The binary and ternary amorphous systems of candesartan cilexetil preparation to improve its solubility
DOI:
https://doi.org/10.22159/ijap.2024v16i5.51141Keywords:
Candesartan cilexetil, l-Arginine, Polyvinylpyrrolidone K25, Amorphous, SolubilityAbstract
Objective: The objectives of this work was to prepare the binary and ternary amorphous systems of candesartan cilextil, characterize these, and evaluate their influence on solubility.
Methods: Candesartan cilexetil was prepared in three amorphous systems, namely candesartan cilexetil-l-arginine binary co-amorphous system (CAN-ARG CAMS), binary solid dispersion of candesartan cilexetil with 10, 20, and 30% of polyvinylpyrrolidone K25 (CAN-PVP K25 ASD), and ternary co-amorphous system candesartan cilexetil-l-arginine with 10, 20, and 30% of polyvinylpyrrolidone K25 (CAN-ARG-PVP K25 CAMS). All amorphous systems were characterized by polarizing microscopy and differential scanning calorimetry (DSC) methods, while the degree of crystallinity was calculated based on powder X-ray diffraction (PXRD) patterns. The solubility test of all amorphous systems of candesartan cilexetil was carried out respectively in water solvent (25±0.5°C) and phosphate buffer solution with a pH of 6.5 that contained 0.70% polysorbate 20 at 37±0.5°C.
Results: The utilization of polarizing microscopy, DSC, and PXRD methods revealed that not all candesartan cilexetil present in the CAN-ARG binary CAMS and CAN-PVP K25 binary ASD transformed into the amorphous form. Nevertheless, in the context of CAN-ARGPVP K25 ternary CAMS, it was seen that the entirety of the candesartan cilexetil transformed from crystalline into amorphous form. The solubility of candesartan cilexetil in water and a pH 6.5 buffer solution was improved by all amorphous systems. The CAN-ARG-PVP K25 ternary CAMS exhibited higher solubility than the two binary amorphous systems.
Conclusion: it can be inferred that the synthesis of binary and ternary amorphous candesartan cilexetil has yielded positive outcomes, resulting in an enhanced solubility of this API.
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