| DOI: 10.29090/psa.2026.03.25.8936 | Pharm Sci Asia 2026; 53(3), 321-333 |
Mixture design for screening polymers in riboflavin effervescent gastroretentive floating tabletsUmme Tabassum Arobi Katha1, Kathie Ling Wee Ping1, Nurul Akmarina Mohd Abdul Kamal1, Mohd Amir Shahlan Mohd Aspar2, Mohd Akmal Azhar1*
1 Faculty of Chemical and Process Engineering Technology, Universiti Malaysia Pahang Al Sultan Abdullah, 26300, Kuantan, Pahang, Malaysia
2 Faculty of Electrical and Electronics Engineering Technology, Universiti Malaysia Pahang Al Sultan Abdullah, 26600, Pekan, Pahang, Malaysia
Oral sustained-release formulations improve therapeutic efficacy and patient compliance. Floating drug delivery systems (FDDS) prolong gastric residence by floating over gastric contents, enhancing upper intestinal absorption. Riboflavin, a water-soluble vitamin with low intestinal uptake, was selected as the model drug to produce direct-compression floating tablets. A mixture design (DOE) approach optimized five polymers, carrageenan, chitosan, Carbopol 940, HPMC K4M, and HPMC K75, combined with effervescent agents. Eighteen formulations were prepared and evaluated for floating lag time and cumulative drug release. Numerical optimization using the desirability function in Design Expert software identified polymer compositions achieving desirability = 1.000, with predicted release of 71–79%: Carrageenan 12–15%, Carbopol 940 4–17%, and HPMC K75 0.6–12%. Based on DOE contour plots and predicted responses, formulations F6, F10, and F12 were selected as optimal screening candidates, exhibiting low release at 6 h and acceptable floating lag times (≤300 s). Contour and 3D surface analysis revealed polymer-specific effects: carrageenan strongly retarded release via gel formation, Carbopol 940 provided intermediate modulation through swelling and diffusion, HPMC K75 offered moderate control, HPMC K4M weak retardation, and chitosan accelerated release. The best formulations balanced buoyancy and sustained release, highlighting carrageenan and Carbopol 940 as key excipients for FDDS. These findings demonstrate the utility of experimental design for excipient screening and the potential to tailor polymer combinations to improve riboflavin bioavailability.
Keyword:
Gastroretentive drug delivery system; Floating tablets; Mixture design (DOE); Riboflavin; Polymer
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