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Effect of PEG 4000 in the crystal engineering of Candesartan Cilexetil for solubility enhancement by Polymer Enriched Bridging Liquid technique
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| Author:
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MANOJ K, SEENIVASAN P, ARUL K, SENTHIL KUMAR M
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| Abstract:
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The major obstacle in the development of the formulation for Candesartan Cilexetil, an effective antihypertensive
agent is the poor bioavailability aroused from poor water solubility. The study was intended for investigating the effect
of polyethylene Glycol 4000 (PEG4000) in the crystal engineering of Candesartan Cilexetil. The Polymer Enriched
Bridging Liquid (PEBL) technique was carried out for the solubility enhancement. The PEG 4000 was incorporated in
the bridging liquid and added during the formation of crystal agglomerates. The yield and drug content were
determined to analyze the incorporation of polymer in the aggregates. Saturation solubility, Micromeritic
characteristics, FT-IR analysis, X-Ray diffraction studies, DSC analysis, SEM and in-vitro dissolution analysis were also
carried for analyzing the improvement of solubility of hydrophobic drug. The yield obtained was satisfactory and the
drug content analysis revealed the inclusion of polymer in the aggregates. The flow property was significantly
improved. The saturation solubility analysis also confirmed the solubility enhancement in water and also in pH 6.5
phosphate buffer of 0.05M containing 0.35% polysorbate 20. The DSC analysis indicated the reduction in crystallinity;
this was supported by XRD analysis having a reduction in the intensity of crystalline peaks. The SEM analysis revealed
the porous nature of the crystal aggregates. The in-vitro dissolution analysis also confirmed the augmentation of
dissolution of crystal aggregates prepared by Polymer enriched bridging liquid technique. The PEBL technique using
PEG4000 as hydrophilic polymer can be considered as an effective technique for the enhancement of flow
characteristics, solubility and dissolution enhancement of Candesartan Cilexetil
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| Keyword:
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Candesartan Cilexetil, PEG4000, Polymer enriched bridging liquid technique, PEBL, solubility enhancement
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| EOI:
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| DOI:
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https://doi.org/10.31838/ijpr/2019.11.04.039
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| Download:
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