Fenoldopam formulations and pro-drug derivatives

摘要

Formulations of fenoldopam are disclosed for repeated administration or continued slow release administration, over prolonged periods of time or targeted slow and regulated delivery. The formulations include those formulations that increase the bioavailability of fenoldopam after oral intake, particularly lipid based nano dispersions and pronanodispersions and surfactant rich formulations. This may be accomplished by entrapment in nanoparticles or liposomal formulations or conjugation to a polymer or small molecule via a soft bond.

主权项

1. A non-infusion pharmaceutical formulation, comprising a composition formulated for delivery of fenoldopam or a derivative of fenoldopam to the human body, which comprises particles of a size of about 5 to 500 nm in an aqueous medium, comprising:
(i) at least one surfactant; (ii) at least one solid component which is a solid at room temperature; (iii) an amphiphilic solvent; and (iv) a compound of the formula wherein either (i) R, R′, R″ and R′″ are H or (ii) R, R′ and R″ are the same or different residues that form an electrostatic salt with the phenolate anion, a metal ion or organometallic molecules that form a complex with one or more phenolic groups, or an organic residue covalently bound to the phenolic residue via a bio-cleavable ester or carbonate bond, and R′″ is a specific residue that forms an electrostatic salt with the amine, a metal ion or atom or an organic residue covalently bound to the amino residue via a bio-cleavable amine, amide, or urea bond.