橡胶基质对麝香壮骨膏中有毒成分体外释放的影响考察  

Effects of Different Rubber Matrix on the Release of Toxic Components in Shexiang Zhuanggu Plaster in vitro

作　　者：李海剑 郭立 Li Haijian;Guo Li(Henan Review and Inspection Center for Food and Drug Control,Zhengzhou 450018,China;Henan Lingrui Pharmaceutical Company Limited)

机构地区：[1]河南省食品药品审评查验中心,郑州450018 [2]河南羚锐制药股份有限公司

出　　处：《中国药师》2022年第5期932-936,共5页China Pharmacist

摘　　要：目的:考察不同橡胶基质对麝香壮骨膏中乌头双酯型生物碱成分体外释放度的影响。方法:采用聚异丁烯和天然橡胶两种类型橡胶制备麝香壮骨膏,依据中国药典2020年版四部通则0931第四法方法1测定两种橡胶贴膏的体外释放度。以高效液相色谱法测定新乌头碱、次乌头碱、乌头碱的累积释放量,比较不同橡胶类型对麝香壮骨膏中有毒成分的体外释放度影响。结果:采用聚异丁烯作为骨架材料制备的麝香壮骨,其中有毒药物乌头双酯型生物碱的单位面积体外累积释放量大于天然橡胶型产品,但在24 h释放过程中,释放总量为60.30μg,没有达到200μg的单次中毒剂量,安全性具有保证。结论:在麝香壮骨膏产品中,采用聚异丁烯代替天然橡胶,可以加快乌头双酯型生物碱的体外释放。Objective:To study the effects of different rubber matrix on the in vitro release of diester alkaloids in Aconitum carmichaeli from Shexiang Zhuanggu plaster.Methods:Shexiang Zhuanggu plaster was prepared respectively with polyisobutylene and natural rubber as the rubber matrix.The method 1 of the fourth method in 0931 general principle of Chinese Pharmacopoeia(2020 Edition)was used to determine the in vitro release of the two kinds of rubber plasters.The cumulative release of mesaconitine,hypaconitine and aconitine was determined by HPLC,and the effects of different rubber types on the release of toxic components in Shexiang Zhuanggu plaster were compared.Results:The in vitro cumulative release per unit area of the toxic drug diester aconitum alkaloids in Shexiang Zhuanggu plaster prepared with polyisobutene as skeleton material was greater than that of natural rubber-based products.However,the total amount of release was 60.30μg in 24 hours,which did not reach the single toxic dose of 200μg.Its safety was guaranteed.Conclusion:In Shexiang Zhuanggu plaster,polyisobutylene can be used instead of natural rubber,which can accelerate the release of Aconitum diester alkaloids in vitro.

关 键 词：聚异丁烯 麝香壮骨膏 体外释放 

分 类 号：R927.1[医药卫生—药学]