Abstract
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 II 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/cm2. 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 Keywords: Tramadol hydrochloride; Glyceryl palmitostearate; Melt granulation; Direct compression; Sustained release.
Highlights
A sustained-release dosage form is defined as “any drug or dosage form modification that prolongs the therapeutic activity of the drug” [1]
The major IR peaks observed in the spectra for tablet formulation were 1737 (C=O stretching, carbonyl group), 1625 (C=C stretching) which are characteristic of glyceryl palmitostearate, and 2780 (C-H stretching), 3392 (N-H stretching vibration, tertiary amine), and 1295 (C-N stretching vibration) which are characteristic of tramadol hydrochloride
This study revealed that as the concentration of lipophilic matrix material increased, drug release from matrices of the met-granulated tablets decreased
Summary
A sustained-release dosage form is defined as “any drug or dosage form modification that prolongs the therapeutic activity of the drug” [1]. The primary objectives of sustained drug delivery are to ensure safety and enhancement of efficacy of drug with improved patient compliance. Glycerides are a family of excipients which have generated considerable interest in the preparation of oral dosage forms Some glycerides such as Precirol ATO 5 (glyceryl palmitostearate) can be used for the preparation of sustained release dosage forms [3]. Melt granulation is a solvent-free process which involves the use of a substance that melts at a relatively low temperature. This substance can be added in the molten form over the substrate or in the solid form, which is heated above its melting point. Sustained release matrix tablets have been produced with Precirol ATO 5 by various methods including melt granulation [10], hot melt extrusion [11] and melt pelletization [6]
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