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Testing lyoequivalency for three commercially sustained-release tablets containing diltiazem hydrochloride
Hamzah A Maswadeh1, Othman A Al-Hanbali, Reem A Kanaan
1Department of Pharmacy, Faculty of Pharmacy and Medical Sciences, Al-Ahliyya Amman University, 19328 Amman, Jordan. maswadehhamza@hotmail.com
Acta Poloniae Pharmaceutica
|March 10, 2010
Summary
Three sustained-release diltiazem hydrochloride tablets were analyzed for drug release kinetics. Two products showed anomalous transport, while one exhibited super case II release, indicating they are not bioequivalent.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Sustained-release (SR) formulations aim to provide controlled drug release over time.
- Diltiazem hydrochloride is a widely used calcium channel blocker for cardiovascular conditions.
- Understanding in vitro release kinetics is crucial for predicting in vivo performance and ensuring product quality.
Purpose of the Study:
- To investigate the in vitro release kinetics of three commercially available sustained-release diltiazem hydrochloride tablets.
- To compare the dissolution profiles and assess the potential bioequivalence of these products.
- To elucidate the drug release mechanisms governing the performance of different SR formulations.
Main Methods:
- In vitro dissolution testing of diltiazem hydrochloride SR tablets at pH 1.1 and 6.8 using USP apparatus.
- Analysis of dissolution data using kinetic models: zero-order, first-order, Higuchi, Hixson-Crowell, and Peppas equations.
- Comparative dissolution profile analysis using mean dissolution time (MDT), f1, and f2 factors to assess lyoequivalence.
Main Results:
- Dilzacard and Dilzem SR tablets exhibited Non-Fickian (anomalous) drug release, with release exponents (n) of 0.59 and 0.54, respectively.
- Bi-Tildiem SR tablets demonstrated super case II transport (n = 1.29), indicative of zero-order release driven by polymer matrix dissolution and relaxation.
- Comparative analysis revealed significant differences in dissolution profiles, indicating the three products are not lyoequivalent.
Conclusions:
- The drug release mechanisms for diltiazem hydrochloride SR tablets vary among commercial products, involving diffusion, dissolution, and polymer relaxation.
- The tested diltiazem hydrochloride SR formulations are not lyoequivalent, suggesting potential differences in their in vivo performance.
- In vitro dissolution studies are essential for characterizing SR drug products and ensuring therapeutic equivalence.
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