烟酸缓释片的生物等效性研究

Study on Bioequivalence of Nicotinic Acid Sustained-Release Tablets

目的建立烟酸血浆浓度测定法,并进行该药的生物等效性研究。方法采用随机双交叉设计,30例健康受试者口服国产烟酸缓释片(受试制剂)和进口烟酸缓释片(参比制剂)各1 500 mg,采用高效液相色谱-质谱串联法测定血浆中烟酸浓度。结果受试制剂与参比制剂的药-时曲线下面积(area under the curve,AUC0→15)分别为(20 046.1±16 286.8)和(21 605.0±18 058.5)ng.h.mL-1,AUC0→∞分别为(20 806.0±16 300.7)和(22 811.2±18 468.3)ng.h.mL-1;Cmax分别为(8 716.3±6 811.2)和(9 570.2±8 217.1)ng.mL-1;tmax分别为(4.414±1.337)和(4.310±1.285)h;t1/2分别为(4.000±4.898)和(2.906±3.393)h。受试制剂的相对生物利用度为(96.6±30.9)%。结论国产烟酸缓释片与进口烟酸缓释片具有生物等效性。

Objective To establish a method for determination of nicotinic acid in human plasma and study its bioequivalence in Chinese healthy volunteers. Methods Thirty healthy volunteers were orally administered with 1 500 mg nicotinic acid（test） tablets in a randomized crossover design.The drug levels in plasma samples were determined by a HPLC-MS/MS method. Results The main pharmacokinetic parameters of the test and reference preparations were as follows：AUC0→15 was（20 046.1±16 286.8）,（21 605.0±18 058.5） ng·h·mL-1,AUC0→∞ was（20 806.0±16 300.7） and（22 811.2±18 468.3） ng·h·mL-1;Cmax was（8 716.3±6 811.2） and（9 570.2±8 217.1） ng·mL-1;tmax was（4.414±1.337） and（4.310±1.285） h;t1/2 was（4.000±4.898） and（2.906±3.393） h.The relative bioavailability of the test tablet was（96.6±30.9） %. Conclusion The domestically made nicotinic acid tablets and those imported are bioequivalent.