Hydroxypropyl-beta-cyclodextrin inclusion of strychnine and preparation method thereof

A cyclodextrin inclusion compound and strychnine technology, which is applied in the direction of non-active ingredients of polymer compounds, medical preparations containing active ingredients, drug combinations, etc., can solve the problem of hydroxypropyl-β without strychnine -Cyclodextrin inclusion technology, unfavorable bioavailability, hidden dangers of co-solvent toxicity, etc., to achieve the effect of improving bioavailability, increasing bioavailability, and improving water solubility
CN102008476AInactive Publication Date: 2011-04-13NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
Publication Date
2011-04-13
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a hydroxypropyl-beta-cyclodextrin inclusion of strychnine and a preparation method thereof. The inclusion is prepared from the strychnine and hydroxypropyl-beta-cyclodextrin in weight ratio of 1: (1-100) by using the preferential inclusion process. Experimental results show that the hydroxypropyl-beta-cyclodextrin inclusion of the strychnine has the advantages of high inclusion rate, great drug loading and good stability, and can significantly improve the water solubility of the strychnine, lead the solubility in water to be more than 20 times that of the strychnine, significantly improve the bioavailability after administration of the strychnine, play a role in reducing the toxicity of the strychnine and lead the clinical application to be safer.
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Description

technical field

[0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a cyclodextrin inclusion compound of strychnine and a preparation method thereof. Background technique

[0002] Strychnine is the main active alkaloid contained in the traditional Chinese medicine Strychnium. Pharmacological studies have shown that strychnine is one of the most promising active ingredients in Strychnium alkaloids: ①Anti-tumor experiments show that Strychnine The activity of strychnine is significantly higher than strychnine, strychnine nitrogen oxides, iso- strychnine and other alkaloid components in strychnine; ②Analgesic and anti-inflammatory tests also show that strychnine has definite Analgesic and anti-arthritis effects, but strychnine has no anti-arthritis and analgesic effects.

[0003] Strychnine is a fat-soluble drug, and its solubility in water is relatively low (less than 2 mg / mL), which is not conducive to the preparation of its p...

Claims

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