AI Article Synopsis
- Melperone is an atypical antipsychotic effective in treating conditions like senile dementia and Parkinson's-related psychosis, currently available in Europe as a syrup and immediate-release tablet.
- New formulations, including controlled-release capsules and orally disintegrating tablets (ODT), have been developed to make it easier for patients who struggle with swallowing pills, targeting a once-daily dosing regimen.
- In vivo tests indicated that these new ODT and capsule formulations are bioequivalent and suitable for further clinical development, demonstrating favorable release profiles and production capabilities for multiple strengths.
Article Abstract
Melperone is an atypical antipsychotic agent that has shown a wide spectrum of neuroleptic properties, particularly effective in the treatment of senile dementia and Parkinson's-associated psychosis, and is marketed in Europe as an immediate-release (IR) tablet and syrup. An orally disintegrating tablet (ODT) dosage form would be advantageous for patients who experience difficulty in swallowing large tablets or capsules or those who experience dysphagia. Controlled-release (CR) capsule and ODT formulations containing melperone HCl were developed with target in vitro release profiles suitable for a once-daily dosing regimen. Both dosage forms allow for the convenient production of dose-proportional multiple strengths. Two ODT formulations exhibiting fast and medium release profiles and one medium release profile capsule formulation (each 50 mg) were tested in vivo using IR syrup as the reference. The two medium release formulations were shown to be bioequivalent to each other and are suitable for once-daily dosing. Based on the analytical and organoleptic test results, as well as the blend uniformity and in-process compression data at various compression forces using coated beads produced at one-tenth (1/10) commercial scale, both formulations in the form of CR capsules and CR ODTs have shown suitability for progression into further clinical development.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3497912 | PMC |
| http://dx.doi.org/10.3109/03639045.2011.653365 | DOI Listing |
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