N,N-dinitramide salts as solubilizing agents for biologically active agents
First Claim
1. A method for increasing the solubility of an ionizable compound in a lipophilic medium, wherein ionization of the compound results in a biologically active cationic species in association with an anionic counterion, the method comprising admixing the ionizable compound with an effective solubility enhancing amount of an N,N-dinitramide salt.
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Abstract
A method is provided for enhancing the solubility of an ionizable compound in a lipophilic medium by admixing the compound with an effective solubility-enhancing amount of an N,N-dinitramide salt. The ionizable compound, upon ionization, gives rise to a biologically active cationic species that ionically associates with the N,N-dinitramide anion N(NO2)2− following admixture with the N,N-dinitramide salt. The biologically active cationic species may be a pharmacologically active cation, in which case the method is useful for enhancing the penetration of the blood-brain barrier by the pharmacologically active cation. In other embodiments, the ionizable compounds are medical imaging or diagnostic agents, or agricultural agents such as pesticides. Salts of biologically active cations and N,N-dinitramide ion are also provided as novel compositions of matter.
31 Citations
76 Claims
- 1. A method for increasing the solubility of an ionizable compound in a lipophilic medium, wherein ionization of the compound results in a biologically active cationic species in association with an anionic counterion, the method comprising admixing the ionizable compound with an effective solubility enhancing amount of an N,N-dinitramide salt.
- 58. A salt of N,N-dinitramide anion and a biologically active cation.
- 62. A pharmaceutical formulation comprising a salt of N,N-dinitramide anion and a pharmacologically active cation in a pharmaceutically acceptable carrier.
- 68. A pharmaceutical formulation comprising (a) an ionizable compound that upon ionization gives a pharmacologically active cation, (b) an effective solubility enhancing amount of an N,N-dinitramide salt, and (c) a pharmaceutically acceptable carrier.
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74. A biologically active agent delivery system comprised of:
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(a) an N,N-dinitramide salt having the formula M+x[N(NO2)2−
]x wherein M is a cation selected from the group consisting of a metal ion and a nitrogen-containing ion, and x is the cationic charge of M; and
(b) an ionizable compound, wherein ionization of the compound results in a pharmacologically active cation. - View Dependent Claims (75, 76)
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Specification