AAPS PharmSciTech

, Volume 10, Issue 2, pp 482–487 | Cite as

SMEDDS of Glyburide: Formulation, In Vitro Evaluation, and Stability Studies

  • Yogeshwar G. Bachhav
  • Vandana B. Patravale
Research Article


The objective of the present investigation was to develop and evaluate self-microemulsifying drug delivery system (SMEDDS) for improving the delivery of a BCS class II antidiabetic agent, glyburide (GLY). The solubility of GLY in oils, cosurfactants, and surfactants was evaluated to identify the components of the microemulsion. The ternary diagram was plotted to identify the area of microemulsion existence. The in vitro dissolution profile of GLY SMEDDS was evaluated in comparison to the marketed GLY tablet and pure drug in pH 1.2 and pH 7.4 buffers. The chemical stability of GLY in SMEDDS was determined as per the International Conference on Harmonisation guidelines. The area of microemulsion existence increased with the increase in the cosurfactant (Transcutol P) concentration. The GLY microemulsion exhibited globule size of 133.5 nm and polydispersity index of 0.94. The stability studies indicated that GLY undergoes significant degradation in the developed SMEDDS. This observation was totally unexpected and has been noticed for the first time. Further investigations indicated that the rate of GLY degradation was highest in Transcutol P.

Key words

degradation glyburide SMEDDS stability studies Transcutol P 



YGB thanks the University Grants Commission, New Delhi, India for the financial support. The authors would like to thank Cipla Pharmaceuticals, Colorcon Asia Pvt. Ltd., Indchem International, BASF India, and Signet Chemicals for the gift samples of the drug and the excipients. The authors would also like to acknowledge Mr. Abhijit Date for his help in the preparation of the manuscript and also for the technical discussion.


  1. 1.
    Groop L, Wahlin-Boll E, Totterman KJ, Melander A, Tolppanen EM, Fyhrqvist F. Pharmacokinetics and metabolic effects of glibenclamide and glipizide in type 2 diabetes. Eur J Clin Pharmacol 1985;28:697–704.PubMedCrossRefGoogle Scholar
  2. 2.
    Wei H, Lobenberg RL. Biorelevant dissolution media as a predictive tool for glyburide a class II drug. Eur J Pharm Sci 2006;19:45–62.CrossRefGoogle Scholar
  3. 3.
    Chalk JB, Patterson M, Smith MT, Eadie MJ. Correlations between in vitro dissolution, in vivo bioavailability and hypoglycaemic effect of oral glibenclamide. Eur J Clin Pharmacol 1986;31:177–82.PubMedCrossRefGoogle Scholar
  4. 4.
    Blume H, Ali SL, Siewert M. Pharmaceutical quality of glibenclamide products: a multinational postmarket comparative study. Drug Dev Ind Pharm 1993;19:2713–41.CrossRefGoogle Scholar
  5. 5.
    Cordes D, Mueller BW. Deactivation of amorphous glibenclamide during dissolution. Eur J Pharm Sci 1996;4:S187.CrossRefGoogle Scholar
  6. 6.
    Varma MM, Jayaswal SB, Singh J. In vitro and in vivo evaluation of fast release solid dispersions of glibenclamide. Indian Drugs 1992;29:608–11.Google Scholar
  7. 7.
    Betageri GV, Makaria KR. Enhancement of dissolution of glyburide by solid dispersion and lyophilization techniques. Int J Pharm 1995;126:155–60.CrossRefGoogle Scholar
  8. 8.
    Tashtoush BM, Al-Qashi ZS, Najib NM. In vitro and in vivo evaluation of glibenclamide in solid dispersion systems. Drug Dev Ind Pharm 2004;30:601–7.PubMedCrossRefGoogle Scholar
  9. 9.
    Sanghavi NM, Venkatesh H, Tandel V. Solubilizaiton of glibenclamide with β-cyclodextrin and its derivative. Drug Dev Ind Pharm 1994;20:1275–83.CrossRefGoogle Scholar
  10. 10.
    Zerrouk N, Corti G, Ancillotti S, Maestrelli F, Cirri M, Mura P. Influence of cyclodextrins and chitosan, separately or in combination, on glyburide solubility and permeability. Eur J Pharm Biopharm 2006;62:241–6.PubMedCrossRefGoogle Scholar
  11. 11.
    Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev 2000;45:89–121.PubMedCrossRefGoogle Scholar
  12. 12.
    Date AA, Patravale VB. Microemulsions: applications in transdermal and dermal delivery. Crit Rev Ther Drug Carrier Syst 2007;24:547–96.PubMedGoogle Scholar
  13. 13.
    Yang SC, Gursoy RN, Lambert G, Benita S. Enhanced oral absorption of paclitaxel in a novel self-microemulsifying drug delivery system with or without concomitant use of P-glycoprotein inhibitors. Pharm Res 2004;21:261–70.PubMedCrossRefGoogle Scholar
  14. 14.
    Gursoy RN, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother 2004;58:173–82.PubMedCrossRefGoogle Scholar
  15. 15.
    Li P, Ghosh A, Wagner RF, Krill S, Joshi YM, Serajuddin ATM. Effect of combined use of nonionic surfactant on formation of oil-in-water microemulsions. Int J Pharm 2005;288:27–34.PubMedCrossRefGoogle Scholar
  16. 16.
    Piclin PS, Homar M, Valant AZ, Perlin MG. Sodium ascorbyl phosphate in topical microemulsions. Int J Pharm 2003;256(1–2):65–73.CrossRefGoogle Scholar
  17. 17.
    Kongan A, Garti N. Microemulsions as transdermal drug delivery vehicles. Adv Colloid Interface Sci 2006;123–126:369–85.CrossRefGoogle Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2009

Authors and Affiliations

  1. 1.Department of Pharmaceutical Sciences and TechnologyInstitute of Chemical TechnologyMatungaIndia

Personalised recommendations