Rectal Absorption of [Asu^<1,7>]-Eel Calcitonin in Rats

概要

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[Asu^<1,7>]-eel calcitonin ([Asu^<1,7>]-ECT) was not absorbed well from rat rectum. Although an unstirred layer may exist as a diffusion barrier for [Asu^<1,7>]-ECT absorption, transport through the epithelial cell membrane is the limiting step for [Asu^<1,7>]-ECT absorption. Coadministration of 0.33M phenylalanine enamine of ethylacetoacetate (PheEtAA), 0.17M diethylethoxymethylenemalonate (DEEMM), 0.6M sodium salicylate (SA), or 0.05M sodium p-chloromercurylphenyl sulfate (p-CMP) increased the rectal [Asu^<1,7>]-ECT absorption significantly. In particular, PheEtAA and DEEMM resulted in a more than 180 times greater AUC of [Asu^<1,7>]-ECT compared to that when [Asu^<1,7>]-ECT alone was administered rectally, and these two adjuvants were more effective than SA and p-CMP on the rectal [Asu^<1,7>]-ECT absorption, though all four adjuvants coadministered at the above concentration with sodium cefmetazole caused similar increases of rectal cefmetazole absorption.
公益社団法人日本薬学会の論文
1985-02-25