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The absorption and metabolism of this compound have not been investigated systematically. This study aims to illustrate the pharmacokinetic characters of GL\u2010V9 by exploring its metabolic status under different administration routes. To further clarify the absorption mechanism of GL\u2010V9, an <jats:italic>in situ<\/jats:italic> single\u2010pass perfusion model and a Caco\u20102 cell monolayer model were used. Meanwhile, a microsomal incubation system was used to evaluate the enzyme kinetic parameters. <jats:italic>In vivo<\/jats:italic>, the obtained gastrointestinal availability (F<jats:sub>a<\/jats:sub> \u00d7 F<jats:sub>g<\/jats:sub>) was 21.28\u00a0\u00b1\u00a05.38%. The unmetabolized fraction in the gut wall (F<jats:sub>gut wall<\/jats:sub>) was 98.59\u00a0\u00b1\u00a09.74%, while the hepatic bioavailability (F<jats:sub>h<\/jats:sub>) was 29.11\u00a0\u00b1\u00a05.22%. These results indicated that poor absorption and extensive metabolism may contribute greatly to the low bioavailability of GL\u2010V9. The effective permeability (P<jats:sub>eff<\/jats:sub>) in the duodenum and jejunum was 1.34\u00a0\u00b1\u00a00.50\u00a0\u00d7\u00a010<jats:sup>\u22124<\/jats:sup> and 0.90\u00a0\u00b1\u00a00.27\u00a0\u00d7\u00a010<jats:sup>\u22124<\/jats:sup>\u00a0cm\/s, respectively. The high permeability of GL\u2010V9 indicated that other unknown factors (such as metabolism) may account for its systemic exposure problem. Studies in rat liver microsomal (RLMs) confirmed this hypothesis, and the Cl<jats:sub>int, CYP450s and UGT<\/jats:sub> of GL\u2010V9 was 0.20\u00a0ml\/min\/mg protein. In conclusion, these results suggest that GL\u2010V9 possesses higher permeability than wogonin and the metabolism of GL\u2010V9 is related to its disposition in rat intestine and liver.<\/jats:p>","DOI":"10.1002\/bdd.2179","type":"journal-article","created":{"date-parts":[[2019,4,1]],"date-time":"2019-04-01T02:25:09Z","timestamp":1554085509000},"page":"151-161","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["Mechanistic study of absorption and first\u2010pass metabolism of GL\u2010V9, a derivative of wogonin"],"prefix":"10.1002","volume":"40","author":[{"given":"Han","family":"Xing","sequence":"first","affiliation":[{"name":"Clinical Pharmacokinetics Laboratory China Pharmaceutical University  Nanjing Jiangsu Province 211198 China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Chang","family":"Ren","sequence":"additional","affiliation":[{"name":"Clinical Pharmacokinetics Laboratory China 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