FORMULATION AND EVALUATION OF CANDESARTAN CO-PRECIPITATE WITH HYDROPHILIC POLYMERS; PREPARATION OF ORODISPERSIBLE TABLETS
Asmaa M. Dewedar*, Ebtessam A. Essa and Ahmed A. Donia
ABSTRACT
Candesartan cilexetil is an angiotensin-receptor blocker that suffer from inadequit and variable oral bioavailability due to its poor aqueous solubility and presystemic metabolism. Therefore, the objectives of this study was to enhance candesartan cilexetil dissolution with subsequent preparation of mouth dispersable tablets. The drug was precipitated from its ethanolic solution over Aerosil 200 as carrier for the deposited microcrystals. To improve surface wettability, the precipitation step was performed in presence of hydrophilic polymer. The selected polymers were polyvinylpyrrolidone 40T (PVP), hydroxypropylmethyl cellulose E5 (HPMC), Poloxamer 407 and polyethylene glycol6000 (PEG). The products were evaluated regarding dissolution pattern. Physical characterization was also evaluated for selected formulations. Thermal behaviour and X-ray powder diffraction results confirmed reduced drug crystalinity. Infra-red spectroscopy indicated drug-excipient compatibilty. All formulations showed imrovement in drug dissolution compared to pure drug. Presence of polymer resulted in higher initial release and dissolution efficiency. Best formulations regarding dissolution were successifly used in the preparation of oral dispersible tablets with fast drug release. Drug precipitation over carrier with large surface area in presence of hydrophilic polymer is a promising approach for enhancing dissolution rate of poorly soluble drugs.
Keywords: Candesartan cilexetil, Aerosil 200, enhance dissolution rate, Orodispersible Tablets.
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