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The purpose of this study was to determine the absorption, distribution, and excretion profiles of fasudil in rats and beagle dogs, respectively, to clarify its pharmacokinetic pattern. A sensitive and reliable LC\u2013MS\/MS method has been developed and established and successfully applied to pharmacokinetic study, including absorption, tissue distribution, and excretion. The results revealed that in the range of 2\u20136 mg\/kg, the pharmacokinetic behavior for instance, AUC and C<jats:sub>max<\/jats:sub>, in rats was observed in a dose dependent manner. However, the plasma concentrations were indicative of a significant gender difference in the pharmacokinetics of fasudil in rats, in terms of absolute bioavailability and excretion. Interestingly, the resulting data obtained from beagle dogs showed that there was no gender difference in the absolute bioavailability of fasudil hydrochloride after single or repeated administrations. In conclusion, this study characterized the pharmacokinetic pattern fasudil both in rats and beagle dogs through absorption, tissue distribution and excretion study. The findings may be valuable and provide a rationale for further study and its safe use in clinical practice.<\/jats:p>","DOI":"10.1002\/bdd.2231","type":"journal-article","created":{"date-parts":[[2020,5,8]],"date-time":"2020-05-08T12:57:34Z","timestamp":1588942654000},"page":"206-220","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["Absorption, tissue disposition, and excretion of fasudil hydrochloride, a RHO kinase inhibitor, in rats and dogs"],"prefix":"10.1002","volume":"41","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-4836-739X","authenticated-orcid":false,"given":"Wenjun","family":"Liu","sequence":"first","affiliation":[{"name":"Anhui Medical University  China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jing","family":"Gao","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Drug Delivery Technology and Pharmacokinetics Tianjin Institute of Pharmaceutical Research  China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xiulin","family":"Yi","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Drug Delivery Technology and Pharmacokinetics Tianjin Institute of Pharmaceutical Research  China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yazhuo","family":"Li","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Drug Delivery Technology and Pharmacokinetics Tianjin Institute of Pharmaceutical Research  China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yong","family":"Zeng","sequence":"additional","affiliation":[{"name":"State Key Laboratory of Drug Delivery Technology and Pharmacokinetics Tianjin Institute of Pharmaceutical Research  China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2020,6,17]]},"reference":[{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.2176\/nmc.50.7"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1002\/jat.1737"},{"key":"e_1_2_8_4_1","doi-asserted-by":"publisher","DOI":"10.4103\/1673-5374.230294"},{"key":"e_1_2_8_5_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1478-3231.2005.01142.x"},{"key":"e_1_2_8_6_1","doi-asserted-by":"publisher","DOI":"10.1177\/0091270006293767"},{"issue":"12","key":"e_1_2_8_7_1","first-page":"1585","article-title":"Fasudil improves cognition of APP\/PS1 transgenic mice via inhibiting the activation of microglia and shifting microglia phenotypes from M1 to M2","volume":"33","author":"Jiezhong Y. 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