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Molecular Effect of PVP on The Release Property of Carvedilol Solid Dispersion

  • Oh, Myeong-Jun (Department of BIN Fusion Technology & Department of Polymer Nano Science Technology, World Class Univ., Chonbuk Nat'l Univ.) ;
  • Shim, Jung-Bo (Department of BIN Fusion Technology & Department of Polymer Nano Science Technology, World Class Univ., Chonbuk Nat'l Univ.) ;
  • Lee, Eun-Yong (Department of BIN Fusion Technology & Department of Polymer Nano Science Technology, World Class Univ., Chonbuk Nat'l Univ.) ;
  • Yoo, Han-Na (Department of BIN Fusion Technology & Department of Polymer Nano Science Technology, World Class Univ., Chonbuk Nat'l Univ.) ;
  • Cho, Won-Hyung (Department of BIN Fusion Technology & Department of Polymer Nano Science Technology, World Class Univ., Chonbuk Nat'l Univ.) ;
  • Lim, Dong-Kyun (Department of BIN Fusion Technology & Department of Polymer Nano Science Technology, World Class Univ., Chonbuk Nat'l Univ.) ;
  • Lee, Dong-Won (Department of BIN Fusion Technology & Department of Polymer Nano Science Technology, World Class Univ., Chonbuk Nat'l Univ.) ;
  • Khang, Gil-Son (Department of BIN Fusion Technology & Department of Polymer Nano Science Technology, World Class Univ., Chonbuk Nat'l Univ.)
  • Received : 2011.03.25
  • Accepted : 2011.06.09
  • Published : 2011.06.20

Abstract

This study aimed to confirm the effect of molecular weight (MW) in solid dispersion of carvedilol with poly-vinylpyrrolidone (PVP) of various MW. Solid dispersion of carvedilol with PVP was prepared by spray-drying method. Scanning electron microscopy (SEM) was used to analyze the surface of solid dispersion samples. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were used to analyze the crystalline of solid dispersion. Fourier transform infrared spectroscopy (FT-IR) was used to analyze the change of chemical structure characteristic of solid dispersion. DSC and XRD show that drug crystalline was changed. FT-IR revealed that chemical structure of solid dispersion comparing the chemical structure of drug was changed. The dissolution studies of solid dispersion presented at simulated gastric juice (pH 1.2). The dissolution rate of solid dispersion was dramatically enhanced than pure drug and the MW of PVP has an effect on the release property of carvedilol in solid dispersion. In conclusion, the present study has confirmed the effect of MW of PVP on release property of solid dispersion formulation of carvedilol with PVP.

Keywords

References

  1. Ahn, Y.S., Lee, H.Y., Hong, K.D., Jung, S.B., Cho, S.H., Rhee, J.M., Lee, H.B., Khang, G., 2004. Effect of types and mixing ratios of water-soluble polymers on in vitro release profile of SD for acyclovir. J. Kor. Pharm. Sci. 34, 289-297.
  2. Cao, Q.R., Kim, T.W., Choi, C.Y., Kwon, K.A., Lee, B.J., 2003. Preparation and dissolution of polyvinylpyrrolidone(PVP)- based SD systems containing solubilizers. J. Kor. Pharm. Sci. 33, 7-14.
  3. Cho, W.H., Lee, Y.H., Oh, M.J., Lee, D., Khang, G., 2010. Solubility characterization and improved dissolution of pranlukast with the surfactant. Int J. Tissue Reg. 1, 37-45.
  4. Cho, W.H., Lee, Y.H., Song, B.J., Yoo, S.C., Lee, D.W., Khang, G., 2010. Improvement of pranlukast dissolution by nano SD. Int J. Tissue Reg. 1, 74-80.
  5. Chung, T.S., Tun, C.M., Pramoda, K.P., Wang, R., 2001. Novel hollow fiber membranes with defined unit-step morphological change. J. Membr Sci. 193, 123-128. https://doi.org/10.1016/S0376-7388(01)00529-4
  6. Dahlberg, C., Fureby, A.M., Schuleit, M., Furo, I., 2010. Polymerdrug interactions and wetting of SDs. Eur J Pharm Sci. 39, 125-133. https://doi.org/10.1016/j.ejps.2009.11.005
  7. Dunn, C.J., Lea, A.P., Wagstaff, A.J., 1997. Carvedilol: a reappraisal of its pharmacological ${\beta}$-blockers in left ventricular dysfunction and heart failure. Drugs. 54, 161-169. https://doi.org/10.2165/00003495-199754010-00015
  8. Eom, S., Yoo, S.C., Song, B.J., Kim, Y.K., Park, H.J., Seong, K.Y., Song, Y.S., Lee, D.W., Khang, G., 2010. Effect of preparation conditions on release behavior of raloxifene HCL-loaded PLGA microspheres. Int J Tissue Reg. 1, 28-36.
  9. Henderson, E.J., Hessel, C.M., Veinot, JG.C., 2008. Synthesis and photoluminescent properties of size-controlled germanium nanocrystals from phenyl trichlorogermane-derived polymers. J. Am Chem Soc. 130, 3624-3632. https://doi.org/10.1021/ja710286a
  10. Jeong, J.K., Khang, G., Rhee, J.M., Shin, H.C., Lee, H.B., 2000. Effect of molecular weight and mixture ratio of PVP on improving the bioavailability of ipriflavone. J. Korean Pharm. Sci. 30(4), 235-239.
  11. Jeong, J.K., Kim, J.H., Khang, G., Rhee, J.M., Lee, H.B., 2002. The preparation and characterization of SD of ipriflavone with PVP. J. Korean Pharm Sci. 32(3), 173-179.
  12. Khang, G., Jeong, J.K., Rhee, J.M., Lee, J.S., Lee, H.B., 2001. Effect of hydrophillic polymers on SD of ipriflavone to improve bioavailability, Macromol. Chem. Symp. 14, 123-132.
  13. Kim, Y.K., Lim, D.K., Lee, S.K., Eom, S., Lee, E.Y., Kim, S.J., Lee, D., Khang, G., 2010. Characterization and enhanced dissolution rate of nateglinide SD by using polyvinylacetal diethylaminoacetate. Int J. Tissue Reg. 1, 101-107.
  14. Lee, E.Y., Oh, M.J., Kim, Y.K., Eom, S., Park, H.J., Seong, K.Y., Kim, S.J., Jo, E.H., Lee, D.W., Khang, G., 2010. Controlled release of rosiglitazone maleate ny SD with cellulose acetate. Int J. Tissue Reg. 1, 88-93.
  15. Lee, J.H., Ku, J., Park, J.S., Park, J.H., Ahn, S.I., Mo, J.H., Kim, Y.T., Rhee, J.M., Lee, H.B., Khang, G., 2008. Improved dissolution and Characterization of solid dispersed atorvastatin calcium. J. Kor. Pharm. Sci. 38(2), 111-117. https://doi.org/10.4333/KPS.2008.38.2.111
  16. Loftsson, T., Vogensen, SB., Desbos, C., Jansook, P., 2008. Carvedilol: solubilization and cyclodextrin complexation: a technical note. AAPS Pharm Sci Tech. 9, 425-430. https://doi.org/10.1208/s12249-008-9055-7
  17. Ohya, H., Jicsh, H., Nrgish, Y., 1993. Studies on distribution and reverse-osmosis properties of cellulose-acetate derivatives for organic-compounds. J. Membrane Sci. 85(1), 1-11. https://doi.org/10.1016/0376-7388(93)85001-D
  18. Park, J.S., Oh, J.M., Kim, Y.T., Lee, J.H., Kim, M.J., Mo, J.H., Kim, M.S., Lee, H.B., Khang, G., 2008. Release behavior from sibutramine microspheres using spray-dryer. Polymer(Korea). 32(3), 193-198.
  19. Park, Y.J., Oh, D.H., Yan, Y.D., Seo, Y.G., Lee, S.N., Choi, H.G., Yong, C.S., 2010. Surface-attached SD. J Pharma Investi. 40, 97-102. https://doi.org/10.4333/KPS.2010.40.S.097
  20. Piera, D.M., Roberta, C. Christine, B., Roberto, G., Etienne. J., Admir, M., Pascal, O., Sante, M., 2007. Characterization and compaction behaviour of nimesulide crystal forms, Int J. Pharm. 342. 137-144. https://doi.org/10.1016/j.ijpharm.2007.05.009
  21. Robert, R., Ruffolo, R.R., Boyle, DA., Brooks, D.P., Feuerstein, G.Z., Venuti, R.P., Lukas, M.A., Paste, G., 1992. Carvedilol: a novel cardiovascular drug with multiple actions, Cardiovasc Drug Rev. 10, 127-157. https://doi.org/10.1111/j.1527-3466.1992.tb00242.x
  22. Tanwar, Y.S., Chauhan, C.S., Sharma, A., 2007. Development and evaluation of carvedilol transdermal patches. Acta Pharm. 57, 151-159. https://doi.org/10.2478/v10007-007-0012-x
  23. Waling, W.D., 1994. "Povidone", in "Handbook of Pharmaceutical Excipients", A Wade and PJ Weller, EDS, 392, American Pharmaceutical Association/The Pharmaceutical Press, Washington, DC/London, 392.

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