Publication number: 20100099621
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 formula wherein R1, R2, R3, and R4 are independently hydrogen, halogen, C1-C4 alkyl, or C1-C4 alkoxy; and R5 is a substituted or unsubstituted C2-C16 alkylene, substituted or unsubstituted C2-C16 alkenylene, substituted or unsubstituted C1-C12 alkyl(arylene), or substituted or unsubstituted aryl(C1-C12 alkylene). 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.
Type:
Application
Filed:
December 18, 2009
Publication date:
April 22, 2010
Applicants:
EMISPHERE TECHNOLOGIES, INC., NOVARTIS AG
Inventors:
William E. Bay, Rajesh K. Agarwal, Kiran Chaudhary, Shingai Majuru, Michael M. Goldberg, JoAnne P. Corvino, Moise Azria, Joseph M. Ault, Simon D. Bateman, Subash Patel, Joseph Sikora, Rebecca F. Yang, Joseph L. Zielinski