Application of 13C CPMAS NMR for qualitative and quantitative characterization of carvedilol and its commercial formulations

J Pharm Sci. 2012 May;101(5):1763-72. doi: 10.1002/jps.23062. Epub 2012 Feb 13.

Abstract

(13) C cross-polarization magic-angle spinning nuclear magnetic resonance (CPMAS NMR) spectroscopy was applied to the identification and characterization of carvedilol (1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)-ethylamino]-propan-2-ol) in pharmaceutical preparations. Solid-state spectra (standard linewidth and lack of signal multiplicity) of carvedilol indicate that its physical form is the same (freebase form II); no other polymorphic forms were detected. The spectra of excipients, recorded under the same conditions, were helpful in their identification. The differences in chemical shifts for tablets I-VI are insignificant and suggest that there are no strong intermolecular drug-excipient interactions. The drugs from six manufacturers contained the same amount (25 mg) of the active substance per tablet; however, tablets differ in size and thus in the concentration of carvedilol. An attempt at quantitation of carvedilol in the dosage forms was made. The cross-polarization kinetics and other measurement parameters affecting the intensity and reproducibility of the spectra were determined. The results revealed a satisfying relationship between the composition of the tablets and the intensity of selected NMR signals. The (13) C CPMAS NMR technique was found to provide accurate quantification of drugs without any chemical preparation, as shown by the particular case of carvedilol's solid formulations.

MeSH terms

  • Adrenergic beta-Antagonists / analysis*
  • Carbazoles / analysis*
  • Carbon Isotopes
  • Carvedilol
  • Chemistry, Pharmaceutical
  • Magnetic Resonance Spectroscopy / methods*
  • Propanolamines / analysis*

Substances

  • Adrenergic beta-Antagonists
  • Carbazoles
  • Carbon Isotopes
  • Propanolamines
  • Carvedilol