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CARBOMER-BASED MATRIX TABLETS: CONTROL OF MELOXICAM RELEASE

DOI: https://doi.org/None
Issue: 
7
Year: 
2017

N.I. Filippova, Professor V.A. Vainshtein, PhD Saint Petersburg State Chemopharmaceutical Academy; 14, Prof. Popov St., Saint Petersburg 197376, Russian Federation

Introduction. Meloxicam is commonly known as a nonsteroidal anti-inflammatory drug. The main adverse effect of the drug is its negative local irritant effect on the gastrointestinal tract (GIT) mucosa. The negative effect can be diminished by controlling the meloxicam release from the tablets within the first 2-4 hours, which is especially important during long-term and cycle administrations. Objective: to investigate the effect of carbomers on the release profile of meloxicam from the tablets and to design the composition of carbomer-controlled release meloxicam tablets. Subjects and methods. Meloxicam, microcrystalline cellulose, lactose monohydrate, Carbopol Ultrez 21, Carbopol 71 G, arespol, calcium stearate, and N-methylglucamine were used to manufacture tablet prototypes. Meloxicam tablets were prepared by wet granulation. Compression was carried out on a KORSCH XP 1 single punch tablet machine. The release of meloxicam from the tablets was investigated using a dissolution test in the medium consisting of phosphate buffer solution, pH 7, on an Erweka DT 728 device. Results. When Carbopol Ultrez 21 and Carbopol 71G were used, the release of meloxicam tended to increase with its higher level in the tablets. The effect was less pronounced in the compositions with Arespol. When there was a low content of meloxicam in the tablets, Carbopol had virtually no effect on the release of the active ingredient. With the higher level of meloxicam (more than 5%) in the tablets, its release was markedly correlated with the content of Carbopol; the acceleration of release ranged from 25 to 60-70%. Conclusion. The meloxicam tablet composition ensuring the reduced local irritant action on the GIT mucosa was designed due to uniform meloxicam release during the preset period of time.

Keywords: 
meloxicam
matrix tablets
carbopol
release

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