正常人口服单剂量和多剂量沙丁胺醇控释胶囊的药代动力学及相对生物利用度

THE PHARMACOKINETICS AND RELATIVE BIOAVAILABITY OF A CONTROLLED──RELEASE FORMULATION OF ALBUTREOL AFTER SINGLE AND MULTIPLE DOSING IN NORMAL VOLUNTEERS

１０名健康志愿者，随机交叉口服单剂量沙丁胺醇控释胶囊或普通片后，利用ＨＰＬＣ测得血浆中沙丁胺醇浓度分别在４．７８±０．２６和２．２６±０．３７ｈ达到峰值１４．４±２．０３和２５．３±６．０３μｇ／ｌ。血药浓度曲线下面积分别为１０９．３±１４．４和１０９．５±１５．８μｇ·ｈ￣（－１）．Ｌ￣（－１）控释胶囊的相对生物利用度为１０１％±１４。８名志愿者随机交叉口服多剂量沙丁胺醇控释胶囊或普通片后，测得其稳态时的Ｃｍａｘ分别为２２．８±２．６和２０．２±１．２μｇ·ｈ￣（－１）·Ｌ￣（－１），Ｃｍｉｎ分别为９．４１＋０．８和８．４９±０．８μｇ／ｌ。两者的血药浓度的波动系数ＦＩ分别为６８．８±６．９和８６．４±８．９。经双单侧ｔ检验法检测，两种制剂具有生物等效性．

the pharmacokinetics and relative bioavailability of a controlled-release formulation of albuterol was determined following a single and multiple oral dose of albuterol given to volnuteers in an open randomized crossover study. After a single oral dose the peak levels in plasma averaged 14.4±2.0 and 25.3±6.0μg/l at 4.87±0.3 and 2.26±0.4h and the AUC were 109.3±14.4 and 109.5±15.8μg·h-1·L-1for controlled-release and conventional formulations respectively. The bioavailability of controlled-release formulation was 101%±14.Following multiple dosing mean steady state Cmax values were 22.8±2.6 and 20.2±1.2μg/l and mean Cmin values were 9.41±0.8 and 8.49±0.8μg/l for controlled-release and comventional formulation respectively.The peak-to-trough fluctuation index(FI)for the two formulation were 68.8±6.9 and 86.40±8.9 respectively.The result of two one-sided tests showed that the two formulation was bioequivalence.