Abstract:
A research was carried out to study the effect of increasing concentration of grewia gum in a binary-binder mixture on granules properties of a composite directly compressible excipient made with local primary materials and to formulate Ibuprofen (IBF) and metronidazole (MNZ) tablets with the best granules. This research was designed based on a fixed amount of Nigerian Tapioca Starch (NTS), while varying ratio of grewia gum (GG), and local acacia sieberiana gum (LASG) in the following percentage ratio: 80:0:20, 80:5:15, 80:10:10, 80:15:5, and 80:20:0 respectively. Slurry of physical mixture of GG and LASG was made using mixture of isopropranol and water (2:1) as granulation fluid. Slurry of NTS was also made and was triturated with the binder slurry. The resultant mixture was stirred vigorously until a semi solid mass was formed which was air dried for 72 h. The dried granules were size reduced by passing through 500 µm sieve size. The granules percent(%) cummulative distribution for various batches showed that the batch A with 20 % LASG showed weaker compact granules than every other batch containing binary binder mixture. The granule compactness increases from 20 % LASG and picked at 20 % GG. In between the batches, granules with 10 % GG and 10 % LASG possessed hybrid compactness which was consistent for particles retained on 180 µm, 250 µm and 355 µm. the average granule size was found to greater than 250 µm and less than 355 µm. It was observed that as the proportion of GG increases while LASG decreases, the granules became stronger, flow rate increases, compressibility decreases and viscosity increases. GrewStarag granules containing 80 % NTS, 10 % GG, and 10 % LASG with the following physicochemical properties was chosen: FR, 15.8 g/s; AR, 14.7°; CI, 8.0 %; HR, 1.08; viscosity, 115 mPa.S^-1. This was employed for the formulation of IBF and MNZ tablets. The tablet target weight was 505 mg, compressed at 7.5 KN. Evaluation of IBF tablets shows acceptable dilution potential for tablets made with 200 mg of GrewStarag and 300 mg of IBF, having crushing strength (CR), disintegration time (DT), and friability (F) values: 58.2+2.4 N, 2 h 20 min., and 1.2 % respectively. Evaluation of MNZ tablets revealed acceptable compacts for dilution potential: 300 mg GrewStarag granules and 200 mg MNZ, having CS, 7.0 +1.0 N; DT, 2 h. 21 min., and 1.10 %. GrewStarag, a new filler-binder can be employed to extend or modified the release of moisture sensitive and poorly compressible active pharmaceutical ingredients for non- disintegrating colon targeted drugs.

Keywords: Directly Compressible Excipient, Coprocessed Filler-binder, Binary-based Filler-binder, Controlled Release Filler-binder, Ibuprofen Tablets, Metronidazole Tablets.