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Tablet formulation containing meloxicam and beta-cyclodextrin: mechanical characterization and bioavailability
Mamdouh M Ghorab1, Heba M Abdel-Salam, Marwa A El-Sayad
1Department of Pharmaceutics, College of Pharmacy, Suez Canal University, Ismailia, Egypt. mghorab@hotmail.com
AAPS Pharmscitech
|March 12, 2005
Summary
Beta-cyclodextrin (beta-CD) enhances meloxicam tablet preparation and bioavailability. This study found beta-CD improves meloxicam solubility, tablet properties, and oral absorption, suggesting its utility in pharmaceutical formulations.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Meloxicam, a non-steroidal anti-inflammatory drug (NSAID), exhibits poor aqueous solubility, limiting its oral bioavailability.
- Beta-cyclodextrin (beta-CD) is a cyclic oligosaccharide known for its ability to form inclusion complexes with poorly soluble drugs, potentially enhancing their physicochemical and pharmacokinetic properties.
Purpose of the Study:
- To evaluate beta-cyclodextrin (beta-CD), alone or blended with lactose, as a vehicle for preparing meloxicam tablets.
- To investigate the impact of beta-CD on the aqueous solubility, dissolution rate, and oral bioavailability of meloxicam.
Main Methods:
- Phase-solubility studies were conducted to determine the interaction between meloxicam and beta-CD.
- Meloxicam tablets were prepared using direct compression and wet granulation techniques with varying concentrations of beta-CD.
- Powder blends, granules, and tablets were characterized for physical properties (flow, compressibility, mechanical strength) and drug content.
- In vitro dissolution studies and a human volunteer study (balanced 2-way crossover) were performed to assess drug release and bioavailability.
Main Results:
- Phase-solubility studies revealed a 1:1 molar inclusion complex formation between meloxicam and beta-CD (A(L)-type diagram).
- All powder blends and granules exhibited satisfactory flow and compressibility.
- Tablets prepared by both direct compression and wet granulation demonstrated acceptable mechanical properties.
- Inclusion of beta-CD significantly enhanced meloxicam's dissolution rate and oral bioavailability, evidenced by increased C(max), K(e), and AUC(0-infinity).
Conclusions:
- Beta-cyclodextrin (beta-CD) effectively improves the aqueous solubility and dissolution rate of meloxicam.
- Direct compression is a viable and efficient method for preparing meloxicam tablets with beta-CD, offering comparable results to wet granulation.
- Beta-CD inclusion significantly enhances the oral bioavailability of meloxicam, making it a promising excipient for improving the efficacy of poorly soluble drugs.