Skip to main content
SpringerLink
Log in

Pharmacokinetic study of an oral piroxicam formulation containing different molar ratios of β-cyclodextrins

  • Original Article
  • Published:
Journal of Inclusion Phenomena and Macrocyclic Chemistry Aims and scope Submit manuscript

Abstract

The objective of this work was to compare the pharmacokinetic parameters of piroxicam-β-cyclodextrin (PIX-CD) complex at molar ratio of 1:1, 1:2.5, 1:3, and 1:4 after an oral administration in rabbits and either to prove or not the Haborn et al. theory which states that the peak plasma concentration (Cmax) of piroxicam increases with an increase of β-cyclodextrin concentration. The results showed an increase in Cmax from 11 ± 1.7, 13.3 ± 6.17 to 17 ± 2.03 μg/ml for piroxicam alone, 1:1 (PIX-CD) and 1:2.5 (PIX-CD), respectively, and declined starting at molar ratio of 1:3 (PIX-CD). However, more rapid drug absorption was observed where the time of peak plasma concentration (Tmax) became shorter and changed from 2 h (Piroxicam alone) to 0.5 h in the presence of cyclodextrin.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3

Similar content being viewed by others

References

  1. Loftsson, Thorsteinn, Jarho, Pekka, Masson, Mar, Järvinen, Tomi: Cyclodextrins in drug delivery. Expert opinion. Drug Deliv. 2, 335–351 (2005)

    CAS  Google Scholar 

  2. Saharan, Vikas A., Kukkar, Vipin, Kataria, Mahesh, Gera, Manoj, Choudhury, Pratim k: Dissolution Enhancement of drugs. Part I: technologies and effect of carriers. Int. J. Health 2(2), 107–124 (2009)

    CAS  Google Scholar 

  3. Bhupendra, G., Prajapati, M., Patel, M.: Conventional and alternative pharmaceutical methods to improve oral bioavailability of lipophilic drugs. Asian J. Pharm. 1(1), 1–8 (2007)

    Google Scholar 

  4. Loftsson, Thorsteinn, Brewster, Marcus E., Màsson, Màr: Role of cyclodextrins in improving oral drug delivery. Am. J. Drug Deliv. 2(4), 261–275 (2004)

    Article  CAS  Google Scholar 

  5. Hardman, J.G., Limbird, L.E.: Goodman and Gilman’s: The Pharmacological Basis of Therapeutics, 9th edn, p. 713. Mc Graw Hill, New York (2001)

    Google Scholar 

  6. Moffat, A.C., Osselton, M.D., Widdop, B.Clarckes: Analysis of Drugs and Poisons, vol. 2, 3rd edn, p. 1463. Pharmaceutical Press, London (2004)

    Google Scholar 

  7. European Patent 07/16 (18/04/2007): CHIESI FARMACEUTICI S.p.a. Procédé de préparation de composés d’inclusion de piroxicam avec de la béta-cyclodextrine

  8. Kummura, E., Bersani-Amado, C.A.: Pharmacokinetic profile of piroxicam β-CD in rat plasma and lymph. Gen. Pharmac. 28(5), 695–698 (1997)

    Article  Google Scholar 

  9. Palma-Aguirre, Jose Antonio, Lopez-Gamboa, Mireya, Carino, Lizbeth, Burke-Fraga, Victoria, Gonzalez-de la Parra, Mario: Relative bioavailability of two oral formulations of piroxicam 20 mg: a single-dose, Randomized-sequence, open-label, two-period crossover comparison in healthy Mexican adult volunteers. Clin. Ther. 32(2), 357–364 (2010)

    Article  CAS  Google Scholar 

  10. Wiseman, E.H., Hobbs, D.C.: Review of pharmacokinetic studies of piroxicam. J. Am. Med. 72, 9–17 (1982)

    Article  CAS  Google Scholar 

  11. Brogden, R.N., Heel, R.C., Speight, T.M., et al.: Piroxicam: a review of its pharmacological properties and therapeutic efficacy. Drug 22, 165–187 (1981)

    Article  CAS  Google Scholar 

  12. Hobbs, D.C., Twomey, T.M.: Piroxicam pharmacokinetics in man: aspirin and antacid interaction studies. J. Clin. Pharmacol 19, 270–281 (1979)

    Article  CAS  Google Scholar 

  13. Schiantarelli, P., Cadel, S.: Piroxicam pharmacologic activity and gastrointestinal damage by oral and rectal route. Arzneim. Forsch 31, 87–92 (1981)

    CAS  Google Scholar 

  14. Dalmora, M.E., Dalmora, S.L., Oliveira, A.G.: Inclusion complex of piroxicam with β-cyclodextrin and incorporation in cationic micro emulsion. In vitro drug release and in vivo topical anti-inflammatory effect. Int. J. Pharm. 22, 45–55 (2001)

    Article  Google Scholar 

  15. Damiani, P.C., Bearzotti, M., Cabezon, M., Olivieri, A.C.: J. Pharm. Biomed. Anal. 17, 233–236 (1998)

    Article  CAS  Google Scholar 

  16. Carrier, Rebecca L.: The utility of cyclodextrins for enhancing oral bioavailability. J. Controlled Release 123, 78–79 (2007)

    Article  CAS  Google Scholar 

  17. Brewster, Marcus E.: Cyclodextrins as pharmaceutical solubilizers. Adv. Drug Deliv. Rev. 59, 645–666 (2007)

    Article  CAS  Google Scholar 

  18. Rajeswari, Challa.: Cyclodextrins in drug delivery: an updated review AAPS Pharm Sci Tech, 6 (2) article 43 (2005)

  19. Shimpi, Shyam, Chauhan, Bhaskar, Shimpi, Prajakta: Cyclodextrins: application in different routes of drug administration. Acta Pharm. 55, 139–156 (2005)

    CAS  Google Scholar 

  20. Loftsson, Thorsteinn, Masson, Mar: Cyclodextrins in topical drug formulations: theory and practice. Int. J. Pharm. 225, 15–30 (2001)

    Article  CAS  Google Scholar 

  21. Oda, Masako, Saitoh, Hiroshi, Kobayashi, Michiya, Aungst, Bruce J.: β-CD as a suitable solubilizing agent for in situ absorption study of poorly water soluble drugs. Int. J. Pharm. 280, 95–102 (2004)

    Article  CAS  Google Scholar 

  22. Osadebe, P.O.: Energetic of the interaction between piroxicam and β-CD in inclusion complexes. Sci. Res. Essays 3(3), 86–93 (2008)

    Google Scholar 

  23. Xiliang, Guo., Yu, Yang.: Study on inclusion interaction of piroxicam with β-CD derivatives. Spectrochimica Acta Part A 59 (2003)

  24. Cavallari, Cristina: Improved dissolution behavior steam-granulated piroxicam. Eur. J. Pharm. Biopharm. 54, 65–73 (2002)

    Article  CAS  Google Scholar 

  25. Rozou, Stavroula: The effect of pH dependent molecular conformation and dimerization phenomena of piroxicam on the drug: cyclodextrin complex stoichiometry and its chromatographic behavior. A new specific HPLC method for piroxicam: cyclodextrin formulations. Eur. J. Pharm. Sci. 21, 661–669 (2004)

    Article  CAS  Google Scholar 

  26. Vanhees, Thierry: Determination of the free/included piroxicam ratio in CD complexes: comparison between UV spectrophotometry and differential scanning calorimetry. Eur. J. Pharm. Sci. 15, 347–353 (2002)

    Article  CAS  Google Scholar 

  27. Acerbi, D.: Pharmacokinetic profile of piroxicam β-CD. Drug Invest. 2, 42–49 (1990)

    Article  Google Scholar 

  28. Szejtli, Jozset: Past, present and future of cyclodextrin research. Pure Appl. Chem. 76(10), 1825–1845 (2004)

    Article  CAS  Google Scholar 

  29. Haborn, I., Ricketts, D., Szejtli, J.: Simulation of pharmacokinetic behavior of drug-cyclodextrin complexes. Pharmazie 39, 830–834 (1984)

    Google Scholar 

  30. Palomares-Alonso, Francisca, et al.: Two ternary albendazole-cyclodextrin-polymer systems: dissolution, bioavailability and efficacy agains Taenia crassiceps cysts. Acta Trop. 113, 56–60 (2010)

    Article  CAS  Google Scholar 

  31. Fawaz, F., et al.: Bioavailability of norfloxacin from PEG6000 solid dispersion and cyclodextrin inclusion complexes in rabbits. Int. J. Pharm. 132, 271–275 (1996)

    Article  CAS  Google Scholar 

  32. Kedzierewicz, F., et al.: Bioavailability study of tolbutamide β-CD inclusion compounds, solid dispersions and bulk powder. Int. J. Pharm. 94, 69–74 (1993)

    Article  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Galenic Pharmaceutical Laboratory, UFR Medicine and Pharmacy, Rouen University, 22 Blvd Gambetta, 76183, Rouen, France

    M. Skiba, T. Boukhris, F. Bounoure & M. Lahiani-Skiba

  2. LAGEP, UMR, CNRS 5007, Villeurbanne, France

    M. Skiba, F. Bounoure, H. Fessi & M. Lahiani-Skiba

  3. Pharmaceutical Laboratory, Department of Engineering Processes, Abderrahmane-Mira-University, Route de Targua Ouzemmour, 06000, Bejaia, Algeria

    F. Bouchal & S. Fatmi

  4. Galenic Pharmaceutical Laboratory, Medicine Faculty, Badji Mokhtar University, Annaba, Algeria

    N. Chaffai

Authors
  1. M. Skiba
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. F. Bouchal
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. T. Boukhris
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. F. Bounoure
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. H. Fessi
    View author publications

    You can also search for this author in PubMed Google Scholar

  6. S. Fatmi
    View author publications

    You can also search for this author in PubMed Google Scholar

  7. N. Chaffai
    View author publications

    You can also search for this author in PubMed Google Scholar

  8. M. Lahiani-Skiba
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to M. Skiba.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Skiba, M., Bouchal, F., Boukhris, T. et al. Pharmacokinetic study of an oral piroxicam formulation containing different molar ratios of β-cyclodextrins. J Incl Phenom Macrocycl Chem 75, 311–314 (2013). https://doi.org/10.1007/s10847-012-0166-0

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s10847-012-0166-0

Keywords

Search

Navigation