溶解度 溶解 差示扫描量热法 傅里叶变换红外光谱 材料科学 核化学 泊洛沙姆 生物利用度 水溶液 化学 溶剂 扫描电子显微镜 化学工程 色谱法 聚合物 有机化学 共聚物 复合材料 工程类 物理 热力学 生物 生物信息学
作者
Rahul K. Mali
出处
期刊:Asian Journal of Pharmaceutics [BRNSS Publication Hub]
卷期号:11 (2) 被引量:4
标识
DOI:10.22377/ajp.v11i02.1299
摘要

Aim: Olmesartan medoxomil (OLM) is a poorly soluble drug and its low aqueous solubility leads to poor dissolution and bioavailability. The aim of this work was to improve the solubility of poorly aqueous soluble drug OLM by solid dispersion (SD) technique. Materials and Methods: A phase solubility study was performed to determine the effect of various polymers on aqueous solubility of drug. The binary SD of OLM was prepared by using poloxamer 407. The SDs were prepared by kneading, melting and solvent evaporation (SE) method by varying drug to carrier ratio. The optimized SD formulations were characterized by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and powder X-ray diffraction (XRD). Fast disintegrating tablets (FDTs) of OLM were formulated using optimized SD. The in vitro evaluation of FDTs was done including stability studies. Results: Phase solubility study indicated 5.3 fold increase in solubility of OLM by Poloxamer 407. The results of FTIR, DSC, SEM, and XRD study showed the conversion of crystalline form of OLM to amorphous form. The results revealed that SD prepared by SE method showed rapid dissolution as compared to other methods. The FDTs of optimized SD containing croscarmellose sodium showed faster and complete in vitro drug release within 20 min. Formulation M6 was found to be optimized formulation owing to its 84.09 dissolution efficiency, 4.82 min mean dissolution time and 100% drug release. Optimized formulation was found to be stable for 3-month period. Conclusion: The results conclusively confirmed successful improvement in dissolution of poorly water-soluble drug OLM.

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