化学发光微粒子免疫法研究甲钴胺在健康人体内的药动学和生物等效性

Investigation of Pharmacokinetics and Bioequivalence of Mecobalamin in Healthy Volunteers by Chemiluminescent Microparticle Immunoassay

目的:研究甲钴胺在健康人体内的药动学和生物等效性。方法:采用自身交叉三周期的实验设计,19名健康受试者分别口服两种甲钴胺制剂1.5 mg后,采用化学发光微粒子免疫法测定血清中甲钴胺的浓度,DAS 3.0软件计算药动学参数,进行等效性评价。结果:受试制剂和参比制剂的甲钴胺药动学参数:tmax分别为(4.2±1.9)h和(4.4±2.4)h,Cmax分别为(322.0±145.4)ng·L-1和(282.2±108.1)ng·L-1,t1/2分别为(19.2±5.3)h和(20.0±6.3)h,AUC0-72分别为(6769.1±2169.4)ng·h·L-1和(6400.6±1921.5)ng·h·L-1,AUC0-∞分别为(7334.2±2376.5)ng·h·L-1和(6992.4±2076.1)ng·h·L-1,受试制剂的相对生物利用度F(0-72)为105.9%±13.2%,F(0-∞)为104.9%±12.6%。结论:本试验建立的血清甲钴胺浓度测试方法简便、准确,两种制剂生物等效。

Objective： To develop a chemiluminescent microparticle immunoassay （CMIA） method for the determination of meco- balamin in human serum to investigate the pharmacokinetics and bioequivalence of meeobalamin. Methods： A single oral dose of two kinds of meeobalamin was given to 19 healthy volunteers in a randomized three-period crossover study. The concentrations of mecobal- amin in serum were assayed by CMIA, the main pharmaeokinetic parameters were analyzed by DAS 3.0 software, and the bioequiva- lenee was evaluated. Results： The main pharmaeokinetic parameters of test and reference mecobalamin tablets were as follows： tmax were （4.2± 1.9）h and （4.4 ±2.4）h,Cmax were （322.0 ± 145.4） ng . L^-1 and （282.2 ±108.1） ng . L^-1 ,t1/2 were （19.2 ±5.3） hand （20.0±6.3）h,AUC0-72were （6769.1±2 169.4） ng.h. L^-1and （6400.6±1 921.5） ng. h. L^-1.F（0-72） and F（0-∞） of the test tablets was 105.9% ± 13.2% and 104.9% ± 12.6% ,respectively; Conclusion： The method is simple and precise. The two tablets are bioequivalent.