罗红霉素胶囊的药动学与相对生物利用度  

Pharmacokinetics and relative bioavailability of roxithromycin capsule

作　　者：蒋学华[1,2,3] 赵语[1,2,3] 陈得光 程强[1,2,3] 赵劲松 周天杰[1,2,3] 

机构地区：[1]华西医科大学药学院 [2]四川抗菌素工业研究所 [3]华西医科大学附属第四医院

出　　处：《中国药学杂志》1997年第4期221-224,共4页Chinese Pharmaceutical Journal

摘　　要：目的：研究罗红霉素胶囊在正常人体内的药动学与相对生物利用度。方法：采用反相高效液相色谱法测定１０名志愿者单剂量ｐｏ３００ｍｇ罗红霉素胶囊与罗力得片后的血药浓度变化情况，计算二者的药动学参数与相对生物利用度，以ＡＵＣ０→∞与ｃｍａｘ／ＡＵＣ为指标，用配对ｔ检验法与双单侧ｔ检验法分析两种制剂的生物等效性。结果：二者药时曲线可用一室模型拟合，二者的Ｋ分别是０．０８８４ｈ－１与０．０８７３ｈ－１；ｔｍａｘ分别是３．１３ｈ与２．９６ｈ；ｃｍａｘ分别是５．０８μｇ·ｍｌ－１与５．５１μｇ·ｍｌ－１；ＡＵＣ０→∞是７６．３７μｇ·ｈ·ｍｌ－１与７９．３４μｇ·ｈ·ｍｌ－１。配对ｔ检验与双单侧ｔ检验结果均表明：二者ＡＵＣ０→∞与ｃｍａｘ／ＡＵＣ０→∞均无显著性差异（Ｐ＞０．０５）。结论：罗红霉素胶囊与罗力得片为生物等效制剂，罗红霉素胶囊的相对生物利用度为９６．２６％。OBJECTIVE: To study the pharmacokinetics and relative bioavailability of roxithromycin capsule. METHODS: The roxithromycin concentrations in plasma were determined by HPLC method following a single oral dose of roxithromycin capsule and roxithromycin tablet respectively given to 10 volunteers in a open randomized cross over test.RESULTS: The concentration time courves of roxithromycin capsule and roxithromycin tablet were conformed to an one compartment open model with a first order absorption. The K was 0.0884 h -1 and 0.0873 h -1 , t max 3.13 h and 2.96 h, c max 5.08 μg·ml -1 and 5.51 μg·ml -1 , AUC 0→∞ 76.37 μg·h·ml -1 and 79.34 μg·h·ml -1 of roxithromycin capsule and roxithromycin tablet respectively. There was no significant difference between the two formulations in the AUC 0→∞ and c max /AUC 0→∞ . CONCLUSION: The results of statistical analysis showed that the two formulations were bioequivalent. The relative bioavailability was 96.26% of roxithromycin capsule.

关 键 词：罗红霉素 生物利用度 药代动力学 

分 类 号：R978.15[医药卫生—药品]