Title:  O/W emulsion composition for eye drops

United States Patent:  6,132,751

Assignee:  Wakamoto Pharmaceutical Co., Ltd. (Tokyo, JP)

Filed:  February 3, 1998

PCT NO:  PCT/JP96/02187

102(e) Date:  February 3, 1998

PCT PUB. Date:  February 20, 1997

Foreign Application Priority Data:  Aug 04, 1995[JP] (7-218307)

An O/W emulsion composition for eye drops comprises a drug selected from the group consisting of fluorometholone, clobetasone butyrate and clobetasol propionate; a phospholipid; liquid paraffine; and water. The O/W emulsion composition is excellent in solubility of fluorometholone, clobetasone butyrate and clobetasol propionate in the tear fluid. Therefore, the composition would exhibit an anti-inflammatory activity identical to or superior to those achieved by the conventional pharmaceutical preparations, by the administration thereof at a dose lower than those for these known drugs. The composition would also be excellent from the economical standpoint and permit reduction of systemic side effects which would be encountered when the conventional drugs are instilled in the eyes.

DISCLOSURE OF THE INVENTION

The present invention has been developed for solving the problems associated with the conventional techniques for solubilizing, in water, drugs hardly soluble in water and therefore, an object of the present invention is to provide a novel composition for eye drops which is excellent in solubility of fluorometholone, clobetasone butyrate and clobetasol propionate in the tear fluid. The inventors of this invention have conducted intensive studies to accomplish the foregoing object, have found out that an O/W emulsion composition which comprises one drug selected from the group consisting of fluorometholone, clobetasone butyrate and clobetasol propionate, a phospholipid, liquid paraffin and water permits the considerable improvement in solubility of fluorometholone, clobetasone butyrate and clobetasol propionate in the tear fluid and thus have completed the present invention.

More specifically, the present invention relates to an O/W emulsion composition which comprises one drug selected from the group consisting of fluorometholone, clobetasone butyrate and clobetasol propionate, a phospholipid, liquid paraffin and water. In the composition of the present invention, solubility of fluorometholone, clobetasone butyrate and clobetasol propionate in the tear fluid can be controlled by appropriately adjusting the mixing ratio of the components of the composition. The fluorometholone, clobetasone butyrate or clobetasol propionate-containing O/W emulsion composition according to the present invention can effectively be used, in the form of an eye drop, for the treatments of various ocular diseases, for instance, inflammatory diseases of external- and anterior-ocular sites such as blepharitis, conjunctivitis, keratitis, scleritis, episcleritis, iritis, iridocyclitis and uveitis as well as inflammatory diseases developed after ocular operations.

Claim 1 of 21 Claims

What is claimed is:

1. An O/W emulsion composition for eye drops, consist essentially of a drug selected from the group consisting of fluorometholone, clobetasone butyrate and clobetasol propionate; a phospholipid; liquid paraffin; and water.

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