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Tablet formulation studies on nimesulide and meloxicam-cyclodextrin binary systems
Buchi N Nalluri1, K P R Chowdary, K V R Murthy
1Department of Pharmaceutical Sciences, Andhra University, Visakhapatnam, India.
AAPS Pharmscitech
|July 12, 2007
Summary
This study developed improved tablet formulations for nimesulide-beta-cyclodextrin (NI-beta-CD) and meloxicam-gamma-cyclodextrin (ME-gamma-CD) binary systems. Direct compression yielded superior dissolution properties and stability compared to wet granulation.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Formulation Development
Background:
- Nimesulide and meloxicam are non-steroidal anti-inflammatory drugs (NSAIDs) with potential for improved oral bioavailability.
- Cyclodextrins (CDs) are widely used complexing agents to enhance drug solubility and dissolution.
- Binary systems of drugs with CDs can improve physicochemical properties for oral dosage forms.
Purpose of the Study:
- To develop and characterize tablet formulations of nimesulide-beta-cyclodextrin (NI-beta-CD) and meloxicam-gamma-cyclodextrin (ME-gamma-CD) binary systems.
- To evaluate the impact of different binary system preparation methods (physical mixtures, kneaded, coevaporated) and molar ratios on tablet properties.
- To compare the dissolution performance and stability of drug-CD formulations against pure drug formulations.
Main Methods:
- Preparation of nimesulide-beta-cyclodextrin and meloxicam-gamma-cyclodextrin binary systems at 1:1 and 1:2 molar ratios using physical mixtures, kneading, and coevaporation techniques.
- Formulation of tablets using wet granulation and direct compression methods incorporating the drug-CD binary systems.
- Evaluation of in vitro dissolution properties, drug content, disintegration time, hardness, and stability under accelerated conditions (40°C ± 2°C, 75% RH) for 6 months.
Main Results:
- Tablet formulations containing drug-CD binary systems exhibited significantly superior dissolution properties compared to pure drug formulations.
- Direct compression method resulted in better dissolution profiles than wet granulation for the prepared tablet formulations.
- Selected tablet formulations demonstrated good stability, maintaining drug content, disintegration time, hardness, and dissolution profiles over the 6-month study period.
Conclusions:
- The development of nimesulide-beta-cyclodextrin and meloxicam-gamma-cyclodextrin binary systems effectively enhances the dissolution properties of these NSAIDs in tablet formulations.
- Direct compression is a preferred method for formulating these drug-CD systems into tablets to achieve optimal dissolution.
- The studied drug-CD formulations exhibit promising stability, supporting their potential for clinical application.
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