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Preparation and evaluation of ziprasidone-phospholipid complex from sustained-release pellet formulation with enhanced bioavailability and no food effect.
- Source :
-
The Journal of pharmacy and pharmacology [J Pharm Pharmacol] 2016 Feb; Vol. 68 (2), pp. 185-94. Date of Electronic Publication: 2016 Jan 08. - Publication Year :
- 2016
-
Abstract
- Objectives: The purpose of this work was to develop ziprasidone-phospholipid complex (ZIP-PLC) in sustained-release pellets to enhance the oral bioavailability and overcome the food effect of ziprasidone.<br />Methods: Ziprasidone-phospholipid complex was formulated by solvent-evaporation method. The complexes were characterized by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and solubility testing. The optimized ZIP-PLC was used to prepare ZIP-PLC sustained-release pellets via extrusion-spheronization method. The pellets were characterized by in vitro drug-release studies and administered to fasted and fed beagle dogs, and their pharmacokinetics were compared with commercial formulation Zeldox capsule as a control.<br />Key Findings: The results of FTIR, SEM, DSC and PXRD studies confirmed the formation of phospholipid complex. Solubility studies showed there was a higher solubility in water for ZIP-PLC than monohydrate ziprasidoe. The in vitro release rate of ziprasidone from the ZIP-PLC sustained-release pellet exhibited controlled-release characteristics with over 95% total release in 12 h. Pharmacokinetic studies in beagle dogs showed ziprasidone with prolong actions, and no food effect was achieved simultaneously in ZIP-PLC sustained-release pellet compared with Zeldox capsule.<br />Conclusions: The results indicated a sustained release with prolonged actions of schizophrenia and bipolar disorder treatment.<br /> (© 2016 Royal Pharmaceutical Society.)
- Subjects :
- Animals
Antipsychotic Agents administration & dosage
Antipsychotic Agents blood
Biological Availability
Delayed-Action Preparations
Dogs
Microscopy, Electron, Scanning
Piperazines administration & dosage
Piperazines blood
Solubility
Spectroscopy, Fourier Transform Infrared
Thiazoles administration & dosage
Thiazoles blood
X-Ray Diffraction
Adjuvants, Pharmaceutic chemistry
Adjuvants, Pharmaceutic pharmacology
Antipsychotic Agents chemistry
Food-Drug Interactions
Phospholipids chemistry
Phospholipids pharmacology
Piperazines chemistry
Technology, Pharmaceutical methods
Thiazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 2042-7158
- Volume :
- 68
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- The Journal of pharmacy and pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 26748446
- Full Text :
- https://doi.org/10.1111/jphp.12510