健康人单剂量口服茶碱控释胶囊的药物动力学

The pharmacokinetics of controlled release theophylline capsule in healthy volunteers after a signle oral dose

目的：研究７ 名健康志愿者单剂量口服茶碱控释胶囊（ 简称ＣＲＴＣ）４００ ｍｇ 后的药物动力学。方法：用紫外法测定健康人血清中茶碱的血药浓度。结果：ＣＲＴＣ的药物动力学参数分别为：Ｔｍａｘ ＝ （７ ．９ ±１．１）ｈ，Ｃｍａｘ ＝ （４．０ ±０ ．９）μｇ·ｍｌ－１ ，Ｔ１／２ｅ ＝（１７ ．２±２ ．６）ｈ，Ｋｅ ＝（０．０４±０．０６）ｈ－１ ，Ｔ１／２ａ＝ （２ ．１±０ ．９）ｈ，Ｋａ＝（０．２３±０．０４）ｈ－ １ ，ＡＵＣ０７２ ＝ （１３８ ．０±１７ ．６）μｇ·ｈ·ｍｌ－ １ 。结论：ＣＲＴＣ的药物动力学参数与国产茶碱控释片（ 简称ＤＣＲＴＴ）［１］ 相比：其吸收减慢，导致达峰时间延长，达峰浓度降低。但其消除减慢，ＣＲＴＣ在体内蓄积，致使其药时曲线下的面积较ＤＣＲＴＴ 大。

OBJECTIVE:The pharmacokinetics of controlled release theophylline capsule(CRTC) was studied after a signle oral dose of 400 mg in 7 healthy volunteers.METHODS:UV method had been used for the determination CRTC in human serum.RESULTS:The pharmacokinetic parameters for CRTC were: T max =( 7.9 ± 1.1 )h, C max =( 4.0 ± 0.9 )μg·ml -1 , T 1/2e =( 17.2 ± 2.6 )h, K e=( 0.04 ± 0.06 )h -1 , T 1/2a =( 2.1 ± 0.9 )h, K a=( 0.23 ± 0.04 )h -1 , AUC 0 72 =( 138.0 ± 17.6 )μg·h·ml -1 respectively.CONCLUSIONS:The pharmacokinetic parameters of CTPC was compared with that of domestic controlled release theophylline tablet(DCRTT):The absorbtion was slower this resulted in T max prolonged, C max reduced,but the slow elimination lead to CRTC stored up in body, AUC 0 72 increased.