Archives of Pharmacal Research

The Pharmaceutical Society of Korea (대한약학회)
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Preparation of Prolonged Release Clarithromycin Microparticles for Oral Use and Their In Vitro Evaluation

  • Genc, Lutfi (Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Technology,Plant, Drug & Scientific Researches Center of Anadolu University (AUBIBAM)) ;
  • Demirel, Muzeyyen (Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Technology) ;
  • Yazan, Yasemin (Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Technology)
  • Published : 2006.10.01
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Abstract

Prolonged release micro particles of clarithromycin (CL) were prepared using Eudragit RL 100 and RS 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 and in 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.

Keywords

References

  1. 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) https://doi.org/10.1016/S0149-2918(01)80062-X
  2. Barradell, L. B., Plosker, G. L., and Mctavish, D., Clarithromycin: A review of its pharmacological properties and therapeutic use in Mycobacterium avium-intracellulare complex infection in patients with Acquired Immune Deficiency Syndrome. Drugs, 46(2), 289-312 (1993) https://doi.org/10.2165/00003495-199346020-00007
  3. 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) https://doi.org/10.1016/j.ijpharm.2004.07.052
  4. Beuving, G., Validation of Analytical Methods. Validation Seminar, Istanbul, 31 May- 01 June 2001
  5. 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) https://doi.org/10.1016/0378-4347(91)80446-J
  6. 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) https://doi.org/10.1128/AAC.39.2.334
  7. 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 of Helicobacter pylori infection. J. Antimicrob. Chemother., 39, 5-12 (1997) https://doi.org/10.1093/jac/39.1.5
  8. 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) https://doi.org/10.1016/S0149-2918(01)80060-6
  9. 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) https://doi.org/10.1016/j.jconrel.2005.02.012
  10. 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 $\varepsilon$-Caprolactone: Comparison with Conventional PLGA Microspheres. Int. J. Pharm., 295, 67-76 (2005) https://doi.org/10.1016/j.ijpharm.2005.01.025
  11. Louis, St., Drug Facts and Comparisons. A Wolters Kluwer Company, USA, p.2189 (1997)
  12. 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 PharmSci. Tech., 3(3), 1-11 (2002)
  13. 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) https://doi.org/10.1016/0731-7085(91)80156-4
  14. Mu, l., 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) https://doi.org/10.1016/j.jconrel.2004.12.023
  15. 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) https://doi.org/10.1248/cpb.40.725
  16. 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) https://doi.org/10.1016/S0032-5910(02)00239-5
  17. 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)
  18. 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-Lipoxygenase inhibitor. Int. J. Pharm., 176, 31-38 (1998) https://doi.org/10.1016/S0378-5173(98)00296-8
  19. Reiley, C. M. and Fell, F., Development and validation of analytical methods. Prog. Pharm. Biomed. Anal., 3, 20-22 (1996)
  20. 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) https://doi.org/10.1023/A:1015844705331
  21. U. S. Pharmacopeia National Formulary, USP 26-NF 21, 3th Ed.,Mack Printing Company: Easton, U.S.A., pp. 2439-2445 (2003)
  22. 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) https://doi.org/10.1016/S0928-0987(98)00040-2