Phutthatiraphap Siriporn, Hayashi Yoshihiro, Fujii Takuto, Kosugi Atsushi, Okada Kotaro, Kadozaki Tetsuo, Ishise Toru, Sakai Hideki, Onuki Yoshinori
Department of Pharmaceutical Physiology, Graduate School of Medicine and Pharmaceutical Sciences, University of Toyama.
Department of Pharmaceutical Technology, Graduate School of Medical and Pharmaceutical Science, University of Toyama.
Chem Pharm Bull (Tokyo). 2018;66(9):896-900. doi: 10.1248/cpb.c18-00390.
To investigate the inhibitory effect of a commercial proton pump inhibitor (lansoprazole) on the gastric proton pump H,K-ATPase in vitro, we used orally disintegrating (OD) tablets including original brand-name and generic tablets. In the course of the development of generic products, dissolution and clinical tests are necessary to ensure their bioequivalence to the original brand-name products; by contrast, there is almost no opportunity to demonstrate their activity in vitro. This study initially compared the similarity of the dissolution of test generic tablets with that of the original brand-name tablets. The dissolution tests for 15 and 30-mg lansoprazole tablets found their dissolution properties were similar. Subsequently, the dissolution media were sampled and then their effects on the H,K-ATPase activity were measured using tubulovesicles prepared from the gastric mucosa of hogs. We confirmed that the inhibitory effects of the generic tablets on H,K-ATPase activity were consistent with those of the original brand-name tablets. Furthermore, lansoprazole contents in each tablet estimated from their inhibitory effects were in good agreement with their active pharmaceutical ingredient content. To our knowledge, this is the first technical report to compare the in vitro biochemical activity of lansoprazole OD tablets between the original brand-name and generic commercial products.
为了在体外研究一种市售质子泵抑制剂（兰索拉唑）对胃质子泵H，K - ATP酶的抑制作用，我们使用了口腔崩解片，包括原研品牌片和仿制药片。在仿制药开发过程中，需要进行溶出度和临床试验以确保其与原研品牌产品的生物等效性；相比之下，几乎没有机会在体外证明其活性。本研究首先比较了受试仿制药片与原研品牌片的溶出度相似性。对15毫克和30毫克兰索拉唑片的溶出度测试发现它们的溶出特性相似。随后，对溶出介质进行取样，然后使用从猪胃黏膜制备的微管泡测量它们对H，K - ATP酶活性的影响。我们证实仿制药片对H，K - ATP酶活性的抑制作用与原研品牌片一致。此外，根据其抑制作用估算的每片兰索拉唑含量与其活性药物成分含量高度一致。据我们所知，这是第一份比较原研品牌和市售仿制药兰索拉唑口腔崩解片体外生化活性的技术报告。
