Year : 2017 | Volume
: 16 | Issue : 3 | Page : 157--167
Physicochemical characterization of olmesartan medoxomil: polymer solid dispersions by hot melt extrusion for dissolution rate enhancement
Zaheer Abbas1, N.G. Nanjunda Swamy2
1 Formulation Development Department, Apotex Research Private Limited, Bangalore, India
2 Retd. Professor, Department of Pharmaceutics, Government College of Pharmacy, Bangalore, India
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. In-vitro 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 in-vitro 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.
Apotex Research Private Limited, Site 1 and 2, Bommasandra Industrial Area, 4th Phase, Jigani Link Road, Bangalore 560099, Karnataka
|How to cite this article:|
Abbas Z, Swamy NN. Physicochemical characterization of olmesartan medoxomil: polymer solid dispersions by hot melt extrusion for dissolution rate enhancement.Egypt Pharmaceut J 2017;16:157-167
|How to cite this URL:|
Abbas Z, Swamy NN. Physicochemical characterization of olmesartan medoxomil: polymer solid dispersions by hot melt extrusion for dissolution rate enhancement. Egypt Pharmaceut J [serial online] 2017 [cited 2018 Dec 17 ];16:157-167
Available from: http://www.epj.eg.net/article.asp?issn=1687-4315;year=2017;volume=16;issue=3;spage=157;epage=167;aulast=Abbas;type=0