Preparation and evaluation of sustained release matrix tablets of tramadol hydrochloride using glyceryl palmitostearate

• Published in: Tropical journal of pharmaceutical research Vol. 9; no. 3
• Main Authors: Deore, Rakesh K, Kavitha, Kunchu, Tamizhmani, Theetha G
• Format: Journal Article
• Language: English
• Published: Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria 31-12-2010
• Subjects: Direct compression; Glyceryl palmitostearate; Melt granulation; Sustained release; Tramadol hydrochloride
• ISSN: 1596-5996; 1596-9827
• DOI: 10.4314/tjpr.v9i3.56289

Purpose: To prepare oral sustained release matrix tablets of a highly
water soluble drug, tramadol hydrochloride, and to evaluate the effect
of concentration of the hydrophobic polymer content and method of
preparation on drug release. Methods: The tablets were a mixture of
both tramadol hydrochloride and glyceryl palmitostearate (GP) prepared
by melt granulation (MG1, MG2, MG3 and MG4 in ratios 1:1, 1:2, 1:3 and
1:4, respectively) or by direct compression (DC, 1:2 ratio). The
hardness of the tablets was measured. Drug/GP interaction was
determined by FT-IR spectroscopy while drug release from the matrix
tablets was studied using USP o (dissolution apparatus. The release
data were subjected to different models in order to evaluate their
release kinetics and mechanisms. Results: The hardness of the tablets
was in the range of 5.30 ± 0.36 - 6.50 ± 0.10 kg/cm 2 . FT-IR
spectra showed that there was no clear interaction between the drug and
the glyceride. Of the formulations (MG1 to MG4) prepared by melt
granulation, MG4 showed the most suitable sustained release, 58.4
± 1.1 % in 12 h (p < 0.05). Drug release (98.2 ± 0.2 % in
8 h) was highest for DC which was prepared by direct compression. Also,
drug release mechanism for the formulations was by Fickian diffusion.
Conclusion: Glyceryl palmitostearate is a suitable matrix-forming agent
to sustain the release of a water-soluble drug such as tramadol
hydrochloride. Melt granulation was a better technique for formulating
the product than direct compression.