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

IF 1.8 Q3 PHARMACOLOGY & PHARMACY Pharmaceutical patent analyst Pub Date : 2022-01-01 Epub Date: 2022-02-17 DOI:10.4155/ppa-2021-0024
Ritu Rathi, Inderbir Singh
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引用次数: 2

Abstract

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.

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多组分晶体损害达沙替尼和选择的共晶体形成:EP2861589B1的专利评估。
由于共结晶技术可以提高药物活性成分的物理、化学和药理学性能,如稳定性、溶解度、溶出率、味道、吸湿性、机械性能、生物利用度、渗透性和治疗活性,因此在药品开发中取得了显著的进展。传统上,共晶可以通过研磨、溶剂蒸发和浆料法制备。然而,复杂的方法,如spa干燥,热熔挤压,超临界流体和激光辐照也被用于生产共晶。所选专利描述了达沙替尼多组分晶体的开发,目的是提高所选药物的水溶性。然而,在探索药用共晶的商业可行性之前,需要充分解决有关毒性、稳定性、大规模生产、人体体内性能和法规的问题。
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来源期刊
Pharmaceutical patent analyst
Pharmaceutical patent analyst PHARMACOLOGY & PHARMACY-
CiteScore
1.80
自引率
0.00%
发文量
22
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