Ziprasidone HCl

Atypical antipsychotic that displays combined serotonin and dopamine receptor antagonism. Displays high affinity at 5-HT2A receptors with a 5-HT2A/D2 affinity ratio greater than any other clinically available atypical antipsychotics (pKi values are 9.38,

Ziprasidone HCl capsules for the adjunctive maintenance treatment of bipolar disorder in adults.[Pubmed:20586686]

Expert Rev Neurother. 2010 Jul;10(7):1031-7.

This article reviews the evidence for the use of ziprasidone for the maintenance treatment of bipolar I disorder in adults as an adjunct to lithium or valproate, as approved by the US FDA in 2009. Ziprasidone is an 'atypical' or 'second-generation' antipsychotic that has garnered clinical interest because of its metabolically friendly tolerability profile. A placebo-controlled trial was conducted in subjects whose most recent episode was manic or mixed, with or without psychotic features, and with symptoms that began no more than 90 days prior to the screening visit. Patients were stabilized during a 10-16-week, open-label period on the combination of ziprasidone 80-160 mg/day plus lithium (0.6-1.2 mEq/l) or valproate (50-125 microg/ml). Patients whose symptoms stabilized for 8 consecutive weeks were randomized to either continue combination treatment with adjunctive ziprasidone or receive lithium or valproate with adjunctive placebo for up to 24 weeks of double-blind treatment. The primary outcome measure was time to intervention for a mood episode during the double-blind period, tested statistically using survival analysis and assessing Kaplan-Meier curves. Of the 584 patients enrolled in the open-label period, 241 (41%) completed. A total of 238 subjects were analyzed for efficacy in the double-blind period (ziprasidone 127, placebo 111). Ziprasidone was superior to placebo in increasing the time to recurrence of a mood episode (p = 0.0104) during the 6 months of double-blind treatment. Only 19.7% (25 out of 127) of the ziprasidone subjects required intervention for a mood episode, compared with 32.4% (36 out of 111) of the placebo subjects (number needed to treat [NNT] 8; 95% CI: 5-62). The most robust effects were noted for the combination of ziprasidone and lithium and for the avoidance of manic/mixed episodes. Ziprasidone had no remarkable effect on weight or blood glucose. Limitations of this study include the enriched sample and exclusion of the most severely ill, and the inclusion of only those patients whose most recent bipolar episode was manic or mixed. Indirect comparisons of adjunctive ziprasidone with adjunctive quetiapine reveals a lower (i.e., more robust) NNT for quetiapine in terms of proportions of subjects experiencing a mood event (NNT: 4), but a higher incidence of bodyweight gain of at least 7% from baseline.

Natural gums as sustained release carriers: development of gastroretentive drug delivery system of ziprasidone HCl.[Pubmed:23352292]

Daru. 2012 Oct 17;20(1):58.

UNLABELLED: BACKGROUND: Objective of this study is to show the potential use of natural gums in the development of drug delivery systems. Therefore in this work gastro retentive tablet formulations of Ziprasidone HCl were developed using simplex lattice design considering concentration of okra gum, locust bean gum and HPMC K4M as independent variables. A response surface plot and multiple regression equations were used to evaluate the effect of independent variables on hardness, flag time, floating time and drug release for 1 h, 2 h, and 8 h and for 24 h. A checkpoint batch was also prepared by considering the constraints and desirability of optimized formulation to improve its in vitro performance. Significance of result was analyzed using ANOVA and p < 0.05 was considered statistically significant. RESULTS: Formulation chiefly contains locust bean gum found to be favorable for hardness and floatability but combined effect of three variables was responsible for the sustained release of drug. The in vitro drug release data of check point batch (F8) was found to be sustained well compared to the most satisfactory formulation (F7) of 7 runs. The 'n' value was found to be between 0.5 and 1 suggesting that release of drug follows anomalous (non-fickian) diffusion mechanism indicating both diffusion and erosion mechanism from these natural gums. Predicted results were almost similar to the observed experimental values indicating the accuracy of the design. In vivo floatability test indicated non adherence to the gastric mucosa and tablets remain buoyant for more than 24 h. CONCLUSIONS: Study showed these eco-friendly natural gums can be considered as promising SR polymers.

Mucoadhesive-floating zinc-pectinate-sterculia gum interpenetrating polymer network beads encapsulating ziprasidone HCl.[Pubmed:26256166]

Carbohydr Polym. 2015 Oct 20;131:108-18.

A novel dual crosslinked low-methoxyl (LM) pectinate-sterculia gum (SG) interpenetrating polymer network (IPN) beads was developed for intragastric ziprasidone delivery. The IPN beads were accomplished by simultaneous ionotropic gelation with zinc acetate and covalent crosslinking with glutaraldehyde. The effects of pectin and SG contents on drug entrapment efficiency (DEE, %), and cumulative drug release after 8h (Q8, %) were studied to optimize the IPN beads using a 3(2) factorial design. The optimized beads encapsulating Ziprasidone HCl (F-O) displayed DEE of 87.98+/-1.15% and Q8 of 58.81+/-1.50% with excellent buoyancy (floating lag time <2min, % buoyancy at 8h >63%) and good mucoadhesivity with the goat gastric mucosa. In most cases, the drug release behaviour obeyed Higuchi kinetics with anomalous transport mechanism. The Zn-pectinate-SG IPN beads were also characterized by SEM, FTIR, DSC and P-XRD analyses.

Ziprasidone HCl is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.

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