张娜,邓树海,宋华先,黄桂华,徐美
ZHANG Na 1; DENG Shu hai 1; SONG Hua xian 1; HUANG Gui hua 1; XU Mei 2 (1 Department of Pharmaceutics;

• 1:山东医科大学药剂教研室!山东济南250012
• 2:山东医科大学药剂教研室!山东济南250012
• 3:山东医科大学药剂教研室!山东济南250012
• 4:山东医科大学药剂教研室!山东济南250012

摘要(Abstract)：

为了比较氯氮平漂浮片 (自制 )和普通片兔体内药物动力学、相对生物利用度及体内外相关性。用 4只新西兰大白兔自身交叉对照、单剂量灌胃氯氮平漂浮片或普通片各 5 0mg ,采用HPLC法测定血浆氯氮平浓度 ,3p97程序拟合血药浓度 时间数据。结果表明氯氮平漂浮片和普通片符合单室模型特征 ,求得药物动力学参数 :tmax分别为 (3 0 5 7± 0 0 5 9)和 (1 188± 0 191)h ;Cmax分别为 (8 795± 0 494)和 (11 182± 3 45 7) μg/mL ;AUC( 0～t) 分别为 (6 6 0 15± 7 0 2 6 )和 (5 4 881±1 180 ) μg/mL·h ;漂浮片相对生物利用度为 (12 0 2 88± 6 2 77) % ;其体内吸收与体外释药有良好的相关性 (r =0 9811)。
To compare the pharmacokinetics and correlation between in vitro release and in vivo absorption characteristics between the clozapine floating sustained release tablets(SRT)and conventional tablets(CT).Four New Zealand rabbits were given orally SRT and CT,with a single dose of 50mg clozapine in self crossover study.The plasma concentration of clozapine was assayed by HPLC and the pharmacokinetic parameters were calculated with 3p97 program by a computer.Concentration time curves of SRT and CT fitted to one compartment open model,respectively.The t max were(3 057±0 059)and(1 188±0 191)h; C max were(8 795±0 494)and(11 182±3 457)μg/mL; AUC (0～t) were(66 015±7 026)and(54 881±1 180)μg/mL·h;the relative bioavailability of SRT was(120 288±6 277)%.It was relatively good in relationship between bioavailability in vivo and dissolution in vitro ( r =0 981 1 ).The results suggested that SRT has a higher bioavailability than CT.

关键词(KeyWords)： 氯氮平;漂浮片;药物动力学;相对生物利用度
clozapine; floating sustained release tablet; pharmacokinetics; relative bioavailability

Abstract:

Keywords:

基金项目(Foundation): 山东医科大学1999年青年科学研究基金资助项目!(4 13910 )

作者(Authors): 张娜,邓树海,宋华先,黄桂华,徐美
ZHANG Na 1; DENG Shu hai 1; SONG Hua xian 1; HUANG Gui hua 1; XU Mei 2 (1 Department of Pharmaceutics;

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