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

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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.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences and Drug Research, Punjabi University, 147002, Patiala, Punjab, India

    Atul Kuksal, Ashok K. Tiwary & Subheet Jain

  2. Department of Pharmaceutical Sciences, Dr Hari Singh Gour University, 470003, Sagar, M.P., India

    Narendra K. Jain

Authors
  1. Atul Kuksal
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  2. Ashok K. Tiwary
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  3. Narendra K. Jain
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  4. Subheet Jain
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Correspondence to Subheet Jain.

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Published: January 3, 2006

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Kuksal, A., Tiwary, A.K., Jain, N.K. et al. Formulation and in vitro, in vivo evaluation of extended- release matrix tablet of Zidovudine: Influence of combination of hydrophilic and hydrophobic matrix formers. AAPS PharmSciTech 7, 1 (2006). https://doi.org/10.1208/pt070101

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  • DOI: https://doi.org/10.1208/pt070101

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