화학공학소재연구정보센터
Polymer(Korea), Vol.33, No.6, 596-601, November, 2009
아세클로페낙 고체분산체의 특성 및 용출률 개선
Characterization and Improved Dissolution Rate of Aceclofenac Solid Dispersion
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초록
아세클로페낙은 높은 결정성을 갖는 난용성 약물이다. 이러한 난용성 약물의 용해도를 증진시키기 위해서 고체분산법을 바탕으로 한 분무건조기를 이용하여 미립구를 제조하였다. PVP-K30을 수용성 담체로 사용하였고 폴록사머는 계면활성화제로 사용하였다. 제조된 아세클로페낙 고체분산체의 특성을 SEM, DSC, XRD 그리고 FT-IR을 이용하여 확인하였다. SEM, DSC, XRD을 통하여 아세클로페낙 고체분산체가 무정형임을 알 수 있었고 FT-IR을 통하여 아세클로페낙과 PVP-K30간에 수소결합을 통해 염을 형성하고 있다는 것을 확인할 수 있었다. 제조된 미립구는 pH 6.8에서 방출을 실시하였으며 시판제인 Airtal®과 용출률을 비교하였으며 분무건조를 통해 제조한 미립구가 시판제인 Airtal® 보다 용출률이 크다는 것을 확인하였다.
We prepared nanoparticles containing insoluble aceclofenac by the method of solid dispersions using spray dryer to improve solubility of aceclofenac. We used PVP-K30 as a water soluble carrier for the solid dispersion and poloxamer as a surfactant. Characterization of aceclofenac solid dispersion was performed by SEM, DSC, XRD and FT-IR. The results of SEM, DSC and XRD demonstrated that aceclofenac is amorphous in solid dispersion. The formation of salt by hydrogen bond between aceclofenac and PVP K-30 was confirmed by FT-IR. The dissolution rate measured in intestinal juice showed the method of solid dispersion improved aceclofenac solubility as compared with a conventional drug(Airtal®). In conclusion, the method of solid dispersion using spray dryer would improve solubility of aceclofenac in oral administration.
  1. Alvarez-Laurena A, Piniella JF, Carrasco E, J. Crystallogr. Spectrosc., 22, 323 (1992)
  2. Lee BJ, Hung H, AAPS Annual Meeting, New Orleans, LA, USA, p14 (1999)
  3. Lee JH, Kim W, Kim DS, Park JH, Ahn SI, Kim YT, Lee TW, Rhee HM, Shin HS, Lee HK, Khang G, Tissue. Eng. Regen. Med., 5, 404 (2008)
  4. Lee JH, Ahn SI, Park JH, Kim YT, Khang G, Rhee JM, Lee HB, Tissue Eng. Regen. Med., 5, 215 (2008)
  5. Kim HS, Kang B, Lee MS, Kim TW, Tissue Eng. Regen. Med., 5, 61 (2008)
  6. Jeong JK, Khang G, Rhee JM, Shin HC, Lee HB, J. Korean Pharm. Sci., 30, 235 (2002)
  7. Ahn YS, Lee HY, Hong KD, Jung SB, Cho SH, Rhee JM, Lee HB, Khang G, J. Korean Pharm. Sci., 34, 169 (2004)
  8. Ahn YS, Lee HY, Hong KD, Jung SB, Cho SH, Rhee JM, Lee HB, Khang G, J. Korean Pharm. Sci., 34, 289 (2004)
  9. Kim YH, Lee JW, Kim MS, Yang SY, Khang G, Lee JS, Lee HB, Tissue Eng. Regen. Med., 3, 96 (2006)
  10. Park JS, Lee JH, Shin HS, Lee TW, Kim MS, Khang H, Rhee JM, Lee HK, Lee HB, Tissue Eng. Regen. Med., 4, 347 (2007)
  11. Lee JH, Lim JY, Ahn SI, Park JH, Kim YT, Hhee JM, Khang G, Tissue Eng. Regen. Med., 5, 451 (1999)
  12. Waliking WD, "“Povidone", in Handbook of Pharmaceutical Excipitients, Wade A, Weller PJ, Editors, American Pharmaceutical Association/The Pharmaceutical Press, washington, DC/London, p 392-399 (1994)
  13. Khang G, Jeong JK, Rhee JM, Lee JS, Lee HB, Polym. Sci. Technol., 13(3), 342 (2002)
  14. Poloxamers(2), BASF ExAct, p.7 (2000)
  15. Lee JH, Kim W, Kim DS, Ahn SI, Park JH, Kim YT, Lee TW, Rhee JM, Shin HS, Lee HK, Khang G, Tissue Eng. Regen. Med., 5, 404 (2008)
  16. Park SW, Lee JH, Kim DS, Kim W, Park JH, Ahn SI, Kim YT, Shin HS, Rhee JM, Khang G, Tissue Eng. Regen. Med., 5, 600 (2008)
  17. Park JS, Oh JS, Oh JM, Kim YT, Lee JH, Mo JH, Lee HB, Khang G, Polym.(Korea), 32(3), 193 (2008)
  18. Chung TS, Tun CM, Pramoda KP, Wang R, J. Membr. Sci., 193(1), 123 (2001)
  19. Lee SD, Korea Patent 10-2000-0027237 (2000)
  20. Nishio H, Hayashi Y, Terashima S, Inflammopharmacology, 15, 266 (2007)