Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
2008-06-10
2008-06-10
Desai, Rita (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
C562S450000, C562S444000
Reexamination Certificate
active
07384982
ABSTRACT:
The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formulawhereinR1, R2, R3, and R4are indepedently hydrogen, halogen, C1-C4alkyl, or C1-C4alkoxy; andR5is a substitued or unsubstituted C2-C16alkylene, substituted or unsubstituted C2-C16alkenylene, substituted or unsubstituted C1-C12alkyl(arylene), or substituted or unsubstituted aryl(C1-C12alkylene). The hydrates and solvates of present invention also have surprisingly greater efficacy for delivering active agents, such as heparin and calcitonin, than their corresponding monosodium salts and free acids. The present invention provides an alcohol solvate, such as ethanol solvate, of a disodium salt of a delivery agent of the formula above. The invention also provides a hydrate of a disodium salt of a delivery agent of the formula above. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.
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Agarwal Rajesh K.
Ault Joseph M.
Azria Mosise
Bateman Simon D.
Bay William E.
Darby & Darby P.C.
Desai Rita
Emisphere Technologies Inc.
Novartis AG
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