摘要
目的对国产与进口吲达帕胺片(抗高血压药)在中国健康人体中的药代动力学进行研究,并对两种制剂的生物等效性进行评价与分析。方法 2008年1月～2009年6月选择60名健康受试者为试验对象,采用自身对照随机交叉试验法,单位剂量口服参比制剂(进口的吲达帕胺片)和受试制剂(国产的吲达帕胺片)2.5mg,两次用药间隔一周。采用液相色谱-串联质谱法(InertsilODS-3色谱柱,pH4磷酸盐缓冲液-乙腈-甲醇55B40B5与甲醇梯度洗脱,240nm波长检测)测定给药后不同时间的全血中吲达帕胺浓度,并计算药物代谢动力学的参数以及相对的生物利用度,并做方差分析和双单侧t检验,最后进行生物等效性分析。结果参加试验的健康人在实验过程中,均未出现药物不良反应。单位剂量口服参比制剂(进口的吲达帕胺片)和受试制剂(国产的吲达帕胺片)的数据如下所示:Cmax分别为(28.30±8.64),(27.05±8.33)μg·L-1;Tmax分别是(2.98±1.52),(2.90±1.22)h;T1/2分别是(14.80±3.68),(14.50±3.85)h;AUCo∞m分别是(552.75±179.25),(529.23±181.98)μg·L-1·h-1;AUCo∞分别是(587.43±211.16),(575.76±195.32)μg·L-1·h-1。结论国产的吲达帕胺制剂与进口的吲达帕胺制剂在体内的吸收、分布与消除过程非常相似,因此两种制剂为生物等效制剂。
Objective To observe the pharmacokinetics and bioequiva- lenee of domestic and imported indapamide tablets in healthy volunteers.Methods A single dose of 2.5 mg indapamide was given to 60 healthy volunteers in a randomized cross—over study.The concentrations of inda.Pamide in plasma weredetermined by HPLC—-MS/MSmethod.The phar- macokinetie parameters were calculated and the bioavailability and bio·equivalence of two formulations wereevaluated.Results After a single dose,the phannacokinetic parametersf or indapamide were as follows：Cmax were（28.30±8.64）,（27.05±8.33）μg·L-1;Tmax were（2.98±1.52）,（2.90±1.22）h;tl/2 were（14.80±3.68）,（14.50±3.85）h;AUCo∞m。were （552.75±179.25）,（529.23 ±181.98）μg·L-1.h-1;AUCo∞ were （587.43±211.16）,（579.76±195.32）μg·L-1. h-1,respectively.Thepa-rameters among themwereno significant difference（Po.05）.Conclusion The results demonstrated that the two preparations were bioequivalent.
出处
《当代医学》
2013年第8期141-142,共2页
Contemporary Medicine
