Journal of Pharmaceutical Investigation

  • 제40권5호
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  • Pages.313-319
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  • 2010
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  • 2093-5552(pISSN)
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  • 2093-6214(eISSN)
한국약제학회 (The Korean Society of Pharmaceutical Sciences and Technology)
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Development and Optimization of a Novel Sustained-release Tablet Formulation for Bupropion Hydrochloride using Box-Behnken Design

  • Cha, Kwang-Ho (Center for Nanotechnology-based New Drug Dosage Form, College of Pharmacy, Chungnam National University) ;
  • Lee, Na-Young (Center for Nanotechnology-based New Drug Dosage Form, College of Pharmacy, Chungnam National University) ;
  • Kim, Min-Soo (Center for Nanotechnology-based New Drug Dosage Form, College of Pharmacy, Chungnam National University) ;
  • Kim, Jeong-Soo (Center for Nanotechnology-based New Drug Dosage Form, College of Pharmacy, Chungnam National University) ;
  • Park, Hee-Jun (Center for Nanotechnology-based New Drug Dosage Form, College of Pharmacy, Chungnam National University) ;
  • Park, Jun-Sung (Center for Nanotechnology-based New Drug Dosage Form, College of Pharmacy, Chungnam National University) ;
  • Cho, Won-Kyung (Center for Nanotechnology-based New Drug Dosage Form, College of Pharmacy, Chungnam National University) ;
  • Hwang, Sung-Joo (Center for Nanotechnology-based New Drug Dosage Form, College of Pharmacy, Chungnam National University)
  • 투고 : 2010.09.03
  • 심사 : 2010.10.09
  • 발행 : 2010.10.20
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초록

The objectives of this study were to evaluate the effect of formulation ingredients on the drug release and to optimize the novel sustained release matrix tablet formulations of bupropion hydrochloride. A three factor, three-level Box-Behnken design was used for the optimization procedure, with the amounts of PEO ($X_1$), citric acid ($X_2$) and Compritol 888 ATO ($X_3$) as the independent variables. The selected dependent variables were the cumulative percentage values of bupropion hydrochloride that had dissolved after 1, 4 and 8 hr. Various dissolution profiles of the drug from sustained release matrix tablets were obtained. Optimization was performed for $X_1$, $X_2$ and $X_3$ using the following target ranges; $30%{\leq}Y_1{\leq}45%$; $70{\leq}Y_2{\leq}85%$; $85%{\leq}Y_3{\leq}100%$. The optimized formulation for bupropion hydrochloride was achieved with 12.5% PEO ($X_1$), 2.5% citric acid ($X_2$) and 10% Compritol 888 ATO ($X_3$). The sustained release matrix tablets with the optimized formulation provided a release profile that was close to predicted values. In addition, the dissolution profiles of the sustained release matrix tablet with the optimized formulation were similar to those of the commercial product Wellbutrin$^{(R)}$ SR tablets ($f_2$=79.83).

키워드

참고문헌

  1. Ascher, J.A., Cole, J.O., Colin, J., 1995. Bupropion : A review of its mechanism of antidepressant activity. J. Clin. Psychiat 56, 395-401.
  2. Barrickman, L.L., Perry, P.J., Allen, A.J., Kuperman, S., Arndt, S.V., Herrmann, K.J., Schumacher, E., 1995. Bupropion versus methylphenidate in the treatment of attention deficit hyperactivity disorder. J. Am. Acad. Child Adolesc. Psychiatry 34, 649-657. https://doi.org/10.1097/00004583-199505000-00017
  3. Cyr, M., Brown, C.S., 1998. Current drug therapy recommendations for the treatment of attention deficit hyperactivity disorder. Drugs 56, 215-223. https://doi.org/10.2165/00003495-199856020-00005
  4. Ferris, R.M., Cooper, B.R., 1993. Mechanism of antidepressant activity of bupropion. J. Clin. Psychiatry Monograph 11, 2-14.
  5. Ford, J.L., Rubinstein, M.H., McCaul, F., Hogan, J.E., Edgar, P.J., 1987. Importance of drug type, tablet shape and added diluents on drug release kinetics from hydroxypropylmethylcellulose matrix tablets. Int. J. Pharm. 40, 223-234. https://doi.org/10.1016/0378-5173(87)90172-4
  6. Furlanetto, S., Cirri, M., Maestrelli, F., Corti, G., Mura, P., 2006. Study of formulation variables influencing the drug release rate from matrix tablets by experimental design. Eur. J. Pharm. Biopharm. 62, 77-84. https://doi.org/10.1016/j.ejpb.2005.07.001
  7. Gonzalez, I.M., Robles, L.V., 2003. Influence of enteric citric acid on the release profile of 4-aminopyridine from HPMC matrix tablets. Int. J. Pharm. 251, 183-193. https://doi.org/10.1016/S0378-5173(02)00598-7
  8. Jamzad, S., Fassihi, R., 2006. Development of a controlled release low dose class II drug-Glipizide. Int. J. Pharm. 312, 24-32. https://doi.org/10.1016/j.ijpharm.2005.12.037
  9. Jefferson, J.W., Pradko, J.F., Muir, K.T., 2005. Bupropion for major depressive disorder: Pharmacokinetic and formulation considerations. Clin. Ther. 27, 1685-1695. https://doi.org/10.1016/j.clinthera.2005.11.011
  10. Kranz, H., Brun, V.L., Wagner, T., 2005. Development of a multi particulate extended release formulation for ZK 811 752, a weakly basic drug. Int. J. Pharm. 299, 84-91. https://doi.org/10.1016/j.ijpharm.2005.04.026
  11. Maggi, L., Bruni, R., Conte, U., 2000. High molecular weight polyethylene oxides (PEOs) as an alternative to HPMC in controlled release dosage forms. Int. J. Pharm. 195, 229-238. https://doi.org/10.1016/S0378-5173(99)00402-0
  12. Maggi, L., Segale, L., Torre, M.L., Ochoa M.E., Conte, U., 2002. Dissolution behaviour of hydrophilic matrix tablets containing two different polyethylene oxides (PEOs) for the controlled release of a water-soluble drug. Dimensionality study. Biomaterials 23, 1113-1119. https://doi.org/10.1016/S0142-9612(01)00223-X
  13. Moore, J.W., Flanner, H.H., 1996. Mathematical comparison of dissolution profiles. Pharm. Tech. 20, 64-74.
  14. Myers, R.H., Montgomery, D.C., 2002. Response Surface Methodology: Process and Product Optimization Using Designed Experiments. John Wiley & Sons, New York, pp. 273-286.
  15. Palamara, K.L., Mogul, H.R., Peterson, S.J., Frishman, W.H., 2006. Obesity: new perspectives and pharmacotherapies. Cardiol. Rev. 14, 238-258. https://doi.org/10.1097/01.crd.0000233903.57946.fd
  16. Settle, E.C., 1998. Bupropion sustained release : side effect profile. J. Clin. Psychiatry 59, 32-36.
  17. Wu, N., Wang, L.S., Tan, D.C., Moochhala, S.M., Yang, Y.Y., 2005. Mathematical modeling and in vitro study of controlled drug release via a highly swellable and dissoluble polymer matrix: polyethylene oxide with high molecular weights. J. Control. Release 102, 569-581. https://doi.org/10.1016/j.jconrel.2004.11.002

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