环孢素胶丸的药代动力学和相对生物利用度

Pharmacokinetics and Relative Bioavailability of Cyclosporin Pearls in Healthy Volunteers

采用高效液相色谱法进行环孢素胶丸的药代动力学和生物利用度研究，１０名健康志愿者随机交叉单剂量ｐｏ温州第二制药厂和瑞士Ｓａｎｄｏｚ公司的环孢胶丸（２００ｍｇ），其血药浓度－时间曲线均符合一级吸收的双室模型，温州产环孢素胶丸的主要药动学参数ｔ１／２Ｋｄ＝１．０９±０．４６ｈ，ｔ１／２α＝０．３４±０．１５ｈ，ｔ１／２β＝５．１３±１．４１ｈ，ｔｍａｘ＝１．１９±０．１９ｈ，Ｃｍａｘ＝８７８．２±１６７．２ｎｇ／ｍｌ，ＡＵＣ＝４１２７．７±８５４．１ｎｇ·ｈ·ｍｌ－１，其相对生物利用度为（１０４．２±１１．９）％

The pharmacokinetics of cyclosporin from Wenzhou and Sandoz pearls was separately studied in healthy male volunteers after single oral administration at the dosage of 200 mg. Cyclosporin concentration in blood was determined by HPLC. The concentration time curve of cyclosporin from Wenzhou was fitted to two compartment model of the first order absorption. The pharmacokinetics parameters were estimated as follows: t 1/2Kd =1.09±0.46 h, t 1/2α =0.34±0.15 h, t 1/2β =5.13±1.41 h, t max =1.19±0.19 h, C max =878.2±167.2 ng/ml,AUC=4127. 7±854.1 ng·h·ml -1 . Relative bioavailability of Wenzhou pearls was 104.2%, compared with Sandoz pearls.