Literature DB >> 31933394

Update on compatibility assessment of empagliflozin with the selected pharmaceutical excipients employed in solid dosage forms by thermal, spectroscopic and chromatographic techniques.

Prakash Niguram1, Surya Narayana Polaka2, Rajeshwari Rathod1, Kiran Kalia1, Abhijeet S Kate1,3.   

Abstract

Empagliflozin (EGF) received USFDA approval in 2014 for oral use to control the glucose levels in adults with type 2 diabetes mellitus. Albeit, a systematic drug-excipient compatibility study of EGF has not been reported in the open literature. As physical and chemical interactions affect the performance of the formulation, this study intended to unveil the drug and excipients interactions which would later help in development of a robust solid dosage form. Differential scanning calorimetry (DSC) was applied as a screening tool for the assessment of compatibility between EGF and the list of excipients mentioned in the EMEA summary of product characteristics (SmPC)-section 6.1, along with mannitol and polyvinylpyrrolidone. Thermogravimetric analysis (TGA), Fourier Transform Infrared Spectroscopy (FTIR), X-ray Powder Diffraction (PXRD) and Hot Stage Microscopy (HSM) methods were utilized to appraise the interpretation of DSC results adequately. Isothermal stress testing (IST) studies of EGF were performed using the selected excipients to check the presence of interaction products (IPs) and the drug content by HPLC. Additional peaks were observed in the EGF-macrogol mixture than the drug peak in the HPLC analysis after two and half months, and those were separated and identified by the Ultra-High Performance Liquid Chromatography-Quadrupole Time of Flight Mass Spectrometry (UHPLC-QTOF-MS). Overall, EGF had shown compatibility with 13 selected excipients; however, initial observation of DSC and IST studies indicated plausible interaction of the EGF with macrogol.

Entities:  

Keywords:  DSC; Drug-Excipient compatibility; LC-MS; PXRD; TGA; empagliflozin

Year:  2020        PMID: 31933394     DOI: 10.1080/03639045.2020.1716371

Source DB:  PubMed          Journal:  Drug Dev Ind Pharm        ISSN: 0363-9045            Impact factor:   3.225


  1 in total

1.  Experimental solubility and thermodynamic modeling of empagliflozin in supercritical carbon dioxide.

Authors:  Gholamhossein Sodeifian; Chandrasekhar Garlapati; Fariba Razmimanesh; Hassan Nateghi
Journal:  Sci Rep       Date:  2022-05-30       Impact factor: 4.996

  1 in total

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