Abstract

To study the pharmacokinetics of matrine (MT) intramuscular administration in rat. Plasma concentration of matrine was determined by HPLC under the following conditions: column (Shim-pack VP-ODS, 4. 6 mm x 150 mm, 5 m); eluent (acetonitrile-0.02 mol ammonium acetate buffer-triethylamine 30: 70: 0.04); flow rate was 1 mL x min(-1) and ultraviolet detection wavelength was set at 220 nm; column temperature 40 degrees C; aliquot injected 20 microL. All data of concentration-time of matrine were treated with pharmacokinetics program DAS 2. 1. 1. A simple, sensitive and reliable method for determining matrine in rat plasma by HPLC was established. The plasma concentration time profiles of MT fitted in with two-compartment models well, and the main pharmacokinetic parameters found for MT after i. m. infusion were as follows: C(max) = 21.113 9 mg x L(-1), t(max) = 0.75 h, t1/2alpha 1.34 h, t1/2beta = 3.509 h, AUC(0-t) = 90.984 mg x h(-1) x L(-1), AUC(0-infinity) = 100.346 mg x h(-1) x L(-1). Compare with oral administration, the matrine is absorbed well and distributes fast with intramuscular administration; the absolute bioavailability of matrine is higher. According to this, the pharmacological action is also stronger and duration is longer.

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