Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1995-05-04
1997-04-22
Levy, Neil S.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514177, 514178, 514179, 514180, 604 20, A61K 31575
Patent
active
056229445
ABSTRACT:
Compositions and methods are provided for enhanced transdermal electrotransport of 17-hydroxy sterol compounds, including testosterone. The parent sterols are modified at the 17-hydroxy position by covalent attachment of a charged chemical modifier. The chemical modifier provides the parent sterol with enhanced transport properties and is hydrolyzed under physiological conditions to release the active parent compound.
The composition comprises a 17-hydroxy sterol/chemical modifier complex, more generally represented by the formula (sterol--O--)C(O)--R--N(R.sup.1)(R.sup.2)(R.sup.3).sup.+. The portion of the complex derived from the chemical modifier is indicated by "C(O)--R--N(R.sup.1)(R.sup.2)(R.sup.3).sup.+ ", where N(R.sup.1)(R.sup.2)(R.sup.3).sup.+ represents a quaternary ammonium group and R.sup.1, R.sup.2, and R.sup.3 are independently selected from the group consisting of lower alkyl, alkyl, aryl, arylalkyl, cycloalkyl, heteroalkyl, and heteroarylalkyl; or R.sup.1 and R.sup.2 together with the nitrogen to which they are attached form a substituted heterocycle and R.sup.3 is lower alkyl, and R is a linking moiety, linking the (sterol--O)--C(O)-- to the nitrogen atom.
REFERENCES:
patent: 5068226 (1991-11-01), Weinshenker et al.
Bodor et al. Improved Delivery Through Biological Membranes XXII--Int. J. Pharmaceutics 35(1987) pp. 47-59.
Banga et al Iontophoretic Delivery of Drugs: Fundamentals Developments and Biomedical Applications--J. of Controlled Release 7 (1988) 1-24.
Cormier Michel J. N.
Hale Ron L.
Lu Amy T.
Solas Dennis W.
Affymax Technologies N.V.
ALZA Corporation
Levy Neil S.
Stevens Lauren L.
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