Preparation and Evaluation of Atorvastatin Calcium Self-microemulsifying Drug Delivery System / 中国药师

ABSTRACT

Objective: To develop and optimize a self-microemulsifying drug delivery system (SMEDDS) formula for improving the dissolution of atorvastatin calcium.Methods: Solubility and pseudo-ternary phase diagram were used to select the suitable type and amount range of oil phase, surfactant and co-surfactant.D-optimal mixture design was used to optimize the formula of atorvastatin calcium SMEDDS.The morphology, particle size distribution and zeta potential of the microemulsion were determined by a dilution method.The in vitro drug release profiles of the marketed atorvastatin calcium tablets and the self-made SMEDDS were compared.Results: The formula of atorvastatin calcium SMEDDS was as follows Capmul MCM as the oil phase, Labrasol as the surfactant and Transcutol P as the co-surfactant with the optimal weight ratio of 13.0∶43.5∶43.5.The self-made SMEDDS was a clear and transparent microemulsion solution with homogeneous small spheres as seen under a transmission electron microscope.The particle size, PdI and zeta potential of the self-made SMEDDS was (34.2±13.6) nm, (0.169±0.04) and (-21.1±1.3) mV, respectively.The in vitro release profile indicated that the accumulated release of the self-made SNEDDS reached up to nearly 100% in 45 min.Conclusion: The optimal formula of atorvastatin calcium SMEDDS optimized by D-optimal mixture design can improve the drug dissolution rate effectively.