Abstract
Objective: This study was aimed to obtain a new excipient that can be used as a polymer matrix for the formulation of controlled release dosage forms.Methods: This study used coprocessing and crosslinking methods on amylose and xanthan gum (XG) to obtain a new excipient that can be usedfor controlled release matrix of pharmaceutical dosage forms. The coprocessing step was conducted by drum drying, and the crosslinking step wasprepared using 6 and 12% sodium trimetaphosphate (STMP). The produced novel excipients were characterized in terms of infrared (IR) spectrum,substitution degree, moisture content, swelling index, and gel strength.Results: Our results showed that amylose–XG excipients crosslinked using 6% STMP have greater gel strength and better swelling indexes thanexcipients crosslinked using 12% STMP. All coprocessed excipients exhibited no differences in their IR spectra, whereas the crosslinked excipientsdid, indicating a structural change due to the addition of phosphate groups. Crosslinking amylose–xanthan-coprocessed excipients using 6% STMPproduced degrees of substitution (DSs) of 7–8 phosphates per 100 monomeric subunits. The excipients had a moisture content of 8.21–12.85%, andthe pH of a 1% solution of excipients was 6.21–6.43. In addition, the swelling index and gel strength of the excipient where both amylose and XG werecrosslinked together Were more than 1 where only amylose was crosslinked.Conclusion: The crosslinking amylose–xanthan-coprocessed excipient using 6% STMP is more suitable for use in controlled release dosage forms,particularly when the polymer ratio is 1:1.
Highlights
Polysaccharides such as pectin, chitosan, starch, guar gum, and xanthan are commonly used in controlled release dosage forms of various pharmaceuticals due to their low cost, biocompatibility, low toxicity, ease of chemical modification, and biodegradability [1,2,3,4]
Many studies have demonstrated the successful application of high-amylose starch crosslinked using different agents, such as epichlorohydrin and sodium trimetaphosphate (STMP), in the development of controlled drug delivery systems [5,8,9]
crosslinked amylose (CLA) with degrees of substitution (DSs) of 6–8 exhibits a good release profile when used as matrix in controlled-release tablets (15–20 h); in contrast, high DS (>10) results in a significant decrease in the drug release time profile (1–3 h), indicating that substitution can cause it to act as a disintegrants [11]
Summary
Synthesis of Co CLA-XG and CL Co-A-XG Two methods, which were modified from the method of Cury et al [16], were used. Three combinations of amylose and XG were produced at 1:1, 1:2, and 2:1 This material was suspended in distilled water, and the pH was adjusted to 11–12 with 4% NaOH. Chemical characterization Chemical characterization of Co CLA-XG and CL Co-A-XG was conducted with respect to pH, number of functional groups, and degree of crosslinking. Functional characterization Functional characterization of Co CLA-XG and CL Co-A-XG powders was conducted on their flow properties, whereas viscosity and rheology, swelling index, and gel strength were assessed on their solutions/gels. Swelling index was determined by comparing the weight of a dry tablet of excipient and the weight after it had been placed in 10 mL of the medium of various pHs. Gel strength was measured using a texture analyzer on a solid gel of 10% Co CLA-XG or CL Co-A-XG that has been cooled to ±4°C for 2 h
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