盐酸二甲双胍缓释片的药动学及相对生物利用度  

Study on relative bioavailability and pharmacokinetics of metformin hydrochloride sustained-release tablets in healthy dogs

作　　者：李华[1] 李嘉煜[1] 聂淑芳[1] 潘卫三[1] 

机构地区：[1]沈阳药科大学药剂教研室,辽宁沈阳110016

出　　处：《中国医院药学杂志》2004年第7期404-406,共3页Chinese Journal of Hospital Pharmacy

摘　　要：目的 :研究盐酸二甲双胍普通市售片与自制缓释片在家犬体内的药动学和相对生物利用度。方法 :6条健康雄犬随机分成 2组 ,进行双交叉自身对照试验。采用反相高效液相色谱法测定家犬血浆中的药物浓度 ,以血药浓度 时间数据计算药动学参数。结果 :盐酸二甲双胍缓释片与普通片的t1/ 2 (ke) 分别为 (8.3± 2 .8)和 (3.8± 2 .1)h ;ke 分别为 (0 .0 9± 0 .0 3)和(0 .2 4± 0 .13)h-1;Tmax分别为 (3.3± 0 .8)h和 (1.5± 0 .8)h ;Cmax分别为 (9.8± 3.5 )和 (14 .6± 4 .3)mg·L-1;AUC0 -∞ 分别为(70 .2± 33.5 )和 (6 2 .5± 2 3.3)mg·h·L-1。经方差分析差异均无显著性 (P >0 .0 5 ) ,自制缓释片的相对生物利用度为112 .3%。结论 :自制盐酸二甲双胍缓释片与普通片具有生物等效性。OBJECTIVE The relative bioavailability between metformin hydrochloride (MH) sustained-release tablets and commercial tablets and the pharmacokinetics were studied in 6 healthy dogs. METHODS The study was conducted in a two-treatment,two-period,two-sequence randomized cross-over trial. The plasma concentration of MH after an oral single-dose in the subjects was determined by HPLC.The important pharmacokinetic parameters were caculated. RESULTS From the plasma concentration-time data of both preparations in the single-dose study,the t 1/2(ke)、k e、t max、C max and AUC 0-∞ for metformin hydrochloride sustained-release tablets and commercial tablets were( 8.3± 2.8) and ( 3.8± 2.1)h,( 0.09± 0.03) and ( 0.24± 0.13) h -1,( 3.3± 0.8) and ( 1.5± 0.8)h,( 9.8± 3.5) and ( 14.6± 4.3)mg·L -1,( 70.2± 33.5) and ( 62.5± 23.3) mg·h·L -1,respectively. A adequate ANOVA analysis showed that there was no significant difference (P> 0.05) between them. The relative bioavailability of the metformin hydrochloride (MH) sustained-release tablet was 112.3%.CONCLUSION These two dosage forms were bioequivalent.

关 键 词：盐酸二甲双胍 高效液相色谱法 药物动力学 相对生物利用度 

分 类 号：R969.1[医药卫生—药理学]