Abstract
Drugs of low aqueous solubility provide a major challenge in the design of modern oral dosage form due to dissolution and bioavailabilty difficulties. The present study was undertaken to investigate the effect of particle size and some formulation additives (sodium laurylsulphate (SLS), Primogel R and Ac-Di-Sol) on the release profile of poorly soluble drug, ibuprofen from compressed tablets. Six batches (A - F) of Ibuprofen granules and tablets were prepared by the wet granulation method. Batches A, B and C contained granules that were fractionated from three sieve fractions (0.42, 0.25 and 0.15 mm respectively) in ascending order of particle size. D, E and F contained 2 % Primogel R, 1 % Ac-Di-Sol and 0.2 % SLS respectively. Tablet properties evaluated as a function of particle size and formulation additives include: hardness, friability and dissolution efficiency at 60 min. Results obtained indicated a decrease in the dissolution rate of the batches as the particle size increased. All the Ibuprofen tablet batches produced exhibited better drug release (in terms of rate and extent of release) than a commercially available sample, Multifen®. The overall and expected in vivo bioavailability in the batches on the basis of dissolution efficiency parameter (DE60) is in the order of E (98.3 %) > D (98.0 %) > A (97.7 %) > F (96.9 %) > B (95.3 %) > C (93.8 %) > Multifen® (26.0%). Statistical comparison of the DE60 parameter indicated a significant difference (p ˂ 0.05) in the results from the formulated batches and the commercially available sample, Multifen®. The results indicated that particle size reduction of granules and the inclusion of formulation additives like SLS, Ac-Di-SOL and Primogel R can be utilized in improving the release profile of Ibuprofen from compressed tablets.
