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Influence of complex solubility on formulations based on lambda carrageenan and basic drugs

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Abstract

The purpose of the present work was to compare the behavior of some drug/carrageenan complexes having different solubility in water, in a controlled release formulation. Diltiazem HCl, bupropion HCl, metoprolol tartrate, and tramadol HCl were used as model drugs. The complexes were characterized by means of solubility measurements, release test at constant surface area, and water uptake measurements, and the results were related to their performance in controlled release formulations. For the more soluble complexes (involving metoprolol and tramadol) the occurrence of gelation after hydration was observed, while diltiazem complex apparently did not gellify; bupropion behavior was intermediate. A correspondence was found between the observed differences in complex solubility and hydration-gelation behavior and the drug release profiles. For all the drugs considered, the release was completed in about 10 to 12 hours, but different kinetics were observed depending on the solubility of the complexes. All the considered complexes seem suitable for controlled release purposes, although the data obtained show the relevance of the complex solubility to drug release profiles.

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Authors and Affiliations

  1. Department of Pharmaceutical Chemistry, University of Pavia, Viale Taramelli 12, 27100, Pavia, Italy

    Carola Aguzzi, Maria Cristina Bonferoni, Silvia Rossi, Franca Ferrari & Carla Caramella

  2. Faculty of Chemical and Pharmaceutical Sciences, University of Cartagena, Campus de Zaragocilla, Cartagena, Colombia

    Maria Rosario Osorio Fortich

Authors
  1. Carola Aguzzi
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  2. Maria Cristina Bonferoni
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  3. Maria Rosario Osorio Fortich
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  4. Silvia Rossi
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  5. Franca Ferrari
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  6. Carla Caramella
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Corresponding author

Correspondence to Carla Caramella.

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Aguzzi, C., Bonferoni, M.C., Fortich, M.R.O. et al. Influence of complex solubility on formulations based on lambda carrageenan and basic drugs. AAPS PharmSciTech 3, 27 (2002). https://doi.org/10.1208/pt030327

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  • DOI: https://doi.org/10.1208/pt030327

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