Physicochemical characterization of olmesartan medoxomil | ||||
| Egyptian Pharmaceutical Journal | ||||
| Volume 16, Issue 3, September 2017, Page 157-167 PDF (1.69 MB) | ||||
| DOI: 10.4103/epj.epj_17_17 | ||||
 View on SCiNiTO | ||||
| Authors | ||||
| Zaheer Abbas; N.G. Nanjunda Swamy | ||||
| Abstract | ||||
| Aim The prime objective of this investigation was to improve solubility and dissolution rate of poorly water-soluble drug, olmesartan medoxomil, by preparation of stable solid dispersions (SDs) of low glass transition temperature employing hot-melt extrusion technique. Materials and methods Soluplus (SOL) was used as a primary solubilizing agent along with different solubility/absorption enhancers such as polyethylene glycol (PEG)-8000 and Kolliphor F127. After extrusion, the extrudates were pelletized, and physical state of the drug was assessed using powder X-ray diffraction and differential scanning calorimetry techniques. Results The SDs were found to be amorphous, thermodynamically and physicochemically stable. Scanning electron microscopy of the formulations revealed a surface, indicating absence of crystallinity. The drug content was found to be in the range of 98.16±1.3 to 99.98±1.1%. The dissolution performance of the extrudates was compared with that of the pure drug, and substantial improvement was observed in the order of SOL-PEG-8000>SOL-KF127>SOL only. drug release rate was Higuchi matrix controlled, and the release rate mechanism was found to be non-Fickian. Stability studies over a period of 3 months indicated amorphous nature of drug in the formulation, and no significant deviations were observed in the drug content and drug dissolution characteristics. Conclusion Hot melt extrusion technology promises an ideal platform for enhancing the solubility and dissolution of poorly water-soluble drugs. The results obtained suggest that olmesartan medoxomil in the form of SDs has potential for oral drug delivery and could be an efficacious approach for enhancing therapeutic potential. | ||||
| Keywords | ||||
| hot-melt extrusion; Kolliphor F127; Olmesartan Medoxomil; polyethylene glycol-8000; Solid dispersion; soluplus | ||||
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