¹Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Bayero University, Kano, Nigeria
²Department of Pharmaceutics, UCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom
³Department of Pharmacology and Therapeutics, Faculty of Pharmaceutical Sciences, Bayero University, Kano, Nigeria
⁴Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Bayero University, Kano, Nigeria
⁵Department of Pharmaceutics and Pharmaceutical Microbiology, Faculty of Pharmaceutical Sciences, Kaduna State University, Kaduna, Nigeria DOI : 10.29228/jrp.2022.00 This research implements a computer-aided formulation development algorithm based on a novel SeDeM-ODT expert system in establishing the design space for paediatric pyridoxine hydrochloride orodispersible tablets (ODTs) using Prosolv® ODTG2, Prosolv® EasyTab SP, and Ludiflash® systems. For each formulation ingredient, expert system-defined preformulation parameter values were experimentally determined according to standardized methods and then normalized to the theoretical radius range [0,10]. Expert diagrams were constructed and the quantitative performance of each ingredient was evaluated using parametric profile index (IPP), flowability (ff’), and compressibility (ffc) functions. The net direct compression capability was quantitatively expressed as the product of expert system reliability and IPP. Direct compression was conducted in an eccentric tablet press and properties were evaluated using weight, dimension, disintegration test, contact angle, tensile strength, x-ray diffraction, and Fourier-transform infrared spectroscopy. The ODTs dissolution profiles were fitted and compared using zero-order, first-order, Hixson-Crowell, and Hopfenberg models. Results of the expert diagram of pyridoxine hydrochloride indicated suboptimal normalized radii values in 8 out of 12 parameters, implying a compromised mechanical zone (ff’=3.61, ffc=2.11). By setting a target ffc for the optimized formulation mix at 5.0, the predicted proportions of the fillers to remedy the direct compression deficits of the drug were computed as 89.00%, 83.23%, and 76.62% for Prosolv® ODTG2 (ffc=5.36), Prosolv® EasyTab SP (ffc=5.58), and Ludiflash® (ffc=5.88), respectively. The produced ODTs were of acceptable target quality, hence the SeDeM-ODT system was considered a reliable formulation tool for establishing the design space of this particular drug-filler systems. Keywords : paediatric-centric formulations; orodispersible systems; computer-aided drug design; expert systems; pyridoxine hydrochloride; direct compaction technology