摘要
本文报道口服阿斯匹林肠溶缓释胶囊及肠溶片后体内水杨酸盐的高效液相色谱测定法及正常人药代动力学和生物利用度研究的结果。12名健康志愿者，随机分为两组，分别交叉口服阿斯匹林肠溶缓释胶囊和肠溶片各600mg。阿斯匹林在体内迅速转化为活性代谢产物水杨酸，测定口服给药后不同时间血中水杨酸的浓度，使用3P87实用药代动力学程序对药一时曲线进行处理，结果表明，水杨酸在体内的代谢过程符合一室模型。单剂空腹口服阿斯匹林肠溶缓释胶囊和肠溶片后，体内水杨酸的平均峰浓度为35．52±8．28mg／L和30．32±8．96mg／L；平均达峰时间为5．70±1．25h和7．40±2．17h开均药-时曲线下面积为328.4±92．2mg／（Lh）和316．0±70．95mg／（L·h)）;消除半衰期为3．11±1．25h和3．84±1．72h；吸收迟滞时间为2．33±0．65h和3．35±1．16h。肠溶缓释胶囊的达峰时间明显短于肠溶片。缓释胶囊对片剂的相对生物利用度为103．9％。
This paper reports a HPLC method for determining the serum concentration of salicylic acid and the pharmacokinetic parameters and bioavai1ability of aspirin enteric suluble controlled-release capsule and enteric-coating tablet.Twelve healthy -volunteers were divided into two groups randomly and administrated 6oOmg of aspirin enteric so1uble controlled-release capsule and enteric coating tablet alternatively with an interval of 7 days.Aspirin is rapidly metabolized into salicylic acid in the body,and serum concentration of salicylic acid was determined by HPLC method. Samples were collected prior to and 1.3.4.5.6.7. 9. 12. 15. 18. 24 hours after oral taking.The results showed that two dosage forms were both fitted to one compartmental model.Cmax of enteric-soluble controlled-release capsule and enteric-coating tablet were 35.5218.28mg/L and 30.32±8.96mg/L;Tpeak were 5.70±1.25h and 7.40±2.17h,AUC were 328.4±92.2mg/(L. h) and 316.01±71.0mg/(L. h),t1/2e were 3.11±2.17h,and 3.84±1.72h,and lag time were 2.33±0.65h and 3.35±1.16h, respectively.Tpeak showed significant difference and other parameters showed no significant differences between enteric-soluble controlled-release capsule and enteric-coating tablet.The bioavailabi1ity of two dosage forms were similar.
出处
《中国药房》
CAS
CSCD
1998年第2期73-74,共2页
China Pharmacy
关键词
阿斯匹林
水杨酸
肠溶缓释胶囊
药代动力学
aspirin, salicylic acid, enteric-soluble controlled-release capsule ,HPLC, bioavailability
