[PDF][PDF] A novel multicompartment dissolution apparatus for evaluation of floating dosage form containing poorly soluble weakly basic drug

RK Parikh, DC Parikh, RR Delvadia… - Dissolution …, 2006 - dissolutiontech.com
RK Parikh, DC Parikh, RR Delvadia, SM Patel
Dissolution Technologies, 2006dissolutiontech.com
Incorporation of a weakly basic drug into a gastro-retentive dosage form yields better
biomedical benefits compared to incorporation into a conventional controlled release
dosage form. Poorly soluble weakly basic drugs may precipitate upon entry into the small
intestine, and this can affect absorption. To study drug release from floating dosage forms
and simultaneously examine the effect of pH change on poorly soluble weakly basic drugs,
a novel multicompartment dissolution system was developed by modifying beakers. The …
Abstract
Incorporation of a weakly basic drug into a gastro-retentive dosage form yields better biomedical benefits compared to incorporation into a conventional controlled release dosage form. Poorly soluble weakly basic drugs may precipitate upon entry into the small intestine, and this can affect absorption. To study drug release from floating dosage forms and simultaneously examine the effect of pH change on poorly soluble weakly basic drugs, a novel multicompartment dissolution system was developed by modifying beakers. The system consists of three serially placed compartments providing gastric, intestinal, and absorption compartment to mimic the in vivo dissolution and absorption in the gastrointestinal tract. A dosage form remained buoyant in the gastric compartment, released drug was allowed to transfer to the intestinal compartment, and soluble drug in the intestinal compartment was allowed to transfer to the absorption compartment through a filter. Dissolution profiles of 75 mg cinnarizine in conventional and floating tablets were studied. The results of conventional tablet showed that although cinnarizine was completely dissolved in the gastric compartment, approximately 50% of cinnarizine was precipitated in the intestinal compartment. A floating cinnarizine tablet showed complete release within 24 hours with nearly zero order release rate, and no precipitation observed in the intestinal compartment, giving 100% of cinnarizine transferred into the absorption compartment. The floating controlled release of poorly soluble weakly basic drug may give considerable biomedical benefits over conventional tablet formulation, which was demonstrated by the proposed novel multicompartment system. Variability of volume in the gastric and intestinal compartments was studied by making further modification in the apparatus. The proposed system may give good in vivo-in vitro correlation, as attempts can be made to mimic in vivo conditions such as gastric volume, gastric secretion, gastric emptying to the intestine, and intestinal absorption.
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