Tablet formulation containing meloxicam and beta-cyclodextrin: mechanical characterization and bioavailability evaluation

AAPS PharmSciTech. 2004 Jul 27;5(4):e59. doi: 10.1208/pt050459.

Abstract

The purpose of this research was to evaluate beta-cyclodextrin (beta-CD) as a vehicle, either singly or in blends with lactose (spray-dried or monohydrate), for preparing a meloxicam tablet. Aqueous solubility of meloxicam in presence of beta-CD was investigated. The tablets were prepared by direct compression and wet granulation techniques. The powder blends and the granules were evaluated for angle of repose, bulk density, compressibility index, total porosity, and drug content. The tablets were subjected to thickness, diameter, weight variation test, drug content, hardness, friability, disintegration time, and in vitro dissolution studies. The effect of beta-CD on the bioavailability of meloxicam was also investigated in human volunteers using a balanced 2-way crossover study. Phase-solubility studies indicated an A(L)-type diagram with inclusion complex of 1:1 molar ratio. The powder blends and granules of all formulations showed satisfactory flow properties, compressibility, and drug content. All tablet formulations prepared by direct compression or wet granulation showed acceptable mechanical properties. The dissolution rate of meloxicam was significantly enhanced by inclusion of beta-CD in the formulations up to 30%. The mean pharmacokinetic parameters (C(max), K(e), and area under the curve [AUC](0-infinity)) were significantly increased in presence of beta-CD. These results suggest that beta-CD would facilitate the preparation of meloxicam tablets with acceptable mechanical properties using the direct compression technique as there is no important difference between tablets prepared by direct compression and those prepared by wet granulation. Also, beta-CD is particularly useful for improving the oral bioavailablity of meloxicam.

Publication types

  • Comparative Study

MeSH terms

  • Adult
  • Biological Availability
  • Chemistry, Pharmaceutical
  • Cross-Over Studies
  • Humans
  • Male
  • Mechanics
  • Meloxicam
  • Solubility
  • Tablets
  • Thiazines / blood
  • Thiazines / chemistry*
  • Thiazines / pharmacokinetics*
  • Thiazoles / blood
  • Thiazoles / chemistry*
  • Thiazoles / pharmacokinetics*
  • beta-Cyclodextrins / blood
  • beta-Cyclodextrins / chemistry*
  • beta-Cyclodextrins / pharmacokinetics*

Substances

  • Tablets
  • Thiazines
  • Thiazoles
  • beta-Cyclodextrins
  • betadex
  • Meloxicam