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In Vitro Dissolution of Felodipine from Extended-Release Pellets

펠로디핀 방출연장형 펠렛의 용출 특성 평가

  • Published : 2007.06.21

Abstract

This study aimed to evaluate and develop $Eudragit^{(R)}$-coated pellets based on the dissolution using the paddle method. As coating materials, two types of $Eudragit^{(R)}$ were applied to obtain either sustained release form or fast released form. The dissolution test was carried out in phosphate buffer solution (pH 6.5) at $37^{\circ}C$, 100 rpm. In order to develop a sustained release preparation containing felodipine, a comparative dissolution study was done using commercial product as a control. The dissolution at 30 min of felodipine from $Eudragit^{(R)}$ RS or RL-coated pellets were 0.96% and 99.65, respectively. The weight ratio of $Eudragit^{(R)}$ RL pellets to RS pellets altered the dissolution rate, but did not optimize the dissolution rate. However, the sustained dissolution of felodipine from pellets was optimized by varying the coating ratios of $Eudragit^{(R)}$ RS. It is suggested that the coating ratio of pellets is the main factor which controls dissolution rate. Taken together, $Eudragit^{(R)}$ RS 30D-coated pellets showed the most comparable dissolution rate pattern to commercial product, $Splendil^{(R)}$. This sustained release pellets for oral delivery system of felodipine was simply manufactured, and drug release behavior was highly reproducible.

Keywords

References

  1. E. Saltiel, A. G. Ellrodt, J. P. Monk and M. S. Langley, Felodipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension, Drugs 36, 387-428 (1988) https://doi.org/10.2165/00003495-198836040-00002
  2. P. H. Dunselman and B. Edgar, Felodipine clinical pharmacokinetics, Clin. Pharmacokinet., 21, 418-430 (1991) https://doi.org/10.2165/00003088-199121060-00003
  3. E. Matianne, L. Jan-Erik and S. Mats, New pharmaceutical formulation, EUPO-Patent, 01113786 (2001)
  4. C. K. Kim and J. S. Park, Solubility enhances for oral drug delivery: can chemical structure manipulation be avoided? Am. J. Drug Del., 2, 113-130 (2004) https://doi.org/10.2165/00137696-200402020-00004
  5. I. K. Chun and J. H. Park, Preparation and controlled release of microcapsules containing ketoprofen-${\beta}$-cyclodextrin solid dispersion, J. Kor. Pharm. Sci., 22, 33-40 (1992)
  6. J. Mielcarek, Studies on inclusion complex of felodipine with ${\beta}$-cyclodextrin, J. Inc. Phenom. Mol. Rec. Chem., 30, 243-252 (1998) https://doi.org/10.1023/A:1007960725895
  7. E. Karavas, E. Georgarakis, D. Bikiaris, T. Thomas, V. Katsos and A. Xenakis, Hydrophilic matrices as carriers in felodipine solid dispersion systems, Progr. Colliod. Polm. Sci., 118, 149-152 (2001) https://doi.org/10.1007/3-540-45725-9_34
  8. Y. S. Gil, S. C. Hong, C. H. Yu, H. J. Shin and J. S. Kim, Improvement of dissolution rate of felodipine suing solid dispersion and its sustained release oral dosage form, J. Kor. Pharm. Sci., 32, 185-190 (2002)
  9. J. K. Lee, S. W. Yang, B. S. Lee, H. R. Jeon, J. Lee, Y. W. Choi, Formulation of sustained-release tablets of felodipine using hydrophilic polymers and non-ionic surfactants, J. Kor. Pharm. Sci., 36, 271-276 (2006)
  10. R. Bodmeier and O. Paeratakul, Multiparticulate Oral Drug Delivery, Marcel Dekker, New York, U.S.A., pp. 143-156 (1994)
  11. A. Dashevsky, K. Wagner and R. Bodmeier, pH-independent release of a basic drug from pellets coated with the extended release polymer dispersion Kollicoat SR 30 D and the enteric polymer dispersion Kollicoat MAE 30 DP, Eur. J. Pharm. Biopharm., 58, 45-49 (2004) https://doi.org/10.1016/j.ejpb.2004.03.013
  12. N. Sinchaipanid, V. Junyaprasert and A. Mitrevej, Application of hot-melt coating for controlled release of propranolol hydrochloride pellets, Powder Technol., 141, 203-209 (2004) https://doi.org/10.1016/j.powtec.2004.02.008
  13. A. Dashevsky, K. Wagner, K. Kolter and R. Bodmeier, Physicochemical and release properties of pellets coated with Kollicoat SR 30 D, a new aqueous polyvinyl acetate dispersion for extended release, Int. J. Pharm., 290, 15-23 (2005) https://doi.org/10.1016/j.ijpharm.2004.10.024
  14. J. Hamdani, A.J. Moes, K. Amighi, Development and in vitro evaluation of a novel floating multiple unit dosage form obtained by melt pelletization, Int. J. Pharm., 322, 96-103 (2006) https://doi.org/10.1016/j.ijpharm.2006.05.052
  15. J. H. Yang, S. B. La, Y. I. Kim and N. S. Kim, Bioavailability of microspheres containing felodipine, Yakhak Hoeji, 44, 440-447 (2000)
  16. R. J. Harwood, Polymethacrylates, Handbook of Pharmaceutical Excipients 3rd edition, American Pharmaceutical Association, The Pharmaceutical Press, pp. 401-406 (2000)
  17. Rohm Pharma, Information Sheet, 'Eudragit$^{\circledR}$ RL' (1998)
  18. Rohm Pharma, Information Sheet, 'Eudragit$^{\circledR}$ RS' (1998)
  19. A. Hoegholm, N. Wiinberg, E. Rasmussen and P. E. Nielsen, Comparative effects of amlodipine and felodipine ER on office and ambulatory blood pressure in patients with mild to moderate hypertension. Danish Multicentre Group, J. Hum. Hypertens. 9, S25-28 (1995)