In vitro and in vivo characterization of amorphous, nanocrystalline, and crystalline ziprasidone formulations

International Journal of Pharmaceutics
Avinash G ThombreW Brett Caldwell

Abstract

Ziprasidone, commercially available as Geodon capsules, is an atypical antipsychotic used in the treatment of schizophrenia and bipolar disorder. It is a BCS Class II drug that shows up to a 2-fold increase in absorption in the presence of food. Because compliance is a major issue in this patient population, we developed and characterized solubilized formulations of ziprasidone in an effort to improve absorption in the fasted state, thereby resulting in a reduced food effect. Three formulations utilizing solubilization technologies were studied: (1) an amorphous inclusion complex of ziprasidone mesylate and a cyclodextrin, (2) a nanosuspension of crystalline ziprasidone free base, and (3) jet-milled ziprasidone HCl coated crystals made by spray drying (CCSD) the drug with hypromellose acetate succinate. The formulations were characterized by in vitro methods appropriate to each particular solubilization technology. These studies confirmed that ziprasidone mesylate - cyclodextrin was an amorphous inclusion complex with enhanced dissolution rates. The ziprasidone free base crystalline nanosuspension showed a mean particle size of 274 nm and a monomodal particle size distribution. In a membrane permeation test, the CCSD showed a 1...Continue Reading

References

Sep 1, 1978·Clinical Pharmacokinetics·A Melander
Jan 1, 1980·Annual Review of Pharmacology and Toxicology·R D Toothaker, P G Welling
Oct 8, 1999·Clinical Pharmacokinetics·B N Singh
Jul 3, 2002·Drugs·Lars E Schmidt, Kim Dalhoff
Jan 14, 2003·The Journal of Clinical Psychiatry·Diana O Perkins
Feb 21, 2003·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Elaine Merisko-LiversidgeEugene R Cooper
Aug 9, 2006·Expert Review of Neurotherapeutics·Nick C Patel, Paul E Keck
Jul 3, 2007·Advanced Drug Delivery Reviews·Filippos KesisoglouYunhui Wu
Jul 3, 2007·Advanced Drug Delivery Reviews·Marcus E Brewster, Thorsteinn Loftsson
Jul 10, 2007·Advanced Drug Delivery Reviews·David J Hauss
Jul 14, 2007·CNS Drug Reviews·William M Greenberg, Leslie Citrome
Jul 14, 2007·Advanced Drug Delivery Reviews·Valentino J Stella, Kwame W Nti-Addae
Nov 11, 2008·International Journal of Nanomedicine·Jens-Uwe A H Junghanns, Rainer H Müller
Dec 2, 2008·Molecular Pharmaceutics·Dwayne T FriesenJ A S Nightingale
Feb 2, 2011·Journal of Pharmaceutical Sciences·Jinyang HongMaura D Mcgonagle
Jun 16, 2011·Pharmaceutical Research·Avinash G ThombreJeffrey A Alderman

❮ Previous
Next ❯

Citations

Jun 12, 2013·International Journal of Pharmaceutics·Chris Brough, R O Williams
Mar 29, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Vivek K PawarManish K Chourasia
Jan 27, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Tahnee J DeningClive A Prestidge
Jan 8, 2016·Journal of Controlled Release : Official Journal of the Controlled Release Society·Tahnee J DeningClive A Prestidge
May 7, 2013·Current Opinion in Solid State & Materials Science·Bo Sun, Yoon Yeo
Jul 3, 2015·Pharmaceutical Development and Technology·Sabyasachi BanerjeeRajendra Prasad Y
Jul 2, 2015·Journal of Controlled Release : Official Journal of the Controlled Release Society·Avinash G ThombreW Brett Caldwell
Jun 30, 2018·The Journal of Pharmacy and Pharmacology·Joseph P O'SheaBrendan T Griffin
Feb 7, 2013·Pharmacological Reviews·Hywel D WilliamsChristopher J H Porter

❮ Previous
Next ❯

Related Concepts

Related Feeds

Bipolar Disorder

Bipolar disorder is characterized by manic and/or depressive episodes and associated with uncommon shifts in mood, activity levels, and energy. Discover the latest research this illness here.