Pharmacokinetic And Bioequivalence Study On Three Preparations Of Cyclosporine A In Chinese Healthy Volunteers

ObjectiveCyclosporine A was used in organ transplantation since 1980'.From then up to now, organ transplantation was into"Cyclosporine era". Cyclosporine A has to be the most extensive immunodepressant. But as a drug with a low therapeutic index, it requires individualized monitoring of blood concentration.This article is designed to study the pharmacokinetics and bioequivalence of cyclosporin A capsules in Chinese healthy volunteers.Methods1.Development of HPLC method for the determination of whole blood concentration of cyclosporin A.There was no interference from endogeneous substances in human whole blood.2.Eighteen healthy volunteers were given a single oral dose of test and reference preparations ,respectively. Blood samples were collected at 0.5,1.0,1.5,2.0,3.0,4.0,6.0,8.0,10.0,12.0,24.0,48.0 h,after oral administration.3. Blood samples of kidney transplantation patients were collected at 0, 0.25, 0.5, 0.75,1.0, 1.5, 2.0, 3.0, 4.0, 6.0, 8.0, 12.0 h after oral administration at the tenth day after operation respectively.4. Determination of ciclosporine A in whole blood of sixty-three kidney transplantation patients by HPLC and FPIA.Results1.The linear range for cyclosporin A was 50～2500μg·L-1(r=0.9951),the minimum quantitation limit was 50μg·L-1. The...