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ISSN 2063-5346
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Eutectics of Oxaprozin: Synthesis, Characterization, and Evaluation for the Management of Osteoarthritis.

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Rohit Wadhwa, Subham, Md. Rageeb Md. Usman, Ram Babu Sharma, Sakshi Tomar
» doi: 10.48047/ecb/2023.12.si7.415

Abstract

The research work described focuses development of a multicomponent solid form of the antiosteoarthritic drug Ozaprozin (OXN) to improve its biopharmaceutical properties. By using mechanochemical synthesis method to create a new solid form of OXN by combining it with coformers that possess antioxidant properties, namely ascorbic acid syringic acid, and nicotinic acid. This combination resulted in the formation of three eutectic mixtures (EMs). The formation of eutectic mixtures was confirmed using differential scanning calorimetry, and the exact stoichiometry of the mixtures (50/50% w/w) was established through phase diagrams and Tammam's triangle. The strong homomeric interaction between the individual components and steric hindrances played a role in the formation of these eutectic mixtures. The eutectic mixtures showed improved apparent solubility (five- to nine-fold) and a significant enhancement in the intrinsic dissolution rate (two- to three-fold) compared to the plain drug. This suggests that the multicomponent solid forms of OXN have the potential to enhance the drug's solubility and dissolution rate, which are crucial factors for drug absorption and bioavailability. Further studies were conducted to evaluate the biopharmaceutical performance of the eutectic mixtures. In vivo pharmacodynamic studies demonstrated a significant improvement in the performance of the eutectic mixtures compared to the pure drug. These findings suggest that the multicomponent solid forms of OXN could potentially enhance the therapeutic efficacy of the drug in the management of osteoarthritis

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