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New immediate release formulation for deterring abuse of methadone
A O Betancourt1, P M Gosselin, R K Vinson
1Pharmaceutical Research and Development, Corealis Pharma Inc., Laval, Qc, Canada.
Pharmaceutical Development and Technology
|May 1, 2012
Summary
New methadone (an opioid analgesic) formulations with alkalizing agents prevent drug abuse by hindering extraction. These anti-abuse tablets maintain therapeutic release in the stomach and show good storage stability.
Area of Science:
- Pharmaceutical Sciences
- Medicinal Chemistry
- Pharmacology
Background:
- Opioid analgesics are frequently abused by extracting them from dosage forms.
- Drug abusers manipulate oral formulations to obtain the opioid for non-prescribed routes of administration.
Purpose of the Study:
- To develop an abuse-deterrent, immediate-release formulation of methadone.
- To utilize methadone as a model drug for creating anti-abuse formulations.
Main Methods:
- Tablets were manufactured combining methadone with alkalizing agents.
- Methadone extraction efficiency was assessed in aqueous and alcohol solvents.
- In vitro dissolution testing evaluated drug release characteristics.
Main Results:
- Meglumine-based formulations successfully prevented 70-100% of methadone extraction.
- The alkalizing agent caused methadone precipitation, retaining it on filters.
- Similar dissolution profiles were observed for meglumine-containing and control tablets in acidic media.
- Formulation stability was confirmed after 6 months of storage under various conditions.
Conclusions:
- Incorporating an alkalizing agent significantly deters the preparation of injectable methadone formulations.
- The developed formulation allows for effective methadone release in gastric environments.
- This strategy balances abuse deterrence with therapeutic efficacy.
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