摘要
目的：研制生物利用度较好的苯巴比妥栓剂。方法：以３种不同基质制成苯巴比妥栓剂，并比较它们在家兔体内的药物动力学。采用荧光偏振免疫分析法测定血药浓度，按二室血管外给药模型进行药物动力学参数模拟。结果：以水溶性基质脂肪酸聚氧乙烯醚（Ｓ－４０型）制成的栓剂的主要药动学参数分别为Ｋａ１．０１±０．２２ｈ－１，Ｔｍａｘ２．４２±０．１１ｈ，Ｃｍａｘ１１．１±１．３μｇ·ｍｌ－１，ＡＵＣ９２４±１１０μｇ·ｈ·ｍｌ－１，均明显优于以３６＃半合成脂肪酸酯和聚乙二醇－４０００为基质的栓剂（Ｐ＜０．０１）。结论：３种栓剂的释药性具有显著性差异，以脂肪酸聚氧乙烯醚（Ｓ－４０型）为基质的栓剂最好。
Aim:To prepare phenobarbital suppository of good bioavailability.Methods:Three kinds of suppositories were made by different excipient,and their pharmacokinetics in rabbit were compared.Serum concentration was determined by FPIA.Results:The parameters of the suppository made with soluble excipient,stearate polyoxylethylene ether (type S40),were Ka 1.01±0.22 h-1,T_max 2.42±0.11 h,Cmax11.1±1.3 μg·ml-1,AUC924±110 μg·h·ml-1 ,markedly higher than that of the other two suppositories (P<0.01).Conclusion:The drug release in three suppositories were different,among them the suppository made of stearate polyoxylethylene ether (type S40) was the best.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
1998年第8期344-346,共3页
Chinese Journal of Hospital Pharmacy
关键词
苯巴比妥
栓剂
药物动力学
生物利用度
phenobarbital,suppository,pharmacokinetics,bioavailability
