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Tablet formulation studies on an oxcarbazepine-beta cyclodextrin binary system
N V Patel1, N P Chotai, M P Patel
1Anand Pharmacy College, Anand, Gujarat, India. Nirav2564@yahoo.co.in
Die Pharmazie
|May 13, 2008
Summary
Developing oxcarbazepine-beta-cyclodextrin (OX-beta-CD) binary systems significantly improved the dissolution of this poorly soluble anti-epileptic drug. Kneaded OX-beta-CD systems in tablet formulations demonstrated superior drug release and stability.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Pharmacy
Background:
- Oxcarbazepine is a BCS Class II anti-epileptic drug with poor water solubility, where dissolution is the rate-limiting factor for absorption.
- Beta-cyclodextrin (beta-CD) is a commonly used excipient for enhancing the solubility and dissolution of poorly water-soluble drugs.
Purpose of the Study:
- To develop and evaluate tablet formulations of oxcarbazepine-beta-cyclodextrin (OX-beta-CD) binary systems to improve drug dissolution.
- To compare the dissolution properties of different binary system preparation methods and tablet manufacturing techniques.
Main Methods:
- Phase solubility studies were conducted to determine the complexation between oxcarbazepine and beta-CD.
- Three types of binary systems were prepared: physical mixtures, kneaded systems, and coevaporated systems at a 1:1 molar ratio.
- Tablet formulations were prepared using wet granulation and direct compression methods.
- Dissolution testing and accelerated stability studies were performed.
Main Results:
- Phase solubility studies confirmed a 1:1 molar complexation of oxcarbazepine with beta-CD.
- The kneaded system (OX-beta-CD KS) exhibited superior dissolution, with 100.10% drug release in 15 minutes, outperforming other binary systems and pure oxcarbazepine.
- Tablet formulations containing OX-beta-CD binary systems, particularly those prepared by kneading and direct compression, showed significantly improved dissolution profiles compared to pure drug formulations.
- Stability studies indicated no significant changes in drug release or content in stored samples.
Conclusions:
- Oxcarbazepine-beta-cyclodextrin binary systems, especially kneaded systems, are effective in enhancing the dissolution properties of poorly soluble oxcarbazepine.
- Tablet formulations incorporating these binary systems offer a viable approach for improving the bioavailability of oxcarbazepine.
- Direct compression method yielded superior dissolution properties compared to wet granulation for these tablet formulations.
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