CAJ | 학술논문

目的以一种进口速释片(IRM)为对照,通过单剂量和多剂量口服给药后,评价国产二甲双胍缓释片(SRM)的相对生物利用度.方法选择18名健康男性受试者,年龄18～22岁,体重55～76 kg,身高166～180 cm,血糖水平4.0～5.9 mmol/L.采用离子对色谱法测定血浆中二甲双胍SRM的浓度.结果与IRM比较,单剂量给药后,SRM的MRT、tmax和t1/2明显延长,cmax显著降低.这一结果与多剂量试验一致.单剂量和多剂量试验中,SRM的相对生物利用度分别为(85.95±0.97)%和(86.44±7.88)%.对数转换后,AUC的90%置信区间分别为0.83～0.88和0.83～0.89,在生物等效的0.80～1.25范围内 .结论 SRM具有缓释动力学特征;单剂量给药的相对生物利用度近似于多剂量给药;两种给药方式均证明SRM和IRM两制剂生物等效.
목적이일충진구속석편(IRM)위대조,통과단제량화다제량구복급약후,평개국산이갑쌍고완석편(SRM)적상대생물이용도.방법선택18명건강남성수시자,년령18～22세,체중55～76 kg,신고166～180 cm,혈당수평4.0～5.9 mmol/L.채용리자대색보법측정혈장중이갑쌍고SRM적농도.결과여IRM비교,단제량급약후,SRM적MRT、tmax화t1/2명현연장,cmax현저강저.저일결과여다제량시험일치.단제량화다제량시험중,SRM적상대생물이용도분별위(85.95±0.97)%화(86.44±7.88)%.대수전환후,AUC적90%치신구간분별위0.83～0.88화0.83～0.89,재생물등효적0.80～1.25범위내 .결론 SRM구유완석동역학특정;단제량급약적상대생물이용도근사우다제량급약;량충급약방식균증명SRM화IRM량제제생물등효.
Purpose To evaluate the relative bioavailability of a domestic sustained-release metformin tablets (SRM) compared against an immediate-release metformin tablets (IRM) using a multiple-dose,two-way crossover design after a single-dose study. Methods Eighteen healthy adult male volunteers,aged 18 to 22 years (mean,20 years),weighing 55 to 76 kg (mean,64 kg) and with height ranging from 166 to 180 cm (mean,173 cm),and blood glucose levels from 4.0 to 5.9 mmol/L (mean,4.3 mmol/L) participated in the study.The concentrations of metformin in plasma were determined using a ion-pair liquid chromatographic method. Results In single-dose study,the mean residence time (MRT),Tmax,and apparent elimination half-life (T1/2) for SRM were significantly longer and Cmax significantly lower than the corresponding values determined for IRM.The similar results were also demonstrated in multiple-dose study.The mean values of the relative bioavaibility of SRM compared with IRM in two administration ways were (85.95±0.97)% and (86.44±7.88)%,respectively.The single-dose and multiple-dose administration of the 90% confidence interval for the ratio of the logarithmic transformed AUC values of SRM over those of IRM were calculated to lie between 0.83 and 0.88,0.83 and 0.89,respectively,being within the acceptable bioequivalence limit of 0.80～1.25. Conclusion SRM was of the characteristic of sustained-release pharmacokinetics.The relative bioavailability for single dosing was similar to that of multiple dosing,and both of the administration ways demonstrated bioequivalence in absorption between SRM and IRM.