Rectal insulin hypoglycaemic compsn. - contg. surfactant or bile acid (salt) as absorption accelerator

摘要

The compsn. is prepd. by mixing (A) insulin, (B) a base for rectal use and (C) an absorption accelerator selected from polyoxyethylene ether nonionic surfactants (HLB value 6-19, 4-30 oxyethylene (EO) units); anionic, cationic and ampholytic surfactants; and bile acids and their alkali metal salts. Wt, ratio (C): (B) is 0.001-0.5:1 (pref. 0.005-0.1:1). A typical compsn. is prepd. by dispersing 2g Na taurocholate and 8000 units of (A) in 98 g maize oil then filling flexible capsules with 1.5 g aliquots. (A) is a hypoglycaemic agent used for treating diabetes presence of (C) gives a hypoglycaemic effect comparable with a similar dose of (A) by injection, thus avoiding the disadvantages of injection without requiring large doses of (A). Typically 0.5-5 units/kg of (A) rectally in the rabbit gives 40-60% reduction of blood glucose level using the new formulations.