New Insight Into Thermodynamical Stability of Carbamazepine

J Pharm Sci. 2019 Aug;108(8):2654-2660. doi: 10.1016/j.xphs.2019.03.027. Epub 2019 Mar 26.

Abstract

Carbamazepine (CBZ)-an antiepileptic drug-belongs to Biopharmaceutics Classification System II Class. It has low solubility and consequently limited bioavailability. One of the ways to improve drugs solubility is amorphization of their structure. Herein, cooling CBZ-at different cooling rates-was investigated as a way to obtain glassy, better soluble form. During preliminary differential scanning calorimetry experiments, some peculiar behavior of the examined material, different from those stated in the literature, was observed. Further investigations using differential scanning calorimetry, thermogravimetric analysis, and polarizing optical microscope revealed that decomposition temperature of CBZ is about 30°C lower than previously assumed. Moreover, high-resolution thermogravimetric measurements indicate that some decomposition processes could start even below the temperature reported as the melting point of the form I of CBZ.

Keywords: Differential scanning Calorimetry (DSC); carbamazepine; glass transition(s); phase transition(s); physical stability; polymorph(s); thermal analysis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anticonvulsants / chemistry*
  • Carbamazepine / chemistry*
  • Drug Stability
  • Solubility
  • Temperature
  • Thermodynamics
  • Transition Temperature

Substances

  • Anticonvulsants
  • Carbamazepine