The Dissolution Property of Raloxifene HCl Solid Dispersion Using Hydroxypropyl Methylcellulose

Myeong Jun Oh; Jung Bo Shim; Hanna Yoo; Ga Young Lee; Hansu Jo; Su Mi Jeong; Soon Hong Yuk; Dongwon Lee; Gilson Khang

Macromolecular Research, Vol.20, No.8, 835-841, August, 2012

DOI10.1007/s13233-012-0127-x Export Citation

The Dissolution Property of Raloxifene HCl Solid Dispersion Using Hydroxypropyl Methylcellulose

Myeong Jun Oh, Jung Bo Shim, Hanna Yoo, Ga Young Lee, Hansu Jo, Su Mi Jeong, Soon Hong Yuk¹, Dongwon Lee , and Gilson Khang^†

Department of BIN Fusion Technology & Department of PolymerNano Science Technology, Chonbuk National University, Jeonbuk, 561-756, Korea
¹College of Pharmacy, Korea University, Chungnam, 339-700, Korea

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In this study, solid dispersion (SD) was prepared by using a spray-drying method. This SD was formulated with raloxifene HCl (RLXH) and hydroxypropylmethylcellulose (HPMC) to enhance the dissolution rates of poorly water-soluble drugs. The particle size distribution was used to analyze the particle size of the original RLXH and SD. The solubility study was used to analyze the effect of HPMC in solubility of the RLXH. Scanning electron microscopy (SEM) was used to analyze the morphological observation of the SD samples. Differential scanning calorimetry(DSC) and X-ray diffraction (XRD) were used to analyze the crystallinity of the RLXH. The crystallinity of RLXH in SD was changed. The interaction between RLXH and HPMC was investigated by Fourier transform infrared spectroscopy (FTIR). The dissolution study presented a simulated gastric juice (pH 1.2). The release rate of RLXH SD was higher than that of the original RLXH due to the decreased particle size and hydrogen bond between drug and carrier. In conclusion, the SD techniques for the improvement of the dissolution rate of RLXH were a useful method.

Keywords:raloxifene HCl;HPMC;solid dispersion;particle size;dissolution rate.

[References]

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Wempe MF, Wacher VJ, Ruble KM, Int. J. Pharm., 346, 25 (2008)
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[Referenced By]

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[3] Wempe MF, Wacher VJ, Ruble KM, Int. J. Pharm., 346, 25 (2008)

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

[5] Kemp DC, Fan PW, Stevens JC, Drug Metab. Dispos., 30, 694 (2002)

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[7] Oh MJ, Shim JB, Lee EY, Yoo H, Cho WH, Lim DK, Lee D, Khang G, J. Pharm. Invest., 41, 179 (2011)

[8] Cho WH, Lee YH, Oh MJ, Lee D, Khang G, Int. J.Tissue Reg., 1, 37 (2010)

[9] Gunawan L, Johari GP, Shanker RM, Pharmcol. Res., 23, 967 (2006)

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

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

[12] Hamdani J, Moes AJ, Amighi K, Int. J. Pharm., 322, 96 (2006)

[13] Heng PW, CHan LW, Tang ESK, Int. J. Pharm., 327, 26 (2006)

[14] Naelap K, Veski P, Pedersen JG, Anov D, Jorgensen P, Kristensen G, Bertelsen P, Int. J. Pharm., 332, 90 (2007)

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

[16] Serajuddin ATM, Sheen PC, Mufson D, Bernstein DF, Augustine MA, J. Pharm. Sci., 77, 414 (1988)

[17] Sheen PC, Khetarpal VK, Cariola CM, Rowlings CE, Int. J. Pharm., 118, 221 (1995)

[18] Jung JY, Yoo SD, Lee SH, Kim KH, Yoon DS, Lee KH, Int. J. Pharm., 187, 209 (1999)

[19] Kim BS, Youn JY, Kim JW, Kim MS, Khang G, Lee HB, Polym. Sci. Technol., 18(6), 549 (2007)

[20] Lee EY, Oh MJ, Kim YK, Eom S, Park HJ, Seong KY, Kim SJ, Jo EH, Lee D, Khang G, Int. J. Tissue Reg., 1, 88 (2010)

[21] Kim YK, Lim DK, Lee SK, Eom S, Lee EY, Kim SJ, Lee D, Khang G, Int. J. Tissue Reg., 1, 101 (2010)

[22] Henderson EJ, Hessel CM, Veinot JGC, J. Am. Chem. Soc., 130(11), 3624 (2008)

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

[24] Lee JH, Ku J, Park JS, Park JH, Ahn SI, Mo JH, Kim YT, Rhee JM, Lee HB, Khang G, J. Kor. Pharm.Sci., 38, 111 (2008)

[25] Park JS, Oh JS, Oh JM, Kim YT, Lee JH, Mo JH, Lee HB, Khang G, Polym.(Korea), 32(3), 193 (2008)

[26] Dahlberg C, Fureby AM, Schuleit M, Furo I, Eur. J.Pharm. Sci., 39, 125 (2010)