Optimization of formulations of chloroquine phosphate tablets containing Ofada rice (Oryza glaberrina) starch as a binder: a Taguchi based grey-relational design

• Published in: Journal of excipients and food chemicals Vol. 11; no. 3
• Main Author: Adenike Okunlola
• Format: Journal Article
• Language: English
• Published: International Pharmaceutical Excipients Council 01.09.2020
• ISSN: 2150-2668

Chloroquine phosphate (CP) is an antimalarial drug that was popular for its fast onset of action, safety in all trimesters of pregnancy, and its beneficial effects in rheumatoid arthritis and lupus erythematosus. CP has poor tableting properties and therefore requires a binder, among other excipients, to form robust tablets. The potential of using Ofada rice (Oryza glaberrina Steud) starch as the binder in tablet formulations of CP was compared to B.P. grade established corn starch. The starches were characterized for morphology (Scanning electron microscopy, SEM), crystallinity (Fourier Transform Infra- Red Spectroscopy, FTIR), swelling, densities, flow, and compressing properties. CP tablets containing the native starches as binders at 5.0 and 10.0% w/w respectively were prepared using wet granulation at compression pressures 56.56 and 113.13 MNm -2 for a period of 15 and 30 seconds. The potential of using Ofada rice starch as a binder was examined using the Taguchi based grey-relational design (L-16 orthogonal array). Binder type, binder concentration, compression pressure, and compression time were the four input parameters used at two levels, while the crushing strength-friability-disintegration time ratio (CSFR/DT) and t 80 were the responses. Grey relational coefficients and grey relational grades were determined to identify the optimal levels of the input parameters. Ofada rice starch had smaller particles, higher swelling, and better compressibility. For the CP tablet formulations, the Ofada rice starch showed greater CSFR/DT values and dissolution times. The Taguchi based grey-relational analysis showed that binder concentration was the most significant individual parameter that influenced both responses while the interaction between binder type and binder concentration had the highest influence. The optimum parameter levels for CSFR/DT and t 80 were CP tablets containing Ofada starch at 5.0% w/w concentration, compressed at 56.56 MNm -2 for 15 seconds. Ofada rice starch shows potential as a binder in tablet formulations.