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AAPS PharmSciTech

, Volume 9, Issue 1, pp 295–301 | Cite as

Preliminary Investigation on the Development of Diltiazem Resin Complex Loaded Carboxymethyl Xanthan Beads

  • Somasree Ray
  • Sabyasachi Maiti
  • Biswanath Sa
Research Article Themed Issue: Oral Controlled Release Development and Technology Guest Editors: Stephen Howard and Jian-Xin Li

Abstract

The objective of this study was to develop a multiunit sustained release dosage form of diltiazem using a natural polymer from a completely aqueous environment. Diltiazem was complexed with resin and the resinate-loaded carboxymethyl xanthan (RCMX) beads were prepared by interacting sodium carboxymethyl xanthan (SCMX), a derivatized xanthan gum, with Al+3 ions. The beads were evaluated for drug entrapment efficiency (DEE) and release characteristics in enzyme free simulated gastric fluid (SGF, HCl solution, pH 1.2) and simulated intestinal fluid (SIF, USP phosphate buffer solution, pH 6.8). Increase in gelation time from 5 to 20 min and AlCl3 concentration from 1 to 3% decreased the DEE respectively from 95 to 79% and 88.5 to 84.6%. However, increase in gum concentration from 1.5 to 2.5% increased the DEE from 86.5 to 90.7%. The variation in DEE was related to displacement of drug from the resinate by the gel forming Al+3 ions. While 75–82% drug was released in 2 h in SGF from various beads, 75 to 98% drug was released in 5 hour in SIF indicating the dependence of drug release on pH of dissolution media. Although the beads maintained their initial integrity throughout the dissolution process in both media, as evident from scanning electron microscopic studies, the faster release in SGF was accounted for higher swelling of the beads in SGF than in SIF. When release data (up to 60%) was fitted in power law expression, the drug release was found to be controlled by diffusion with simultaneous relaxation phenomena.

Key words

carboxymethyl xanthan beads diltiazem entrapment release resinate 

Notes

Acknowledgements

The authors wish to thank M/s. Sun Pharmaceutical Industries Ltd., and M/s Ion Exchange (India) Pvt. Ltd., for the generous gift of diltiazem and Indion 254 respectively. Authors are also grateful to Dr P Chakraborty, Professor, Metallurgy Department, Jadavpur University for carrying out the Scanning Electron Microscopic studies.

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Copyright information

© American Association of Pharmaceutical Scientists 2007

Authors and Affiliations

  1. 1.Gupta College of Technological SciencesAsansol-1India
  2. 2.Centre for Advanced Research in Pharmaceutical Sciences, Department Of Pharmaceutical TechnologyJadavpur UniversityKolkataIndia
  3. 3.Division of Pharmaceutics, Department of Pharmaceutical TechnologyJadavpur UniversityKolkataIndia

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