PVP K30/Eudragit EPO에 의한 셀레콕시브 고체분산체의 용출률 향상 및 특성

전대연; 장지은; 이정환; 양재원; 박상미; 임동권; 강길선; Dae Yeon Jeon; Ji Eun Jang; Jeong Hwan Lee; Jae Won Yang; Sang Mi Park; Dongkwon Lim; Gilson Khang

Polymer(Korea), Vol.38, No.4, 434-440, July, 2014

Export Citation

PVP K30/Eudragit EPO에 의한 셀레콕시브 고체분산체의 용출률 향상 및 특성

Characterization and Improvement of Dissolution Rate of Solid Dispersion of Celecoxib in PVP K30/Eudragit EPO

전대연, 장지은, 이정환, 양재원, 박상미, 임동권, 강길선 ^†

전북대학교 BIN융합공학과, 고분자나노공학과

Dae Yeon Jeon, Ji Eun Jang, Jeong Hwan Lee, Jae Won Yang, Sang Mi Park, Dongkwon Lim, and Gilson Khang^†

Dept. of BIN Fusion Technology, Department of PolymerNano Science Technology and Polymer BIN Fusion Research Center, Chonbuk National University, 567 Baekje-daero, Jeonju 561-756, Korea

E-mail:

초록

셀레콕시브는 높은 결정성을 갖는 난용성 약물로서 이러한 난용성 약물의 용해도를 증진시키기 위해 고체분산법을 바탕으로 한 분무건조기를 이용하여 고체분산체를 제조하였다. PVP K30과 Eudragit EPO를 수용성 담체로 사용하였고 폴록사머 407은 계면활성제로 사용하였다. 제조된 셀레콕시브 고체분산체의 특성을 SEM, DSC, XRD 그리고 FTIR을 이용하여 확인하였다. SEM과 DSC 그리고 XRD를 통하여 셀레콕시브 고체분산체가 무정형임을 알 수 있었다. 제조된 고체분산체는 pH 1.2에서 용출을 실시하였으며 시판제인 Celebres® 용출률을 비교하였으며 분무건조를 통해 제조한 고체분산체가 Celebres® 보다 용출률이 크다는 것을 확인하였다.

We prepared nanoparticles containing insoluble celecoxib by the method of solid dispersions using a spray dryer to improve solubility of celecoxib. We used PVP K30 and Eudragit EPO as water-soluble carriers for the solid dispersion, and poloxamer 407 as a surfactant. Characterization of celecoxib solid dispersion was performed by scanning electron microscope (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR). The results of SEM, DSC and XRD demonstrated that celecoxib is amorphous in solid dispersion. The dissolution rate measured in intestinal juice showed that the method of solid dispersion improved celecoxib solubility as compared with a conventional drug (Celebres®). In conclusion, solid dispersion formulation prepared by a spray dryer would improve the solubility of celecoxib in oral administration.

Keywords:celecoxib;Eudragit EPO;PVP K30;spray drying;solid dispersion.

[References]

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Hwang JS, Kim SH, Cho SH, Huh KM, Polym.(Korea), 37(4), 442 (2013)
Leuner C, Dressman J, Eur. J. Pharm. Biopharm., 50, 47 (2000)
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Khang G, Kim SW, Cho JC, Rhee JM, Yoon SC, Lee HB, Bio-Med. Mater. Eng., 11, 89 (2001)
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Horter D, Dressman JB, Adv. Drug Deliver. Rev., 46, 75 (2001)
van Drooge DJ, Hinrichs WLJ, Visser MR, Frijlink HW, Int. J. Pharm., 310, 220 (2006)
Merisko-Liversidge E, Liversidge GG, Cooper ER, Eur. J. Pharm. Sci., 18, 113 (2003)
Rasenack N, Hartenhauer H, Muller BW, Int. J. Pharm., 254, 137 (2003)
Rasenack N, Muller BW, Pharmaceut. Res., 19, 1894 (2002)
Muralidhar S, Rao GD, Reddy BM, Narayana TV, Ramesh R, Int. J. Comper. Pharm., 2, 1 (2011)
Muralidhar S, Rao GD, Nizami SA, Reddy KT, Reddy SR, JAPR, 1, 74 (2010)
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Nashed YE, Mitra AK, Spectrochim. Acta A, 59, 2033 (2003)
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McGuigan C, Slater MJ, Parry NR, Perry A, Harris S, Bioorg. Med. Chem. Lett., 10, 645 (2000)
Hergert LA, Escandar GM, Talanta, 60, 235 (2003)
Yue ME, Jiang TF, Shi YP, Talanta, 62, 695 (2004)
Pokharkar VB, Mandpe LP, Padamwar MN, Ambike AA, Mahadik KR, Paradkar A, Powder Technol., 167(1), 20 (2006)
Rodier E, Lochard H, Sauceau M, Letourneau JJ, Freiss B, Fages J, Eur. J. Pharm. Sci., 26, 184 (2005)
Vilhelmsen T, Eliasen H, Schaefer T, Int. J. Pharm., 303, 132 (2005)
Woo Y, Na K, Inter. J. Tissue. Reg., 3, 63 (2012)
Yang DH, Chun HJ, Inter. J. Tissue. Reg., 4, 41 (2013)
Lee JH, Jeong JS, Park SW, Kim DS, Kim W, Ahn SI, Park JH, Kim YT, Shin HS, Rhee JM, Khang G, Tissue Eng. Regen. Med., 5, 750 (2008)
Kim YT, Park HJ, Lee YH, Hong HK, Eom S, Kim YK, Lee EY, Choi MG, Lee JJ, Cho YB, Khang G, Polym.(Korea), 33(6), 596 (2009)

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[3] Leuner C, Dressman J, Eur. J. Pharm. Biopharm., 50, 47 (2000)

[4] Lee EY, Oh MJ, Kim SH, Seong KY, Lee YH, Kim SJ, She HS, Lee D, Khang G, Polym.(Korea), 35(2), 113 (2011)

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[9] Merisko-Liversidge E, Liversidge GG, Cooper ER, Eur. J. Pharm. Sci., 18, 113 (2003)

[10] Rasenack N, Hartenhauer H, Muller BW, Int. J. Pharm., 254, 137 (2003)

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