Interaction of Indomethacin with the Vehicle Component Diisopropyl Adipate

概要

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The interactions of the potent antiinflammatory agent indomethacin with diisopropyl adipate and n-octanol were studied under various conditions. Diisopropyl adipate has been used as a typical additive in preparations for the percutaneous absorption of indomethacin, and n-octanol is known to form hydrogen-bonds with various drugs. The association constants were determined from the change in the partition of indomethacin between n-hexane containing diisopropyl adipate or n-octanol and water. Both the neutral and anionic forms of indomethacin were found to associate with these additives in a 1 : 2 molar ratio, but with different association constants. The association of indomethacin with n-octanol was found to be dependent on pH, but that with diisopropyl adipate was independent on pH. The affinity of indomethacin for diisopropyl adipate was much smaller than that of the neutral form of indomethacin for n-octanol. It was also found, from an analysis of the solubilities of indomethacin in various esters, that the association constants of indomethacin with esters are about the same. The weak, but pH-independent association of indomethacin with diisopropyl adipate is suggested to be important for the induction of percutaneous absorption of indomethacin.
社団法人日本薬学会の論文
1986-03-25