中国药业2017，Vol.26Issue(2)：8-12,5.DOI:10.3969/j.issn.1006-4931.2017.02.003
溶出度测定方法与布洛芬缓释胶囊体内血药浓度和退热效应的相关性研究
Correlation Research between the Drug Dissolution Test and Blood Drug Concentration in Vivo and Antipyretic Effect for Ibuprofen Sustained-Release Capsules
摘要
Abstract
Objective To set up the new method for drug dissolution test of Ibuprofen sustained-release capsules(ISRC)and evaluate the correlation between the drug dissolution tested by new method and the drugblood concentration in vivo and the antipyretic ef-fect. Methods ISRC were selected for experimental drugs. The new method of ISRC dissolution test was established,which included dis-solution medium pH=7. 6 buffer of phosphate,dissolution device one of paddle method,the speed of the paddle 50 r/min. To compared with the method of 2010 edition of China pharmacopoeia PartⅡ,the dissolution of ISRC tested by two method were monitored with fiber-optic in site dissolution testing equipment. The oral of single dosage of ISRC was used to rabbits,the drug blood concentrations of different time were measured. The model of rabbit fever was adopted by endotoxin,and the antipyretic effect of ISRC was checked. Results The course of drug dissolution tested by the new method in vitro emerged unsustained-release effect. The time of the percent of close to the largest accumulation drug dissolution of the new method in vitro,and of the peak drug blood concentration in vivo was better correlation. The peak drug blood concentration and the largest antipyretic effect were consistent. Conclusion When pH value of dissolution medium is increased,the process of sustained-release of ISRC in vitro is changed and otherwise its in vitro-in vivo correlation would be better than the results of the method in the China Pharmacopoeia.关键词
布洛芬缓释胶囊/药物溶出度/测定方法/血药浓度/退热效应/体内外相关性Key words
ibuprofen sustained-release capsules/drug dissolution/assay method/drug blood concentration/antipyretic effect/correlation between in vivo and in vitro分类
医药卫生引用本文复制引用
耿东升,马光霞,赵婷..溶出度测定方法与布洛芬缓释胶囊体内血药浓度和退热效应的相关性研究[J].中国药业,2017,26(2):8-12,5.基金项目
新疆维吾尔自治区自然科学基金[2013211A119]。 （）
