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Multicomponent crystal compromising dasatinib and selected co-crystals formers: a patent evaluation of EP2861589B1

机译:多组分晶体妥协达沙替尼和选定的共晶形成器:EP2861589B1的专利评估

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摘要

Cocrystallization has gained significant prominence in pharmaceutical product development because of the enhancement of physical, chemical and pharmacological properties of active pharmaceutical ingredients, such as stability, solubility, dissolution rate, taste, hygroscopicity, mechanical property, bioavailability, permeability and therapeutic activity. Traditionally, co-crystals can be prepared by a grinding, solvent evaporation and slurry method. However, sophisticated methods such as spa drying, hot-melt extrusion, supercritical fluid and laser irradiation are also reported to be used for producing co-crystals. The selected patent describes the development of multicomponent crystals of dasatinib, with an aim to enhance the aqueous solubility of a selected drug. However issues surrounding the toxicity, stability, large scale manufacture, in vivo performance in human beings and regulations require adequate addressal prior to exploring the commercial viability of pharmaceutical co-crystals.
机译:由于增强了活性药物成分的物理、化学和药理学性质,如稳定性、溶解度、溶解速率、味道、吸湿性、机械性能、生物利用度、渗透性和治疗活性,共结晶在医药产品开发中获得了重要地位。传统上,共晶体可以通过研磨、溶剂蒸发和浆液法制备。然而,据报道,诸如水疗干燥、热熔挤出、超临界流体和激光辐照等复杂方法也用于生产共晶体。所选专利描述了达沙替尼多组分晶体的开发,旨在提高所选药物的水溶性。然而,在探索药物共晶体的商业可行性之前,围绕毒性、稳定性、大规模制造、人体体内性能和法规的问题需要充分解决。

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