AAPS PharmSciTech

, Volume 7, Issue 1, pp E1–E9

Formulation and in vitro, in vivo evaluation of extended- release matrix tablet of Zidovudine: Influence of combination of hydrophilic and hydrophobic matrix formers

  • Atul Kuksal
  • Ashok K. Tiwary
  • Narendra K. Jain
  • Subheet Jain
Article

DOI: 10.1208/pt070101

Cite this article as:
Kuksal, A., Tiwary, A.K., Jain, N.K. et al. AAPS PharmSciTech (2006) 7: E1. doi:10.1208/pt070101

Abstract

The aim of the present study was to prepare and characterize extended-release matrix tablets of zidovudine using hydrophilic Eudragit RLPO and RSPO alone or their combination with hydrophobic ethyl cellulose. Release kinetics was evaluated by using United States Pharmacopeia (USP)-22 type I dissolution apparatus. Scanning electron microscopy was used to visualize the effect of dissolution medium on matrix tablet surface. Furthermore, the in vitro and in vivo newly formulated sustained-release zidovudine tablets were compared with conventional marketed tablet (Zidovir, Cipla Ltd, Mumbai, India). The in-vitro drug release study revealed that either Eudragit preparation was able to sustain the drug release only for 6 hours (94.3%±4.5% release). Combining Eudragit with ethyl cellulose sustained the drug release for 12 hours (88.1%±4.1% release). Fitting the in vitro drug release data to Korsmeyer equation indicated that diffusion along with erosion could be the mechanism of drug release. In vivo investigation in rabbits showed sustained-release pharmacokinetic profile of zidovudine from the matrix tablets formulated using combination of Eudragits and ethylcellulose. In conclusion, the results suggest that the developed sustained-release tablets of zidovudine could perform therapeutically better than conventional dosage forms, leading to improve efficacy and better patient compliance.

Keywords

anti-HIV drugZidovudinematrix tabletssustained releasemechanismscanning electron microscopy

Copyright information

© American Association of Pharmaceutical Scientists 2006

Authors and Affiliations

  • Atul Kuksal
    • 1
  • Ashok K. Tiwary
    • 1
  • Narendra K. Jain
    • 2
  • Subheet Jain
    • 1
  1. 1.Department of Pharmaceutical Sciences and Drug ResearchPunjabi UniversityPatialaIndia
  2. 2.Department of Pharmaceutical SciencesDr Hari Singh Gour UniversitySagarIndia