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目的:制备新型大剂量盐酸二甲双胍渗透泵控释片,以市售控释片为对照,对服用渗透泵片的Beagle犬进行体内药代动力学研究,并对体外释放和体内吸收的相关性做出评价。方法:选用聚环氧乙烷(PEO)和十二烷基硫酸钠(SDS)等为主要辅料,制备盐酸二甲双胍单层渗透泵片;用f2相似因子法考察剂型的体外释放行为,并与市售控释片释放度进行比较;采用单剂量和多剂量交叉试验进行Beagle犬体内药代动力学研究。结果:与市售控释片进行比较,相似因子f2=75.0。单剂量和多剂量犬体内试验相对生物利用度分别为(101.31±15.81)%和(99.46±12.55)%。结论:自制盐酸二甲双胍渗透泵片具有与市售片相似的缓释效果,主要药代动力学参数无显著差异,两个制剂的生物利用度接近。
OBJECTIVE: To prepare a new type of high-dose metformin hydrochloride osmotic pump controlled release tablets. The controlled release tablets were taken as control. The in vivo pharmacokinetics of Beagle dogs with osmotic pump tablets were studied. The correlation between in vitro release and in vivo absorption Comment. Methods: Polyethylene oxide (PEO) and sodium dodecyl sulfate (SDS) were selected as the main excipients to prepare metformin hydrochloride monolayer osmotic pump tablets. The in vitro release behavior of the formulations was investigated by f2 similarity factor method. The controlled release tablets were compared. The single-dose and multi-dose crossover tests were used to study the pharmacokinetics of Beagle dogs. Results: Compared with the commercial controlled release tablets, the similarity factor f2 = 75.0. The relative bioavailability of single-dose and multi-dose in vivo tests were (101.31 ± 15.81)% and (99.46 ± 12.55)%, respectively. CONCLUSION: Self-made metformin hydrochloride osmotic pump tablets have sustained-release effect similar to the commercially available tablets with no significant difference in the main pharmacokinetic parameters. The bioavailability of the two formulations is similar.