title: A study on the PK and BA profiles in the mouse body for leonurine O/O microemulsion with determination by the LC-MS/MS method.
abstract: Leonurine (LE) has been found to have therapeutic efficacy in cerebral thrombosis, but its poor solubility in water leads to very low bioavailability. In this article, a leonurine O/O microemulsion (LE-ME) was prepared and investigated for its in vivo pharmacokinetic behavior and bioavailability in the mouse body using an aqueous suspension of leonurine (LE-SWW) for the control group. A simple, sensitive and specific method, HPLC-MS/MS, was developed for detection of the LE content in mouse plasma using n-benzoyl-L-arginine ethyl ester as an internal standard. The results demonstrated that the C max of LE-ME was 2.46-fold higher than that of the suspension following oral administration. The absolute bioavailability was 10.95 %, while that of the suspension was only 1.78 %. The T 1/2β and MRT of LE-ME were 3.04- and 4.19-fold those of the suspension, respectively. In addition, following intramuscular administration of LE-ME, the absolute bioavailability was 37.45 %. The results indicated that LE-ME is a promising drug-delivery system to enhance the absorption and bioavailability of LE.
authors.affiliation: Department of Pharmaceutics, Anhui University of Chinese Medicine, 103 Mei Shan Road, Hefei, Anhui, China.
authors.forename: Yanan
authors.initials: Y
authors.lastname: Sun
authors.affiliation: Department of Pharmaceutics, Anhui University of Chinese Medicine, 103 Mei Shan Road, Hefei, Anhui, China.
authors.forename: Xiang
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Key Laboratory of R&D of Chinese Medicine, Anhui University of Chinese Medicine, Hefei, 20038, Anhui, China.
authors.forename: Tao
authors.initials: T
authors.lastname: Lu
authors.affiliation: Department of Pharmaceutics, Anhui University of Chinese Medicine, 103 Mei Shan Road, Hefei, Anhui, China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Yuan
authors.affiliation: Department of Pharmaceutics, Anhui University of Chinese Medicine, 103 Mei Shan Road, Hefei, Anhui, China.
authors.forename: Qi
authors.initials: Q
authors.lastname: Ding
authors.affiliation: Department of Pharmaceutics, Anhui University of Chinese Medicine, 103 Mei Shan Road, Hefei, Anhui, China. lchchem@126.com.
authors.forename: Chuanhua
authors.initials: C
authors.lastname: Lu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001120:Arginine / Q000031:analogs & derivatives / Q000737:chemistry; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods; D004655:Emulsions / Q000737:chemistry* / Q000493:pharmacokinetics*; D005707:Gallic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D012995:Solubility; D013535:Suspensions / Q000737:chemistry / Q000493:pharmacokinetics; D053719:Tandem Mass Spectrometry / Q000379:methods; D014867:Water / Q000737:chemistry
chemical_list: D004655:Emulsions; D013535:Suspensions; D014867:Water; C013587:leonurine; D005707:Gallic Acid; D001120:Arginine; C009727:benzoylarginine ethyl ester
keywords: Bioavailability; Leonurine; Microemulsion; Pharmacokinetic