Evaluation of Drug Release From Coated Pellets Based on Isomalt, Sugar, and Microcrystalline Cellulose Inert Cores

Abstract

Abstract. The objective of the present study was to investigate the effect of the pellet core materials isomalt, sugar, and microcrystalline cellulose on the in vitro drug release kinetics of coated sustainedrelease pellets as well as to evaluate the influence of different ratios of polymethacrylate copolymers exhibiting different permeability characteristics on the drug release rate. For characterization of the drug release process of pellets, the effect of osmolality was studied using glucose as an osmotically active agent in the dissolution medium. The pellet cores were layered with diclofenac sodium as model drug and coated with different ratios of Eudragit® RS30D and Eudragit® RL30D (ERS and ERL; 0:1 and 0.5:0.5 and 1:0 ratio) in a fluid bed apparatus. Physical characteristics such as mechanical strength, shape, and size proved that the inert cores were adequate for further processing. The in vitro dissolution tests were performed using a USP Apparatus I (basket method). The results demonstrated that, besides the ratio of the coating polymers (ERS/ERL), the release mechanism was also influenced by the type of starter core used. Sugar-and isomalt-type pellet cores demonstrated similar drug release profiles.

Optimising the in vitro and in vivo performance of oral cocrystal formulations via spray coating

“…Regarding the starter cores, no major differences were observed in terms of composition, except the lower release rate obtained from TAP beads which may be related to a stronger interaction between the SDM and the acidic groups in the core instead of the 4ASA. However, other authors have reported significant differences in drug release depending on the composition of the core material [45][46][47]. As expected, the particle size of the beads has a significant effect on the physicochemical characteristics of the cocrystal.…”

Solvent-Free Melt Electrospinning for Preparation of Fast Dissolving Drug Delivery System and Comparison with Solvent-Based Electrospun and Melt Extruded Systems

“…Sustained drug release is generally needed in the case of drug‐loaded implants,1 tissue scaffolds (tissue engineering),2 and wound dressings3 to attain an adequate long‐term effect. However, in the case of oral dosage forms, enhanced dissolution is often required, in addition to sustained drug release,4–6 to achieve sufficient bioavailability 7. It is a significant challenge for pharmaceutical technologists because of the increasing number of drugs with poor water solubility 8,9…”

Influence of Free-Flow Excipients on Functional Performance of Noveonaa1 in Controlled-Release Tablets

“…In controlled release diclofenac sodium pellets, based on isomalt, sugar, and microcrystalline cellulose, it was comparatively observed that dissolution rates for the soluble sucrose-and isomalt-based pellets were similar and were significantly higher compared to those of the microcrystalline cellulose-based pellets [24]. Table 2 summarizes the calculated regression parameters for the release profile of metronidazole tablets containing a fixed proportion of Noveon AA1 (20%) and different proportions of GalenIQ 720.…”