Solubility Enhancement of Piroxicam Using Co-Crystallization Technique

Shubham G. Wagh, S. Pande
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Abstract

Co-crystallization is an effective crystal engineering technique for modifying the crystal structure and physiochemical properties of drugs. Pharmaceutical co-crystals are nonionic supramolecular complexes and can be used to altered physiochemical properties such as solubility, stability and bioavailability in pharmaceutical development without affecting chemical composition of API. Piroxicam is a Non-selective COX inhibitors (traditional NSAIDs) used to reduce the pain, inflammation, and stiffness caused by rheumatoid arthritis and osteoarthritis. Piroxicam belongs to class II drug in BCS classification i.e. low solubility and high permeability. The major problem of this class drug is its low solubility in biological fluids, which results into poor bioavailability after oral administration. The purpose of this study was to prepare pharmaceutical co-crystals of Piroxicam to enhance solubility and dissolution rate by using co-crystallization technique. The co-former used in this study is Para-Aminobenzoic acid, Acetamide and Thiourea. The Optimized co-crystal was characterized by DSC, FTIR, XRPD, SEM and other pharmaceutical properties like solubility and melting point were also evaluated.
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用共结晶技术提高吡罗昔康的溶解度
共结晶是一种有效的改变药物晶体结构和理化性质的晶体工程技术。药物共晶是一种非离子超分子复合物,在药物开发过程中可以改变诸如溶解度、稳定性和生物利用度等理化性质,而不会影响原料药的化学组成。吡罗昔康是一种非选择性COX抑制剂(传统的非甾体抗炎药),用于减轻由类风湿关节炎和骨关节炎引起的疼痛、炎症和僵硬。吡罗昔康在BCS分类中属于ⅱ类药物,即低溶解度和高通透性。这类药物的主要问题是其在生物液体中的溶解度低,这导致口服给药后生物利用度差。本研究的目的是利用共晶技术制备吡罗昔康的药用共晶,以提高其溶解度和溶出速度。本研究使用的共成体是对氨基苯甲酸、乙酰胺和硫脲。通过DSC、FTIR、XRPD、SEM对优化后的共晶进行了表征,并对其溶解度、熔点等理化性质进行了评价。
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