Absorption of Steroid Hormones from the Human Small Intestine1

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Abstract
Absorption of steroid hormones was measured as disappearance rate from the human small intestine during steady state perfusion of aqueous solutions through a transintestinal tube. Absorption correlated inversely with the extent of hydroxylation of the molecule put into the gut. Esters or ethers of polyhydroxysteroids were more rapidly absorbed than the parent compounds. Lipoidal molecules lacking[long dash]OH were very rapidly absorbed. Cortisol absorption rate (weight/unit time) was directly proportional to concentration, suggesting that steroid hormones are absorbed by diffusion. The unabsorbed residues from cortisol acetate and 1-methyl-[DELTA]1-androstenolone acetate were chiefly the parent unesterified steroids. Thus, steroid esters may be hydrolyzed intraluminally, and hence be absorbed as both free steroid and ester. In general, steroid hormones and their derivatives are well absorbed from aqueous solutions. Small intestinal absorption rate of the dissolved molecule is not crucial for determining potency by the oral route. Resistance to inactivation is essential for activity after administration per os.

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