Skip to main content
Log in

Preparation of prolonged release clarithromycin microparticles for oral use and theirin vitro evaluation

  • Articles
  • Drug Efficacy
  • Published:
Archives of Pharmacal Research Aims and scope Submit manuscript

Abstract

Prolonged release microparticles of clarithromycin (CL) were prepared using EudragitRL 100 andRS 100 by spray-drying and casting-drying techniques. For the characterization of those microparticles, preparation yield, particle size distribution, X-ray diffraction, thermal behavior, active agent content andin vitro dissolution from the microparticles were performed. HPLC was used for the assay of clarithromycin and the assay method was validated. All the formulations obtained showed prolonged release when compared to pure clarithromycin. Microparticles prepared by spray-drying method had a slower release compared to those of casting-drying method. Spray-drying method seems to be a more suitable method to prepare microparticles for prolongation in release.

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

Access this article

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

Instant access to the full article PDF.

Similar content being viewed by others

References

  • Adam, D., Glaser-Caldow, E., Wachter, J., Brueckner, O.-J., Hein, J., Kroemer, B., and Hirsch, J., Comparative efficacy of clarithromycin modified rlelase and immediate relaese formulations in the treatment of lower respiratory tract infection.Clin. Ther., 23(4), 585–595 (2001).

    Article  PubMed  CAS  Google Scholar 

  • Barradell, L. B., Plosker, G. L., and Mctavish, D., Clarithromycin: A review of its pharmacological properties and therapeutic use inMycobacterium avium-intracellulare complex infection in patients with Acquired Immune Deficiency Syndrome.Drugs, 46(2), 289–312 (1993).

    Article  PubMed  CAS  Google Scholar 

  • Bele, M., Dmitrasinovic, D., Planinsek, O., Salobir, M., Srcic, S., Gabescek, M., and Jamnik, J., Silica coating on clarithromycin.Int. J. Pharm., 291, 149–153 (2005).

    Article  PubMed  CAS  Google Scholar 

  • Beuving, G., Validation of Analytical Methods. Validation Seminar, Istanbul, 31 May–01 June 2001.

  • Chu, S.-Y., Sennello, L. T., and Sonders, R. C., Simultaneous determination of clarithromycin and 14-hydroxy-clarithromycin in plasma and urine using HPLC with electronical detection.J. Chromatogr., 571, 199–208 (1991).

    Article  PubMed  CAS  Google Scholar 

  • Conte, J. E., Golden, J. A., Duncan, S., Mckenna, E., and Zurlinden, E., Intra-pulmonar pharmacokinetics of clarithromycin and of erythromycin.Antimicrob. Agents Chemother., 39(2), 334–338 (1995).

    PubMed  CAS  Google Scholar 

  • Erah, P. O., Goddard, A. F., Barrett, D. A., Shaw, P. N., and Spillr, R. C., The stability of amoxycillin, clarithromycin and metronidazole in gastric juice: relevance to the treatment ofHelicobacter pylori infection.J. Antimicrob. Chemother., 39, 5–12 (1997).

    Article  PubMed  CAS  Google Scholar 

  • Guay, D. R. P., Gustavson, L. E., Devcich, K. J., Zhang, J., Cao, G., and Olson, C. A., Pharmacokinetics and tolerability of extended-release clarithromycin.Clin. Ther., 23(4), 566–577 (2001).

    Article  PubMed  CAS  Google Scholar 

  • Kim, S. J., Hahn, S. K., Kim, M. J., Kim, D. H., and Lee, Y. P., Development of a novel sustained release formulation of recombinant human growth hormone using sodium hyaluronate microparticles.J. Control. Release, 104, 323–335 (2005).

    PubMed  CAS  Google Scholar 

  • Li, Y., Zhu, K. J., Zhang, J. X., Jiang, H. L., Liu, J. H., Hao, Y. L., Yasuda, H., Ichimaru, A., and Yamamoto, K., In vitro and in vivo studies of cyclosporin A-Loaded microspheres based on copolymers of lactide and ε-Caprolactone: Comparison with Conventional PLGA Microspheres.Int. J. Pharm., 295, 67–76 (2005).

    Article  PubMed  CAS  Google Scholar 

  • Louis, St., Drug Facts and Comparisons. A Wolters Kluwer Company, USA, p. 2189 (1997).

    Google Scholar 

  • Martin, T. M., Bandi, N., Shulz, R., Roberts, C. B., and Kompella, U. B., Preparation of budesonide and budesonide-PLA microparticles using supercritical fluid precipitation technology.AAPS Pharm Sci. Tech., 3(3), 1–11 (2002).

    Article  Google Scholar 

  • Morgan, D. K., Brown, D. M., Rotsch, T. D., and Plasz, A. C., A reversed-phase HPLC method for the determination and identification of clarithromycin as the drug substance and in various dosage forms.J. Pharm. Biomed. Anal., 9(3), 261–269 (1991).

    Article  PubMed  CAS  Google Scholar 

  • Mu, I., Teo, M.-M., Ning, H.-Z., and Feng, S.-S., Novel powder formulations for controlled delivery of poorly soluble anticancer drug: Application and investigation of TPGS and PEC in spray-dried particulate system.J. Control. Release, 103, 565–575 (2005).

    Article  PubMed  CAS  Google Scholar 

  • Nakagawa, Y., Itai, S., Yoshida, T., and Nagai, T., Physicochemical properties and stability in the acidic solution of a new macrolide antibiotic, clarithromycin, in comparison with erythromycin.Chem. Pharm. Bull., 40(3), 725–728 (1992).

    PubMed  CAS  Google Scholar 

  • Oneda, F. and Ré, M. I., The effect of formulation variables on the dissolution and physical properties of spray-dried microspheres containing organic salts.Powder Technol., 130, 377–384 (2003).

    Article  CAS  Google Scholar 

  • Pav, B., Misztal, G., Hopkala, H., and Drozd, J., Development and validation of a HPLC method for the determination of cetrizine in pharmaceutical dosage forms.Pharmazie, 57, 313–315 (2002).

    Google Scholar 

  • Perng, C. Y., Kearney, A. S., Patel, K., Palepu, N. R., and Zuber, G., Investigation of formulation approaches to improve the dissolution of SB-210661 a poorly water soluble 5-Lipoxy-genase inhibitor.Int. J. Pharm., 176, 31–38 (1998).

    Article  CAS  Google Scholar 

  • Reiley, C. M. and Fell, F., Development and validation of analytical methods.Prog. Pharm. Biomed. Anal., 3, 20–22 (1996).

    Google Scholar 

  • Rotsch, T. D., Spanton, M., Cugier, P., and Plasz, A. C., Determination of clarithromycin as a conta-minant on surfaces by HPLC using electronical detection.Pharm. Res., 8(8), 989–991 (1991).

    Article  PubMed  CAS  Google Scholar 

  • U. S. Pharmacopeia National Formulary, USP 26-NF 21, 3th Ed., Mack Printing Company Easton, U.S.A., pp. 2439–2445 (2003).

    Google Scholar 

  • Yonemochi, E., Kitahara, S., Maeda, S., Yamamura, S., Oguchi, T., and Yamoto, K., Physicochemical properties of amorphous clarithromycin obtained by grinding and spray drying.Eur. J. Pharm. Sci., 7, 331–338 (1999).

    Article  PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Genç, L., Demirel, M. & Yazan, Y. Preparation of prolonged release clarithromycin microparticles for oral use and theirin vitro evaluation. Arch Pharm Res 29, 921–927 (2006). https://doi.org/10.1007/BF02973915

Download citation

  • Received:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF02973915

Key words

Navigation