Shittu A.O., Oyi A.R., Isah A.B., Ibrahim M.A.
Department of Pharmaceutics and Pharmceutical Technology, Faculty of Pharmaceutical Sciences, University of Jos, Nigeria; Department of Pharmaceutics and Pharmaceutical Microbiology, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria, Nige
Shittu, A.O., Department of Pharmaceutics and Pharmceutical Technology, Faculty of Pharmaceutical Sciences, University of Jos, Nigeria; Oyi, A.R., Department of Pharmaceutics and Pharmaceutical Microbiology, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria, Nigeria; Isah, A.B., Department of Pharmaceutics and Pharmaceutical Microbiology, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria, Nigeria; Ibrahim, M.A., Department of Pharmaceutics and Pharmceutical Technology, Faculty of Pharmaceutical Sciences, University of Jos, Nigeria
A research was conducted to design and evaluate a highly functional 3-component composite filler- binder for direct compression. Tapioca starch (NTS) was modified physically at molecular level by annealing and enzyme hydrolyzed to obtain microcrystalline tapioca starch (MCTS) which was coprocessed with LMH and microcrystalline cellulose (MCC) to yield Microcrystarcellac (MSCL). NTS was extracted from cassava tuber (Mannihot italive utilismo) using a standard method. The powder suspensions were prepared in concentration of 40 %w/w in five separate conical flasks. The starch granules were annealed for 1 h and subsequently hydrolyzed with α-amylase at 58° and pH 7 for 1, 2, 3, 4, and 5 h in a water bath. The reaction was terminated and neutralized with 0.1 N HCL and 0.1 N NaOH respectively. The MCTS was washed, recovered by sedimentation and air dried at room temperature for 72 h. Following characterization, the granules that were modified for 3 h, sieved fraction >75-250 μm was coprocessed with α- lactose monohydrate(α-LMH) and Microcrystalline cellulose (MCC) at concentrations of 10-50 % (MCTS), 45-25 %(α-LMH), 45-25 %(MCC). Granule size ranges >75 - 250 μm, and >90 - 250 μm were characterized and compacted at a range of compression load 2.5 to 12.5 KN. Average flow rate, angle of repose and carr's index were 2 g/s, 31.6°, 13.4 % respectively for MSCL (granule size range >90 - 250 μm and component ratio of MCTS, α-LMH, and MCC is 20: 40:40). The corresponding values for the direct physical mixture of MCTS, α-LMH and MCC are 0.45 g/s, 47.5°, 52 % respectively. MSCL have improved functionality over direct physical mixture of the primary excipients. MSCL was compared with Starlac®, Cellactose® and MCC. The onset of plastic deformation P y (yield value) are: MSCL (22.3 MNm -2)>Cellactose (24.2 MNm -2)>MCC (25 MNm -2)>Starlac (143 MNm -2). The degree of plastic deformation occurring during compression (P k) is in the following order: MSCL (16.3 MNm -2)>Starlac®(17 MNm -2)>MCC (18.6 MNm -2)>Cellactose® (19.1 MNm -2). MSCL is more superior in functionality than Starlac, Cellactose and MCC. The dilution potential obtained for MSCL compacted with paracetamol (PCM) and ascorbic acid (AA) as active drug (API) are: 50 % AA with MSCL, 45 % PCM with MSCL. The hardness of MSCL containing 45 % PCM, 70 N; MSCL containing 50 % AA, 68 N. MSCL can be used to formulate tablets of both poorly compressible API and moisture sensitive API.
alpha lactose; amylase; ascorbic acid; excipient; lactose; microcrystalline cellulose; paracetamol; starch; article; cassava; composite material; concentration (parameters); flow rate; hydrolysis; Mannihot italive utilismo; moisture; pH measurement; room temperature; sedimentation rate; sensitivity analysis; tapioca; temperature measurement