Mechanochemical synthesis of drug–drug and drug–nutraceutical multicomponent solids of olanzapine,CrystEngComm

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Mechanochemical synthesis of drug–drug and drug–nutraceutical multicomponent solids of olanzapine
CrystEngComm ( IF 2.6 ) Pub Date : 2020/01/08 , DOI: 10.1039/c9ce01504c
Kashyap Kumar Sarmah _{1,

2,

3,

4} , Nilamoni Nath _{1,

2,

3,

4} , Dharmaraj R. Rao _{4,

5,

6,

7} , Ranjit Thakuria _{1,

2,

3,

4}

Affiliation

Drug–drug and drug–nutraceutical multicomponent solids of an antipsychotic drug olanzapine (OLN) are prepared using mechanochemistry. Drug molecules, viz., nateglinide (NAT) and pyrazinoic acid (PZO) as well as nutraceuticals, namely, 2,4,6-trihydroxybenzoic acid (246THBA), gallic acid (GA) and sinapic acid (SPA) are used as coformers in this study. After neat grinding (NG), incomplete conversion (partially amorphous) was observed, whereas liquid-assisted grinding (LAG) resulted in the formation of coamorphous OLN–NAT and crystalline salts/salt hydrates of OLN with rest of the coformers, which were characterized using a combination of techniques, including single crystal X-ray diffraction. The OLN–NAT coamorphous salt has a potential scope for development as a combination drug in order to suppress the increase in the blood sugar level, a common side-effect observed during the monotherapy of psychiatric patients using OLN. The equilibrium solubility study shows a substantial enhancement in the solubility of olanzapinium pyrazinoate compared to that of the pure base.

中文翻译：

奥氮平的药物-药物和药物-营养多组分固体的机械化学合成

抗精神病药物奥氮平（OLN）的药物-药物和药物-营养保健品的多组分固体是使用机械化学方法制备的。药物分子，即。，那格列奈（NAT）和吡嗪酸（PZO）以及营养品，即2,4,6-三羟基苯甲酸（246THBA），没食子酸（GA）和芥子酸（SPA）被用作本研究的共形成剂。经过纯磨（NG）后，观察到不完全转化（部分为非晶态），而液体辅助磨削（LAG）导致共晶OLN-NAT以及OLN的结晶盐/盐水合物与其余共形成物的形成使用多种技术的组合，包括单晶X射线衍射。OLN-NAT非晶盐作为一种联合药物具有潜在的开发潜力，可以抑制血糖水平的升高，这是在使用OLN的精神病患者单药治疗期间观察到的常见副作用。

更新日期：2020-02-13

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