| Abstrakt: |
Background: Sacubitril/valsartan, marketed as Azmarda (manufactured by the innovator company) is a cocrystal consisting 6 sacubitril and valsartan molecules, along with sodium cations and water molecules. This formulation is considered a major mechanism of benefit of this molecule. This study was aimed to assess various brands of sacubitril/valsartan in the market for the presence of the cocrystal forms and compare them with Azmarda. a brand of sacubitril/valsartan manufactured by the innovator company. Methods: The study involved analysis of various marketed products containing sacubitril/valsartan tablets, including Azmarda. Both the Azmarda and marketed products were characterized using differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD). Sodium content and dissolution studies were also performed . Results: A total of 16 brands of marketed products including Azmarda were studied. During DSC studies, unique melting pattern was observed in Azmarda, with exothermic peaks of sacubitril/valsartan detected at 140°C and 102°C, respectively. PXRD analysis revealed that none of the products exhibited the same crystal lattice as Azmarda. Azmarda, with a sodium level of 1.773%, was comparable to brand 2 (1.61%), brand 4 (1.73%), and brand 7 (1.58%). Azmarda demonstrated 64% release of sacubitril and 57% release of valsartan within 30 minutes in 0.1N HCl. Brand 7, brand 12, and brand 13 showed 52%, 57%, and 52% release of sacubitril, respectively, and 45%, 52%, and 48% release of valsartan, respectively, in 30 minutes. Conclusion: The absence of identical crystal lattice structures, highlights absence of cocrystalsin generic formulations. Such variations may impact the bioavailability and efficacy, emphasizing the importance of ensuring consistent and reliable therapeutic outcomes. [ABSTRACT FROM AUTHOR] |
