The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Apr. 22, 1997

Filed:

May. 04, 1995
Applicant:
Inventors:

Ron L Hale, Woodside, CA (US);

Amy T Lu, Los Altos, CA (US);

Dennis W Solas, San Francisco, CA (US);

Michel J Cormier, Mountain View, CA (US);

Assignees:

Affymax Technologies N.V., Middlesex, GB;

Alza Corporation, Palo Alto, CA (US);

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
A61K / ;
U.S. Cl.
CPC ...
514181 ; 514177 ; 514178 ; 514179 ; 514180 ; 604 20 ;
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.


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