Formula optimization of simvastatin self-emulsifying drug delivery system and its pharmacokinetics in Beagle dogs
Dan Su · 2009
Aim:To optimize the formula of simvastatin self-emulsifying drug delivery system (SEDDS) and the release kinetics.Methods:In this research,screening the formula of simvastatin SEDDS on the basis of the solubility of simvastatin in various kinds and ratios of surfactants and oil phases.Reverse dialysis bag technique was developed for assay of simvastatin SEDDS.Results:The optimized formula of simvastatin SEDDS was composed of simvastatin 20 mg,IPM 240 mg,Cremophor RH-40 160 mg,0.5% of SLS.The pharmacokinetic parameters of the test and reference drugs were as follow:tmax(4.10±1.70) and (2.7±0.8) h,cmax(24.14±15.90) ng/mLand (27.85±12.94) ng/mL,t1/2 (6.27±3.03) h and (2.83±0.37) h and AUC0-τ (214.05±127.72) h ·ng/mL and (142.77±66.54) h ·ng/mL,respectively.The relative bioaviliability of the test product to the reference was (141.60±24.80)%.Conclusion:The self-emulsifying drug delivery system of simvastatin were prepared successfully.The dosage form significantly increased the bioavailability.