乙琥胺在兔体内从栓剂中的释放及直肠吸收
Release and rectal absorption of ethosuximide from suppositories in rabbits.
作者信息
Ghazy F S, Mohamed M S, Kassem A A, Elhoseiny B M
机构信息
Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, ARE.
出版信息
Pharmazie. 1988 Jul;43(7):484-5.
Ethosuximide was formulated in different suppository bases. In vitro release experiment demonstrated more rapid and higher release of the drug from water soluble polyethylene glycol (PEG) bases than from Witepsol fatty bases. Rectal administration in PEG 400:4000 and 400:6000 to rabbits gave high plasma levels where Cmax was 45.66 and 42.66 micrograms.ml-1, respectively; while, in the presence of Witepsol E76 and W35 it was 34.00 and 28.33 micrograms.ml-1, respectively. The systemic availability was 89.39%, 82.72%, 58.80% and 47.45% when the bases were PEG 400:4000, PEG 400:6000, Witepsol E76 and Witepsol W35, respectively.
乙琥胺被制成不同的栓剂基质。体外释放实验表明，该药物从水溶性聚乙二醇（PEG）基质中的释放比从Witepsol脂肪基质中更快且释放量更高。对兔子直肠给药PEG 400:4000和PEG 400:6000时，血浆水平较高，Cmax分别为45.66和42.66微克·毫升-1；而在Witepsol E76和W35存在的情况下，Cmax分别为34.00和28.33微克·毫升-1。当基质分别为PEG 400:4000、PEG 400:6000、Witepsol E76和Witepsol W35时，全身利用率分别为89.39%、82.72%、58.80%和47.45%。
Zotero 插件