Kurosawa N, Morishima S, Owada E, Ito K
Hokkaido Institute of Pharmaceutical Sciences, Japan.
Yakugaku Zasshi. 1993 Apr;113(4):321-6. doi: 10.1248/yakushi1947.113.4_321.
In order to obtain a basic knowledge for developing the rectal dosage form of salbutamol (SB), a comparison of the bioavailability was made between oral and rectal administrations. After the intravenous, oral and rectal dosing of SB solution in rabbits, SB and its glucuronide (SBG) in plasma and urine were determined. The bioavailability estimated by the area under the blood concentration-time curve (AUC) of SB from 0 to 9 h after oral and rectal administrations were 1.1 +/- 0.5% and 7.8 +/- 2.2% (mean +/- S. E., n = 5), respectively. Percent of dose excreted in urine as total SB (SB+SBG) 10 h after oral and rectal administrations were 77.3 +/- 3.82% and 9.80 +/- 0.15% (mean +/- S. E., n = 3), respectively, which indicating relatively good oral and poor rectal SB absorption. A partial avoidance of first-pass-effects might contribute to higher bioavailability after the rectal administration.
为了获得开发沙丁胺醇（SB）直肠剂型的基础知识，对口服和直肠给药后的生物利用度进行了比较。在给兔静脉注射、口服和直肠给药SB溶液后，测定血浆和尿液中的SB及其葡糖醛酸苷（SBG）。口服和直肠给药后0至9小时，根据SB血药浓度-时间曲线（AUC）估算的生物利用度分别为1.1±0.5%和7.8±2.2%（平均值±标准误，n = 5）。口服和直肠给药10小时后，以总SB（SB+SBG）形式经尿液排泄的剂量百分比分别为77.3±3.82%和9.80±0.15%（平均值±标准误，n = 3），这表明SB口服吸收相对良好而直肠吸收较差。直肠给药后较高的生物利用度可能部分归因于首过效应的部分规避。
