Improvement of physicochemical properties of an antiepileptic drug by salt engineering.

AAPS PharmSciTech
Ziyaur RahmanMansoor A Khan

Abstract

The focus of the present investigation was to evaluate the feasibility of using cyclamic salt of lamotrigine in order to improve its solubility and intrinsic dissolution rate (IDR). The salt was prepared by solution crystallization method and characterized chemically by fourier transform infrared spectroscopy (FTIR), proton ((1)H) and carbon ((13)C) nuclear magnetic resonance (liquid and solid, NMR) spectroscopy, physically by powder X-ray diffraction (PXRD), thermally by differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA), physicochemically for solubility, IDR, solution and solid-state stability, and polymorphism by solution recrystallization and slurry conversion studies. The FTIR, NMR, PXRD, DSC, and TGA spectra and thermograms indicated the salt formation. The salt formation increased lamotrigine solubility by 19-fold and IDR by 4.9-fold in water. The solution and solid-state stability were similar to parent molecule and were resistant to polymorphic transformation. In conclusion, cyclamic salt of lamotrigine provides another potential avenue for the pharmaceutical development of lamotrigine with improved physicochemical properties especially for pediatric population. It is also possible that approp...Continue Reading

References

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Oct 14, 2009·Biopharmaceutics & Drug Disposition·Hiten J ShahChhagan N Patel
Jan 27, 2011·Pharmaceutical Development and Technology·Ziyaur RahmanMansoor A Khan

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Citations

Sep 15, 2015·Journal of Pharmaceutical Sciences·Ekaterina A GorkovenkoBoris N Savenko
Nov 1, 2013·Journal of Pharmaceutical and Biomedical Analysis·Katarzyna Paradowska, Iwona Wawer
Jun 27, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Ziyaur RahmanMansoor A Khan
Aug 18, 2016·Drug Development and Industrial Pharmacy·Xiaoting LiTianhong Zhang
Sep 25, 2019·Drug Development and Industrial Pharmacy·Sogra F Barakh AliZiyaur Rahman
Jan 4, 2017·Journal of Pharmaceutics·Ahmed Mahmoud Abdelhaleem Ali, Mayyas Mohammad Ahmad Al-Remawi
Mar 4, 2021·Pharmaceutical Development and Technology·Afrooz HamidehMansoor A Khan
Jun 7, 2017·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Meng LiEcevit Bilgili
Aug 22, 2021·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Alaa H SalamaAbeer A A Salama

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