Ophthalmic solution containing diquafosol, method for producing same, and method for preventing formation of insoluble precipitate

Abstract

An ophthalmic solution containing diquafosol to which a chelating agent is added, wherein the formation of an insoluble precipitate during storage and a lowering in filtration performance in a production process (a filtration / sterilization process), said insoluble precipitate formation and said lowering in filtration performance being observed in conventional ophthalmic solutions containing diquafosol, are inhibited. It is also confirmed that the ophthalmic solution containing diquafosol to which a chelating agent is added shows an improved ability to retain the effect during storage. Therefore, the present invention provides an ophthalmic solution containing diquafosol, said ophthalmic solution having stable physicochemical properties in the course of production, distribution and storage by a patient, in particular, enabling efficient filtration / sterilization in the production process, and, moreover, having an excellent ability to retain the effect during storage. Also, the present invention provides a method for preventing the formation of an insoluble precipitate from an aqueous ophthalmic solution containing diquafosol or a salt thereof, said method comprising adding a chelating agent to the aqueous ophthalmic solution.

Description

technical field [0001] The invention relates to an eye drop and a preparation method thereof. The eye drop is an aqueous eye drop containing diquafosol (Diquafosol) or its salt at a concentration of 0.1-10% (w / v) (hereinafter referred to as Simply called "diquafosol ophthalmic solution"), the ophthalmic solution suppresses the generation of insoluble precipitates by containing a chelating agent. In addition, the present invention also relates to a method for suppressing generation of insoluble precipitates from an aqueous eye drop containing diquafosol or a salt thereof by adding a chelating agent to the aqueous eye drop. Background technique [0002] Diquafosol is a purinergic receptor agonist, also known as P 1 , P 4 - Di(uridine-5') tetraphosphate or Up 4 U, as disclosed in Patent No. 3652707 (Patent Document 1), is known to have an effect of promoting tear secretion. In addition, Cornea, 23(8), 784-792(2004) (Non-Patent Document 1) discloses that by administering eye...

AI Technical Summary

Problems solved by technology

Especially for eye drops that generate precipitates during distribution or storage by patients, since the precipitates cannot be removed afterwards, they are not ideal as eye drops

In addition, when precipitates are generated during the preparation process, although the precipitates can be removed during the process of filter sterilization of the eye drops, the efficiency of filter sterilization will be deteriorated due to clogging of the filter filter during filtration. Issues such as increased preparation costs

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