Enhancement of Dissolution of Atorvastatin Tablets by Using Self-emulsifying Microemulsion Technology

Abstract

Atorvastatin is a first-line drug in the treatment of hyperlipidemia. However, the poor water-solubility of atorvastatin affects its bioavailability. Formulating a self-emulsifying microemulsion system (SMEDDS) before combining and compressing tablets helps to increase dissolution and stability and is the simple preparation method chosen in this study. Objective: to improve the dissolution of tablets containing atorvastatin. Material and Methods: Atorvastatin raw materials (China) were provided by ADC Co., Ltd. Research. SMEDDSs consisting of a mixture of oil, surfactant, and cosurfactant, when diluted with an aqueous medium, spontaneously formed fine o/w microemulsion with less than 100 nm in droplet size were surveyed. Then, SMEDDS-containing tablets were prepared using the direct compression method. Results: M3F4 (Capryol 90 – 20%, Cremophor RH40 – 40%, and propylene glycol – 40%) was the SMEDDS formulation that met the criteria for durability in different environments. M3F4's particle size was 22.08 nm. The combined tablet formulation including Avicel PH102, Syloid xdp 3050:SMEDDS (1:1), polyvinyl pyrrolidone 30, sodium starch glycolate, talc, and magnesium stearate improved dissolution (99.42% after 30 minutes) compared with the formulation containing ingredients (29.76% after 30 minutes). The dissolution of atorvastatin tablets was improved by the self-microemulsification technique.