Stability of(-)-Gossypol in Simulated Conditions of Human Stomach, Intestines and in Biological Fluids

WU Bing-bing; TANG Hui; ZHANG Bo; FENG Rong

doi:10.13422/j.cnki.syfjx.2016180001

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Stability of(-)-Gossypol in Simulated Conditions of Human Stomach, Intestines and in Biological Fluids

更新时间：2024-01-04

- Stability of(-)-Gossypol in Simulated Conditions of Human Stomach, Intestines and in Biological Fluids
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 22, Issue 18, Pages: 1-4(2016)
- 作者机构：
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- DOI：10.13422/j.cnki.syfjx.2016180001
  CLC： R285
- Published：2016
- 稿件说明：
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WU Bing-bing, TANG Hui, ZHANG Bo, et al. Stability of(-)-Gossypol in Simulated Conditions of Human Stomach, Intestines and in Biological Fluids [J]. Chinese journal of experimental traditional medical formulae, 2016, 22(18): 1-4.
DOI：

WU Bing-bing, TANG Hui, ZHANG Bo, et al. Stability of(-)-Gossypol in Simulated Conditions of Human Stomach, Intestines and in Biological Fluids [J]. Chinese journal of experimental traditional medical formulae, 2016, 22(18): 1-4. DOI： 10.13422/j.cnki.syfjx.2016180001.

摘要

目的：考察左旋棉酚在不同生理pH及不同生物介质中的体外稳定性，为该药物的制剂开发提供参考。方法：取左旋棉酚分别在不同生理（pH 1.2～8.0）的缓冲液、人工胃肠液、离体生物介质中进行孵育，利用HPLC测定不同介质中左旋棉酚的含量变化，流动相乙腈-0.3%甲酸水溶液（80：20），检测波长234 nm，考察左旋棉酚的降解情况及酶稳定性，建立其降解速率方程。结果：左旋棉酚在pH 1.2盐酸溶液、模拟人工胃液及大鼠离体胃内容物中未出现明显降解，孵育12 h后降解率均<10%，左旋棉酚孵育12 h后在pH 6.8，7.4，8.0磷酸盐缓冲液中的降解率分别为64.7%，78.6%，84.4%，且在离体大鼠小肠、大肠内容物及肝组织匀浆中极不稳定，发生了较大程度降解，8 h后分别降解81.3%，96.9%，97.3%。降解特征类似于其在不同生理pH的缓冲液中。结论：左旋棉酚在碱性环境中明显降解而在酸性环境中不易降解；在大鼠胃内容物中较稳定，而在小肠、大肠菌群及肝脏中极易降解。

Abstract

Objective: To investigate the in vitro stability of(-)-gossypol in different physiological pH and biological sample. Method: (-)-Gossypol was incubated in different phosphate buffer solutions with pH of 1.2-8.0

artificial gastrointestinal fluid and isolated biological media.The concentration of(-)-gossypol was determined by HPLC to investigate the degradation kinetics and the enzymatic stabilities of(-)-gossypol. Result: (-)-Gossypol was stable in pH 1.2 dilute hydrochloric acid solution

artificial gastric juice and ingastric contents

after 12 h of incubation

degradation rate of(-)-gossypol was less than 10%.(-)-Gossypol was unstable in phosphate buffer solutions at pH 6.8

7.4 and 8.0 after 12 h of incubation.The degradation rates of(-)-gossypol in small intestinal contents

large intestine contents and liver homogenates were 81.3%

96.9%and 97.3%after 8 h

degradation profiles of(-)-gossypol in gastric contents

small intestinal contents

large intestine contents and liver homogenates were similar to that in the aqueous buffer. Conclusion: (-)-Gossypol is stable in acid environment

but it is unstable in phosphate buffer solutions at different pH.(-)-Gossypol is stable in gastric contents

but it is unstable in liver homogenate

small intestine and large intestine bacteria.

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