RESUMEN
Objective To evaluate the release characteristics in vitro, pharmacokinetics in rabbits and in vivo-in vitro correlation of silymarin phospholipid complex microporous osmotic pump controlled release tablets（SM-PC MPOP）. Methods The release characteristics of SM-PC MPOP in vitro were detected by HPLC in the artificial gastric fluid. Six beagle dogs were subjected to double cycle cross control, which were given SM-PC MPOP and Legalon（30 mg/kg）. The concentration of silybin in plasma was determined by HPLC and the data were processed by software. Results The cumulative release rate of SM-PC MPOP in vitro was over 85% in 12 h. The pharmacokinetics in beagle dogs showed that SM-PC MPOP and legalon conformed to double compartment first-order absorption model and the pharmacokinetic parameters were obtained: tmax:（3.2±0.4）and（0.9±0.1）h, Cmax:（0.298 6±0.068 9）and（0.629 9±0.076 5）μg/ml, AUC0→24:（2.996 8±0.583 3）and（2.268 9±0.432 8）h·μg /ml. The relative bioavailability of SM-PC MPOP was（162.21 ± 30.82）%. Conclusion SM-PC MPOP could release slowly, which could increase the relative bioavailability significantly. The correlation between the absorption in vivo and release in vitro was fine（r = 0.839 0）.
RESUMEN
Objective To prepare osmotic pump-controlled release tablets of total flavones in Lysimachia clethroides.Methods Two components of the extract from L.clethroides,rutin and naringenin-7-O-glucoside were used to evaluate the release behavior of osmotic pump controlled release tablets.Single factor investigation was carried out on the membrane compositions and orifice variables,and uniform design was used to optimize the formulation of coating mambrane.Results The membrane weight,PEG400 content,and dibutyl phthalote(DBP) content were the main factors influencing the drug release,and based on 45% and 8.5% of cellulose acetate,respectively,to prepare osmotic pump-controlled release tablets could achieve the desired zero-order release profile.Conclusion The formulation and technology are simple and easy to be carried out.Osmotic pump-controlled release tablets have a stable drug release bahavior and a good reproducibility.