Aminomethyl derivatives of biologically active substances, and enhanced delivery thereof across topical membranes

A pharmaceutical composition in unit dosage form adapted for topical administration to a human or non-human animal in need thereof comprising a biologically effective amount of an aminomethyl derivative of a biologically active substance having the formula:

• ##STR44## wherein:
• (Z--(N)-- is the N-dehydro residue of a biologically active organic substance having the formula;
• ##STR45## wherein:
• R and R.sub.1 may be the same or different and are selected from the group consisting of H;
• cycloalkyl groups having up to 10 carbon atoms;
• or straight or branched chain alkyl, alkenyl, or alkynyl of 1 to 10 carbon atoms;
• R.sub.2 and R.sub.3 together with the nitrogen atom to which they are bonded form a morpholine ring;
• x is 1;
• y is 2;
• or a non-toxic pharmaceutically acceptable adduct, oxide, or other derivative thereof and a pharmaceutically acceptable, topically administrable carrier therefor, said aminomethyl derivative having an enhanced delivery across topical membranes of said animal upon topical application as compared with said underivatized biologically active substance and being capable of exerting said biological activity after delivery across said topical membrane.