CN1528327A - Complex external medicine speical for acne and preparing method thereof - Google Patents
Complex external medicine speical for acne and preparing method thereof Download PDFInfo
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- CN1528327A CN1528327A CNA031583822A CN03158382A CN1528327A CN 1528327 A CN1528327 A CN 1528327A CN A031583822 A CNA031583822 A CN A031583822A CN 03158382 A CN03158382 A CN 03158382A CN 1528327 A CN1528327 A CN 1528327A
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Abstract
The present invention relates to a compound medicine for external application for curing acne and its preparation method. Its composition contains the following two active components: (wt%) 0.01-2% of tretinoin and 0.25-5% of antimicrobial. Said compound medicine can be made into liniment or anhydrous ointment, and 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 of specially controlling acne and preparation method thereof.
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, 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 of specially controlling acne.
The object of the present invention is achieved like this: a kind of compound external-use medicine of specially controlling acne is characterized in that: contain following effective active composition (percentage by weight) in the medium carrier of compound external-use medicine: tretinoin 0.01～2%, antimicrobial drug 0.25～5%.
The preparation method of described compound external-use medicine is: described two kinds of effective active compositions are dissolved in an amount of cosolvent, and 10～15% glycerol, an amount of azone, antioxidant is dissolved in the adequate amount of ethanol, after treating all the components dissolving, add adequate amount of ethanol again, two kinds of effective active compositions meet the percentage by weight of claim 1 in medicine, and the formation liniment stirs.
The preparation method of described compound external-use medicine can also be: described two kinds of effective active compositions are dissolved in 5～10% the ethanol stand-by; Liquid paraffin with 5～10%, 8～15% wool grease, an amount of emulsifying agent, an amount of antioxidant and vaseline are mixed and heated to 70 ℃; After propylene glycol with 10～20% is heated to 70 ℃, the mixture that adds liquid paraffin, wool grease, emulsifying agent, antioxidant and vaseline stirs, to be cooled during to 60 ℃, add the ethanol that is dissolved with two kinds of effective active compositions, use an amount of vaseline at last, two kinds of effective active compositions meet the percentage by weight of claim 1 in medicine,, restir evenly forms anhydrous ointment.
Tretinoin is known anti-acne active drug.First generation external preparation is mainly alltrans tretinoin and 13 along tretinoin.Topical application is applicable to gently, the moderate acne, is primarily aimed at the hair follicle keratotic plug, and is effective to non-inflammatory acne.It dissolves blackhead, makes the pilosebaceous unit inflammation be able to drain, is unfavorable for anaerobe growth, and make antibacterials be easy to penetrate in the pilosebaceous unit to press down to strengthen, bactericidal action.In addition, alltrans tretinoin itself also has anti-leukocyte chemotaxis activity.Its shortcoming is the skin irritation that has concentration to rely on, and the individual tolerance difference, but under clinical working concentration, generally can be accepted by patient.
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.
Tretinoin has selected for use first generation product alltrans tretinoin or 13 to form compound recipe along tretinoin with different antibacterials among the present invention, and first generation tretinoin raw material is easy to get low price.
Preparation of the present invention is liniment or anhydrous ointment, overcome first generation tretinoin unsettled shortcoming in aqueous solution, clinic trial proves, affinity, stretchability, easy cleaning, the comfortableness of it and skin are all accepted by doctor and patient, and the shelf-life is obviously long than gel preparation.
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 alltrans tretinoin 0.025% (percentage by weight, down together) and Clindamycin Hydrochloride 1%, and medium carrier adopts glycerol, cosolvent, azone, antioxidant and ethanol.
Embodiment 2:
The effective active composition of present embodiment adopts 13 along tretinoin 0.025% and erythromycin 2%, and medium carrier adopts glycerol, cosolvent, azone, antioxidant and ethanol.
Embodiment 3:
The effective active composition of present embodiment adopts alltrans tretinoin 0.025% and chloromycetin 1%, and medium carrier adopts glycerol, cosolvent, azone, antioxidant and ethanol.
Embodiment 4:
The effective active composition of present embodiment adopts 13 along tretinoin 0.03% and tetracycline 2%, and medium carrier adopts glycerol, cosolvent, azone, antioxidant and ethanol.
Embodiment 5:
Earlier two kinds of effective active compositions among embodiment 1 or embodiment 2 or embodiment 3 or the embodiment 4 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 adequate amount of ethanol again until the gross weight of pharmaceutical preparation (make two kinds of effective active compositions meet its percentage by weight in the medicine), the formation liniment stirs.
Embodiment 6:
The effective active composition of present embodiment adopts alltrans tretinoin 0.025% and metronidazole 0.75%, and medium carrier adopts liquid paraffin, wool grease, emulsifying agent, antioxidant, ethanol, propylene glycol and vaseline.
Embodiment 7:
The effective active composition of present embodiment adopts 13 along tretinoin 0.025% and tinidazole 1%, and medium carrier adopts liquid paraffin, wool grease, emulsifying agent, antioxidant, ethanol, propylene glycol and vaseline.
Embodiment 8:
The effective active composition of present embodiment adopts alltrans tretinoin 0.05% and secnidazole 2%, and medium carrier adopts liquid paraffin, wool grease, emulsifying agent, antioxidant, ethanol, propylene glycol and vaseline.
Embodiment 9:
The effective active composition of present embodiment adopts 13 along tretinoin 0.025% and ofloxacin 0.3%, and medium carrier adopts liquid paraffin, wool grease, emulsifying agent, antioxidant, ethanol, propylene glycol and vaseline.
Embodiment 10:
The effective active composition of present embodiment adopts alltrans tretinoin 0.05% and ciprofloxacin 0.5%, and medium carrier adopts liquid paraffin, wool grease, emulsifying agent, antioxidant, ethanol, propylene glycol and vaseline.
Embodiment 11:
Earlier two kinds of effective active compositions among embodiment 6 or embodiment 7 or embodiment 8 or embodiment 9 or the embodiment 10 are dissolved in the ethanol of total amount 5～10% stand-by; The liquid paraffin of total amount 5～10%, the wool grease of total amount 8～15%, an amount of emulsifying agent, an amount of antioxidant and vaseline are mixed and heated to 70 ℃; After the propylene glycol of total amount 10～20% is heated to 70 ℃, the mixture that adds liquid paraffin, wool grease, emulsifying agent, antioxidant and vaseline stirs, to be cooled during to 60 ℃, add the ethanol that is dissolved with two kinds of effective active compositions, transfer to the gross weight (make two kinds of effective active compositions meet its percentage by weight in the medicine) of pharmaceutical preparation at last with an amount of vaseline, restir evenly forms anhydrous ointment.
Claims (5)
1, a kind of compound external-use medicine of specially controlling acne is characterized in that: contain following effective active composition (percentage by weight) in the medium carrier of compound external-use medicine: tretinoin 0.01～2%, antimicrobial drug 0.25～5%.
2, the compound external-use medicine of specially controlling acne according to claim 1 is characterized in that: the tretinoin in the effective active composition that contains in the described medium carrier is that alltrans tretinoin or 13 is along tretinoin.
3, the compound external-use medicine of specially controlling 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 erythromycin 0.5～5%, or chloromycetin 0.25～0.5%, 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%.
4, the preparation method of the described compound external-use medicine of claim 1, it is characterized in that: described two kinds of effective active compositions 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 adequate amount of ethanol again, two kinds of effective active compositions meet the percentage by weight of claim 1 in medicine, and the formation liniment stirs.
5, the preparation method of the described compound external-use medicine of claim 1 is characterized in that: described two kinds of effective active compositions are dissolved in the ethanol of total amount 5～10% stand-by; The liquid paraffin of total amount 5～10%, 8～15% wool grease, an amount of emulsifying agent, an amount of antioxidant and vaseline are mixed and heated to 70 ℃; After the propylene glycol of total amount 10～20% is heated to 70 ℃, the mixture that adds liquid paraffin, wool grease, emulsifying agent, antioxidant and vaseline stirs, to be cooled during to 60 ℃, add the ethanol that is dissolved with two kinds of effective active compositions, use an amount of vaseline at last, two kinds of effective active compositions meet the percentage by weight of claim 1 in medicine, and restir evenly forms anhydrous ointment.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031583822A CN1528327A (en) | 2003-09-29 | 2003-09-29 | Complex external medicine speical for acne and preparing method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CNA031583822A CN1528327A (en) | 2003-09-29 | 2003-09-29 | Complex external medicine speical for acne and preparing method thereof |
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| CN1528327A true CN1528327A (en) | 2004-09-15 |
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| CNA031583822A Pending CN1528327A (en) | 2003-09-29 | 2003-09-29 | Complex external medicine speical for acne and preparing method thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101884642A (en) * | 2010-07-30 | 2010-11-17 | 哈尔滨乐泰药业有限公司 | Compound emulsifiable paste for treating acne and preparation method thereof |
| CN105997850A (en) * | 2016-08-01 | 2016-10-12 | 朱玉水 | Externally applied ointment for treating acnes and preparation method thereof |
| CN106727283A (en) * | 2016-12-26 | 2017-05-31 | 侯俊领 | It is a kind of to treat metronidazole erythromycin compound ointment of face acnes and preparation method thereof |
| CN111803652A (en) * | 2020-08-04 | 2020-10-23 | 北京瀚梅生物科技有限公司 | Use of a compound for treating acne in the preparation of a pharmaceutical or cosmetic composition for treating acne |
-
2003
- 2003-09-29 CN CNA031583822A patent/CN1528327A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101884642A (en) * | 2010-07-30 | 2010-11-17 | 哈尔滨乐泰药业有限公司 | Compound emulsifiable paste for treating acne and preparation method thereof |
| CN105997850A (en) * | 2016-08-01 | 2016-10-12 | 朱玉水 | Externally applied ointment for treating acnes and preparation method thereof |
| CN106727283A (en) * | 2016-12-26 | 2017-05-31 | 侯俊领 | It is a kind of to treat metronidazole erythromycin compound ointment of face acnes and preparation method thereof |
| CN106727283B (en) * | 2016-12-26 | 2019-06-14 | 侯俊领 | A kind of metronidazole erythromycin compound ointment and preparation method thereof for treating face acnes |
| CN111803652A (en) * | 2020-08-04 | 2020-10-23 | 北京瀚梅生物科技有限公司 | Use of a compound for treating acne in the preparation of a pharmaceutical or cosmetic composition for treating acne |
| CN111803652B (en) * | 2020-08-04 | 2021-09-14 | 南通康是美生物科技有限公司 | Use of a compound for treating acne in the preparation of a pharmaceutical or cosmetic composition for treating acne |
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