沙丁胺醇在家兔体内的时间药代动力学

CHRONOPHARMACOKINTICS OF SALBUTAMOL IN RABBITS

沙丁胺醇（Ｓａｌ）抗哮喘作用的昼夜节律，可能与其在体内的药代动力学的昼夜差别有关。为此本文给家兔灌胃２ｍｇ·ｋｇ－１Ｓａｌ，用ＨＰＬＣ荧光检测１０：００ｈ和２２：００ｈ两个时间动物体内血药浓度。结果表明，Ｓａｌ的药动学参数存在明显的昼夜差别。Ｔｐ白天为（２．２８±０．２０）ｈ，夜间为（１．２５±０．３０）ｈ（Ｐ＜０．０５）；ＡＵＣ白天为（０．４１±０．０９）ｍｍｏｌ／Ｌ·ｈ，夜间为（０．３０±０．０５）ｍｍｏｌ／Ｌ·ｈ（Ｐ＜０．０５）；Ｔ１／２白天是（２．７２±０．２２）ｈ，夜间为（１．８６±０．１３）ｈ（Ｐ＜０．０５）；Ｃｍａｘ昼夜无差别。

The circadian changes in the pharmacokinetics of salbutamol in rabbits were studied.All aminals were kept for a minimum period two weekes to adapt to an enviromental room equipped with an automatically timed 12 hour light 12 hour dark illumination cycle before these experiments.Levels of salbutamol(ig salbutamol 2 mg·kg-1) in plasma of two groupes of rabbis were detected by HPLC with a fluorescent detector at 10:00 o'clock and 22: 00 o'clock.Pharmacokinetic parameters showed remarkable circadian changes. Tp was (2.28±0.20) h during the day and(0.25±0.30) h during the night(P<0.05);AUC was(0.41±0.09) mmol·L-1·h during the day and(0.30±0.05) mmol·L-1·h during the night(P<0.05);T1/2 was(2.72±0.22)h during the day and(1.86±0.13) h during the night(P<0.05);Cmax does not change during the day and night.