Effects of carbohydrate polymers in self-microemulsified tablets on the bioavailability of atorvastatin: In vitro-in...

The concentrations of crospovidone (CP), maltodextrin and microcrystalline cellulose (MCC) have been optimized in the development of self-microemulsified tablets (SMET) to improve the oral bioavailability of an anti-hyperlipidemic drug, atorvastatin, and the in-vivo pharmacokinetic parameters of the optimized SMET were compared with those of a commercial tablet in rabbits.

Self microemulsified liquids (SELS) were prepared with oleic acid, Span 40 and Tween 80. SELS were converted into SMET by adsorption, followed by compression using factors such as CP, maltodextrin and MCC, which were optimized through a 2(3)-factorial design considering responses such as the disintegration time and, the times for 50% and 80% of the drug to be released.

The results indicated that CP and MCC were inversely related to the responses, while maltodextrin was directly related to the responses. The droplet size of the disintegrated SMET oil globules was within 2.73 to 4.77 μm. The Cmax and AUC0-∞ of the optimized SMET were found to be 32.5% and 38.8% higher, respectively, than those of the commercial tablet.

The present results indicate that the bioavailability of the SMET of atorvastatin is better than the commercial formulation.