CN103932978A - Anthralin ointment and preparation process thereof - Google Patents
Anthralin ointment and preparation process thereof Download PDFInfo
- Publication number
- CN103932978A CN103932978A CN201410152400.4A CN201410152400A CN103932978A CN 103932978 A CN103932978 A CN 103932978A CN 201410152400 A CN201410152400 A CN 201410152400A CN 103932978 A CN103932978 A CN 103932978A
- Authority
- CN
- China
- Prior art keywords
- anthra
- derm
- aqueous solution
- dithranol
- agent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
Abstract
The invention discloses an anthralin ointment and a preparation process thereof. The ointment is prepared from anthralin, lactic acid, glycerinum and a hydroxypropyl methyl cellulose E50 aqueous solution. The preparation method comprises the following steps: adding anthralin into lactic acid, and stirring to dissolve to obtain a clean solution for later use; dissolving hydroxypropyl methyl cellulose in water to prepare a hydroxypropyl methyl cellulose aqueous solution, adding glycerinum, uniformly stirring, and then adding medicine liquor for later use during stirring to obtain the anthralin ointment. According to the ointment disclosed by the invention, anthralin is dissolved in lactic acid, so that the stability of anthralin is improved, degradation is less after being placed for a long term, and the product is free from a layering phenomenon.
Description
technical field
The invention belongs to pharmaceutical preparations technology field, in particular to a kind of external preparation of dithranol, relate in particular to a kind of Anthra-Derm agent and preparation technology thereof.
Background technology
Psoriasis is a kind of common chronic inflammatory disease dermatoses.It belongs to the disease of polygenic inheritance, can be by multiple motivating factor, as wound, infection, medicine etc. all may bring out this disease in susceptible individual.Typical cutaneous manifestations is the red speckle that boundary clearly has silvery white squama.The lighter can show as the patella ulnaris position speckle of several silver coin sizes, and severe one also can be got involved by whole skin.Its physiological pathology mechanism is mainly the abnormal and immune activation of epidermal hyperplasia differentiation.Because psoriasis is a kind of chronic disease, and it is wider to involve crowd, and the life impact that it causes patient is very large.Pruritus, squama and visible speckle are puzzlement patient's subject matter.The white psoriasis prevalence in Europe is 2% left and right, and the prevalence of the U.S. is 4.6%.China's investigation in 1984 finds that psoriatic prevalence is 0.123%.Along with various factorss such as urbanization process quickening, environmental pollution, social competition's aggravations, Chinese psoriatic prevalence increases year by year.According to Shanxi province Taiyuan city, Xichang City, Sichuan Province, Hebei province's Langfang City, Henan Province's Jiaozuo City, Zibo City of Shandong Province and Inner Mongolia Autonomous Region Hailar City Epidemiologic Study of Psoriasis result demonstration in totally six different geographical cities in 2010, it is 0.47% that current psoriatic prevalence has increased, and estimates that the existing disease patient of current China psoriasis has exceeded 3,000,000 people.
Dithranol (Dithranol) has another name called anthraline (Anthralin), dithranol, trade name Se Genuolin (Cignolin), chemical name 1,8-dihydroxy-9-anthrone, for the anthracyclinone derivatives of synthetic, being used for the treatment of psoriasis has had the history of 92 years.Dithranol is yellow or fallow crystallization or powder, and odorless dissolves in chloroform, atomic molten in ethanol, and almost insoluble in water, its structural formula is as follows:
Dithranol is extremely unstable, in the dark gets final product autoxidation, at daylight, ultraviolet radiation, be exposed to the speed that can obviously accelerate oxidation under air, hot environment.Main oxidation product is 1,8-istizin, dithranol dimer and anthraquinone dimer.1,8-istizin is still unstable, can be further oxided.The open one of CN103006537A is used for the treatment of psoriatic gel preparation and preparation technology thereof, and composition and weight proportion thereof that this dithranol gel contains are: 0.5 part of dithranol, 10 parts of carbomers, 100 parts of glycerol, 10 parts of triethanolamine, Azone10 part.CN102139111A discloses a kind of water-soluble substrate, is melted altogether to mix and makes: 50～60 parts of polyoxyethylene (40) stearates (S-40), 30 parts of fatty alcohol-polyoxyethylene ether, 10～20 parts of glycerol by the component of following weight portion; This patented technology also discloses described water-soluble substrate in the application of preparing in dithranol water soluble preparation, taking described water-soluble substrate as solvent adds dithranol and salicylic acid, be mixed with by percentage to the quality containing dithranol 0.1%～5%, containing salicylic acid 2% can be water-soluble body of paste or column.Above two kinds of patented technologies are not studied the stability of prepared dithranol preparation, and therefore the quality of its product after long term storage is troubling.
In addition, the dithranol preparation of external is dithranol white vaseline ointment clinically at present, and it does not dissolve in water, medicine eccysis inconvenience, easily pollution clothes.
Summary of the invention
In view of the deficiencies in the prior art, the object of the invention is to study by the prescription to preparation and technique, thereby a kind of Anthra-Derm agent of effectively avoiding dithranol oxidative degradation is provided.
Particularly, the object of the invention is to be achieved through the following technical solutions:
A kind of Anthra-Derm agent, described Anthra-Derm agent is prepared from by dithranol, lactic acid, glycerol and hydroxypropyl emthylcellulose aqueous solution.
Object of the present invention can also realize like this: described Anthra-Derm agent is prepared from by following mass percent by dithranol, lactic acid, glycerol and hydroxypropyl emthylcellulose aqueous solution:
Dithranol 0.1%
Lactic acid 0.5%-1.5%
Glycerol 40%-50%
Hydroxypropyl emthylcellulose aqueous solution 49%-60%.
Further preferably, described Anthra-Derm agent is prepared from by following mass percent by dithranol, lactic acid, glycerol and hydroxypropyl emthylcellulose aqueous solution:
Dithranol 0.1%
Lactic acid 0.8%-1.0%
Glycerol 44%-50%
Hydroxypropyl emthylcellulose aqueous solution 49%-55%.
Anthra-Derm agent of the present invention, the aqueous solution that wherein said hydroxypropyl emthylcellulose aqueous solution is HPMC E50, concentration is 5%-12%(W/V).Again further preferably, the concentration of aqueous solution of described HPMC E50 is 8%(W/V).
The invention provides the preparation technology of above-mentioned Anthra-Derm agent, this technique comprises the steps:
(1) dithranol is added in lactic acid, be stirred to dissolve, obtain settled solution, for subsequent use;
(2) hydroxypropyl emthylcellulose is dissolved in water and is mixed with hydroxypropyl emthylcellulose aqueous solution, add glycerol, stir, then in stirring, add the solution of step (1), obtain Anthra-Derm agent.
Preferably, the preparation technology of dithranol ointment as mentioned above, the aqueous solution that wherein said hydroxypropyl emthylcellulose aqueous solution is HPMC E50, concentration is 5%-12%(W/V).
Further preferably, the preparation technology of dithranol ointment as mentioned above, the concentration of aqueous solution of wherein said HPMC E50 is 8%(W/V).
The present invention is surprised to find that dithranol is dissolvable in water in lactic acid, therefore creatively dithranol is dissolved in the lactic acid of specific consumption, then this solution is added in the ointment base of hydroxypropyl emthylcellulose aqueous solution and glycerol preparation, obtained Anthra-Derm agent.Compared with prior art, because medicine dissolution is in ointment base, the Anthra-Derm agent quality homogeneous that therefore prepared by the present invention.In addition, find through accelerated test study, Anthra-Derm agent good stability prepared by the present invention, this is indicating said preparation less degradation after long term storage, not stratified.The 3rd, because ointment base can dissolve in water, ensure that the ointment of preparing with it is applied in after skin eccysis convenient, be difficult for pollution clothes.
Detailed description of the invention
Following examples further describe preparation process of the present invention and beneficial effect, embodiment is only for the object of illustration, do not limit the scope of the invention, within the apparent change that those of ordinary skill in the art make according to the present invention simultaneously and modification are also contained in the scope of the invention.
the preparation of embodiment 1 Anthra-Derm agent
Dithranol 1g
Lactic acid 5g
Glycerol 500g
5% hydroxypropyl emthylcellulose water E50 solution 494g
Preparation technology:
(1) dithranol of recipe quantity is mixed with lactic acid, stir, obtain settled solution, for subsequent use;
(2) HPMC E50 is dissolved in water, preparation 5% HPMC E50 aqueous solution, adds recipe quantity glycerol, stirs, for subsequent use;
(3) under agitation step (1) solution is joined in step (2) solution, after stirring evenly, obtain Anthra-Derm agent.
the preparation of embodiment 2 Anthra-Derm agent
Dithranol 1g
Lactic acid 14g
Glycerol 440g
12% HPMC E50 aqueous solution 545g
Preparation technology:
(1) dithranol of recipe quantity is mixed with lactic acid, stir, obtain settled solution, for subsequent use;
(2) HPMC E50 is dissolved in water, preparation 15% HPMC E50 aqueous solution, adds recipe quantity glycerol, stirs, for subsequent use;
(3) under agitation step (1) solution is joined in step (2) solution, after stirring evenly, obtain Anthra-Derm agent.
the preparation of embodiment 3 Anthra-Derm agent
Dithranol 1g
Lactic acid 8g
Glycerol 500g
8% HPMC E50 aqueous solution 491g
Preparation technology:
(1) dithranol of recipe quantity is mixed with lactic acid, stir, obtain settled solution, for subsequent use;
(2) HPMC E50 is dissolved in water, preparation 10% HPMC E50 aqueous solution, adds recipe quantity glycerol, stirs, for subsequent use;
(3) under agitation step (1) solution is joined in step (2) solution, after stirring evenly, obtain Anthra-Derm agent.
the preparation of embodiment 4 Anthra-Derm agent
Dithranol 1g
Lactic acid 10g
Glycerol 489g
8% HPMC E50 aqueous solution 500g
Preparation technology:
(1) dithranol of recipe quantity is mixed with lactic acid, stir, obtain settled solution, for subsequent use;
(2) HPMC E50 is dissolved in water, preparation 10% HPMC E50 aqueous solution, adds recipe quantity glycerol, stirs, for subsequent use;
(3) under agitation step (1) solution is joined in step (2) solution, after stirring evenly, obtain Anthra-Derm agent.
the preparation of comparative example's 1 Anthra-Derm agent
Dithranol 1g
Glycerol 499g
8% HPMC E50 aqueous solution 500g
Preparation technology:
(1) dithranol was pulverized to 200 mesh sieves, recipe quantity takes, for subsequent use, for subsequent use;
(2) HPMC E50 is dissolved in water, preparation 8% HPMC E50 aqueous solution, adds recipe quantity to add glycerol, stirs, for subsequent use;
(3) under agitation step (1) medicine is joined in step (2) solution, after stirring evenly, obtain Anthra-Derm agent.
the preparation of comparative example's 2 Anthra-Derm agent
Dithranol 1g
Acetic acid 10g
Glycerol 489g
8% HPMC E50 aqueous solution 500g
Preparation technology:
(1) dithranol of recipe quantity is mixed with acetic acid, stir, obtain settled solution, for subsequent use;
(2) HPMC E50 is dissolved in water, preparation 10% HPMC E50 aqueous solution, adds recipe quantity glycerol, stirs, for subsequent use;
(3) under agitation step (1) solution is joined in step (2) solution, after stirring evenly, obtain Anthra-Derm agent.
the preparation of comparative example's 3 Anthra-Derm agent
Dithranol 1g
Phosphatase 11 0g
Glycerol 489g
8% HPMC E50 aqueous solution 500g
Preparation technology:
(1) dithranol of recipe quantity is mixed with phosphoric acid, stir, obtain settled solution, for subsequent use;
(2) HPMC E50 is dissolved in water, preparation 10% HPMC E50 aqueous solution, adds recipe quantity glycerol, stirs, for subsequent use;
(3) under agitation step (1) solution is joined in step (2) solution, after stirring evenly, obtain Anthra-Derm agent.
the stability study of embodiment 4 Anthra-Derm agent
The preparation of reference substance solution: precision takes through 105 DEG C of dithranol reference substance 20mg of dry 2 hours, puts in 50ml measuring bottle, adds glacial acetic acid and makes in right amount to dissolve and be diluted to scale, shake up, precision measures 5ml, puts in 50ml measuring bottle, be diluted to scale with glacial acetic acid, shake up, to obtain final product.
The preparation of need testing solution: precision takes this product appropriate (being approximately equivalent to dithranol 2mg) and puts in 50ml beaker, adds glacial acetic acid 10ml, puts heating in water-bath and makes substrate fusing, constantly stir and extract 3 minutes, put the cooling substrate that makes in psychrolusia and solidify, extracting solution is filtered, filtrate is put in 50ml measuring bottle, substrate uses same method to extract again 3 times, use glacial acetic acid 10ml, extracting solution is all filtered in same measuring bottle, adds glacial acetic acid and is diluted to scale at every turn, shake up, to obtain final product.
Algoscopy precision measures reference substance solution and the each 5ml of need testing solution, put respectively in 25ml measuring bottle, each precision adds 5% sodium nitrite solution (new system before use) 1ml, shake up (filtering if desired), according to spectrophotography (two annex IV A of Chinese Pharmacopoeia version in 2010), wavelength place at 450nm measures trap, calculates, and to obtain final product.
Table 1 Anthra-Derm agent stability test
Can find out from the result of the test of table 1, Anthra-Derm prepared by embodiment of the present invention 1-4 is through accelerating investigation, and content, related substance do not change substantially, may be because lactic acid becomes ester with dithranol, thereby improve stability; Comparative example 1 does not add lactic acid, and related substance obviously increases, and content obviously declines; Comparative example 2 adopts acetic acid to replace lactic acid, and comparative example 3 adopts phosphoric acid to replace lactic acid, and its effect is all poor.
Claims (8)
1. an Anthra-Derm agent, is characterized in that: described Anthra-Derm agent is prepared from by dithranol, lactic acid, glycerol and hydroxypropyl emthylcellulose aqueous solution.
2. Anthra-Derm agent according to claim 1, is characterized in that: described Anthra-Derm agent is prepared from by following mass percent by dithranol, lactic acid, glycerol and hydroxypropyl emthylcellulose aqueous solution:
Dithranol 0.1%
Lactic acid 0.5%-1.5%
Glycerol 40%-50%
Hydroxypropyl emthylcellulose aqueous solution 49%-60%.
3. Anthra-Derm agent according to claim 2, is characterized in that: described Anthra-Derm agent is prepared from by following mass percent by dithranol, lactic acid, glycerol and hydroxypropyl emthylcellulose aqueous solution:
Dithranol 0.1%
Lactic acid 0.8%-1.0%
Glycerol 44%-50%
Hydroxypropyl emthylcellulose aqueous solution 49%-55%.
4. according to the Anthra-Derm agent described in claim 1-3 any one, it is characterized in that: the aqueous solution that described hydroxypropyl emthylcellulose aqueous solution is HPMC E50, concentration is 5%-12%(W/V).
5. Anthra-Derm agent according to claim 4, is characterized in that: the concentration of aqueous solution of described HPMC E50 is 8%(W/V).
6. according to a preparation technology for Anthra-Derm agent described in claim 1-3 any one, it is characterized in that this technique comprises the steps:
(1) dithranol is added in lactic acid, be stirred to dissolve, obtain settled solution, for subsequent use;
(2) hydroxypropyl emthylcellulose is dissolved in water and is mixed with hydroxypropyl emthylcellulose aqueous solution, add glycerol, stir, then in stirring, add the solution of step (1), obtain Anthra-Derm agent.
7. the preparation technology of Anthra-Derm agent according to claim 6, is characterized in that: the aqueous solution that described hydroxypropyl emthylcellulose aqueous solution is HPMC E50, concentration is 5%-12%(W/V).
8. the preparation technology of Anthra-Derm agent according to claim 7, is characterized in that: the concentration of aqueous solution of described HPMC E50 is 8%(W/V).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410152400.4A CN103932978B (en) | 2014-04-16 | 2014-04-16 | A kind of Anthra-Derm agent and preparation technology thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410152400.4A CN103932978B (en) | 2014-04-16 | 2014-04-16 | A kind of Anthra-Derm agent and preparation technology thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103932978A true CN103932978A (en) | 2014-07-23 |
| CN103932978B CN103932978B (en) | 2016-11-02 |
Family
ID=51181038
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410152400.4A Expired - Fee Related CN103932978B (en) | 2014-04-16 | 2014-04-16 | A kind of Anthra-Derm agent and preparation technology thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103932978B (en) |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4287214A (en) * | 1979-09-24 | 1981-09-01 | Scott Eugene J Van | Dithranol compositions stabilized with alpha hydroxyacids |
| CN101032465A (en) * | 2007-04-17 | 2007-09-12 | 孙猛 | Dithranol stick |
| WO2012053007A1 (en) * | 2010-10-21 | 2012-04-26 | Cadila Healthcare Limited | Topical pharmaceutical compositions containing nanodroplets for the treatment psoriasis |
| CN102935063A (en) * | 2012-11-08 | 2013-02-20 | 山东省皮肤病性病防治研究所 | Acetyl dithranol paste and preparation method thereof |
| CN103006537A (en) * | 2011-12-11 | 2013-04-03 | 西安泰科迈医药科技有限公司 | Gel preparation for treating psoriasis and preparation method thereof |
-
2014
- 2014-04-16 CN CN201410152400.4A patent/CN103932978B/en not_active Expired - Fee Related
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4287214A (en) * | 1979-09-24 | 1981-09-01 | Scott Eugene J Van | Dithranol compositions stabilized with alpha hydroxyacids |
| CN101032465A (en) * | 2007-04-17 | 2007-09-12 | 孙猛 | Dithranol stick |
| WO2012053007A1 (en) * | 2010-10-21 | 2012-04-26 | Cadila Healthcare Limited | Topical pharmaceutical compositions containing nanodroplets for the treatment psoriasis |
| CN103006537A (en) * | 2011-12-11 | 2013-04-03 | 西安泰科迈医药科技有限公司 | Gel preparation for treating psoriasis and preparation method thereof |
| CN102935063A (en) * | 2012-11-08 | 2013-02-20 | 山东省皮肤病性病防治研究所 | Acetyl dithranol paste and preparation method thereof |
Non-Patent Citations (3)
| Title |
|---|
| 伦格等主编、吴寿岭主译: "《奈特内科学：第2版》", 31 January 2012, 北京大学医学出版社 * |
| 田洪青等: "地蒽酚蜡棒治疗寻常型银屑病", 《中国新药与临床杂志》 * |
| 贾叙锋等: "卡泊三醇联合乳酸软膏治疗银屑病效果分析", 《浙江临床医学》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN103932978B (en) | 2016-11-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2827069C (en) | Sildenafil-free base-containing film preparation and method for producing same | |
| CN102871936B (en) | Nano-carrier loaded with rhodiola rosea extract and preparation method and application thereof | |
| JP2010530904A (en) | Coenzyme Q10 nano-emulsion composition | |
| JP2019500416A (en) | Pharmaceutical composition containing dutasteride and propylene glycol monolaurate and method for preparing the same | |
| CN106491644A (en) | A kind of fullerene soft capsule and preparation method | |
| JP6043429B2 (en) | 2,2 ', 6,6'-Tetraisopropyl-4,4'-biphenol soft capsule preparation and method for producing the same | |
| JP2008024651A (en) | Method for suppressing color development of catechin | |
| CN104257627A (en) | Glue solution for traditional Chinese medicine soft capsule with good stability and preparation method thereof | |
| CN103932978B (en) | A kind of Anthra-Derm agent and preparation technology thereof | |
| GB2031728A (en) | Stable erythromycin solution and process therefor | |
| CN102727463A (en) | Formula and preparation method for ursodeoxycholic acid soft capsules | |
| CN105213206A (en) | A kind of enoxolone liposome and preparation method thereof | |
| US20150174245A1 (en) | Transparent gel | |
| KR20190142601A (en) | Injection or eye drops in which indirubin is solubilized using glacial acetic acid and polyoxy-35-castor oil, and manufacturing method the same | |
| JP2010030906A (en) | Chemical preparation of poorly water-soluble medicine, method for producing the medicine chemical preparation and method for producing diluted medicine chemical preparation | |
| CN103169748A (en) | Shikonin microcapsule and preparation method thereof | |
| JPH0132207B2 (en) | ||
| CN101623260B (en) | Cefepime hydrochloride proliposome preparation | |
| CN107041126A (en) | For the composition for forming compound, the compound that is consequently formed and for the oral composition for including the compound | |
| WO2019227746A1 (en) | Chitosan oral solution and preparation method therefor | |
| CN105125490A (en) | Florfenicol nano-emulsion and preparation method thereof | |
| JP2010235574A (en) | Fucoxanthin clathrate | |
| AU2020355939B2 (en) | Rutin compositions | |
| JPH0242020A (en) | Danazol composition | |
| JPH03145432A (en) | Stable eye drop |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Guan Wei Inventor after: Gui Yunfei Inventor after: Yue Hu Inventor after: Xu Renxiang Inventor after: Ma Yong Inventor after: He Tongyuan Inventor after: Zhang Qijun Inventor before: Zhang Defang |
|
| COR | Change of bibliographic data | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20160906 Address after: 720000 Shaanxi province Xi'an Beilin District Road No. 182 persimmon Applicant after: XI'AN KEDA HAIR & SCALP CARE HOSPITAL Address before: Baoji City, Shaanxi Province Dongfeng Road 721000 District 45 No. Third Hospital of PLA Applicant before: Bai Lingqiang |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20161102 Termination date: 20200416 |
|
| CF01 | Termination of patent right due to non-payment of annual fee |