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Crystal Engineering of Pharmaceutical Cocrystals ud

机译:药物晶体的晶体工程 ud

摘要

Cocrystals have recently gained attention as attractive alternate solid forms for drug development. A pharmaceutical cocrystal is a single crystalline homogenous phase consisting of a drug molecule and ligand i.e. cocrystal former that is excipient or another drug molecule [1,2]. The different components in the cocrystal are neutral in nature when compared to salts that have ionized components. [1,2,3]. The components in a cocrystal exist in a definite stoichiometric ratio, and assemble via non-covalent interactions such as hydrogen bonds, ionic bonds, π-π or van der Waals interactions. Cocrystals thus possess different composition and structure when compared to the crystals of parent components.udExamples in the preceding section show that cocrystallization alters the molecular interactions and composition of pharmaceutical materials. As such one can expect changes in physico-chemical properties such as chemical stability [4], hygroscopicity [5], dissolution rates and solubility [6] compressibility [6] due to cocrysallization of pharmaceutical materials. udTo formulate Pharmaceutical Cocrystal(s) will be used two drugs which proton-acceptor and/ or proton-donor functional groups can form syntons toward H-bonding with appropriate to them functional group encompassed in their structure. The selection of drug models will be done according to their performance of dual or complementary pharmacological responds in therapy. The formulated cocrystal of two drug molecules will present New Chemical Entity (NCE) that offer opportunity to be cover with patent protection and further to be used as single Active Pharmaceutical ingrediant in combo i.e. fixed pharmaceutical formulation that perform dual action in therapy.udResearch methodology encompasses the drug cocrystal screening toward applying procedures for crystallization, and analytical techniques for characterization of formed cocrystal in solid state and in solution, respectively.ud
机译:共晶作为药物开发的吸引人的替代固体形式最近受到关注。药物共晶体是由药物分子和配体组成的单晶均相,即作为赋形剂或另一种药物分子的共晶体形成剂[1,2]。与具有离子化成分的盐相比,共晶中的不同成分本质上是中性的。 [1,2,3]。共晶体中的组分以确定的化学计量比存在,并通过非共价相互作用(例如氢键,离子键,π-π或范德华相互作用)组装。因此,与母体成分的晶体相比,共晶体具有不同的组成和结构。上一节中的示例表明,共结晶会改变药物材料的分子相互作用和组成。因此,由于药物材料的凝聚作用,人们可以期待理化性质的变化,例如化学稳定性[4],吸湿性[5],溶出度和溶解度[6]可压缩性[6]。为了配制药物共晶体,将使用两种药物,它们的质子受体和/或质子供体官能团可以形成氢键键合的同质子,并具有适合其结构中包含的官能团。药物模型的选择将根据其在治疗中双重或互补药理学反应的表现来进行。由两种药物分子组成的共晶体将呈现出新化学实体(NCE),该新化学实体提供了获得专利保护的机会,并可进一步用作组合中的单一活性药物成分,即在治疗中起双重作用的固定药物制剂。涵盖了针对共晶过程的药物共晶筛选,以及分别表征固态和溶液形式共晶的分析技术。

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