CN103932978B - A kind of Anthra-Derm agent and preparation technology thereof - Google Patents
A kind of Anthra-Derm agent and preparation technology thereof Download PDFInfo
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- CN103932978B CN103932978B CN201410152400.4A CN201410152400A CN103932978B CN 103932978 B CN103932978 B CN 103932978B CN 201410152400 A CN201410152400 A CN 201410152400A CN 103932978 B CN103932978 B CN 103932978B
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Abstract
The invention discloses a kind of Anthra-Derm agent and preparation technology thereof, this ointment is prepared from by dithranol, lactic acid, glycerol, HPMC E50 aqueous solution, and preparation method is: is added by dithranol in lactic acid, is stirred to dissolve, obtain settled solution, standby；Hydroxypropyl methyl cellulose is dissolved in water and is configured to hydroxypropyl methyl cellulose aqueous solution, add glycerol, stir, in stirring, then add standby medicinal liquid, obtain Anthra-Derm agent.Dithranol is dissolved in lactic acid by the present invention, improves the stability of dithranol, and less degradation after long-term placement, product is without lamination.
Description
Technical field
The invention belongs to pharmaceutical preparations technology field, in particular to the external preparation of a kind of dithranol, particularly relate to
A kind of Anthra-Derm agent and preparation technology thereof.
Background technology
Psoriasis is that a kind of common chronic inflammatory skin is sick.It belongs to the disease of polygenic inheritance, can be swashed by multiple
The factor of sending out, all may induce this disease such as wound, infection, medicine etc. in susceptible individual.Typical cutaneous manifestations is that boundary understands
The red speckle with silvery white squama.The lighter can behave as the patella ulnaris position speckle of several silver coin size, and severe one can also
Whole skin is got involved.Its physiological pathology mechanism is mainly the exception of epidermal hyperplasia differentiation and immune activation.Due to psoriasis
Being a kind of chronic disease, and it is relatively wide to involve crowd, the life impact that patient is caused by it is the biggest.Pruritus, squama and visible
Speckle is the subject matter of puzzlement patient.The white psoriasis prevalence in Europe is about 2%, and the prevalence of the U.S. is
4.6%.China's investigation in 1984 finds that psoriatic prevalence is 0.123%.Along with urbanization process quickening, environmental pollution,
The various factors such as social competition's aggravation, Chinese psoriatic prevalence increases the most year by year.According to Shanxi province Taiyuan city in 2010,
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 totally six
The Epidemiologic Study of Psoriasis result in individual different geographical city shows, current psoriatic prevalence has increased and is
0.47%, estimate that the existing disease patient of current China psoriasis is more than 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, it is used for having treated psoriasis
There is the history of 92 years.Dithranol is yellow or fallow crystallization or powder, and odorless dissolves in chloroform, the most atomic
Molten, the most insoluble in water, its structural formula is as follows:
Dithranol extremely unstable, in the dark gets final product autoxidation, irradiates at daylight, ultraviolet, is exposed to air, high temperature ring
The speed of oxidation can be substantially accelerated under border.Main oxidation product is 1,8-istizin, dithranol dimer and anthraquinone dimerization
Body.1,8-istizin is the most unstable, can be further oxided.The open one of CN103006537A is used for treating psoriatic coagulating
Glue preparation and preparation technology thereof, composition and weight proportion thereof that this dithranol gel contains be: dithranol 0.5 part, carbomer
10 parts, glycerol 100 parts, triethanolamine 10 parts, Azone10 part.CN102139111A discloses a kind of water-soluble bases, by as follows
The co-melting mixing of component of weight portion is made: polyoxyethylene (40) stearate (S-40) 50～60 parts, fatty alcohol-polyoxyethylene ether
30 parts, glycerol 10～20 parts；This patented technology also discloses described water-soluble bases answering in preparing dithranol water soluble preparation
With, i.e. add dithranol and salicylic acid with described water-soluble bases for solvent, be configured to by percentage to the quality containing dithranol 0.1%
～5%, water soluble body of paste containing salicylic acid 2% or column.Both the above patented technology does not has prepared ground
The stability of anthrol preparation is studied, and therefore its product quality after long term storage is troubling.
It addition, the dithranol preparation of external the most clinically is dithranol white vaseline ointment, it is insoluble in water, medicine
Thing eccysis inconvenience, easy pollution clothes.
Summary of the invention
In view of the deficiencies in the prior art, it is an object of the invention to by the prescription of preparation and technique are studied, from
And a kind of Anthra-Derm agent being prevented effectively from dithranol oxidative degradation is provided.
Specifically, it is an object of the invention to be achieved through the following technical solutions:
A kind of Anthra-Derm agent, described Anthra-Derm agent is by dithranol, lactic acid, glycerol and hydroxypropyl methyl fiber
Element aqueous solution is prepared from.
The purpose of the present invention can also be achieved in that: described Anthra-Derm agent is by dithranol, lactic acid, glycerol and hydroxypropyl
Ylmethyl cellulose aqueous solution is prepared from by following mass percent:
Dithranol 0.1%
Lactic acid 0.5%-1.5%
Glycerol 40%-50%
Hydroxypropyl methyl cellulose aqueous solution 49%-60%.
It is further preferred that described Anthra-Derm agent is by dithranol, lactic acid, glycerol and hydroxypropyl methyl cellulose water
Solution is prepared from by following mass percent:
Dithranol 0.1%
Lactic acid 0.8%-1.0%
Glycerol 44%-50%
Hydroxypropyl methyl cellulose aqueous solution 49%-55%.
Anthra-Derm agent of the present invention, wherein said hydroxypropyl methyl cellulose aqueous solution is hydroxypropyl methyl
The aqueous solution of cellulose E50, concentration is 5%-12%(W/V).The most preferably, described HPMC E50
Concentration of aqueous solution be 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, standby；
(2) hydroxypropyl methyl cellulose is dissolved in water it is configured to hydroxypropyl methyl cellulose aqueous solution, add glycerol,
Stir, in stirring, then add the solution of step (1), obtain Anthra-Derm agent.
Preferably, the preparation technology of dithranol ointment described above, wherein said hydroxypropyl methyl cellulose is water-soluble
Liquid is the aqueous solution of HPMC E50, and concentration is 5%-12%(W/V).
It is further preferred that the preparation technology of dithranol ointment described above, wherein said hydroxypropyl methyl fiber
The concentration of aqueous solution of element E50 is 8%(W/V).
The present invention is surprised to find that dithranol is dissolvable in water in lactic acid, and dithranol is the most creatively dissolved in specific use
In the lactic acid of amount, then this solution is added in the ointment base of hydroxypropyl methyl cellulose aqueous solution and glycerol, obtain
Anthra-Derm agent.Compared with prior art, owing to medicine dissolution is in ointment base, the dithranol that therefore prepared by the present invention
Ointment quality is homogeneous.It addition, find through accelerated test study, Anthra-Derm agent good stability prepared by the present invention, this
Imply that said preparation less degradation after long term storage, not stratified.3rd, owing to ointment base can dissolve in water, it is ensured that with
After its ointment prepared is applied in skin, eccysis is convenient, is difficult to pollution clothes.
Detailed description of the invention
Following example further describe preparation process and the beneficial effect of the present invention, and embodiment is only used for the mesh of illustration
, do not limit the scope of the invention, simultaneously those of ordinary skill in the art according to the present invention made obvious change and
Within modification is 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 methyl cellulose water E50 solution 494g
Preparation technology:
(1) dithranol of recipe quantity is mixed with lactic acid, stir, obtain settled solution, standby；
(2) HPMC E50 is dissolved in water, prepares 5% HPMC E50 aqueous solution, add
Enter recipe quantity glycerol, stir, standby；
(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, standby；
(2) HPMC E50 is dissolved in water, prepares 15% HPMC E50 aqueous solution,
Add recipe quantity glycerol, stir, standby；
(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, standby；
(2) HPMC E50 is dissolved in water, prepares 10% HPMC E50 aqueous solution,
Add recipe quantity glycerol, stir, standby；
(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, standby；
(2) HPMC E50 is dissolved in water, prepares 10% HPMC E50 aqueous solution,
Add recipe quantity glycerol, stir, standby；
(3) under agitation step (1) solution is joined in step (2) solution, after stirring evenly, obtain Anthra-Derm agent.
The preparation of comparative example 1 Anthra-Derm agent
Dithranol 1g
Glycerol 499g
8% HPMC E50 aqueous solution 500g
Preparation technology:
(1) dithranol being pulverized 200 mesh sieves, recipe quantity weighs, standby, standby；
(2) HPMC E50 is dissolved in water, prepares 8% HPMC E50 aqueous solution, add
Enter recipe quantity and add glycerol, stir, standby；
(3) under agitation step (1) medicine is joined in step (2) solution, after stirring evenly, obtain Anthra-Derm agent.
The preparation of comparative example 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, standby；
(2) HPMC E50 is dissolved in water, prepares 10% HPMC E50 aqueous solution,
Add recipe quantity glycerol, stir, standby；
(3) under agitation step (1) solution is joined in step (2) solution, after stirring evenly, obtain Anthra-Derm agent.
The preparation of comparative example 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, standby；
(2) HPMC E50 is dissolved in water, prepares 10% HPMC E50 aqueous solution,
Add recipe quantity glycerol, stir, standby；
(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 weighs the dithranol reference substance 20mg being dried 2 hours through 105 DEG C, puts 50ml amount
In Ping, adding glacial acetic acid and make dissolving in right amount and be diluted to scale, shake up, precision measures 5ml, puts in 50ml measuring bottle, dilute with glacial acetic acid
Release to scale, shake up, to obtain final product.
The preparation of need testing solution: precision weighs this product appropriate (being approximately equivalent to dithranol 2mg) and puts in 50ml beaker, on the rocks
Acetic acid 10ml, puts heating in water-bath and makes ma trix melting, be stirred continuously extraction 3 minutes, puts cooling in psychrolusia and makes matrix set, will
Extracting solution filter, filtrate is put in 50ml measuring bottle, substrate again with same method extract 3 times, use glacial acetic acid 10ml every time, extracting solution all filter into
In same measuring bottle, add glacial acetic acid and be diluted to scale, shake up, to obtain final product.
Algoscopy precision measures reference substance solution and each 5ml of need testing solution, puts in 25ml measuring bottle respectively, and each precision adds
5% sodium nitrite solution (brand-new before use) 1ml, shakes up (filtering if desired), according to spectrophotography (Chinese Pharmacopoeia version in 2010
Two annex IV A), at the wavelength of 450nm, measure trap, calculate, to obtain final product.
Table 1 Anthra-Derm agent stability test
From the result of the test of table 1 it can be seen that the accelerated investigation of Anthra-Derm prepared of embodiment of the present invention 1-4, contain
Measure, have being basically unchanged of related substance, it may be possible to because lactic acid becomes ester with dithranol, thus improve stability；Comparative example 1
Not adding lactic acid, have related substance substantially to increase, content is decreased obviously；Comparative example 2 uses acetic acid to replace lactic acid, contrast to implement
Example 3 uses phosphoric acid to replace lactic acid, and its effect is the most poor.
Claims (7)
1. an Anthra-Derm agent, it is characterised in that: described Anthra-Derm agent is by dithranol, lactic acid, glycerol and hydroxypropyl
Ylmethyl cellulose aqueous solution is prepared from by following mass percent:
Dithranol 0.1%
Lactic acid 0.5%-1.5%
Glycerol 40%-50%
Hydroxypropyl methyl cellulose aqueous solution 49%-60%
Further, the mass percent summation of above each component is 100%.
Anthra-Derm agent the most according to claim 1, it is characterised in that: described Anthra-Derm agent by dithranol,
Lactic acid, glycerol and hydroxypropyl methyl cellulose aqueous solution are prepared from by following mass percent:
Dithranol 0.1%
Lactic acid 0.8%-1.0%
Glycerol 44%-50%
Hydroxypropyl methyl cellulose aqueous solution 49%-55%.
Anthra-Derm agent the most according to claim 1 and 2, it is characterised in that: described hydroxypropyl methyl cellulose water
Solution is the aqueous solution of HPMC E50, and concentration is 5%-12%(W/V).
Anthra-Derm agent the most according to claim 3, it is characterised in that: described HPMC E50
Concentration of aqueous solution is 8%(W/V).
5. the preparation technology of an Anthra-Derm agent according to claim 1 or claim 2, it is characterised in that this technique includes as follows
Step:
(1) dithranol is added in lactic acid, be stirred to dissolve, obtain settled solution, standby；
(2) hydroxypropyl methyl cellulose is dissolved in water it is configured to hydroxypropyl methyl cellulose aqueous solution, add glycerol, stirring
Uniformly, in stirring, then add the solution of step (1), obtain Anthra-Derm agent.
The preparation technology of Anthra-Derm agent the most according to claim 5, it is characterised in that: described hydroxypropyl methyl fiber
Element aqueous solution is the aqueous solution of HPMC E50, and concentration is 5%-12%(W/V).
The preparation technology of Anthra-Derm agent the most according to claim 6, it is characterised in that: described hydroxypropyl methyl fiber
The concentration of aqueous solution of element E50 is 8%(W/V).
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| Application Number | Priority Date | Filing Date | Title |
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| 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 |
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| CN201410152400.4A CN103932978B (en) | 2014-04-16 | 2014-04-16 | A kind of Anthra-Derm agent and preparation technology thereof |
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| Publication Number | Publication Date |
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| CN103932978A CN103932978A (en) | 2014-07-23 |
| CN103932978B true CN103932978B (en) | 2016-11-02 |
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| CN201410152400.4A Expired - Fee Related CN103932978B (en) | 2014-04-16 | 2014-04-16 | A kind of Anthra-Derm agent and preparation technology thereof |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101032465A (en) * | 2007-04-17 | 2007-09-12 | 孙猛 | Dithranol stick |
| 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 |
Family Cites Families (2)
| 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 |
| WO2012053007A1 (en) * | 2010-10-21 | 2012-04-26 | Cadila Healthcare Limited | Topical pharmaceutical compositions containing nanodroplets for the treatment psoriasis |
-
2014
- 2014-04-16 CN CN201410152400.4A patent/CN103932978B/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101032465A (en) * | 2007-04-17 | 2007-09-12 | 孙猛 | Dithranol stick |
| 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 (2)
| Title |
|---|
| 卡泊三醇联合乳酸软膏治疗银屑病效果分析;贾叙锋等;《浙江临床医学》;20111130;第13卷(第11期);第1266-1267页，尤其是第1266页左栏第1.2节第10行、第1267页左栏第12-15行 * |
| 地蒽酚蜡棒治疗寻常型银屑病;田洪青等;《中国新药与临床杂志》;20060131;第25卷(第1期);第57-59页，尤其是第58页左栏第9-10行 * |
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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 |
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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 |
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