Abstract
The objective of this study is to design and evaluate Ziprasidone Floating pellets, which prolongs the release rate of the drug while extending the residence time of the drug within the body environment and without causing undeliterious effects to the subject. Ziprasidone and controlled matrix polymer granules were prepared by different granulation techniques in the ratio of 1:1, 1:1.5 and 1:2.Ziprasidone multi unit formulations comprising cellulose polymers were prepared by wet granulation technique, where as the Ziprasidone multi unit formulations comprising lipoidal / fatty polymers were prepared by melt granulation technique. Ziprasidone multi unit formulations with drug and polymer proportion as 1:1, F1 and F2 formulations consisting Cellulose polymers HPMC K4M and HPMC K100 respectively were prepared by wet granulation technique.
 Keywords: Ziprasidone, wet granulation, Floating pellets, melt granulation and polymer.
Highlights
Ziprasidone is a psychotropic agent belonging to the chemical class of benzisoxazole .C21H21ClN4OS 5-[2-[4-(1, 2-benzothiazol-3-yl) piperazin-1-yl]ethyl]-6-chloro-1, dihydroindol-2-one.Ziprasidone functions as an antagonist at the dopamine D2 and serotonin 5-HT2A and 5-HT1D receptors, and as an agonist at the 5-HT1A receptor
Ziprasidone and controlled matrix polymer granules were prepared by different granulation techniques in the ratio of 1:1, 1:1.5 and 1:2.Ziprasidone multi unit formulations comprising cellulose polymers were prepared by wet granulation technique, where as the Ziprasidone multi unit formulations comprising lipoidal / fatty polymers were prepared by melt granulation technique
Ziprasidone multi unit formulations with drug and polymer proportion as 1:1, F1 and F2 formulations consisting Cellulose polymers HPMC K4M and HPMC K100 respectively were prepared by wet granulation technique
Summary
Ziprasidone is a psychotropic agent belonging to the chemical class of benzisoxazole .C21H21ClN4OS 5-[2-[4-(1, 2-benzothiazol-3-yl) piperazin-1-yl]ethyl]-6-chloro-1, dihydroindol-2-one.Ziprasidone functions as an antagonist at the dopamine D2 and serotonin 5-HT2A and 5-HT1D receptors, and as an agonist at the 5-HT1A receptor. Ziprasidone is a psychotropic agent belonging to the chemical class of benzisoxazole. Ethyl]-6-chloro-1, dihydroindol-2-one.Ziprasidone functions as an antagonist at the dopamine D2 and serotonin 5-. HT2A and 5-HT1D receptors, and as an agonist at the 5-HT1A receptor. Ziprasidone inhibits the synaptic reuptake of serotonin and norepinephrine. The mechanism of action by which Ziprasidone exerts its antischizophrenic effect is unknown but is potentially mediated through a combination of dopamine D2 and serotonin 5-HT2 antagonism. In the absence of food, ziprasidone's oral bioavailability is 60%, and absorption may reach 100% if ziprasidone is taken with a meal containing at least 500 kcal.The mean apparent volume of distribution of Ziprasidone is 1.5 L/kg.It is extensively protein bound with over 99% of the drug bound to plasma proteins, primarily albumin and alpha1-acid glycoprotein. The half life of ziprasidone is 6-7 hours. The present work was carried with an in house experimental design to prepare multi unit granule GFDDS employing successful cellulose
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