STABILIZED FORMULATION OF ALPHA ADRENERGIC RECEPTOR ANTAGONISTS AND USE THEREOF

摘要

PROBLEM TO BE SOLVED: To provide a stable liquid formulation containing an α adrenergic receptor antagonist for increasing blood flow.

SOLUTION: The stable liquid formulation includes the α adrenergic receptor antagonist having pH in the range of 2.0 to 6.0 and a low dose, an aqueous solvent, and a metal chelating agent. The α adrenergic receptor antagonist is selected from the group consisting of phentolamine, phentolamine hydrochloride, mesylic acid phentolamine, tolazoline, yohimbine, rauwolscine, doxazosin, labetalol, prazosin, terazosin, trimazosin and any pharmaceutically permitted salt thereof, and particularly phentolamine mesylate is preferable. The metal chelating agent is preferably selected from the group consisting of diammonium ethylenediamine triacetate, hydroxyethyl-ethylenediamine triacetic acid, diethylenetriamine pentaacetic acid, nitriloacetic acid, citric acid and EDTA.

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