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KMID : 0370219940380050488
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Yakhak Hoeji
1994 Volume.38 No. 5 p.488 ~ p.495
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Physicochemical Stability of Leucine Enkephalin and [D-알라^(2)]-Leucine Enkephalinamide in Buffered Aqueous Solution
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박인숙/Park, In Sook
전인구/Chun, In Koo
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Abstract
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To evaluate the feasibility of transmucosal delivery of leucine enkephalin (Leu-Enk) and its synthetic analog, [D-ala2]-leucine enkephalinamide (YAGFL), their physicochemical stabilities in aqueous buffered solutions were first investigated using a stability indicating high performance liquid chromatography. The degradation of Leu-Enk and YAGFL followed the pseudo-first-order kinetics. From the pH-rate profiles, it was found that the maximal stability of the two pentapeptides was at the pH of about 5.0. The shelf lives (tom,) for the degradation of Leu-Enk and YAGFL at pH 5.0 and 40t were found to be 48.13 and 50.9 days, respectively. From the temperature dependence of the degradation, activation energies for Leu-Enk and YAGFL were calculated to be 13.61 and 13.47 kcal/mole, respectively. A higher ionic strength and a higher initial peptide concentration in buffered solution slowed the degradation of the two pentapeptides. The addition of 2-hydroxypropyl-(3-cyclodextrin into the peptide solution did not affect the stability significantly.
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