Enhancement of Valsartan Dissolution Rate by the Increased Porosity of Pellets Using Supercritical CO2: Optimization via Central Composite Design
Tóm tắt
The aim of this research was to optimize the enhancement the porosity of pellet containing valsartan (VAL) using carbon dioxide at supercritical pressure (scCO2) via central composite design (CCD) to increase the release at simulated gastrointestinal fluids (pH 1.2 and 6.8). To prepare the pellet, an extrusion/spheronization apparatus was used. Central composite design was applied to reach the optimum % porosity, dissolution efficiency (DE %) for both different pH. The size, shape, mechanical properties, porosity, specific surface area, pore size, pre-, and post-scCO2 pellets were analyzed for surface shape as well as in vitro drug release behavior was investigated. The maximum % porosity (42.89%), DE % at pH 1.2 (36.08%), and at pH 6.8 (99.68%) were observed when 50 °C, 200 bar, 72 min, and 27 min were the temperature, pressure, soaking time, and depressurize time, respectively. Pre- and post-scCO2 pellet release rates were much greater at pH 1.2 than the VAL powder form, with around 30 to 50% of the release occurring at 6 h, sequential. At pH 6.8, post-scCO2 pellets release almost 100% of the drug in 30 min, while the VAL powder and pre-scCO2 pellets release approximately 72% and 92% of the drug during 6 h, respectively. Thus, the dissolving rate of the poorly water-soluble VAL was improved by using a post-scCO2 pellet in pH 1.2 and pH 6.8 environments by an increase in the porosity of the pellet due to the scCO2 treatment.
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