Pharmacokinetic study of matrine injection in rats with different administration ration routes by LC-MS/MS method / 中国药学杂志

ABSTRACT

OBJECTIVE: To investigate the pharmacokinetics of matrine injection by different routes of administration. METHODS: Twenty healthy SD rats were enrolled in this study. They were randomly divided into two groups and received intraperitoneal and intravenous administration of matrine injection at dose of 15 mg·kg-1 respectively. Blood samples (0.3-0.4 mL) were immediately collected into heparinized tubes before injection and at 0.033, 0.083, 0.167, 0.333, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 12 h after injection. Plasma sample concentrations were determined by a validated LC-MS/MS method. The pharmacokinetic parameters including AUC0-12, AUC0-∞, MRT0-12, MRT0-∞, t½, Vd, CL and ρmax were calculated. RESULTS: The main pharmacokinetic parameters for matrine after intraperitoneal and intravenous administration at dose of 15 mg·kg-1 were as followsAUC0-12 (10 166±2 426), (12 217±2 968) ng·mL-1·h;AUC0-∞ (10 230±2 432), (12 300±3 031)- ng·mL-1·h;MRT0-12 (1.91±0.41), (2.14±0.54) h;MRT0-∞ (2.01±0.41), (2.26±0.64) h; t½(2.26±0.89), (2.60±1.25) h;Vd(4 998±2 010), (6 175±2 540) mL;CL (1 531±315.0), (1 727±475.6) mL·h-1·kg-1; ρmax (5 246±1 187), (8 503±1 101) ng·mL-1, respectively. The bioavailability of intraperitoneal administration is 83.21%. CONCLUSION: No significant differences were observed in AUC, MRT, t½ and CL values of matrine between different administrations except for ρmax and Vd.