Formulation and in vitro, in vivo evaluation of extended- release matrix tablet of zidovudine: influence of combination of hydrophilic and hydrophobic matrix formers.
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.
Kuksal
Atul
A
Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab, India- 147002.
Tiwary
Ashok K
AK
Jain
Narendra K
NK
Jain
Subheet
S
D000818:Animals; D019380:Anti-HIV Agents / Q000008:administration & dosage*; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D005260:Female; D006863:Hydrogen-Ion Concentration; D008297:Male; D008855:Microscopy, Electron, Scanning; D011817:Rabbits; D012995:Solubility; D013607:Tablets; D015215:Zidovudine / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics
D019380:Anti-HIV Agents; D003692:Delayed-Action Preparations; D013607:Tablets; D015215:Zidovudine