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New developments in sustained-release antihypertensive therapy: formulation and pharmacokinetic considerations
J G Devane1, S Mulligan, M Kavanagh
1Elan Pharmaceutical Research Corporation, Gainesville, Georgia 30504.
The American Journal of Cardiology
|April 30, 1992
Summary
A new sustained-release (SR) nifedipine formulation offers consistent 24-hour blood pressure control. This novel approach minimizes peak-to-trough fluctuations for improved patient outcomes.
Area of Science:
- Pharmacology
- Drug Delivery Systems
- Cardiovascular Medicine
Background:
- Nifedipine is a calcium channel blocker used for hypertension.
- Conventional nifedipine requires multiple daily doses.
- Achieving consistent 24-hour plasma concentrations is challenging.
Purpose of the Study:
- To develop and evaluate a novel once-daily, sustained-release (SR) nifedipine formulation.
- To compare the pharmacokinetics of the SR formulation with conventional nifedipine.
- To assess the gastrointestinal behavior of the SR tablet.
Main Methods:
- Development of a sustained-release (SR) nifedipine formulation using the INDAS approach.
- Pharmacokinetic studies comparing SR nifedipine to divided doses of conventional nifedipine.
- Evaluation of gastrointestinal transit and tablet disintegration characteristics.
Main Results:
- The SR formulation achieved lower peak plasma nifedipine levels and reduced peak-to-trough fluctuations.
- Prolonged plasma profile with extended Tmax and longer half-life observed.
- The large intestine was identified as the primary site of absorption for the SR tablet.
Conclusions:
- The novel INDAS-based SR nifedipine formulation provides consistent 24-hour absorption and effective blood pressure control.
- This formulation offers a simplified dosing regimen with improved pharmacokinetic profiles.
- The unique release characteristics ensure sustained nifedipine delivery throughout the dosing interval.