摘要
８名健康志愿者自身交叉对照，口服单剂量曲尼司特缓释胶囊或普通胶囊２００ｍｇ后，利用ＨＰＬＣ法测得血浆中曲尼司特浓度分别在４．５±０．８和３．２±１．３ｈ达到峰值２９．８±３．８和３６．５±６．３ｍｇ／Ｌ。血药浓度曲线下面积分别为４６１．６±７７．５和４５１．３±８９．１ｍｇ·ｈ－１·Ｌ－１，缓释胶囊的相对生物利用度为１０３．３±１０．３％。８名志愿者自身交叉口服多剂量曲尼司特缓释胶囊（１５０ｍｇ，ｂｉｄ）或普通胶囊（１００ｍｇ，ｔｉｄ）后，测得其稳态时的Ｃｍａｘ分别为４１．３±８．０和４２．７±１１．５ｍｇ／Ｌ，Ｃｍｉｎ分别为２４．５±５．８和２１．２±７．６ｍｇ／Ｌ。两者的血药浓度的波动系数ＦＩ分别为５６．２±１０．０和６８，３±３０．２。经双单侧ｔ检验，两种胶囊具有生物等效性。
The relative biavailability of a slow released and conventional formulations of tranilast were determined after a single and multiple oral dose of tranilast given to & volunteers in an open randomized crossover study. After a single oral dose (200 mg)the peak levels in plasma averaged 29.8±3.8 and 36.5±6.3 mg/ L at 4.5±0.8 and 3.2±1.3 h and t he AUC were 461.6±77.5 and 45 1.3±89.1 mg. h-1. L-1 for slow-released and conventional formulations respectively.The relative bioavailavility of slow - released formulation was 103.3±10.3%.Following multiple dosing mean steady state Cmax values were 43.1±7.6 and 42.7±11.5 mg/L and mean Cmin values were 24.5±5.8 and 21.2±7.6 mg/L for slow released and conventional formulation respectively. The peak-to-through fluctuation index(FI)for the two formulations were 56.2±10.0 and 68.3±30.2,respectively.The result of two one sided tests showed that the two formulations were bioequivalent.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1996年第3期164-167,共4页
The Chinese Journal of Clinical Pharmacology
