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KMID : 0369819940240010001
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Jorunal of Korean Pharmaceutical Sciences
1994 Volume.24 No. 1 p.1 ~ p.9
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Degradation and Stabilization of Methionine Enkephalin and [ D - Ala 2 ] - methionine Enkephalinamide in the Corneal Extracts of Rabbits
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이치호/Lee CH
이경진/전인구/성영기/신영희/Lee KJ/Chun IK/Sung YG/Shin YH
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Abstract
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In order to study systemic peptide delivery through the ocular route, the stabilities of methionine enkephalin (Met-Enk) and [D-ala²]-methionine enkephalinamide (YAGFM) in the corneal extracts of rabbits were investigated using reversed phase HPLC. Met-Enk was found to be hydrolyzed most rapidly in the corneal epithelium, but YAGFM was relatively stable. Aminopeptidases appeared to contribute over 60% to the degradation of Met-Enk and the degradation rate of Met-Enk followed the first order kinetics. The half-lives of Met-Enk in the extracts of the corneal epithelium and endothelium were 36 and 673 min, respectively. From the effects of enzyme inhibitors, it was found that the application of the mixture of amastatin, thimerosal and EDTA was very useful for the inhibition of peptide degradation.
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KEYWORD
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