RESUMO
Hepatic disease is one of the high-prevalence diseases in China, of which gastrointestinal bleeding is a common complication treated by proton pump inhibitors. Vonoprazan is a novel proton pump inhibitor which acts better than lansoprazole in pharmacokinetics and pharmacodynamics. In this study, the pharmacokinetics of vonoprazan was compared between acute hepatic injury and normal condition in rats. Results showed that the exposure (AUC) of vonoprazan was significantly higher in rats with acute hepatic injury than in normal rats, and the metabolites formation rates of vonoprazan also slowed down, which might be due to the change of activity of enzymes and transporters. This find may provide a theoretical basis for the dose regulation of vonoprazan in patients with hepatic injury.
RESUMO
Guizhi Fuling Capsule (GZFL), composed of Cassia Twig, Pachyma Cocos, Cortex Moutan, Radices Paeoniae Alba, and Peach Kernel, is a compound Chinese medicine preparation refined by modern technology. Modern pharmacology study shows that GZFL has pharmacological activities such as anti-inflammatory, analgesic, antitumor, smooth muscle relaxing, endocrine adjusting, and immunity enhancing activities. GZFL can be used in treatment of gynecological disease such as uterine fibroids, pelvic inflammatory disease, dysmenorrheal, and endometriosis in clinic, and it can be also used for the treatment of varicocele, hyperplasia of prostate, stroke, and carotid atherosclerosis. The phase II clinical trials of GZFL in treatment of primary dysmenorrhea in the United States of America have already finished. This paper makes a systematic review of the pharmacological activities and clinical applications of GZFL in recent years, in order to provide reference for its further development and utilization.
RESUMO
Drug metabolism studies, including in vivo and in vitro metabolism studies, are significant in the design of candidate compounds and screening of lead compounds at drug discovery/development stages. Compared with in vivo metabolism studies, in vitro metabolism studies have the advantages of rapidity, simplicity, without consumption of large amounts of samples and animals. Moreover, it is convenient for researchers to observe the selective interaction between compound and target. Therefore, in vitro metabolism studies are appropriate for high throughput screening of compounds which are lack of metabolism information and have been widely used during drug discovery stages. This article briefly introduced the application of in vitro drug metabolism studies based on the metabolic stability, reaction phenotyping and metabolic drug-drug interactions, aiming to raise valuable evaluation strategies for innovative drug discovery in China.