene and 17-hydroxy-11-dehydrocorticosterone and comprise gel, cream, ointment, liniment and solution etc., 17-hydroxy-11-dehydrocorticosterone includes the compositions that dexamethasone, cortisone acetate, fludrocortisone, glycyrrhizic acid etc. are formed, can be used for serious acne treatment, for example tuberosity, cyst etc.The content of 17-hydroxy-11-dehydrocorticosterone composition (percentage by weight) is 0.01%-0.1%, and optimum content is 0.05%.
Still can add the 3rd component-corticosteroid hormone in the compound preparation that above-mentioned adapalene and antibacterials are formed, it is dexamethasone, cortisone acetate, fludrocortisone, glycyrrhizic acid etc., form serious acne treatments such as tuberosity, cyst, this type of the 3rd component concentrations is (percentage by weight) 0.01%-0.1%, and the best is 0.05%.
Adapalene can be formed the compound external-use preparation with Azelaic Acid, cimetidine, benzoyl peroxide, tanshinone and comprise gel, cream, ointment, liniment and solution etc., the content of adapalene composition (percentage by weight) is 0.01%-1%, and optimum content is 0.1%
When adapalene and Azelaic Acid composition compound recipe were used for the treatment of acne, the concentration of adapalene was 0.01%-1%, and optium concentration is 0.1%; The concentration of Azelaic Acid is (percentage by weight) 5%-30%, and the best is 20%.Make gel, cream and ointment.
When adapalene and cimetidine composition compound recipe were used for the treatment of acne, the concentration of adapalene was 0.01%-1%, and optium concentration is 0.1%; The concentration of cimetidine (percentage by weight) is 0.5%-5%, and the best is 2%.Make gel, cream, ointment, liniment and solution.
When adapalene and benzoyl peroxide composition compound recipe were used for the treatment of acne, the concentration of adapalene was 0.01%-1%, and optium concentration is 0.1%; The concentration of benzoyl peroxide is (percentage by weight) 1%-10%, and the best is 5%.Make gel, cream and ointment.
When adapalene and tanshinone composition compound recipe were used for the treatment of acne, the concentration of adapalene was 0.01%～1%, and optium concentration is 0.1%; The concentration of tanshinone is 0.1%-10%, and the best is 1%, 2%, 3%, 4%, 5%.Make gel, cream, ointment, liniment and solution.
Excipient commonly used is Acritamer 940, poloxamer, Macrogol 200, PEG400, Macrogol 2000, Macrogol 4000, polyethylene glycol 6000, water, 1,2-propylene glycol, glycerol, phenoxyethanol disodium edetate, methyl hydroxybenzoate, propylparaben, hard ester acid, glyceryl monostearate, paregal O, liquid paraffin, triethanolamine, Borax, sodium sulfite etc.
Pharmacological effect
In light, the moderate acne vulgaris patient in 15-30 year, random packet, carry out the clinical research of an adapalene folk prescription gel and compound recipe adapalene gel (containing adapalene 0.1% and clindamycin phosphate 1) contrast, compare, the patient carries out Heal Thyself under guidance, every day in the h.d. medication once, continuous 8 weeks.During the research, except that above-mentioned two preparations face uses, do not use other any topical therapeutic medicine.In the minimizing of acne lesion quantity, compound preparation especially significantly is better than single preparations of ephedrine to the inflammation damnification effect than single preparations of ephedrine significant effective.The mean percentage that damage quantity reduces after 8 weeks of treatment is summarised in the following table continuously:
| The mean percentage that 8 weeks damage quantity reduces | ||
| Effect changes | Group 1 | Group 2 |
| Adapalene N=15 | Adapalene+clindamycin phosphate N=18 | |
| Non-inflammation damnification | ????32％ | 34％ |
| Inflammation damnification | ????31％ | 55％ |
| Total damage | ????31％ | 45％ |
Beneficial effect of the present invention:
1, because the acne occurrence cause is many-sided, therefore when clinical treatment, adopt different prescription adapalenes and other antibiotics and/or 17-hydroxy-11-dehydrocorticosterone to make external preparation according to pathogenic factor, with strong points, therapeutic effect is good.
2, adopt external more convenient, just focus is had effect, very little to other position effects of health.
3, medicine and excipient all are to buy than being easier to.
Specific embodiment
The compound gel of example 1. adapalenes and erythromycin
Prescription (making 1000g)
Principal agent and supplementary product consumption (g) concentration (%)
Adapalene 1.00g 0.1%
Erythromycin 20.0g 2.0%
Acritamer 940 10.0g
Poloxamer 10.0g
1,2-propylene glycol 82.5g
Phenoxyethanol 2.50g
Sodium hydroxide 2.00g
Disodium edetate 0.10g
Methyl hydroxybenzoate 1.0g
Water 861g
Preparation technology
1. supplementary material is prepared: principal agent adapalene and erythromycin are crossed 100 mesh sieves, and carbomer is standby in 80 ℃ of vacuum dryings 1 hour.
2. the carbomer of getting recipe quantity adds water 500g, stirs fast 30 minutes, leaves standstill 30 minutes.
3. the poloxamer of getting recipe quantity adds phenoxyethanol again in propylene glycol, make into solution after, add the adapalene and the erythromycin of recipe quantity, stirred 20 minutes, add in the lump in above-mentioned (step 2) solution, stirred mix homogeneously 20 minutes.
4. the sodium hydroxide of getting recipe quantity adds water to 50ml, makes dissolving, shakes up, and adds disodium edetate, and jolting makes dissolving, adds to above-mentionedly (in the step 3) solution, to stir mix homogeneously 10 minutes.
5. the methyl hydroxybenzoate of getting recipe quantity adds water 200g, and heating (60 ℃) makes dissolving, adds to after the cooling above-mentionedly (in the step 4) solution, to add the water of residue recipe quantity, stirred 10 minutes, make even.
6. the degassing.
7. measure the content and the pH value of intermediate.
8. be loaded in the flexible pipe of 15 gram specifications, loading amount is that 10g/ props up.
The compound gel of example 2. adapalenes and clindamycin phosphate
Prescription (making 1000g)
Principal agent and supplementary product consumption (g) concentration (%)
Adapalene 1.00g 0.1%
Clindamycin phosphate 10.0g 1.0%
Acritamer 940 10.0g
Poloxamer 10.0g
1,2-propylene glycol 82.5g
Phenoxyethanol 2.50g
Sodium hydroxide 2.00g
Disodium edetate 0.10g
Methyl hydroxybenzoate 1.0g
Water 881g
Preparation technology: with example 1.
The compound gel of example 3. adapalenes and benzoyl peroxide
Prescription (making 1000g)
Principal agent and supplementary product consumption (g) concentration (%)
Adapalene 1.00g 0.1%
Benzoyl peroxide 50.0g 5.0%
Acritamer 940 10.0g
Poloxamer 10.0g
1,2-propylene glycol 82.5g
Phenoxyethanol 2.50g
Sodium hydroxide 2.00g
Disodium edetate 0.10g
Methyl hydroxybenzoate 1.0g
Water 841g
Preparation technology: with example 1.
The compound gel of example 4. adapalenes and Azelaic Acid
Prescription (making 1000g)
Principal agent and supplementary product consumption (g) concentration (%)
Adapalene 1.00g 0.1%
Azelaic Acid 100.0g 10.0%
Acritamer 940 10.0g
Poloxamer 10.0g
1,2-propylene glycol 82.5g
Phenoxyethanol 2.50g
Sodium hydroxide 2.00g
Disodium edetate 0.10g
Methyl hydroxybenzoate 1.0g
Water 791g
Preparation technology: the adding technology of adapalene is with example 1; Azelaic Acid dissolves in hot water earlier, adds mixing in people's remainder again, makes gel.
The compound recipe cream of example 5. adapalenes and cimetidine
Prescription (making 1000g)
Principal agent and supplementary product consumption (g) concentration (%)
Adapalene 1.0g 0.1%
Cimetidine 20.0g 2.0%
Hard ester acid 70g
Glyceryl monostearate 50g
Peregal o 17.7g
Liquid paraffin 122g
Glycerol 200g
Triethanolamine 24g
Borax 4g
Sodium sulfite 2g
Methyl hydroxybenzoate 0.25g
Propylparaben 0.18g
Disodium edetate 0.5g
Water 490g
Preparation technology:
1. supplementary material is prepared: liranaftate, cimetidine are standby in 60 ℃ of vacuum dryings.
2. hard ester acid, glyceryl monostearate, peregal o, the liquid paraffin of getting recipe quantity place in the oil phase pot, and heating in water bath to 85 ℃ makes thawing.The liranaftate and the cimetidine of recipe quantity are added in the oil phase pot, be stirred to dissolving fully, water-bath kept 5 minutes.
3. glycerol, the water of getting recipe quantity place in the water pot, in heating in water bath to 60 ℃.Again triethanolamine, Borax, sodium sulfite, methyl hydroxybenzoate, propylparaben, disodium edetate are added in the water pot, be stirred to dissolving fully, heating in water bath to 85 ℃.
4. earlier 1/3rd water is placed in the emulsifying pot, constant temperature adds oil phase, stirs, and slowly the water of remainder is added again, stirs rapidly.
5. be stirred to room temperature, the degassing, the content of mensuration ointment.Be loaded on after qualified in the flexible pipe of 10 gram specifications, loading amount is that 10g/ props up.
The compound recipe cream of example 6. adapalenes and tanshinone
Prescription (making 1000g)
Principal agent and supplementary product consumption (g) concentration (%)
Adapalene 1.0g 0.1%
Tanshinone 20.0g 2.0%
Hard ester acid 70g
Glyceryl monostearate 50g
Peregal o 17.7g
Liquid paraffin 122g
Glycerol 200g
Triethanolamine 24g
Borax 4g
Sodium sulfite 2g
Methyl hydroxybenzoate 0.25g
Propylparaben 0.18g
Disodium edetate 0.5g
Water 490g
Preparation technology is with example 5.
Claims (7)
1, the pharmaceutical composition (percentage by weight) of treatment acne contains 0.01%-1% adapalene and antibiotics and/or 17-hydroxy-11-dehydrocorticosterone or Azelaic Acid or cimetidine or benzoyl peroxide or tanshinone or metronidazole or tinidazole, and all the other are excipient.
2, pharmaceutical composition according to claim 1 is characterized in that wherein antibiotics component content (percentage by weight) is erythromycin 1%-10% or chloromycetin 1%-5% or clindamycin hydrochloride or clindamycin phosphate 0.1%-5% or metronidazole 0.1%-5% or tinidazole 0.1%-5%.
3, pharmaceutical composition according to claim 2 is characterized in that wherein antibiotics optimal components content (percentage by weight) is erythromycin 2% or 3%; Chloromycetin be 2% or clindamycin hydrochloride be 1% clindamycin phosphate be 1% or metronidazole be 1% or 2%; Or tinidazole is 1% or 1.5%.
4, pharmaceutical composition according to claim 1 is characterized in that wherein 17-hydroxy-11-dehydrocorticosterone is dexamethasone or cortisone acetate or fludrocortisone or glycyrrhizic acid.
5, pharmaceutical composition according to claim 4 is characterized in that 17-hydroxy-11-dehydrocorticosterone component content (percentage by weight) 0.01%-0.1%, and the best is 0.05%.
6, pharmaceutical composition according to claim 1 is characterized in that wherein (percentage by weight) Azelaic Acid 5%-20%, the best is 20%, or benzoyl peroxide (percentage by weight) 1%-10%, the best is 5%, or cimetidine (percentage by weight) 0.5%-5%, the best is 2%, or tanshinone (percentage by weight) 0.1%-10%, and the best is 1% or 2%.
7, pharmaceutical composition as claimed in claim 1 is used in the medicine of preparation treatment acne.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA03115154XA CN1518985A (en) | 2003-01-24 | 2003-01-24 | A group of medication compsn. for treating acne |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA03115154XA CN1518985A (en) | 2003-01-24 | 2003-01-24 | A group of medication compsn. for treating acne |
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| Publication Number | Publication Date |
|---|---|
| CN1518985A true CN1518985A (en) | 2004-08-11 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA03115154XA Pending CN1518985A (en) | 2003-01-24 | 2003-01-24 | A group of medication compsn. for treating acne |
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| CN (1) | CN1518985A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009050451A1 (en) * | 2007-10-15 | 2009-04-23 | Botanic Century (Beijing) Co. Ltd | Antibacterial composition comprising salvia extracts |
| CN103006681A (en) * | 2012-12-04 | 2013-04-03 | 哈尔滨乐泰药业有限公司 | Compound emulsifiable paste for treating acne and preparation method thereof |
| CN106729722A (en) * | 2016-11-21 | 2017-05-31 | 江苏山信药业有限公司 | A kind of method and compound preparation for preparing stabilization compound preparation |
-
2003
- 2003-01-24 CN CNA03115154XA patent/CN1518985A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009050451A1 (en) * | 2007-10-15 | 2009-04-23 | Botanic Century (Beijing) Co. Ltd | Antibacterial composition comprising salvia extracts |
| US20100292318A1 (en) * | 2007-10-15 | 2010-11-18 | Zhong Zhong | Antibacterial composition comprising salvia extracts |
| US9283256B2 (en) | 2007-10-15 | 2016-03-15 | Botanic Century (Beijing) Co. Ltd. | Antibacterial composition comprising Salvia extracts |
| CN103006681A (en) * | 2012-12-04 | 2013-04-03 | 哈尔滨乐泰药业有限公司 | Compound emulsifiable paste for treating acne and preparation method thereof |
| CN106729722A (en) * | 2016-11-21 | 2017-05-31 | 江苏山信药业有限公司 | A kind of method and compound preparation for preparing stabilization compound preparation |
| CN106729722B (en) * | 2016-11-21 | 2020-05-12 | 成都山信药业有限公司 | Method for preparing stable compound preparation and compound preparation |
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Open date: 20040811 |