Physicochemical characterization of β-cyclodextrin and hydroxy ethyl β-cyclodextrin complexes of rifampicin

Authors

  • B. PRAKASH RAO Al-Ameen College of Pharmacy, Hosur Road, Bangalore (India)-560027
  • SARASIJA SURESH Al-Ameen College of Pharmacy, Hosur Road, Bangalore (India)-560027
  • C. NARENDRA Krupanidhi College of Pharmacy, Koramangala, Bangalore-34
  • C BALASANGAMESHWER National Tuberculosis Institute, Sadashiva Nagar, Bangalore-03

Keywords:

Cyclodextrins, characterization, DSC, FTIR, Rifampicin, SEM, and Thermal Stability, in vitro anti-tubercular activity

Abstract

An attempt was made to optimize the oral delivery of rifampicin by formation of inclusion complexes with cyclodextrinsincluding β-Cyclodextrin (β-CD), and hydroxy-ethyl-β-cyclodextrin (HEβ-CD). The aim of the study was to increase thesolubility, stability of rifampicin by way of complexation and to evaluate the effect of cyclodextrin on its anti-tubercularactivity. The phase solubility studies showed that it followed Type-AL solubility curve and the slope of the line is lessthan one, indicating 1:1 molar ratio of drug to complexing agent. Cyclodextrin complexes were prepared by kneading(KN) and common solvent (CS) methods. The physical mixtures (PM) were also prepared in the same ratio. In case ofβ-CD complexes, a 2 fold increase in solubility was observed with CS complex. Formation of complex with side chain4-methyl piperazin-1-ylimino-methyl of rifampicin was confi rmed by FTIR. Formation of complex was confi rmed by DSC,SEM, and powder x-ray diffraction studies. In vitro anti-tubercular activity of rifampicin was found to be enhanced in case of all the complexes indicated by a reduction in MIC of rifampicin to half. Inclusion complexation with β-CDand hydroxy ethyl β-cyclodextrin improved its physico-chemical properties and in vitro anti-tubercular activity.

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Published

2006-03-20

How to Cite

1.
PRAKASH RAO B, SURESH S, NARENDRA C, BALASANGAMESHWER C. Physicochemical characterization of β-cyclodextrin and hydroxy ethyl β-cyclodextrin complexes of rifampicin. Ars Pharm [Internet]. 2006 Mar. 20 [cited 2024 Aug. 24];47(1):37-59. Available from: https://revistaseug.ugr.es/index.php/ars/article/view/5015

Issue

Vol. 47 No. 1 (2006)

Section

Original Articles

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