Use of calcium carbonate as an excipient for release of poorly water soluble drugs: The case of carbamazepine.

Int J Pharm

Pharmaceutical Sciences Department, University of Perugia, via del Liceo 1, 06123 Perugia, Italy. Electronic address:

Published: November 2020

AI Article Synopsis

  • Carbamazepine (CBZ) is a poorly soluble drug classified as BCS class II, known for its variable bioavailability and different polymorphic forms.
  • The study evaluated the effects of calcium carbonate (CaCO) as a safe and eco-friendly excipient on the physicochemical properties, solubility, and release of CBZ.
  • Results showed that using CaCO enhanced the solubility and drug release of CBZ, potentially due to CaCO's ability to dissolve in acidic environments and its impact on drug crystallinity and interactions.

Article Abstract

Carbamazepine (CBZ) is a poorly water soluble drug owing to the Biopharmaceutic Classification System (BCS) class II. It is characterized by a variable bioavailability and by the presence of different polymorphs. In this paper the effects of CaCO on the physicochemical properties of CBZ and its solubility and release were evaluated. CaCO is a naturally non-toxic biomineral and was chosen because it is a safe, cheap and eco-friendly excipient able to dissolve in an acidic environment. Composites with different CBZ loadings were prepared by ball milling and antisolvent method. The composites were characterized by X-ray powder diffraction, differential scanning calorimetry analysis and attenuated total reflectance FT-IR which revealed that both the presence of CaCO and the preparation procedure affect the polymorphic form crystallinity and intermolecular interactions among the drug molecules. Scanning electron microscopy showed that small drug crystals with different crystalline forms were deposited on the surface of the CaCO particles. Solubility and dissolution tests showed an increase in the apparent solubility of CBZ and improved drug release. These results demonstrated that CaCO affected the drug release properties likely due to its pH-sensitive characteristics.

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http://dx.doi.org/10.1016/j.ijpharm.2020.119860DOI Listing

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