Polymer Particle Size Influence on Indomethacin Release from Tamarind Seed Polyose: A Potential Sustained-Release Excipient - Pharmaceutical Technology

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Polymer Particle Size Influence on Indomethacin Release from Tamarind Seed Polyose: A Potential Sustained-Release Excipient


Pharmaceutical Technology




Hydrophilic polymers are used to prepare sustained-release formulations because of their safety and stability (1). These polymers also aid the controlled release of water-soluble and water-insoluble drugs. The release behavior of drugs is the complex interaction of swelling, diffusion, and erosion (2). Synthetic hydrophilic polymers are used more often than natural polymers, but because of the costs associated with synthetic polymers, researchers are now showing interest in the nonsynthetic polymers such as gums.

Tamarind seed polyose (TSP) is a polysaccharide gum extracted from the seeds of Tamarindus indica (lmli). TSP is a polymer with an average molecular weight of 52,350 and a monomer of mainly three sugars—glucose, galactose, and xylose—in a molar ratio of 3:1:2 (3). It is insoluble in organic solvents and dispersible in hot water to form a highly viscous gel such as a mucilaginous solution with a broad pH tolerance and adhesivety (4, 5). In addition, it is nontoxic and nonirritant with haemostatic activity (4). It had been previously used in some drug formulations (5, 6).

For this study, TSP was used to prepare sustained-release formulations of indomethacin (IND), an anti-inflammatory drug substance with a short half-life of 2.4 ± 0.4 h (7). Its dosage regimen is 25 mg thrice daily, with peptic ulceration as its major side effect. IND is a suitable candidate for a sustained-release formulation. Tablets were prepared using direct compression because a wet granulation method would cause an initial swelling of the polymer, thereby affecting the swelling profile of the various fractions during release testing of the matrix tablets.

Materials and methods

Materials. TSP was extracted according to the method described by Nandi et al. (8). After extraction, the dried material was milled into powder form with a pestle and mortar. Six particle-size fractions were obtained by sieving with various mesh-number test sieves. Indomethacin was supplied by Unicure India Pvt. Ltd. (Noida, India) and magnesium stearate was obtained from Amrut Industrial Products (Lucknow, India). Indomethacin and magnesium stearate were used as supplied.

Micromeritic property study. The bulk and tapped densities of the powder were determined with a measuring cylinder, and true density was determined using a liquid pycnometer with benzene as the displacement fluid. The porosity was determined using the equation









in which E, ρbulk, and ρtrue are the porosity, bulk density, and true density, respectively. The flowability (indicated by the angle of repose, Hausner ratio, and Carr's index) of the powder also was studied. The angle of repose was measured using the fixed-height method. Carr's index was calculated using the equation









and









is the Hausner ratio.

Swelling profile study. The swelling profile was determined by transferring accurately weighed 1 g of each fraction into separate 100-mL stoppered measuring cylinders. These were made up to volume with distilled water and observations made for increases in volume of the TSP. Readings were taken at specified times until a constant volume was observed in each of the cylinders.


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