Jaydip Bhola, Dhaval Mori, Soniwala M M, Chavda Jayant
B.K. Mody Government Pharmacy College, Polytechnic Campus, Near Ajidam, Rajkot, Gujarat, India.
Saudi Pharm J. 2020 Jun;28(6):737-745. doi: 10.1016/j.jsps.2020.04.016. Epub 2020 May 8.
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. 3 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 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.
依非韦伦由于其较差的水溶性和较高的log P值，表现出低且可变的生物利用度。本研究旨在通过使用一种简单、可扩展且经济高效的液固压缩技术来改善依非韦伦的溶出度。将药物溶解在二乙二醇单乙基醚中以制备液体药物，随后将其与载体和包衣材料混合以制成自由流动且可压缩的粉末。采用三因素全因子设计来优化制剂，其中将硅铝酸盐US2/玉米淀粉比例和载体/包衣材料比例作为自变量。溶出度试验结果证明，液固压缩物的溶出速率明显高于含有纯药物的片剂。差示扫描量热法（DSC）和X射线衍射（XRD）研究结果表明，药物从液固压缩物中的高溶出可能是因为药物处于无定形状态或分子分散在压缩物的内部基质中。
