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Olanzapinium salts, isostructural solvates, and their physicochemical properties

机译:奥氮平鎓盐,同构溶剂化物及其理化性质

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Solubility and dissolution play a crucial role in the activity and efficacy of an oral drug. Olanzapine is an antipsychotic drug of the Biopharmaceutics Classification System (BCS) class II category. Several solvates, cocrystals, salts, and amorphous forms of olanzapine have been prepared to study materials properties and its X-ray crystal structures were classified. We report herein a few salts, solvates, and solvate polymorphs of olanzapine to improve the physicochemical properties and study novel structural motifs. Olanzapinium dimaleate monofumaric acid is the first case of a ternary cocrystal of an active pharmaceutical ingredients (API) in the CSD database with maleate ion and fumaric acid coformers. The olanzapine disalts, olanzapinium dipicrate, dimaleate, and dimaleate monofumaric acid, contain a novel structural motif, different from the dimer motif characteristic of the four structural categories reported in the literature.
机译:溶解性和溶解性在口服药物的活性和功效中起着至关重要的作用。奥氮平是生物药物分类系统(BCS)II类的抗精神病药。制备了奥氮平的几种溶剂化物,共晶体,盐和无定形形式,以研究材料的性能,并对其X射线晶体结构进行了分类。我们在这里报告了奥氮平的一些盐,溶剂化物和溶剂化物多晶型物,以改善其理化性质并研究新颖的结构图案。双马来酸富马酸单富马酸是CSD数据库中具有马来酸离子和富马酸共形成剂的活性药物成分(API)三元共结晶的首例。奥氮平二盐,二油酸奥氮哌铵,二马来酸和二马来酸一富马酸具有新颖的结构基序,与文献中报道的四个结构类别的二聚体基序不同。

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