Article
  • Characterization and Improved Dissolution Rate of Aceclofenac Solid Dispersion
  • Kim YT, Park HJ, Lee YH, Hong HK, Eom S, Kim YK, Lee EY, Choi MG, Lee JJ, Cho YB, Khang G
  • 아세클로페낙 고체분산체의 특성 및 용출률 개선
  • 김윤태, 박현진, 이영현, 홍희경, 엄신, 김용기, 이은용, 최명규, 이재준, 조용백, 강길선
Abstract
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.

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.

Keywords: aceclofenac; solid dispersion; PVP K-30; spray-drying

References
  • 1. Alvarez-Laurena A, Piniella JF, Carrasco E, J. Crystallogr. Spectrosc., 22, 323 (1992)
  •  
  • 2. Lee BJ, Hung HAAPS 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 SDKorea Patent 10-2000-0027237 (2000)
  •  
  • 20. Nishio H, Hayashi Y, Terashima S, Inflammopharmacology, 15, 266 (2007)
  •  
  • Polymer(Korea) 폴리머
  • Frequency : Bimonthly(odd)
    ISSN 0379-153X(Print)
    ISSN 2234-8077(Online)
    Abbr. Polym. Korea
  • 2023 Impact Factor : 0.4
  • Indexed in SCIE

This Article

  • 2009; 33(6): 596-601

    Published online Nov 25, 2009

  • Received on Jul 20, 2009
  • Accepted on Sep 10, 2009