A water-soluble multi-use eyedrops composition for the treatment of dry eye syndrome containing rebamipide and a method for solubilization and stabilization thereof

摘要

The present invention relates to a water-soluble multi-dose eyedrop composition for treating dry eye syndrome comprising rebamipide, and a method for solubilizing and stabilizing the same. More specifically, the present invention relates to an eyedrop composition for treating dry eye syndrome which, by including a preservative and a chelating agent in a disposable water-soluble rebamipide-containing eyedrop, can remain stable without forming precipitates during storage, and is characterized by comprising ingredients that are safe to be used as a multi-dose eyedrop; and to a preparation method of the same. The eyedrop composition of the present invention is characterized by comprising a base for solubilizing rebamipide, a stabilizing agent for maintaining a stabilized supersaturated state, a preservative, a chelating agent for enhancing effects of the preservative, a buffer of a particular kind for keeping physiologically suitable pH in the range of 7-8, and an osmotic pressure regulator. The preparation method comprises: dissolving a preservative in water; adding a base to the water to dissolve rebamipide or a pharmaceutically acceptable salt thereof, and a stabilizing agent in the water, to produce a water-soluble eyedrop of pH 10-11; dissolving at least one osmotic pressure regulator selected from a buffer and a non-ionic osmotic pressure regulator in the eyedrop; after adjusting the eyedrop to pH 7-8, dissolving a chelating agent in the eyedrop; filtering the eyedrop by a syringe filter; and sterilizing the eyedrop. The eyedrop thus prepared is in the state of an aqueous solution; is stable at room temperature or when frozen or refrigerated; and is stable even when stored frozen or at room temperature.