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

A technology for inclusion complex of strychnine hydroxypropyl and cyclodextrin, which is applied in the directions of non-active components of polymer compounds, drug combinations, non-central pain relievers, etc., and can solve the problem of no strychnine hydroxypropyl- β-cyclodextrin inclusion technology, hidden dangers of cosolvent toxicity, unfavorable bioavailability, etc., to achieve the effect of improving bioavailability, improving water solubility, and improving bioavailability

Inactive Publication Date: 2015-01-07
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Strychnine is a fat-soluble drug, and its solubility in water is relatively low (less than 2mg / mL), which is not conducive to the preparation of its preparation and its bioavailability after administration
For example, during the preparation of strychnine gel, due to the low solubility, strychnine will be precipitated from the hydrogel matrix, which limits the increase of drug concentration
Another example is to make injections, which need to add a large amount of co-solvents. The potential toxicity of co-solvents may bring hidden dangers to clinical medication.
According to reports, the bioavailability of oral and transdermal administration of strychnine is only 30~35%.
And experiments have shown that strychnine has adverse reactions such as central nervous system toxicity while exerting tumor or analgesic and anti-inflammatory effects.
[0004] In recent years, a number of strychnine preparations aimed at solving the problems of solubility and bioavailability have been reported, such as microemulsions, liposomes, nanoparticles, etc., such as Chinese invention patent: 200510026516.4, which discloses a nano Strychnine liposome transdermal spray preparation and its preparation method and application, 200810236293.8 discloses a strychnine complex phospholipid liposome and its preparation method and application in pharmacy, 200910235087.X discloses a Nuxychnium total alkaloid sustained-release dropping pills and its preparation method, 02148438.4 discloses a Nuxychnium sustained-release preparation and its preparation method, 200510026515.X discloses a nano strychnine liposome and its preparation method, 01100654.4 discloses a nano strychnine preparation drug and its preparation method, etc., but the above preparation process is generally complicated, and there is no research report on strychnine hydroxypropyl-β-cyclodextrin inclusion technology

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of strychnine hydroxypropyl-β-cyclodextrin inclusion compound

[0028] Weigh 1g of strychnine, dissolve it in 6ml of ethanol to obtain strychnine ethanol solution, set aside, take 6g of hydroxypropyl-β-cyclodextrin, grind it into a paste with 12ml of distilled water, then mix the strychnine Add the ethanol solution to the hydroxypropyl-β-cyclodextrin paste for clathration, after the dropwise addition, grind at 40°C for 2 hours, dry in vacuum, and wash away the strychnine drug that is not clathrated with dichloromethane , and dry to obtain strychnine hydroxypropyl-β-cyclodextrin inclusion compound.

[0029] The obtained strychnine hydroxypropyl-β-cyclodextrin inclusion compound was dissolved in distilled water to prepare a solution with a strychnine concentration of 20 mg / ml, and the inclusion rate was 96%.

Embodiment 2

[0030] Example 2 Preparation of strychnine hydroxypropyl-β-cyclodextrin inclusion compound

[0031] First weigh 1g of strychnine, dissolve it in 4ml of ethanol to obtain a strychnine solution, and set aside, then weigh 10g of hydroxypropyl-β-cyclodextrin, dissolve it in 30ml of distilled water, and stir magnetically at a constant temperature of 40°C Add the strychnine solution dropwise to the aqueous solution of hydroxypropyl-β-cyclodextrin for inclusion, continue magnetic stirring for 3 hours after the addition, spray dry, wash away the unincluded drug with chloroform, After drying, the strychnine hydroxypropyl-β-cyclodextrin inclusion compound is obtained.

[0032] The obtained strychnine hydroxypropyl-β-cyclodextrin inclusion compound was dissolved in distilled water to prepare a solution with a strychnine concentration of 23 mg / ml, and the inclusion rate was 94%.

Embodiment 3

[0033] Example 3 Preparation of strychnine hydroxypropyl-β-cyclodextrin inclusion compound

[0034] First weigh 1g of strychnine, dissolve it in 10ml of acetone to obtain a solution of strychnine in acetone, and set aside, then weigh 20g of hydroxypropyl-β-cyclodextrin, dissolve it in 40ml of distilled water, and stir at 40°C Add the strychnine solution dropwise to the aqueous solution of hydroxypropyl-β-cyclodextrin for inclusion, continue ultrasonic oscillation for 1.5 hours after the addition, lyophilize, wash away the unincluded drug with ether, and dry , That is, strychnine hydroxypropyl-β-cyclodextrin inclusion compound. Dissolve the clathrate with distilled water, filter, add syrup, adjust the pH value, and prepare oral liquid.

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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.

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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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/475A61K47/40A61P35/00A61P29/00
Inventor 蔡宝昌陈军陈志鹏李磊
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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