Stability of [D-Ala$^2$]-Methionine Enkephalinamide in Aqueous Solution

수용액중 [D-알라$^2$-메치오닌엔케팔린아미드의 안정성

  • 전인구 (동덕여자대학교 약학대학) ;
  • 양윤정 (동덕여자대학교 약학대학) ;
  • 이치호 (부산대학교 약학대학)
  • Published : 1993.04.01

Abstract

To evaluate the feasibility of transmucosal delivery of methionine enkephalin analog, [$D-Ala^2$]-me-thionine enkephalinamide (YAGFM), the influence of pH, temperature, ionic strength and initial peptide concentration on the physicochemical stability of YAGFM in aqueous buffered solutions were investigated using a stability-indicating HPLC method. The degradation of YAGFM followed the pseudo-first-order kinetics. From the pH-rate profile, the maximum stability of YAGFM was shown to be at the pH of about 5.0. The halflife for the degradation of YAGFM was found to be 181.3 days at pH 5.0 and $37^{\circ}C.$ Arrhenius plots of the data obtained at 25~$45^{\circ}C$ were reasonably linear with a correlation coefficient greater than 0.99, and the activation energy was calculated to be 8.9 kcal/mole. A higher ionic strength and/or a higher peptide concentration in buffered solutions retarded the degradation of YAGFM.

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