在模拟人工胃肠道环境中博落回主要生物碱类成分的稳定性特征分析

摘要

目的:为解释博落回中4个生物碱(原阿片碱、别隐品碱、血根碱、白屈菜红碱)生物利用低的原因,对这四个生物碱在模拟人工胃肠道环境下的稳定性进行考察.方法:采用HPLC测定博落回中4个生物碱在不同pH缓冲液、人工胃液(pH=1.3)和人工肠液(pH=6.8)中的稳定性.结果:原阿片碱和别隐品碱在酸性、中性、碱性、人工胃液及人工肠液环境下8h回收率为97.16％ ～ 101.89％;血根碱在pH =6.8磷酸盐缓冲液、水、pH =7.8 ～8.0磷酸盐缓冲液及人工肠液中8h回收率为48.81％～60.53％;白屈菜红碱在pH =5.8磷酸盐缓冲液、pH =6.8磷酸盐缓冲液、水及人工肠液中8h的回收率为81.21％ ～93.48％;在pH =7.8 ～8.0磷酸盐缓冲液中8h回收率为57.43％.结论:原阿片碱和别隐品碱的稳定性不受pH的影响,血根碱和白屈菜红碱随pH升高稳定性降低,博落回中4个生物碱在模拟人工胃肠道环境中的稳定性结果与其在不同pH环境中一致,为阐明博落回散在体内的药代动力学特点提供科学依据.%Objective:In order to explain the reasons of low bioavailability of four alkaloids (protopine,allocrypto pine,sanguinarine,chelerythrine) in Macleaya cordata,the study explored the stability of four alkaloids in the simulated gastrointestinal environment.Methods:A high performance liquid chromatography method was used to determine the stability of four alkaloids in M.cordata under the environment of different pH media,artificial gastric juice (pH =1.3) and artificial intestinal juice (pH =6.8).Results:The recovery rate of protopine and allocryptopine were ranging from 97.16％ to 101.89％ in the environment of acidic,neutral,alkalinity media,artificial gastric juice and artificial intestinal juice for 8 h.The recovery rate of sanguinarine was 48.81％-60.53 ％ in the environment of pH =6.8 phosphate buffer solution (PBS),water,pH =7.8-8.0 PBS and artificial intestinal juice for 8 h.The recovery rate of chelerythrine was 81.21％-93.48％ in the environment of pH =5.8 PBS,pH =6.8 PBS,water and artificial intestinal juice for 8 h,while in the environment of pH =7.8-8.0 PBS for 8 h,the recovery rate of chelerythrine was 57.43％.Conclusion:The stability of protopine and allocryptopine was not affected by pH.While along with the increase of pH,the stability of sanguinarine and chelerythrine was reduced.The stability of four alkaloids in M.cordata under the simulated gastrointestinal environment accorded with the environment of different pH media.The results provide a scientific basis for clarifying the pharmacokinetic characteristics of Sangrovit.