Jiangang Chen, Xiaoli Bian, Sanqi Zhang, Guangde Yang
{"title":"两种新型喹唑啉PI3K/mTOR双抑制剂的药代动力学和组织分布研究。","authors":"Jiangang Chen, Xiaoli Bian, Sanqi Zhang, Guangde Yang","doi":"","DOIUrl":null,"url":null,"abstract":"<p><p>S<sub>1</sub> and S<sub>2</sub>, two structurally similar quinazoline derivatives, are novel anticancer drugs targeting the PI3K/AKT/mTOR signaling pathway channel. However, their pharmacokinetic and tissue distribution characteristics are unknown, which has hindered further development and in-depth studies. In this study, a simple, rapid and sensitive method using high performance liquid chromatography was established and validated to quantitatively study the pharmacokinetics and tissue distribution profiles of S<sub>1</sub> and S<sub>2</sub> in rats following intravenous injection. The results indicated that after intravenous injection, the elimination of S<sub>1</sub> and S<sub>2</sub> fit the two-compartment model and linear pharmacokinetics characteristics were observed. Furthermore, S<sub>1</sub> and S2 were widely distributed and found in high concentrations in liver and kidney tissues and a small proportion of S<sub>1</sub> and S<sub>2</sub> could cross the blood-brain barrier and be distributed in the brain. The current findings will contribute to interpretation and understanding the relationship between dosage and pharmacodynamic effects of S<sub>1</sub> and S<sub>2</sub>.</p>","PeriodicalId":19971,"journal":{"name":"Pakistan journal of pharmaceutical sciences","volume":null,"pages":null},"PeriodicalIF":0.7000,"publicationDate":"2023-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Pharmacokinetics and tissue distribution study of two novel quinazoline PI3K/mTOR dual-inhibitors, potential anticancer agents.\",\"authors\":\"Jiangang Chen, Xiaoli Bian, Sanqi Zhang, Guangde Yang\",\"doi\":\"\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>S<sub>1</sub> and S<sub>2</sub>, two structurally similar quinazoline derivatives, are novel anticancer drugs targeting the PI3K/AKT/mTOR signaling pathway channel. However, their pharmacokinetic and tissue distribution characteristics are unknown, which has hindered further development and in-depth studies. In this study, a simple, rapid and sensitive method using high performance liquid chromatography was established and validated to quantitatively study the pharmacokinetics and tissue distribution profiles of S<sub>1</sub> and S<sub>2</sub> in rats following intravenous injection. The results indicated that after intravenous injection, the elimination of S<sub>1</sub> and S<sub>2</sub> fit the two-compartment model and linear pharmacokinetics characteristics were observed. Furthermore, S<sub>1</sub> and S2 were widely distributed and found in high concentrations in liver and kidney tissues and a small proportion of S<sub>1</sub> and S<sub>2</sub> could cross the blood-brain barrier and be distributed in the brain. The current findings will contribute to interpretation and understanding the relationship between dosage and pharmacodynamic effects of S<sub>1</sub> and S<sub>2</sub>.</p>\",\"PeriodicalId\":19971,\"journal\":{\"name\":\"Pakistan journal of pharmaceutical sciences\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.7000,\"publicationDate\":\"2023-09-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pakistan journal of pharmaceutical sciences\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pakistan journal of pharmaceutical sciences","FirstCategoryId":"3","ListUrlMain":"","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Pharmacokinetics and tissue distribution study of two novel quinazoline PI3K/mTOR dual-inhibitors, potential anticancer agents.
S1 and S2, two structurally similar quinazoline derivatives, are novel anticancer drugs targeting the PI3K/AKT/mTOR signaling pathway channel. However, their pharmacokinetic and tissue distribution characteristics are unknown, which has hindered further development and in-depth studies. In this study, a simple, rapid and sensitive method using high performance liquid chromatography was established and validated to quantitatively study the pharmacokinetics and tissue distribution profiles of S1 and S2 in rats following intravenous injection. The results indicated that after intravenous injection, the elimination of S1 and S2 fit the two-compartment model and linear pharmacokinetics characteristics were observed. Furthermore, S1 and S2 were widely distributed and found in high concentrations in liver and kidney tissues and a small proportion of S1 and S2 could cross the blood-brain barrier and be distributed in the brain. The current findings will contribute to interpretation and understanding the relationship between dosage and pharmacodynamic effects of S1 and S2.
期刊介绍：
Pakistan Journal of Pharmaceutical Sciences (PJPS) is a peer reviewed multi-disciplinary pharmaceutical sciences journal. The PJPS had its origin in 1988 from the Faculty of Pharmacy, University of Karachi as a biannual journal, frequency converted as quarterly in 2005, and now PJPS is being published as bi-monthly from January 2013.
PJPS covers Biological, Pharmaceutical and Medicinal Research (Drug Delivery, Pharmacy Management, Molecular Biology, Biochemical, Pharmacology, Pharmacokinetics, Phytochemical, Bio-analytical, Therapeutics, Biotechnology and research on nano particles.
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