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Cyclodextrin inclusion compound containing resibufogenin and preparation and application

A technology of cyclodextrin inclusion compound and repobugenin, which is applied in the field of pharmacy, can solve the problems of difficult control of uniformity, low solubility, unfavorable preparation and other problems in the preparation of solid preparations

Inactive Publication Date: 2017-10-27
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the problems of high toxicity and side effects, low solubility, unfavorable preparation of liquid preparations, and difficulty in controlling the uniformity of preparation of solid preparations, the present invention provides a cyclodextrin inclusion compound Its preparation method and use

Method used

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  • Cyclodextrin inclusion compound containing resibufogenin and preparation and application
  • Cyclodextrin inclusion compound containing resibufogenin and preparation and application
  • Cyclodextrin inclusion compound containing resibufogenin and preparation and application

Examples

Experimental program
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Effect test

Embodiment 1

[0064] Example 1 Preparation of a Repobugenin β-Cyclodextrin Inclusion Compound by Solvent Method

[0065] Accurately weigh 7.69mg of repobugenin and 22.70mg of β-cyclodextrin, add to 20mL of 50% ethanol solution, 400r / min, 50°C magnetic stirring for 2h to dissolve completely, the solution is evaporated to dryness in a 50°C water bath, and reduced Vacuum-dried to obtain a white powder. Wash with 10mL ethyl acetate for 3-5 times until the TLC chromatography of the washing solution did not show any drug spots, and then drained to obtain a white loose powder, which was the inclusion complex of repobugenin β-cyclodextrin thing.

Embodiment 2

[0066] Example 2 Preparation of a Repobugenin Hydroxypropyl β-Cyclodextrin Inclusion Compound by Solvent Method

[0067] Accurately weigh 7.69 mg of repobugenin and 28.62 mg of hydroxypropyl β-cyclodextrin, add them to 20 mL of 50% ethanol solution, stir at 400 r / min, 50 ° C for 2 h to completely dissolve the solution, and rotate the solution in a 50 ° C water bath Evaporate to dryness, and dry under reduced pressure to obtain a white powder. Wash with 10 mL of ethyl acetate for 3-5 times until the TLC chromatography of the washing liquid does not show drug spots, and then drain to obtain a white loose powder, which is the hydroxypropyl β-cyclodextrin inclusion complex.

Embodiment 3

[0068] Example 3 Preparation of a Repobugenin γ-Cyclodextrin Inclusion Compound by Solvent Method

[0069] Accurately weigh 7.69mg of repobugenin and 25.94mg of γ-cyclodextrin, add to 20mL of 50% ethanol solution, 400r / min, 50°C magnetic stirring for 2h to dissolve completely, the solution is evaporated to dryness in a 50°C water bath, and reduced Dry under vacuum to obtain a white powder. Wash with 10 mL of ethyl acetate for 3-5 times until the TLC chromatography of the washing solution shows no drug spots, and then drain to obtain a white loose powder, which is the inclusion compound of resibufagenin γ-cyclodextrin.

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Abstract

The invention relates to a cyclodextrin inclusion compound containing resibufogenin and a preparation method of the cyclodextrin inclusion compound. The cyclodextrin inclusion compound consists of resibufogenin and an inclusion material at a mole ratio of 1:(1-100), and the preparation method comprises the following steps: dissolving resibufogenin, cyclodextrin and derivatives thereof into a proper amount of a solvent, stirring, and drying, thereby obtaining the cyclodextrin inclusion compound containing resibufogenin. The cyclodextrin inclusion compound containing resibufogenin, provided by the invention, is high in water solubility, low in toxicity, small in blood vessel irritation and high in stability, is capable of ensuring uniformity of preparations, has remarkable anti-tumor functions, is expected to be made into oral tablets, capsules or vein injections, and has great clinical application values.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a new inclusion compound of repobugenin and cyclodextrin and a preparation method of the inclusion compound. The present invention also relates to the use of the inclusion compound of lipobufagenin cyclodextrin. Background technique [0002] Resibufogenin (Resibufogenin, chemical formula C 24 h 32 o 4 ) is the main active ingredient in Bufo bufo gargarizans Cantor or B.melanostictus Schoeider, the white slurry secreted by the ear and skin glands of Bufo bufo bufo gargarizans Cantor or B.melanostictus Schoeider, which is processed and dried. Heart, local anesthesia and other activities (Liu Junshan, Zhang Dongmei, Kurihara Hiroshi, Ye Wencai. Research progress on anti-tumor effect of toad venom and its active ingredients. International Journal of Pharmaceutical Research [J]. 2009,36:115-120; Tang Xinwei, Xiao Jie , Song Jian, Zou Qiang, Wang Ruixue, Li Yanqi, Yang Tai. Study on Selective...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/60A61K31/585A61P35/00A61P9/04
CPCA61K31/585
Inventor 刘东春王东曹子薇陈换平夏明钰代英辉白雷毛心蕊孙晓媛李园园
Owner SHENYANG PHARMA UNIVERSITY
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