Preparation, Characterization and Pharmacokinetics in Vivo of Oxymatrine–Phospholipid Complex

The aim of the present study was to prepare oxymatrine– phospholipid complex to enhance oral bioavailability of oxymatrine and to study its physicochemical properties and to compare the pharmacokinetic characteristics and bioavailability after oral administration of oxymatrine– phospholipid complex in rats. Using tetrahydrofuran as a reaction medium, oxymatrine and phospholipids were resolved into the medium, after the organic solvent was removed under vacuum condition, oxymatrine–phospholipid complex was formed. The new complex’s physicochemical properties including differential scanning calorimetry (DSC), X-ray diffraction (XRD), N-octanol/water Partition Coefficient were tested. The concentrations of oxymatrine after oral administration of oxymatrine–phospholipids complex and oxymatrine at different time in rats were determined by HPCE. The pharmacokinetic parameters were computed by software program 3p87. The data showed that oxymatrine and phospholipids in the oxymatrine–phospholipid complex were combined by noncovalent bond, not forming a new compound and the solubility of oxymatrine –phospholipid complex in n-octanol was effectively enhanced. The better hepatocytes permeability was obtained by the phospholipid complex. We found that mean plasma concentration–time curve of oxymatrine after oral administration of oxymatrine–phospholipid complex and oxymatrine in rats was both in accordance with open two-compartment model with firstorder absorption. Pharmacokinetic parameters of oxymatrine ,physical mixture and the complex in rats were T max 1.71, 1.91and 2.17 h, C max 0.164,0.247 and 0.437 μg·ml, AUC 0–∞ 2.87, 3.23 and 9.43μg·h·ml, respectively. The bioavailability of oxymatrine in rats was increased remarkably after oral administration of oxymatrine–phospholipid complex comparing to oxymatrine and the physical mixture. This was mainly due to an impressive improvement of the lipophilic property of oxymatrine–phospholipid complex. *Corresponding author: Hai-Long Yuan, 302 Hospital of PLA&PLA Institute of Chinese Materia Medica, Beijing, China, Tel: 86-10-66933324; Fax: 86-10-63879915; E-mail: [email protected] Received August 19, 2009; Accepted October 23, 2009; Published October 23, 2009 Citation: Yue PF, Yuan HL, Yang M, Zhu WF (2009) Preparation, Characterization and Pharmacokinetics in Vivo of Oxymatrine–Phospholipid Complex. J Bioequiv Availab 1: 099-102. doi:10.4172/jbb.1000015 Copyright: © 2009 Yue PF, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Preparation, Characterization and Pharmacokinetics in Vivo of Oxymatrine–Phospholipid Complex Peng-Fei YUE, Hai-Long YUAN*, Ming Yang, Wei-Feng ZHU Jiangxi University of Traditional Chinese Medicine,Nanchang 330004 Key Lab of Modern Preparation of TCM, Ministry of Education, Nanchang 330004 302 Hospital of PLA&PLA Institute of Chinese Materia Medica, Beijing 100039