10-acetyl-dithranol hydrogel and preparation method thereof

A technology of dithranol hydrogel agent and acetyl dithranol, which is applied in the field of medicines, can solve the problems of unacceptability of patients, skin irritation, telangiectasia, etc., and achieves the effects of less pollution of clothes, easy cleaning, and reduced irritation.

Inactive Publication Date: 2009-03-11
SHANDONG PROVINCIAL INST OF DERMATOLOGY & VENEREOLOGY
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  • Summary
  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

Although the above-mentioned medicines are effective, there are the following disadvantages: external use of glucocorticoids can cause local skin atrophy, telangiectasia, folliculitis, etc., and large-scale application may also cause systemic side effects due to systemic absorption, and even aggravate the condition; Intrinsic odor and oil stains cannot be effectively overcome, making it difficult for patients to accept; vitamin D 3 Derivatives cannot be produced domestically, rely on imports, and are expensive and difficult to promote; retinoic acid drugs have obvious skin irritation
In addition, improvements have also been made in the preparation of dithranol water. Dithranol water wax sticks have been developed, and liposomes and microencapsulated dithranol water have been developed, but they still cannot fundamentally solve the problem of dithranol water. Problems with stimuli causing adverse reactions
[0004] Since the 1980s, many scholars at home and abroad have carried out research on the search for dithranol water derivatives, and found that adding a side chain to the water chemical structure C-10 of dithranol can not only prevent it from being oxidized into a dimer, Increases stability and can reduce its stimulatory effect, but the longer the side chain, the weaker its therapeutic effect
Studies have found that 10-butyryl anthranol water has no obvious side effects of skin irritation and staining, and its curative effect can be close to that of anthranol water. Basic research shows that 10-butyryl anthranol water has a similar effect to anthranol water. But so far there is no report of 10-butyryldithranol aqueous preparation as a new drug

Method used

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  • 10-acetyl-dithranol hydrogel and preparation method thereof

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Embodiment

[0011] 10-acetyldithranol hydrogel of the present invention, it is made into the raw material of the weight ratio of gel comprising:

[0012] 1. 3g of 10-acetyldithranol, 17g of salicylic acid, 120g of glycerin, 9408g of carbomer, 0.5g of ethylparaben, 7ml of triethanolamine, 0.5g of ascorbic acid, 3ml of ethanol, 0.5ml of essence, and 700ml of purified water.

[0013] 2. 23.7g of 10-acetyldithranol, 23g of salicylic acid, 160g of glycerin, carbomer-94012g, 1.5g of ethylparaben, 12ml of triethanolamine, 1.5g of ascorbic acid, 7ml of ethanol, 1.5ml of essence, purified water 850ml.

[0014] 3. 11g of 10-acetyldithranol, 20g of salicylic acid, 150g of glycerin, carbomer-94010g, 1g of ethylparaben, 10ml of triethanolamine, 0.5g of ascorbic acid, 5ml of ethanol, 1ml of essence, and 800ml of purified water.

[0015] The preparation method of the present invention: dithranol raw materials: benzene; pyridine; acetyl chloride; anhydrous sodium sulfate; distilled water; glacial acetic...

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Abstract

The invention discloses a 10-acetyl dithranol hydrogel and a preparation method thereof. The hydrogel is prepared from the raw materials by weight proportion as follows: 3g-23.7g of 10-acetyl dithranol, 17g-23g of salicylic acid, 120g-160g of glycerol, 8g-12g of carbomer-940, 0.5g-1.5g of ethyl hydroxy benzoate, 7ml-12ml of triethanolamine, 0.5g -1.5g of ascorbic acid, 3ml-7ml of ethanol, 0.5ml-1.5ml of essence and 700ml-850ml of purified water. The 10-acetyl dithranol hydrogel has the advantages of inhibiting the proliferation of epidermal cells by reducing DNA synthesis, inhibiting the respiration of mitochondrion, recovering relevant enzyme in skin lesion caused by psoriasis, and inhibiting the functions of monocytes. As the increasing concentration therapy is adopted, the drug stays at the skin lesion for 24 hours; when the transient touch therapy is adopted, the irritation can be reduced.

Description

technical field [0001] The invention relates to medicines, and is a 10-acetylthranol hydrogel and a preparation method thereof. Background technique [0002] The current anti-psoriasis topical drugs mainly include the following categories: potent glucocorticoids, vitamin D 3 Derivatives, tars, dithranol water and vitamin A acids. Although the above-mentioned medicines are effective, there are the following disadvantages: external use of glucocorticoids can cause local skin atrophy, telangiectasia, folliculitis, etc., and large-scale application may also cause systemic side effects due to systemic absorption, and even aggravate the condition; Intrinsic odor and oil stains cannot be effectively overcome, making it difficult for patients to accept; vitamin D 3 Derivatives cannot be produced domestically, rely on imports, and are expensive and difficult to promote; retinoic acid drugs have obvious skin irritation. [0003] Dithranol (Dithranol) chemical name is 1,8-dihydroxy-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/222A61K31/60A61K47/34A61P17/06A61K47/10A61K47/18A61K47/22
Inventor 张福仁杨宝琦
Owner SHANDONG PROVINCIAL INST OF DERMATOLOGY & VENEREOLOGY
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