Efavirenz displays low and variable bioavailability because of its poor aqueous solubility and high log P-value. The present investigation was aimed to improve the dissolution profile of efavirenz by using a simple, scalable and cost-effective technique of liquisolid compact. The drug was dissolved in Trancutol-HP for preparing the liquid medicament which was subsequently mixed with carrier and coating material to make free-flowing and compressible powder. 3² full factorial design was used to optimize the formulation in which the Neusilin US2/Corn starch ratios and carrier/coating material ratio were selected as independent variables. The results of in-vitro dissolution test proved that liquisolid compacts have significantly higher dissolution rate than tablets containing pure drug. Results of DSC and XRD studies suggested that the high dissolution of the drug from the liquisolid compacts was possibly because of the drug either being in an amorphous state or being molecularly dispersed within the internal matrix of compacts.

Efavirenz的水溶性差，log P值高，显示出较低的可变生物利用度。本研究旨在通过使用一种简单，可扩展且具有成本效益的液固压块技术来改善依非韦伦的溶出度。将药物溶解在Trancutol-HP中，以制备液体药物，然后将其与载体和包衣材料混合，制成自由流动和可压缩的粉末。使用3 ²全因子设计来优化配方，其中选择Neusilin US2 /玉米淀粉比例和载体/涂层材料比例作为自变量。体外结果溶出度试验证明，液状固体压片的溶出度明显高于含纯药物的片剂。DSC和XRD研究的结果表明，药物从液体固体压块中的高度溶解可能是由于药物处于无定形状态或分子分散在压块的内部基质中。