CN1528328A - Complex external medicine for treating acne - Google Patents
Complex external medicine for treating acne Download PDFInfo
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- CN1528328A CN1528328A CNA031583830A CN03158383A CN1528328A CN 1528328 A CN1528328 A CN 1528328A CN A031583830 A CNA031583830 A CN A031583830A CN 03158383 A CN03158383 A CN 03158383A CN 1528328 A CN1528328 A CN 1528328A
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Abstract
The present invention relates to a compound medicine for external application for curing acne. Its composition contains the following two active components: (wt%) 0.01-2% of tazarotene and 0.25-5% of antimicrobial. Said compound medicine can be made into emulsifiable paste or gel or liniment or film preparation. Said compound medicine has the following therapeutic functions: dissolving keratotic plug, regulating keratosis, resisting microbe, relieving inflammation and reducing secondary factor of sebaceous secretion, so that it can obtain obvious therapeutic effect.
Description
Technical field:
The present invention relates to a kind of external used medicine for the treatment of acne, especially a kind of compound external-use medicine for the treatment of acne.
Background technology:
Acne is the sebaceous gland chronic disease, can be divided into inflammatory and non-inflammatory acne two classes, is the second largest commonly encountered diseases of department of dermatologry, and sickness rate accounts for dermatosis 7～10%, and sicken age covered between 11～30 years old, and the men and women all can suffer from.
Existing known following four kinds of pathogenic factorss and link play a crucial role in acne takes place, develops and lapses to: 1, the microbial action in hair follicle and the sebaceous gland unit, it at first is anaerobic propanoic acid Propiobacterium, inferior is advantage suppuration bacterium such as aerobic epidermis and staphylococcus aureus, has the Saccharomycodes of thinking also to participate in morbidity; 2, androgen and sebaceous gland hyperfunctioning, the former comprises that androgen one receptor affinity increases and/or the 5a-reductase activity strengthens, and highly active 2H-testosterone is increased; The latter refers to that mainly the sebaceous hyperplasia of androgen-dependent and sebum secretion increase; 3, abnormal cornification of pilosebaceous duct finally causes the follicular orifice acne to form and the cutin thromboembolism, and brings out and aggravates inflammation; 4, the breaking-up of the startup of inflammation and Pilo-Sebaceous inflammation.
Medicine is the main means of treatment seat skin ulcer, and the medicine of anti-acne is the focus of domestic and international dermatology drug research, its action principle mainly around and at above-mentioned morbidity link.Medicine anti-acne subsystem and local two kinds of approach, topical therapeutic is primarily aimed at slight acne and participates in the moderate remedy of acne, and severe acne also needs topical therapeutic to be cooperated under the prerequisite of composite treatment.For the main rule of treatment of acne be antibiotic, disappear light; For the main rule of treatment of non-inflammatory acne is the dissolving acne.
The medicine of existing treatment acne mostly is folk prescription, acts on more single.The medicine that for example is primarily aimed at acne mostly is antibiotic, comprises erythromycin, clindamycin (comprising phosphate and hydrochlorate), chloromycetin, mainly plays antibacterial action, has antiinflammatory action concurrently; And the medicine that is primarily aimed at non-inflammatory acne has tretinoin, benzoyl peroxide, salicylic acid, lactic acid etc., and wherein benzoyl peroxide has very strong antibacterial action simultaneously.
The subject matter that folk prescription treatment exists is that effect is single, at most can only be at 1-2 the link of falling ill (as the antibiotic antiinflammatory that adds, or antibiotic add anti-keratotic plug).In addition, the molten angle of above-mentioned acne medicine has local excitation and/or irritated effect more, and benzoyl peroxide has strong oxidation, as form compound preparation, quality is difficult for stable, makes compatibe drug concentration, the curative effect fluctuation, aspects such as preservation condition, shelf-life and ease of use all are a greater impact.
Summary of the invention:
The objective of the invention is to: the problem that exists in the single preparations of ephedrine use at the treatment acne provides a kind of new compound external-use medicine that cures mainly acne.
The object of the present invention is achieved like this: a kind of compound external-use medicine for the treatment of acne is characterized in that: contain following effective active composition (percentage by weight) in the medium carrier of compound external-use medicine: tazarotene 0.01～2%, antimicrobial drug 0.25～5%.
The tretinoin medicines topical application is effective anti-acne medicine, the part is applicable to gently, the moderate acne, and its action principle makes hair follicle-sebaceous gland inflammation be able to drain for the dissolving acne, be unfavorable for anaerobe growth, make medicine be easy to penetrate in the pilosebaceous unit to press down, bactericidal action to strengthen.Also scalable epithelial cell differentiation reduces the antiinflammatory action that keratotic plug forms and anti-leukocyte chemotaxis is arranged simultaneously.
Tazarotene is that with the advantage that first generation tretinoin medicines is compared receptor-selective is strong, and target site is clear and definite, stability is better, and topical application mainly retains in skin, and metabolism is rapid, percutaneous penetrates in the system hardly, and the local skin zest is lighter relatively, does not almost have systemic adverse reactions.
The common feature of the antibacterials of selecting for use in this compound recipe is: these medicines are to relevant The main pathogenic fungi such as anaerobism propanoic acid Propiobacterium and the aerobic skin suppuration bacterium (staphylococcus aureus of acne morbidity, staphylococcus epidermidis, inhibitory action streptococcus etc.) is all arranged, thereby alleviate and eliminate the infection link of morbidity.
In addition, this seminar has found that selected antibacterials are in the antimicrobial while, also has the leukocyte chemotaxis of inhibition activity, this is to the release of inflammation-inhibiting medium, alleviate disorganization, reducing stimulates the sebum secretion inducement, the startup and the development of blocking-up acne inflammation link, and the clinical inflammatory symptom of mitigate acne plays an important role.
This shows, the invention has the advantages that: the present invention is the main constituent that comprises tretinoin and anti-microbial type two classes treatment acne with the compound preparation form, complementation and synergism on the pharmacology, have been brought into play with the curative effect effect of bringing into play 3 kinds (and more than) simultaneously (dissolution angular embolization, regulate keratinization, antimicrobial, anti-inflammatory, alleviate the secondary factor of sebum secretion etc.), make therapeutical effect more comprehensively, deeply, curative effect is more satisfied.
The specific embodiment:
Below the nonrestrictive part embodiment that the present invention relates to that exemplified.
Embodiment 1:
The effective active composition of present embodiment adopts tazarotene 0.1% (percentage by weight, together following) and hydrochloric acid (or phosphoric acid) clindamycin 1%, medium carrier adopts hexadecanol, vaseline, liquid paraffin, glyceryl monostearate, glycerol, solubilizing agent, emulsifying agent, ethyl hydroxybenzoate and distilled water.
Embodiment 2:
The effective active composition of present embodiment adopts tazarotene 0.05% and erythromycin 2%, and medium carrier adopts hexadecanol, vaseline, liquid paraffin, glyceryl monostearate, glycerol, solubilizing agent, emulsifying agent, ethyl hydroxybenzoate and distilled water.
Embodiment 3:
Earlier the ethyl hydroxybenzoate with two kinds of effective active compositions among embodiment 1 or the embodiment 2 and 0.1% is dissolved in the solubilizing agent; Again the hexadecanol of total amount 8～12%, the vaseline of total amount 5～10%, the liquid paraffin of total amount 8～12%, the glyceryl monostearate and an amount of emulsifier of total amount 5～10% are heated to 80～85 ℃; The glycerol of total amount 0.5～5% and an amount of distilled water are mixed and heated to 80～85 ℃, and with the mixture mixing and emulsifying of itself and above-mentioned hexadecanol, vaseline, liquid paraffin, glyceryl monostearate and emulsifying agent; Mixture after the emulsifying is left thermal source, stir when being cooled to 65 ℃, add the solubilizing agent that is dissolved with two kinds of effective active compositions and ethyl hydroxybenzoate, the formation emulsifiable paste stirs.
Embodiment 4:
The effective active composition of present embodiment adopts tazarotene 0.1 and chloromycetin 0.5%, and medium carrier adopts carbomer, ethanol, propylene glycol, EDTA-2Na, ethyl hydroxybenzoate, nertralizer and distilled water.
Embodiment 5:
The effective active composition of present embodiment adopts tazarotene 0.025% and tetracycline 2%, and medium carrier adopts carbomer, ethanol, propylene glycol, EDTA-2Na, ethyl hydroxybenzoate, nertralizer and distilled water.
Embodiment 6:
Earlier two kinds of effective active compositions among embodiment 4 or the embodiment 5 are dissolved in the ethanol of total amount 5～20%, the ethyl hydroxybenzoate of total amount 0.1% is dissolved in the propylene glycol of total amount 0.01～2%; The EDTA-2Na that adds total amount 0.05～2% with an amount of distilled water dissolves, and the carbomer that adds total amount 1～10% is swelled into glue; With stirring in the above-mentioned solution adding colloidal sol, with an amount of nertralizer pH value is transferred to 5～7, the formation gel stirs.
Embodiment 7:
The effective active composition of present embodiment adopts tazarotene 0.05% and metronidazole 2%, and medium carrier adopts glycerol, cosolvent, azone, antioxidant and ethanol.
Embodiment 8:
The effective active composition of present embodiment adopts tazarotene 0.025% and tinidazole 1%, and medium carrier adopts glycerol, cosolvent, azone, antioxidant and ethanol.
Embodiment 9:
The effective active composition of present embodiment adopts tazarotene 0.05% and secnidazole 2%, and medium carrier adopts glycerol, cosolvent, azone, antioxidant and ethanol.
Embodiment 10:
Earlier two kinds of effective active compositions among embodiment 7 or embodiment 8 or the embodiment 9 are dissolved in an amount of cosolvent, and the glycerol of total amount 10～15%, an amount of azone, antioxidant is dissolved in the adequate amount of ethanol, after treating all the components dissolving, add the gross weight of adequate amount of ethanol until pharmaceutical preparation again, the formation liniment stirs.
Embodiment 11:
The effective active composition of present embodiment adopts tazarotene 0.05% and ofloxacin 0.5%, and medium carrier adopts solubilizing agent, glycerol, film former and distilled water.
Embodiment 12:
The effective active composition of present embodiment adopts tazarotene 0.025% and ciprofloxacin 0.5%, and basic total amount matter carrier adopts solubilizing agent, glycerol, film former and distilled water.
Embodiment 13:
Earlier two kinds of effective active compositions among the embodiment 10 are dissolved in the solubilizing agent; With an amount of distilled water film former is swelled into the glycerol mixing that gluey back adds total amount 5～30%, to be dissolved with the solubilizing agent of two kinds of effective active compositions adds in the swollen jelly, add the gross weight of an amount of distilled water until pharmaceutical preparation again, the formation liniment stirs.
Claims (3)
1, a kind of compound external-use medicine for the treatment of acne is characterized in that: contain following effective active composition (percentage by weight) in the medium carrier of compound external-use medicine: tazarotene 0.01～2%, antimicrobial drug 0.25～5%.
2, the compound external-use medicine of treatment acne according to claim 1, it is characterized in that: antimicrobial drug in the effective active composition that contains in the described medium carrier and content thereof are Clindamycin Hydrochloride 0.5～2%, or clindamycin phosphate 0.5～2%, or erythromycin 0.5～5%, or chloromycetin 0.25～2%, or tetracycline 0.25～2.5%, or metronidazole 0.5～5%, or tinidazole 0.5～5%, or secnidazole 0.5～5%, or ofloxacin 0.2～2%, or ciprofloxacin 0.2～2%.
3, the compound external-use medicine of treatment acne according to claim 1 is characterized in that: two kinds of effective active compositions that described compound external-use medicine contains form emulsifiable paste or gel or liniment or liniment with after medium carrier mixes.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03158383 CN1210041C (en) | 2003-09-29 | 2003-09-29 | Complex external medicine for treating acne |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03158383 CN1210041C (en) | 2003-09-29 | 2003-09-29 | Complex external medicine for treating acne |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1528328A true CN1528328A (en) | 2004-09-15 |
| CN1210041C CN1210041C (en) | 2005-07-13 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03158383 Expired - Lifetime CN1210041C (en) | 2003-09-29 | 2003-09-29 | Complex external medicine for treating acne |
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| Country | Link |
|---|---|
| CN (1) | CN1210041C (en) |
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102595892A (en) * | 2009-07-16 | 2012-07-18 | 施泰福实验室股份有限公司 | Tazarotene derivatives |
| CN102600196A (en) * | 2012-02-21 | 2012-07-25 | 江苏圣宝罗药业有限公司 | Externally applied medicine composition for treating common acne |
| 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 |
| CN103405781A (en) * | 2013-08-26 | 2013-11-27 | 江苏圣宝罗药业有限公司 | Pharmaceutical composition of compound clindamycin and tazarotene lipid complex |
| CN104138353A (en) * | 2013-09-05 | 2014-11-12 | 江苏中丹制药有限公司 | Tazarotene gelata and preparation method thereof |
| CN107468637A (en) * | 2016-06-08 | 2017-12-15 | 厦门恩成制药有限公司 | Compound tazarotene urea external preparation and preparation method thereof |
| US9949996B2 (en) | 2011-06-24 | 2018-04-24 | Gri Bio, Inc. | Prevention and treatment of inflammatory conditions |
| WO2018209262A1 (en) * | 2017-05-12 | 2018-11-15 | Valeant Pharmaceuticals North America | Topical compositions and methods for treating skin diseases |
| US10426787B2 (en) | 2015-06-18 | 2019-10-01 | Bausch Health Us, Llc | Topical compositions and methods for treating psoriasis |
| US11311482B2 (en) | 2017-05-12 | 2022-04-26 | Bausch Health Us, Llc | Topical compositions and methods for treating skin diseases |
-
2003
- 2003-09-29 CN CN 03158383 patent/CN1210041C/en not_active Expired - Lifetime
Cited By (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102595892A (en) * | 2009-07-16 | 2012-07-18 | 施泰福实验室股份有限公司 | Tazarotene derivatives |
| RU2678561C2 (en) * | 2011-06-24 | 2019-01-30 | ДжиАрАй Био, Инк. | Prevention and treatment of inflammatory conditions |
| US11660309B2 (en) | 2011-06-24 | 2023-05-30 | Gri Bio, Inc. | Prevention and treatment of inflammatory conditions |
| US10925886B2 (en) | 2011-06-24 | 2021-02-23 | Gri Bio, Inc. | Prevention and treatment of inflammatory conditions |
| US9949996B2 (en) | 2011-06-24 | 2018-04-24 | Gri Bio, Inc. | Prevention and treatment of inflammatory conditions |
| RU2678561C9 (en) * | 2011-06-24 | 2019-03-05 | ДжиАрАй Био, Инк. | Prevention and treatment of inflammatory conditions |
| CN102600196A (en) * | 2012-02-21 | 2012-07-25 | 江苏圣宝罗药业有限公司 | Externally applied medicine composition for treating common acne |
| CN102600196B (en) * | 2012-02-21 | 2013-03-27 | 江苏圣宝罗药业有限公司 | Externally applied medicine composition for treating common acne |
| 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 |
| CN103405781A (en) * | 2013-08-26 | 2013-11-27 | 江苏圣宝罗药业有限公司 | Pharmaceutical composition of compound clindamycin and tazarotene lipid complex |
| CN104138353A (en) * | 2013-09-05 | 2014-11-12 | 江苏中丹制药有限公司 | Tazarotene gelata and preparation method thereof |
| CN104138353B (en) * | 2013-09-05 | 2016-06-22 | 江苏中丹制药有限公司 | A kind of Tazarotene gel agent and preparation method thereof |
| US10426787B2 (en) | 2015-06-18 | 2019-10-01 | Bausch Health Us, Llc | Topical compositions and methods for treating psoriasis |
| AU2016279801B2 (en) * | 2015-06-18 | 2021-09-09 | Valeant Pharmaceuticals North America | Topical compositions comprising a corticosteroid and a retinoid for treating psoriasis |
| US11648256B2 (en) | 2015-06-18 | 2023-05-16 | Bausch Health Ireland Limited | Topical compositions and methods for treating psoriasis |
| US11679116B2 (en) | 2015-06-18 | 2023-06-20 | Bausch Health Ireland Limited | Topical compositions and methods for treating psoriasis |
| US11679115B2 (en) | 2015-06-18 | 2023-06-20 | Bausch Health Ireland Limited | Topical compositions and methods for treating psoriasis |
| CN107468637A (en) * | 2016-06-08 | 2017-12-15 | 厦门恩成制药有限公司 | Compound tazarotene urea external preparation and preparation method thereof |
| WO2018209262A1 (en) * | 2017-05-12 | 2018-11-15 | Valeant Pharmaceuticals North America | Topical compositions and methods for treating skin diseases |
| JP2020519656A (en) * | 2017-05-12 | 2020-07-02 | ボシュ ヘルス ユーエス，エルエルシー． | Topical compositions and methods for treating skin disorders |
| US11311482B2 (en) | 2017-05-12 | 2022-04-26 | Bausch Health Us, Llc | Topical compositions and methods for treating skin diseases |
| JP7410720B2 (en) | 2017-05-12 | 2024-01-10 | ボシュ ヘルス アイルランド リミテッド | Topical compositions and methods for treating skin diseases |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1210041C (en) | 2005-07-13 |
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Effective date of registration: 20191216 Address after: 518000 1 Guanqing Road, Guanlan high tech park, Guanhu street, Longhua District, Shenzhen, Guangdong Patentee after: CHINA RESOURCES SANJIU MEDICAL & PHARMACEUTICAL Co.,Ltd. Address before: 210042, Chiang Kai Shek temple, Xuanwu District, Jiangsu, Nanjing 100 Patentee before: Institute of Dermatology, Chinese Academy of Medical Sciences |
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| CX01 | Expiry of patent term | ||
| CX01 | Expiry of patent term |
Granted publication date: 20050713 |