目的:研究盐酸二甲双胍肠溶片与普通片的药动学和生物利用度。方法:受试者交叉口服单剂量(1000 mg)肠溶片与普通片,用反相高效液相色谱法测定血药浓度。结果:两种片剂的主要药动学参数分别为Cmax(2.9±0.7)mg·L-1和(2.6±0.6)mg·L-1,Tmax为(2.6±0.4)和(2.3±0.5)h ,T1/2Ka为(0.87±0.26)h和(0.81±0.23)h,T1/2Ke为(1.6±0.4)h和(1.9±0.6)h,AUC为(12.2±1.1)mg·L-1·h-1和(11.9±1.2)mg·L-1·h-1。肠溶片相对于普通片的生物利用度F为(103.0±12.0)%。结论:两种剂型的各药动学参数之间差异均无显著性(P>0.05),经双向单侧t检验,两制剂具有生物等效性。
Abstract
OBJECTIVE The pharmacokinetics and bioavailability of metformin hydrochloride enteric dissolve tablets were compared with stomach dissolving tablets.METHODS Plasma levels of metformin were detected by RP-HPLC method.RESULTS The parameters of the two formulations for metformin: Cmax of enteric and stomach dissolving tablets were (2.9±0.7) mg·L-1 and (2.6±0.6)mg·L-1,Tmax(2.6±0.4) h and(2.3±0.5)h;T1/2Ka(0.87±0.26) h and (0.81±0.23) h;T1/2Ke(1.6±0.4)and(1.9±0.6)h, AUC(12.2±1.1)and(11.9±1.2) mg·L-1·h-1 respectively.The relative bioavailability of enteric dissolving tablets was (103.0±12.0)%.CONCLUSIONS There was no significant difference in pharmacokinetic parameters. It was demonstrated that the two preparations were bioequivalent by one two-sidest tests.
关键词
盐酸二甲双胍 /
肠溶片 /
药动学 /
生物利用度 /
反相高效液相色谱法
{{custom_keyword}} /
Key words
metformin hydrochloride /
enteric dissolve tablets /
pharmacokinetics /
bioavailability /
RP-HPLC
{{custom_keyword}} /
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
参考文献
[1]刘京,申竹芳,谢明智.HPLC法测定盐酸二甲双胍肠溶胶囊及片剂的人体药代动力学及其生物利用度[J].中国临床药理学杂志,1994,10(3):175.
[2]Caille G, Lacasse Y, Raymond M, et al. Bioavailability of metformin in tablet form usimg a new high pressure liquid chromatography assay method[J]. Biopharm Drug Dispos,1993,14:257.
[3]胡绍文,郭瑞林. 实用糖尿病学[M]. 北京:人民军医出版社出版,1998.112.
{{custom_fnGroup.title_cn}}
脚注
{{custom_fn.content}}