Preparation and investigation of mixtures containing lidocaine base and β-cyclodextrin

  • Anita Tatai
  • Zoltán Aigner
  • István Erős
  • Mihály Kata
Original Article


The effects of β-cyclodextrin (β-CD) on the solubility properties of lidocaine base were studied. Products were prepared by physical mixing, kneading, spray-drying and precipitation methods in drug : β-CD ratios of 3:1, 2:1, 1:1, 1:2 and 1:3. Some auxiliary materials (hydroxy acids, etc.) were also used. The solubility and the rate of dissolution both in distilled water and in artificial gastric juice, the in vitro diffusion, the thermoanalytical properties (TG, DTG, DSC and DTA) and the surface tension were determined, and the measured results were compared with the corresponding data for lidocaine hydrochloride.


β-Cyclodextrin Inclusion complexation In vitro diffusion Lidocaine base Rate of dissolution Thermoanalytical investigations 


  1. 1.
    The Merck Index, 11th edn., p. 863. Merck and Co., Inc., Rahway, N.J., USA (1989)Google Scholar
  2. 2.
    European Pharmacopoeia, 5th edn., vol. 2, pp. 1913–1914 and 2264–2265. Council of Europe, Strasbourg, France (2004)Google Scholar
  3. 3.
    Szejtli, J.: Cyclodextrins and their Inclusion Complexes, p. 99. Akadémiai Kiadó, Budapest, Hungary (1982)Google Scholar
  4. 4.
    Schubert, A. et al.: In: Szejtli, J. (ed.) Proceedings of the 1st International Symposium on Cyclodextrins, pp. 195–203. Budapest, Hungary, September 30–October 2 (1981)Google Scholar
  5. 5.
    Ferenczy, T. et al.: In: Szejtli, J. (ed.) Proceedings of the 1st International Symposium on Cyclodextrins, pp. 443–449. Budapest, Hungary, September 30–October 2 (1981)Google Scholar
  6. 6.
    Szemán, J. et al.: In: Huber, O., Szejtli, J. (eds.) Proceedings of the 4th International Symposium on Cyclodextrins, pp. 393–398. Munich, FRG, April 20–22 (1988)Google Scholar
  7. 7.
    Fredro-Kumbaradzi, E. et al.: Sci. Pharm. 69(Suppl 1), S222–S223 (2001)Google Scholar
  8. 8.
    Másson, M., Sigfússon, S.D., Loftsson, T.: Program and Abstracts of 11th International Cyclodextrin Symposium, p. 40. Reykjavik, Iceland (2002)Google Scholar
  9. 9.
    Morales, C.M. et al.: Proceedings of the 13th International Cyclodextrin Symposium. Torino, Italy, 3-P21 (2006)Google Scholar
  10. 10.
    Dollo, X. et al.: Int. J. Pharm. 131, 219–228 (1996); 136, 165–174 (1996)Google Scholar
  11. 11.
    J. Incl. Phenom. Macrocyclic Chem. 1–50 (1985–2005)Google Scholar
  12. 12.
    Pharmacopoeia Hungarica, 8th edn., vol. 2, pp. 2176–2177. Medicina, Budapest, Hungary (2004)Google Scholar
  13. 13.
    Frömming, K.-H., Szejtli, J.: Cyclodextrins in Pharmacy, pp. 38, 72, 88–94. Kluwer Academic Publishers, Dodrecht (1994)Google Scholar
  14. 14.
    Szente, L., Szejtli, J. et al.: Solution for Insolubility Problems of Base-Type Drugs: Multicomponent Cyclodextrin Complexation. In: Proceedings 1st World Meeting APGI-APV, Budapest, 9/11 May (1995)Google Scholar
  15. 15.
    Higuchi, T., Connors, K.A.: Phase solubility techniques. Adv. Anal. Chem. Instr. 4, 117–212 (1965)Google Scholar
  16. 16.
    Banker, G.S., Rhodes, C.T.: Modern Pharmaceutics, Drugs and the Pharmaceutical Sciences, vol. 40. Marcel and Dekker, Inc., New York and Basel (1990)Google Scholar
  17. 17.
    Becher, P.: Emulsions. Technical Kiadó, Budapest, Hungary (1965)Google Scholar
  18. 18.
    Parrott, E.L.: Pharmaceutical Technology. Burgess Publishing Co., Minneapolis, USA, p. 122 (1971)Google Scholar
  19. 19.
    Stricker, H.: Pharm. Indust. 31, 794 (1969); 33, 157 (1971); 35, 13 (1973)Google Scholar
  20. 20.
    Sartorius Resorptionsmodell SM 16750. Booklet, FRG (1976)Google Scholar
  21. 21.
    Kata, M., Ambrus, R., Aigner, Z.: Preparation and investigation of inclusion complexes containing nifluminic acid and cyclodextrins. J. Incl. Phenom. Macro. Chemistry 44, 123–126 (2002)CrossRefGoogle Scholar
  22. 22.
    Hassan, H.B., Kata, M., Erős I., Aigner, Z.: Preparation and investigation of inclusion complexes containing gemfibrozil and DIMEB. J. Incl. Phenom. Macro. Chem. 50, 219–225 (2004)CrossRefGoogle Scholar
  23. 23.
    Aigner, Z., Kata, M.: STP Pharma Sci. 9, 279–282 (1999)Google Scholar

Copyright information

© Springer Science+Business Media, Inc. 2007

Authors and Affiliations

  • Anita Tatai
    • 1
  • Zoltán Aigner
    • 1
  • István Erős
    • 1
  • Mihály Kata
    • 1
  1. 1.Department of Pharmaceutical TechnologyUniversity of SzegedSzegedHungary

Personalised recommendations