609340-34-3Relevant academic research and scientific papers
Versatile Salts as a Strategy to Modify the Biopharmaceutical Properties of Venlafaxine and a Potential Hypoglycemic Effect Study
Du, Guanhua,Gong, Ningbo,Lu, Yang,Wang, Ying,Yu, Hongmei,Zhang, Baoxi,Zhang, Hailu,Zhang, Yong
, p. 3131 - 3139 (2020)
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.
