Inclusion Complex of Analgesic and Antiinflammatory agents with Cyclodextrins (I): Enhancement of Dissolution of Ibuprofen by $2-Hydroxypropyl-{\beta}-cyclodextrin$

시클로덱스트린과 소염진통제 간의 포접복합체에 관한 연구(I): 2-히드록시프로필-${\beta}$-시클로덱스트린에 의한 이부프로펜의 용출 증가

  • 오인준 (전남대학교 약학대학 약학과) ;
  • 박정규 (전남대학교 약학대학 약학과) ;
  • 이용복 (전남대학교 약학대학 약학과) ;
  • 신상철 (전남대학교 약학대학 약학과)
  • Published : 1993.03.20

Abstract

Inclusion complex of ibuprofen with $2-Hydroxypropyl-{\beta}-cyclodextrin\;(HP-{\beta}-CD)$ in aqueous solution and in the solid state was evaluated by the solubility method and the instrumental analysis such as infrared spectroscopy, thermal analysis and x-ray diffractometry. The aqueous solubility of ibuprofen was increased linearly with the increase in the concentration of $HP-{\beta}-CD$, showing an $A_L$ type phase solubility diagram. The results showed that the dissolution rate of ibuprofen was significantly increased by complexation with $HP-{\beta}-CD$. $Ibuprofen-HP-{\beta}-CD$ complex enhanced the mean plasma concentration levels and the area under plasma concentration-time curve after oral administration compared to those of the drug alone. It is concluded that the complex of ibuprofen with $HP-{\beta}-CD$ increases the dissolution rate and improves the bioavailability of the ibuprofen by the formation of a water-soluble complex.

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