【摘要】 以英国 Ｇｌａｘｏ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ生产的沙丁胺醇控释片（Ｖｏｌｍａｘ， ８ ｍｇ）为参比制剂，采用随机分组交叉试验设计方法，考察 ２０名健康男性志愿受试者单剂量和多剂量口服成都地奥公司生产的硫酸沙丁胺醇缓释胶囊（Ｓａｌｂｕｔａ， ８ ｍｇ）后的药代动力学和相对生物利用度，ＨＰＬＣ－紫外检测器测定血浆中沙丁胺醇的浓度。用３Ｐ８７药动学程序对结果进行处理。单剂量给药时，Ｓａｌｂｕｔａ和Ｖｏｌｍａｘ分别在５５０±０．８５ｈ和５．３０±０.９５ ｈ达到峰浓度１０.６１±３.９４ｎｇ·ｍＬ-１和１０．５２±２．５９ ｎｇ·ｍＬ-１，血药浓度曲线下面积分别为 １２４.７４±３３.８６ｈ·ｎｇ．ｍＬ－１和 １２６.０２±３８．１７ｈ·ｎｇ·ｍＬ－１，Ｓａｌｂｕｔａ的相对生物利用度为９８.９８±１２.０４％。多剂量给药达稳态时，Ｃ分别为１２.９４±３.３５ｎｇ·ｍＬ－１和１２.６±３.３６ｎｇ·ｍＬ．Ｃ　分别为５.８４±１.３４ ｎｇ·ｍＬ－１和６.１６±１.３３ｎｇ·ｍＬ-１，平均稳态血药浓度 Ｃａｖ分别为 ８.７２±２．１７ ｎｇ·ｍＬ-１和 ８．６７±２．１６ ｎｇ·ｍＬ-１，波动度 ＤＦ分别为 ８１.８２±１７.７４％和７６.０３±２０.４８％更多还原

【Abstract】 The pharmacokinetics and relative bioavailability of a sustained-release capsule of albuterol （Salbuta） made by CDDA （China） were investigated following a single and multiple oral dose given to 20 healthy male volunteers in a randomized 2-way cross-over study. The controlled-release tablet of albuterol （Volmax） made by Glaxo （U.K.） was used as reference preparation. Plasma concentration of albuterol was determined by a newly developed HPLC method with UV detection. After a single oral dose the peak concentrations C_max were 10,6± 3.94 ng·mL-1 and 10.52±2.59 ng·mL-1 at 5.50±0.85 h and 5.30±0.95 h and the AUC0　 were 124.74±33.86 h·ng· mL-1 and 126.02±38. 17 h.ng·mL-1 for Salbuta and Volmax respectively. The relative bioavailability of Salbuta was 98.98±12.04%. Following multiple dosing, mean steady state C values were 12.94±3.35 ng·mL-1 and 12.60± 3.36 ng.mL-1, mean C values were 5.84±1.34 ng.mL-1 and 6. 16±1.33 ng·mL-1, the degree of fluctuation （DF） was 81.82±17.74% and 76.03±20.48% for the two formulations respectively. The results of statistical comparison showed that the two preparations were bioequivalent.更多还原