Pharmacokinetics of Sinomenine Hydrochloride Controlled-release Pellets in Beagle Dogs

OBJECTIVE To determine pharmacokinetic parameters of sinomenine hydrochloride controlled-release pellets in Beagle dogs and calculate the relative bioavailability.METHODS To use a high performance liquid chromatography (HPLC) method with the mobile phase consisted of methanol-acetonitrile -0.05 mol·L-1 ammonium dihydrogen phosphate solution (50∶12∶190), column temperature was 30 ℃, flow rate of mobile phase was 0.7 mL·min-1 and wavelength of detector was set at 264 nm. RESULTS In the range of 50-4 000 ng·mL-1, the linear between peak-area ratios of sinomenine hydrochloride to IS and drug concentration was good,R=3.6×10-4C＋0.02，r=0.996 4. The precision and recovery were fit for Ch.P(2005)Vol Ⅱ. The pharmacokinetic parameters were t1/2（19.9±4.3）and（17.8±2.1）h,Cmax(638±128)and（1 738±396） ng·mL-1,Tmax（6.2±1.1） and（7.0±1.0）h, AUC0～t（20.2 ±3.3） and（22.8±5.0） h·μg·mL-1 for test and reference preparations, respectively. The relative bioavailability was（90.1±10.4）%.CONCLUSION The concentration-time curve of sinomenine hydrochloride controlled-release pellets in Beagle dogs was flatter and the duration was longer. The present studies achieved our prospective aims.