Objective: To study pharmacokinetic parameters and absolute bioavailability for oral use of sinomenine tablet in beagle dogs.
Method: Applying to double cycle self crossover design, a single oral or intravenous dose of 10 mg x kg(-1) sinomenine was given to 10 beagle dogs. Drug concentrations in plasma were determined by HPLC. The pharmacokinetic parameters were calculated by 3P97 pharmacokinetic program.
Result: The concentration-time curves of oral administration fitted to one compartment model in the beagle dogs. The T(max), C(max), t1/2 and AUC(0-T) was (82.5 +/- 13.9) min, (0.15 +/- 0.027) mg x L(-1), (87.6 +/- 28.3) min and (28.43 +/- 3.48) mg x min x L(-1), respectively. The concentration -time curves of i.v. fitted to two compartment model in the beagle dogs. The t1/2beta and AUC(0-T) was (106.7 +/- 120.2) min and (93.32 +/- 82.08) mg x min x L(-1). The absolute bioavailability for oral use was (30.46 +/- 4.24)%.
Conclusion: The absolute bioavailability of sinomenine is low, and the elimination of sinomenine tablet is fast.
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