AAPS PharmSciTech

, Volume 14, Issue 2, pp 639–648

Formulation and Development of Extended-Release Micro Particulate Drug Delivery System of Solubilized Rifaximin

  • Rohan V. Karanje
  • Yogita V. Bhavsar
  • Kirti H. Jahagirdar
  • Kiran S. Bhise
Research Article

DOI: 10.1208/s12249-013-9949-x

Cite this article as:
Karanje, R.V., Bhavsar, Y.V., Jahagirdar, K.H. et al. AAPS PharmSciTech (2013) 14: 639. doi:10.1208/s12249-013-9949-x
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Abstract

Rifaximin (RFX), a semi-synthetic antibiotic belonging to BCS class IV category, has been used in the treatment of traveler’s diarrhea. An attempt has been made to improve aqueous solubility of RFX in the presence of β-cyclodextrin (β-CD) and hydroxy propyl β-cyclodextrin (HP-β-CD) and control its release in the gut by enteric coating. The stoichiometric proportion of RFX and complexing agent’s β-CD and HP-β-CD were determined by phase solubility studies. RFX–β-CD and RFX–HP-β-CD were prepared in 1:2 ratio by solvent evaporation technique using rota-evaporator with yield of 78% and 84% respectively followed by their evaluation using different techniques such as saturation solubility, Fourier transform infrared, differential scanning calorimeter, powder X-ray diffractometer, in vitro antimicrobial activity. The saturation solubility of RFX had improved from 0.0736 mg/ml to 0.2354 mg/ml and 0.5681 mg/ml in presence of β-CD and HP-β-CD respectively resulting in an increased zone of inhibition in the later complex during antimicrobial studies. The RFX–HP-β-CD complex particles were coated with eudragit L 100 (EL 100) by spray drying technique. The 32 factorial design was applied to formulate the micro particles. All formulations exhibited pH dependant drug release. The % EE was 69% and the release of RFX was retarded by enteric coating in the optimized batch FB2. Therefore, it can be concluded that solubility of some BCS class IV drugs can be improved by β-CD complexation and release of such inclusion complexes can be retarded to increase the residence time of RFX in the gastrointestinal tract.

Key word

cyclodextrin complexeseudragit L100micro particlesrifaximinspray dryer

Abbreviations

ANOVA

Analysis of variance

β-CD

Beta-cyclodextrin

BCS

Biopharmaceutical classification system

R

Coefficient of correlation

°C

Degree Celsius

% DR

Percentage drug release

DSC

Differential scanning calorimeter

% EE

Percentage entrapment efficiency

EL 100

eudragit L 100

HP-β-CD

Hydroxy propyl β cyclodextrin

mm

Millimeter

mg

Milligram

ml

Milliliter

PBS pH 6.8

Phosphate buffer solution pH 6.8

PXRD

Powder X-ray diffractometer

P

Probability

RFX

Rifaximin

rpm

Revolution per minute

SEM

Scanning electron microscopy

USP

United state pharmacopeia

Copyright information

© American Association of Pharmaceutical Scientists 2013

Authors and Affiliations

  • Rohan V. Karanje
    • 1
  • Yogita V. Bhavsar
    • 1
  • Kirti H. Jahagirdar
    • 1
  • Kiran S. Bhise
    • 1
  1. 1.Department Of PharmaceuticsMCE Society’s Allana College of PharmacyCamp PuneIndia