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Effect of acidifier on the dissolution property of a solid dispersion of raloxifene HCl

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Abstract

Hydroxypropylmethylcellulose (HPMC)-based solid dispersions (SDs) and physical mixtures (PMs) were prepared to enhance the dissolution rate of poorly water-soluble drugs. The roles of the acidifiers on structural crystallinity and drug dissolution rate were investigated. A poorly water-soluble drug, raloxifene HCl (RXH), was used as the model drug. The SDs and PMs were prepared with HPMC, drugs, and acidifiers using the spray-drying method and then compressed into tablets. The dissolution rate of RXH from SDs was ranked by acidifiers in increasing order: glycolic acid, citric acid, and fumaric acid. On the other hand, the acidifiers in PMs did not significantly affect the drug dissolution rate. Scanning electron microscopy was used to analyze the surface morphology of the SD and PM samples. Differential scanning calorimetry and X-ray diffraction were used to analyze the SD crystallinity. Fourier-transform infrared spectroscopy was used to analyze the characteristic changes of the SD chemical structure. The in vitro release behavior of SDs and PMs was examined in simulated gastric fluid. The dissolution rate of RXH from SDs and PMs was higher than that of the pure drug. The dissolution rate of RXH from SDs was higher than that of PMs and original RXH due to the decreased particle size and hydrogen bond between the drug and the carrier.

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References

  1. J. D. Termine, J. Bone Miner. Matab., 14, S25 (1994).

    Article  Google Scholar 

  2. C. S. Cho, T. H. Shin, J. L. Lim, K. Y. Moon, D. K. Kim, and Y. W. Choi, Korean J. Chem. Eng., 27, 1906 (2010).

    Article  CAS  Google Scholar 

  3. M. F. Wempe, V. J. Wacher, and K. M. Ruble, Int. J. Pharm., 346, 25 (2008).

    Article  CAS  Google Scholar 

  4. J. Trontelj, T. Vovk, M. Bogataj, and A. Mrhar, Pharmcol. Res., 52, 334 (2005).

    Article  CAS  Google Scholar 

  5. D. C. Kemp, P. W. Fan, and J. C. Stevens, Drug Metab. Dispos., 30, 694 (2002).

    Article  CAS  Google Scholar 

  6. Y. S. Ahn, H.Y. Lee, K. D. Hong, S. B. Jung, S. H. Cho, J. M. Rhee, H. B. Lee, and G. Khang, J. Kor. Pharm. Sci., 34, 289 (2004).

    CAS  Google Scholar 

  7. M. J. Oh, J. B. Shim, E. Y. Lee, H. Yoo, W. H. Cho, D. K. Lim, D. Lee, and G. Khang, J. Pharm. Invest., 41, 179 (2011).

    Article  CAS  Google Scholar 

  8. W. H. Cho, Y. H. Lee, M. J. Oh, D. Lee, and G. Khang, Int. J. Tissue Reg., 1, 37 (2010).

    Google Scholar 

  9. L. Gunawan, G. P. Johari, and R. M. Shanker, Pharmcol. Res., 23, 967 (2006).

    Article  CAS  Google Scholar 

  10. M. Efentakis, S. Koligliati, and M. Vlachou, Int. J. Pharm., 311, 147 (2006).

    Article  CAS  Google Scholar 

  11. M. Efentakis, and S. Politis, Eur. Polym. J., 42, 1183 (2006).

    Article  CAS  Google Scholar 

  12. J. Hamdani, A. J. Moës, and K. Amighi, Int. J. Pharm., 322, 96 (2006).

    Article  CAS  Google Scholar 

  13. P. W. Heng, L. W. CHan, and E. S. K. Tang, Int. J. Pharm., 327, 26 (2006).

    Article  CAS  Google Scholar 

  14. K. Naelapää, P. Veski, J. G. Pedersen, D. Anov, P. J. H. G. Kristensen, and P. Bertelsen, Int. J. Pharm., 332, 90 (2007).

    Article  Google Scholar 

  15. M. Moneghini, A. Carcano, G. Zingone, and B. Perissutti, Int. J. Pharm., 175, 177 (1998).

    Article  CAS  Google Scholar 

  16. A. T. M. Serajuddin, P. C. Sheen, D. Mufson, D. F. Bernstein, and M. A. Augustine, J. Pharm. Sci., 77, 414 (1988).

    Article  CAS  Google Scholar 

  17. P. C. Sheen, V. K. Khetarpal, C. M. Cariola, and C. E. Rowlings, Int. J. Pharm., 118, 221 (1995).

    Article  CAS  Google Scholar 

  18. J. Y. Jung, S. D. Yoo, S. H. Lee, K. H. Kim, D. S. Yoon, and K. H. Lee, Int. J. Pharm., 187, 209 (1999).

    Article  CAS  Google Scholar 

  19. B. S. Kim, M. S. Kim, and H. B. Lee, Polym. Sci. Technol., 18, 549 (2007).

    CAS  Google Scholar 

  20. E. Y. Lee, M. J. Oh, Y. K. Kim, S. Eom, H. J. Park, K. Y. Seong, S. J. Kim, E. H. Jo, D. Lee, and G. Khang, Int. J. Tissue Reg., 1, 88 (2010).

    Google Scholar 

  21. Y. K. Kim, D. K. Lim, S. K. Lee, S. Eom, E. Y. Lee, S. J. Kim, D. Lee, and G. Khang, Int. J. Tissue Reg., 1, 101 (2010).

    Google Scholar 

  22. E. J. Henderson, C. M. Hessel, and J. G. C. Veinot, J. Am. Chem. Soc., 130, 3624 (2008).

    Article  CAS  Google Scholar 

  23. D. M. Piera, C. Roberta, B. Christine, G. Roberto, J. Etienne, M. Admir, O. Pascal, and M. Sante, Int. J. Pharm., 342, 137 (2007).

    Article  Google Scholar 

  24. C. Dahlberg, A. M. Fureby, M. Schuleit, I. Furó, Eur. J. Pharm. Sci., 39, 125 (2010).

    Article  CAS  Google Scholar 

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Authors and Affiliations

  1. Department of BIN Fusion Technology & Department of PolymerNano Science Technology, Chonbuk National University, Jeonbuk, 561-756, Korea

    Jung Bo Shim, Jung Keun Lee, Hansu Jo, Ji Hye Hwang, Su Mi Jeong, Jae Il Jo, Dongwon Lee & Gilson Khang

  2. College of Pharmacy, Korea University, Chungnam, 339-700, Korea

    Soon Hong Yuk

Authors
  1. Jung Bo Shim
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  2. Jung Keun Lee
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  3. Hansu Jo
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  4. Ji Hye Hwang
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  5. Su Mi Jeong
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  6. Jae Il Jo
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  7. Dongwon Lee
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  8. Soon Hong Yuk
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  9. Gilson Khang
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Correspondence to Gilson Khang.

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Shim, J.B., Lee, J.K., Jo, H. et al. Effect of acidifier on the dissolution property of a solid dispersion of raloxifene HCl. Macromol. Res. 21, 42–48 (2013). https://doi.org/10.1007/s13233-013-1005-x

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  • DOI: https://doi.org/10.1007/s13233-013-1005-x

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