• Journal of Pharmaceutical Investigation
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• v.30 no.3
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• pp.179-189
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• 2000

Clebopride malate(Cm) is a new benzamide drug which has a potent central antidopaminergic activity possessing antiemetic and anxiolytic properties. A purpose of this study was to assess the feasibility of formulating sustained release preparation by dispersing a drug in hydrophilic polymeric matrices and double layered tablets(DLT), using HPMC, carbopol, PEO, PVP/VA and other polymers as a rate controlling barrier. The matrix and DLT showed optimum dissolution pattern up to 8 hours and the contents of polymer were optimized at 30% level in this preparation. After an oral administration in beagle dog, Cm concentration was determined by use of GC-ECD and pharmacokinetic parameters were calculated by Vallner's method. The AUC of DLT showed similar results and the duration of action was increased 55% compared to that of regular release dosage form. The calculated absorption rate effectiveness(ARE) and controlled release effectiveness(CRE) for DLT increased 50% compared to that of matrix, the overall effectiveness(E) of this product appears to be about 70%. in vivo effectiveness test, DLT showed significant differences from control on antiemetic action of Cm. In consequence, it was possible to conclude that double layered tablet might be a good candidate for the sustained release dosage forms.

• Journal of Yeungnam Medical Science
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• v.4 no.1
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• pp.59-63
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• 1987

The measurement of gastric emptying time is useful in differentiation of the hypochondriac neurosis from the functional gastrointestinal disturbance, and also useful in searching the hidden gastrointestinal disease in patients who are believed as the functional gastrointestinal disturbance. We confirmed in this study that the more delayed gastric emptying time was measured in functional gastrointestinal disturbance compared to normal group, and more shortened gastric emptying time was found after treatment with dopamine antagonist (cleboril) in this group.