Archives of Pharmacal Research

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Evaluation of In-Vitro Dissolution and In-Vivo Absorption for Two Different Film-Coated Pellets of Clarithromycin

  • Zhang Xiang-rong (Department of Pharmacy, Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University) ;
  • Chen Xiao-yan (Department of Pharmacy, Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University) ;
  • Hu Lian-Dong (Department of Pharmaceutics, Shenyang Pharmaceutical University) ;
  • Tang Xing (Department of Pharmaceutics, Shenyang Pharmaceutical University) ;
  • Li San-Ming (Department of Pharmaceutics, Shenyang Pharmaceutical University) ;
  • Zhong Da-fang (Department of Pharmacy, Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University)
  • Published : 2005.08.01
Download PDF
⟨ Previous Next ⟩

Abstract

The aim of this study was to compare two formulations of film-coated pellets containing c1arithromycin after single oral dose study in healthy male volunteers. Two formulations with different coating polymers were prepared: formulation-1 (F-1) was prepared by incorporating three kinds of pH-dependent gradient-release coated pellets into capsules and formulation-2 (F-2) was prepared by coated with an insoluble semiosmotic film. Release profiles of filmcoated pellets were evaluated using paddle method under different conditions. Pharmacokinetic profiles of these formulations were obtained in three healthy male volunteers and compared to commercially available immediate release (IR) tablets. The relative bioavailability based on the $AUC_{0-24h}$ was found to be $96.2\%\;and\;58.7\%$ for F-1 and F-2 compared with IR, and the $T_{max}$ was delayed.

Keywords

References

  1. Amidon, G. L., Lennemas, H., Shah, V. P., and Crison, J. R., A theoretical basis for a biopharmaceutical drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res., 12, 413-420 (1995) https://doi.org/10.1023/A:1016212804288
  2. Amighi, K., Timmermans, J., Puigadevall, J., Baltes, E., and Moes, A. J., Peroral sustained-release film-coated pellets as a means to overcome physicochemical and biological drugrelated problems. I. In vitro development and eveluation. Drug Dev. Ind. Pharm., 24, 509-515 (1998) https://doi.org/10.3109/03639049809085651
  3. Arimori, K., Miyamoto, S., Fukuda, K., Nakamura, C., and Nakano, M., Characteristic difference in gastrointestinal excretion of clarithromycin and roxithromycin. Biopharm. Drug Dispos., 19, 433-438 (1998) https://doi.org/10.1002/(SICI)1099-081X(199810)19:7<433::AID-BDD122>3.0.CO;2-Z
  4. Bodmeier, R., Tableting of coated pellets. Eur. J. Pharm. Biopharm., 43, 1-8 (1997) https://doi.org/10.1016/S0939-6411(96)00028-8
  5. Chu, S. Y., Deaton, R., and Cavanaugh, J., Absolute bioavailability of clarithromycin after oral administration in humans. Antimicrob. Agents Chemother., 36, 1147-1150 (1992a) https://doi.org/10.1128/AAC.36.5.1147
  6. Chu, S. Y., Granneman, G. R., Pichotta, P. J., Decout, J. P., Girault, J., and Fourtilan, J. B., Effect of moderate or severe hepatic impairment on clarithromycin pharmacokinetics. J. Clin. Pharmacol., 33, 480-485 (1993) https://doi.org/10.1002/j.1552-4604.1993.tb04692.x
  7. Chu, S. Y., Park, Y., Locke, C., Wilson, D. S., and Cavanaugh, J. C., Drug-food interaction potential of clarithromycin, a new macrolide antimicrobial. J. Clin. Pharmacol., 32, 32-36 (1992b) https://doi.org/10.1002/j.1552-4604.1992.tb03784.x
  8. Dressman, J. B., Berardi, R. R., Dermentzoglou, L. C., Russell T. L., Schmaltz, S. P., Barnett, J. L., and Jarvenpaa, K. M., Upper gastrointestinal (GI) pH in young, healthy men and women. Pharm. Res., 7, 756-761 (1990) https://doi.org/10.1023/A:1015827908309
  9. Erah, P. O., Barrett, D. A., and Shaw, P. N. Ion-pair highperformance liquid chromatographic assay method for the assessment of clarithromycin stability in aqueous solution and in gastric juice. J. Chromatogr. B., 682, 73-78 (1996) https://doi.org/10.1016/0378-4347(96)00064-3
  10. Grubel, P. and Cave, D. R., Factors affecting solubility and penetration of clarithromycin through gastric mucus. Alim. Pharmacol. Ther., 12, 569-576 (1998) https://doi.org/10.1046/j.1365-2036.1998.00329.x
  11. Guay, D. R., Gustavson, L. E., Devcich, K. J., Zhang, J., Cao, G., and Olson, C. A., Pharmacokinetics and tolerabilty of extended-release clarithromycin. Clin. Ther., 23, 566-577 (2001) https://doi.org/10.1016/S0149-2918(01)80060-6
  12. Nakagawa, Y., Itai, S., Yoshida, T., and Nagai, T., Physicochemical properties and stability in the acidic solution of a new macrolide antibiotic, clarithromycin, in comparision with erythromycin. Chem. Pharm. Bull., 40, 725-728 (1992) https://doi.org/10.1248/cpb.40.725
  13. Rodvold, K. A., Clinical pharmacokinetics of clatrithromycin. Clin. Pharmacokinet., 37, 385-398 (1999) https://doi.org/10.2165/00003088-199937050-00003
  14. Sathe, P. M., Tsong Y., and Shah V. P., In-vitro dissolution profile comparision: statistics and analysis, model dependent approch. Pharm. Res., 13, 1799-1803 (1996) https://doi.org/10.1023/A:1016020822093
  15. Sousa, J. J., Sousa, A., Moura, M. J., Podczeck, F., and Newton, J. M., The influence of core materials and film coating on the drug release from coated pellets. Int. J. Pharm., 233, 111-122 (2002) https://doi.org/10.1016/S0378-5173(01)00921-8