CN1568978B - Composition for preventing and treating whelk - Google Patents
Composition for preventing and treating whelk Download PDFInfo
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- CN1568978B CN1568978B CN 03149550 CN03149550A CN1568978B CN 1568978 B CN1568978 B CN 1568978B CN 03149550 CN03149550 CN 03149550 CN 03149550 A CN03149550 A CN 03149550A CN 1568978 B CN1568978 B CN 1568978B
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- acne
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- metronidazole
- comedo
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Abstract
The invention relates to a composition for preventing and treating whelk, in particular the composition for preventing and treating acne / pimple.
Description
Invention field
The present invention relates to be used to prevent or treat the compositions of comedo, especially, be used for the treatment of or prevent compositions as acne and/or acne.
Background technology
Comedo (acne, acne) pilosity is born among the crowd of adolescence or oily skin.There are buccal, lower jaw and forehead in the good position of sending out, also sees shirtfront or back.What have is grain of rice shape, and what have is the pustule sample, and outbreak repeatedly is difficult to cure.Especially long acne at face has not only had a strong impact on attractive in appearancely, and has caused pressure mentally for adolescence, produces the psychology of feeling oneself inferior, even directly influences work, studying and living.
Modern medicine thinks that the genesis mechanism of acne and reason mainly contain the following aspects: 1, the adolescence hormone secretion is too much, and sebum secretion is hyperfunction, produces excessive oils and fats, fatty acid, cause sebaceous gland not smooth, hair follicle tube wall keratinization material increases and blocks the hair follicle hole, causes inflammation, and forms acne.
2, the hair follicle obstruction makes the breeding (mainly being corynebacterium acnes or Staphylococcus albus) in a large number under anaerobic condition of partial antibacterial, causes suppurative folliculitis, i.e. comedo (acne, acne).
3, because of the effect of individual inheritance's factor, how much relevant sebaceous gland size, quantity and secretion be.The food of edible higher fatty acid or pungent stimulation has certain influence to the secretion of skin sebaceous gland, makes the hair follicle secretion not smooth, forms comedo (acne, acne).4, medicine also can cause comedo (acne, acne), as hormones or vitamin A deficiency.5, adolescence women's menstrual cycle, variation has taken place in the hormone in vivo level, and the smegma disorder can make comedo (acne, acne) increase the weight of.
6, due to the extraneous factor, contain lanoline or vaseline is the cosmetics of raw material, block the normal drainage of hair follicle as life-time service; Dust in air, harmful substance stick to does not in time remove cleaning on the skin, block hair follicle and form comedo (acne, acne).
In sum, the reason that causes comedo is many-sided.The medicine that is used for the comedo treatment at present is broadly divided into following a few class: 1, suppress the material that corynebacterium acnes causes infection, as benzoyl peroxide, Tetracyclines etc.; 2, the material of dissolving horny layer class is as retinoic acid; 3, reduce the sebum secretion hormone medicine, as estrogen such as diethylstilbestrol, antiandrogen preparation.Said medicine has certain limitation or side effect, and practical effect is unsatisfactory.
Summary of the invention
The inventor has now found that after deliberation and the material that suppresses corynebacterium acnes is united with the cuticular material of dissolving use can effectively prevent and/or slow release or treatment comedo such as symptoms such as acne or acne, and effect obviously is better than any the independent use of above-mentioned two kinds of materials, the oils and fats that for example can remove in the sebaceous gland blocks, the excessive secretion that suppresses sebum dissolves comedo (acne, acne) or disappears; Corynebacterium acnes or Staphylococcus albus had suppress and killing action, especially to pustule class comedo, antiinflammatory action is obvious, and local inflammation such as red, swollen is disappeared rapidly; Chamfering repaired damaged wound surface fast, do not stay or reduce the formation of cicatrix; Eliminate the pigmentation that acne is left over fast.
Therefore, first aspect present invention relates to the compositions that is used to prevent or treat comedo, and it comprises the material that suppresses corynebacterium acnes, the material of dissolving keratodermatitis, and excipient or carrier.
Second aspect present invention relates to the compositions that is used to prevent or treat comedo, and it comprises the material that suppresses corynebacterium acnes, the material of dissolving keratodermatitis, material and the excipient or the carrier of removal skin pigment.
The material that further aspect of the present invention relates to the material that suppresses corynebacterium acnes and dissolving keratodermatitis is united and is used for preparing the product purposes that is used to prevent or treat comedo.
Further aspect of the present invention relates to the material that suppresses corynebacterium acnes, and the material one of the material of dissolving keratodermatitis and removal skin pigment is used from the product purposes that preparation is used for preventing or treating comedo.
According to the present invention, used term " comedo " is meant that skin surface occurs among the present invention as symptoms such as acne or acne.
According to the present invention, term used herein " material that suppresses corynebacterium acnes " is selected from metronidazole, tinidazole, secnidazole, ornidazole, clindamycin, lincomycin or has other material that suppresses corynebacterium acnes character.
According to the present invention, used term among the present invention material of keratodermatitis " dissolving " can be selected from Retinamido-ester, retinoic acid or have the material of similar dissolving keratodermatitis.
According to the present invention, the material of used removal skin pigment or the material of eliminating the pigmentation that causes because of comedo can be selected from Azelaic Acid among the present invention, vitamin C, vitamin E or with they kin materials.
According to the present invention, excipient that the present invention is used or carrier are selected from material below one or more: dermal osmosis accelerator, diluent, cosolvent, solubilizing agent, emulsifying agent, thickening agent, stabilizing agent, aromatic and pH regulator agent etc.
Dermal osmosis accelerator can be selected from following one or more materials among the present invention: (1) cholic acid salt: glycocholate, cholate, deoxycholate, taurocholate, glucose cholate, CDC, bird rope deoxycholate etc.; (2) saturated or unsaturated fatty acid and ester thereof: as lauric acid, oleic acid, nutmeg acid, capric acid, laurate, caprylate, decanoin, cetylate, ethyl lactate, triacetyl glycerine; (3) alcohols; As propylene glycol, isopropyl alcohol, hexadecanol, lauryl alcohol, oleyl alcohol etc.; (4) ethers: (5) sulfoxide classes such as polyoxyethylene laurel ether, polyoxyethylene octyl ether: as dodecyl methyl sulfoxide, dimethyl sulfoxide etc.; (6) amide-type: as N, dinethylformamide, N,N-dimethylacetamide, hexamethylene lauramide; (7) lactams: the tall and erect ketone of dodecyl nitrogen, hold together the tall and erect ketone of cattle base nitrogen etc.; (8) ion-type, nonionic surfactant: as sodium lauryl sulphate, sad monoglyceride, Tween 80, span 20 etc.; And/or the beta cyclodextrin class of (9) beta cyclodextrin or alkyl replacement: as dimethyl beta cyclodextrin, hydroxypropyl beta cyclodextrin etc.
The stabilizing agent that is added in the present composition has antioxidant, has said for example: sodium pyrosulfite, sodium sulfite, sodium sulfite, sodium thiosulfate, ascorbic acid, thiourea, cysteine, tocopherol or lecithin etc.The 0.01%-5% (w/v) that preferably accounts for the compositions weight of aforementioned stable agent consumption.PH buffer agent in the present composition has been said citric acid buffer salt, acetate buffer salt or phosphate-buffered salt etc. for example, and consumption is 0.1mol/L-0.2mol/L.
Beta cyclodextrin of being spoken of among the present invention and alkyl substituent thereof have been said for example: beta cyclodextrin, hydroxypropyl beta cyclodextrin, dimethyl beta cyclodextrin etc.; Also can use cellulose derivative such as carboxymethyl cellulose, hydroxypropyl methylcellulose in the present composition, above-mentioned beta cyclodextrin compounds or cellulose derivative all can form the clathrate of effective ingredient in the compositions such as Retinamido-ester or metronidazole; Polyethylene glycols, polyvidone etc. can form the solid dispersion of effective ingredient in the product, thereby help the absorption of effective ingredient in the product; Above-claimed cpd can be used for the adjusting of preparation toughness simultaneously, prolongs the time of contact of product, improves bioavailability.This class material also has polyacrylic acid, polyvinyl alcohol, carbopol etc.
The content of the material of dissolving keratodermatitis such as Viaminate and retinoic acid accounts for the 0.05-2% (w/w) of compositions gross weight in the present composition, is preferably 0.1-0.3 weight %.
The content of the material of employed inhibition corynebacterium acnes such as metronidazole or tinidazole or clindamycin accounts for the 0.01-10% (w/w) of compositions gross weight in the present composition, is preferably 0.5-5 weight %.
Compositions also can contain materials such as Azelaic Acid, vitamin C or vitamin E among the present invention.
Compositions of the present invention has excellent permeability, smears secondary every day, and the oils and fats that can remove in the sebaceous gland blocks, and suppresses the excessive secretion of sebum; To inhibition and killing action being arranged, especially to pustule class comedo (acne, acne) as corynebacterium acnes or Staphylococcus albus; Antiinflammatory action is obvious, and local inflammation such as red, swollen is disappeared rapidly; Chamfering repaired damaged wound surface fast, do not stay or reduce the formation of cicatrix.The present composition can also be eliminated the pigmentation that acne is left over fast.Therefore, the present composition is easy to use, safe, compliance good.
The specific embodiment
The following examples are used for further specifying the present invention, but do not mean that any limitation of the invention.
Comparative example 1 contains the compositions of Retinamido-ester
The composition consumption
Viaminate 0.2g
Laurocapram 2ml
Propylene glycol 20ml
Triacetyl glycerine 70ml
Polyethylene Glycol is to 100ml
Viaminate was pulverized the 40-80 mesh sieve, standby; 2ml laurocapram, 20ml propylene glycol, 70ml triacetyl glycerine and Polyethylene Glycol are made the 100ml liquid mixture, standby; The Viaminate fine powder of crossing the 40-80 mesh sieve above the 0.2g is dissolved in the aforesaid liquid mixture, promptly surely.
Comparative example 2 contains the compositions of metronidazole
The composition consumption
Metronidazole 1.0g
Laurocapram 2ml
Propylene glycol 20ml
Triacetyl glycerine 70ml
Polyethylene Glycol is to 100ml
The 1.0g metronidazole was pulverized the 40-80 mesh sieve, standby; Then laurocapram, propylene glycol, triacetyl glycerine, the PEG400 of amount shown in top are made the 100ml liquid mixture, standby; Standby metronidazole fine powder is dissolved in the aforesaid liquid mixture, promptly surely.
Embodiment 3 present compositions and preparation thereof
The composition consumption
Viaminate 0.2g
Metronidazole 1.0g
Azelaic Acid 5.0g
Laurocapram 2ml
Propylene glycol 30ml
Triacetyl glycerine 60ml
PEG400 is to 100ml
Respectively Viaminate and metronidazole were pulverized the 40-80 mesh sieve, standby; Laurocapram, propylene glycol, triacetyl glycerine, the PEG400 of above-mentioned amount are made the 100ml liquid mixture, standby; 0.2g Viaminate, 1.0g metronidazole and 5.0g Azelaic Acid fine powder after sieving above inciting somebody to action respectively are dissolved in the aforesaid liquid mixture, promptly surely.
Embodiment 4 present compositions and preparation thereof
The composition consumption
Viaminate 0.2g
Metronidazole 1.0g
Vitamin C 3.0g
Laurocapram 2ml
Propylene glycol 30ml
Triacetyl glycerine is to 100ml
Respectively Viaminate, metronidazole and vitamin C were pulverized the 40-80 mesh sieve, standby; Laurocapram, propylene glycol, the triacetyl glycerine of amount shown in top are made the 100ml liquid mixture, standby; The top consumption of use and Viaminate, metronidazole and the vitamin C fine powder of 40-80 mesh sieve respectively excessively are dissolved in the aforesaid liquid mixture, promptly surely.
Embodiment 5 present compositions and preparation thereof
The composition consumption
Viaminate 0.2g
Metronidazole 3.0g
Vitamin E 5.0g
Laurocapram 2ml
Propylene glycol 30ml
Triacetyl glycerine is to 100ml
Respectively Viaminate, metronidazole were pulverized the 40-80 mesh sieve, standby; Laurocapram, propylene glycol, triacetyl glycerine, the vitamin E of amount shown in top are made the 100ml liquid mixture, standby; Consumption and cross Viaminate, the metronidazole fine powder of 40-80 mesh sieve the sixth of the twelve Earthly Branches above using respectively is dissolved in the aforesaid liquid mixture, promptly surely.
The present invention is illustrated by above description and embodiment, and it is described as nonrestrictive, does not limit claim scope of the present invention.
The observation of embodiment 6 clinical efficacies
Physical data
The comedo patient is totally 90 examples, wherein male 46 examples, women 44 examples; 16～39 years old age; Average 32.15～42.4 months time limits of morbidity; The state of an illness increases the weight of 25 examples (56.8%) before passing through in state of an illness duration of seizure 4.1 ± 3.5 week～8.9 ± 8.2 weeks, women's case, is divided into 3 groups at random, every group 30 example.
Treatment and observational technique: each is organized case and stops using before treatment other oral and at least 3 weeks of medicine for external use, smears two deuterzooid medicines then every day.Weekly further consultation once, observe the curative effect and toxic and side effects.
Curative effect is judged: both fully recovering, skin lesion all disappears; Produce effects is that skin lesion at least 70% disappears; Transfer skin lesion well to and disappear 30～70%; Invalid for smearing medicine treatment one month continuously, skin lesion does not have improvement.Efficacy result is seen attached list.
The efficacy result of three kinds of liniments of subordinate list relatively
Illustrate: group 1 is comparative example 1 compositions; Group 2 is comparative example 2 compositionss; Group 3 is embodiment 3 compositionss.
Toxic and side effects: all do not occur after 3 groups of case liniments are smeared stimulating and allergy sufferers.
Conclusion: the embodiment of the invention 3 compositions group cure rates are 70%, compare p＜0.01 with two single medicine groups, and significant difference is arranged.Prove that the present composition of the present invention has synergism, the compositions that is better than independent use Retinamido-ester or metronidazole evident in efficacy.
Claims (3)
1. liniment, it is made up of following component and amount:
Viaminate 0.2g
Metronidazole 1.0g
Azelaic Acid 5.0g
Laurocapram 2ml
Propylene glycol 30ml
Triacetyl glycerine 60ml
PEG400 is to 100ml.
2. liniment, it is made up of following component and amount:
Viaminate 0.2g
Metronidazole 1.0g
Vitamin C 3.0g
Laurocapram 2ml
Propylene glycol 30ml
Triacetyl glycerine is to 100ml.
3. liniment, it is made up of following component and amount:
Viaminate 0.2g
Metronidazole 3.0g
Vitamin E 5.0g
Laurocapram 2ml
Propylene glycol 30ml
Triacetyl glycerine is to 100ml.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03149550 CN1568978B (en) | 2003-07-16 | 2003-07-16 | Composition for preventing and treating whelk |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03149550 CN1568978B (en) | 2003-07-16 | 2003-07-16 | Composition for preventing and treating whelk |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1568978A CN1568978A (en) | 2005-01-26 |
| CN1568978B true CN1568978B (en) | 2010-05-05 |
Family
ID=34472582
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03149550 Expired - Fee Related CN1568978B (en) | 2003-07-16 | 2003-07-16 | Composition for preventing and treating whelk |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1568978B (en) |
Families Citing this family (3)
| 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 |
| CN102716194B (en) * | 2012-02-13 | 2014-08-06 | 谢雁鸣 | Polygonum capitatum composition for preventing or treating whelk |
| CN105311058A (en) * | 2014-07-29 | 2016-02-10 | 上海百好博化工有限公司 | Preparation for killing propionibacterium acnes |
-
2003
- 2003-07-16 CN CN 03149550 patent/CN1568978B/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN1568978A (en) | 2005-01-26 |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20100505 Termination date: 20130716 |