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Versatile Salts as a Strategy to Modify the Biopharmaceutical Properties of Venlafaxine and a Potential Hypoglycemic Effect Study
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2020-03-19 , DOI: 10.1021/acs.cgd.0c00007 Ningbo Gong 1, 2 , Yong Zhang 2 , Ying Wang 1 , Hongmei Yu 1 , Baoxi Zhang 1 , Hailu Zhang 3 , Yang Lu 1 , Guanhua Du 4
Crystal Growth & Design ( IF 3.2 ) Pub Date : 2020-03-19 , DOI: 10.1021/acs.cgd.0c00007 Ningbo Gong 1, 2 , Yong Zhang 2 , Ying Wang 1 , Hongmei Yu 1 , Baoxi Zhang 1 , Hailu Zhang 3 , Yang Lu 1 , Guanhua Du 4
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Venlafaxine (VLF) is a widely prescribed antidepressant thought to have little effect on glucose metabolism, but some clinical reports showed that a VLF overdose may cause hypoglycemia. The raw material of VLF hydrochloride is metastable and may cause problems during the manufacturing and storage process. Here, salt formation was employed to modify the biopharmaceutical properties, and the hypoglycemic potential of these salt forms was also investigated. Four organic acid salts with phthalic acid (PA), 4-chlorobenzoic acid (4-CA), 4-hydroxybenzoic acid (4-HA), and sulfanilic acid (SA) were obtained for the first time. These products were fully characterized by single crystal and powder X-ray diffraction, solid-state nuclear magnetic resonance, differential scanning calorimetry, and thermogravimetric analysis. Stability measurements revealed that most of these forms held superior phase stability against temperature, moisture, and illumination. All salts show significantly improved solubility relative to VLF. The glucose consumption test was also performed in vitro, VLF:HCl could significantly increase glucose consumption and have a higher glucose consumption index. VLF:PA, VLF:4-CA, VLF:4-HA, and VLF:SA demonstrated no hypoglycemia side effect.
中文翻译：
多种盐作为修饰文拉法辛生物药物特性的策略和潜在的降血糖作用研究
Venlafaxine（VLF）是一种被广泛处方的抗抑郁药，被认为对葡萄糖代谢影响很小，但是一些临床报告显示，VLF过量可能会引起低血糖症。VLF盐酸盐的原料是亚稳态的，可能在制造和存储过程中引起问题。在这里，盐的形成被用来改变生物药物特性，并且还研究了这些盐形式的降血糖潜力。首次获得了四种分别与邻苯二甲酸（PA），4-氯苯甲酸（4-CA），4-羟基苯甲酸（4-HA）和磺胺酸（SA）的有机酸盐。这些产品通过单晶和粉末X射线衍射，固态核磁共振，差示扫描量热法和热重分析进行了全面表征。稳定性测量表明，这些形式中的大多数都具有针对温度，湿度和光照的优异相稳定性。相对于VLF，所有盐均显示出显着改善的溶解度。体外还进行了葡萄糖消耗试验，VLF：HCl可以显着增加葡萄糖消耗并具有更高的葡萄糖消耗指数。VLF：PA，VLF：4-CA，VLF：4-HA和VLF：SA无低血糖副作用。
更新日期：2020-03-19
中文翻译：
多种盐作为修饰文拉法辛生物药物特性的策略和潜在的降血糖作用研究
Venlafaxine（VLF）是一种被广泛处方的抗抑郁药，被认为对葡萄糖代谢影响很小，但是一些临床报告显示，VLF过量可能会引起低血糖症。VLF盐酸盐的原料是亚稳态的，可能在制造和存储过程中引起问题。在这里，盐的形成被用来改变生物药物特性，并且还研究了这些盐形式的降血糖潜力。首次获得了四种分别与邻苯二甲酸（PA），4-氯苯甲酸（4-CA），4-羟基苯甲酸（4-HA）和磺胺酸（SA）的有机酸盐。这些产品通过单晶和粉末X射线衍射，固态核磁共振，差示扫描量热法和热重分析进行了全面表征。稳定性测量表明，这些形式中的大多数都具有针对温度，湿度和光照的优异相稳定性。相对于VLF，所有盐均显示出显着改善的溶解度。体外还进行了葡萄糖消耗试验，VLF：HCl可以显着增加葡萄糖消耗并具有更高的葡萄糖消耗指数。VLF：PA，VLF：4-CA，VLF：4-HA和VLF：SA无低血糖副作用。
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