چکیده (انگلیسی):

The purpose of this research was to evaluate β-cyclodextrin
(β-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 β-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 β-CD on the bioavailability
of meloxicam was also investigated in human volunteers
using a balanced 2-way crossover study. Phase-solubility
studies indicated an AL-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 β-CD in the formulations up
to 30%. The mean pharmacokinetic parameters (Cmax, Ke, and
area under the curve [AUC]0-∞) were significantly increased in
presence of β-CD. These results suggest that β-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, β-CD is particularly useful for improving the oral
bioavailablity of meloxicam.