Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1998-02-03
2000-10-17
Dees, Jose' G.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424427, 424428, A61F 200, A61F 1300
Patent
active
061327514
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to an O/W emulsion composition for eye drops. More specifically, the present invention relates to an O/W emulsion composition for eye drops which comprises a drug selected from the group consisting of fluorometholone, clobetasone butyrate and clobetasol propionate, a phospholipid, liquid paraffin and water and which is excellent in solubility of fluorometholone, clobetasone butyrate and clobetasol propionate in the tear fluid.
BACKGROUND ART
Fluorometholone, clobetasone butyrate and clobetasol propionate used in the present invention are synthetic adrenocortical hormones each exhibiting a strong anti-inflammatory action and, in particular, fluorometholone and clobetasone butyrate are drugs effective for treating inflammatory diseases at external-ocular and anterior-ocular sites. However, these drugs are hardly soluble in water and therefore, it is impossible to dispense these drugs like the usual aqueous eye drops. For this reason, fluorometholone and clobetasone butyrate have been used in ophthalmology in the form of an aqueous suspension prepared by pulverizing crystals of each drug into fine particles and dispersing and suspending the particles in an appropriate amount in an aqueous solution for eye drops, but these aqueous suspensions suffer from problems such that they are bad in feeling when they are applied to the eyes and that the fine particles thereof precipitate and solidify at the bottom of the container thereof, as a result, they are never redispersed uniformly even if the suspension is vigorously shaken. Moreover, solubility of crystal particles of fluorometholone and clobetasone butyrate in the tear fluid is low and therefore, the bioavailability thereof is also low.
In general, drugs hardly soluble in water have been solubilized therein by the use of various kinds of surfactants or other additives having effects similar to those of the surfactants. However, such additives used in commercially available eye drops as medical additives have been limited to those having relatively weak solubilization ability from the viewpoint of safety. Therefore, it is difficult to solubilize drugs hardly soluble in water such as fluorometholone, clobetasone butyrate and clobetasol propionate in an amount effective for preparing pharmaceutical preparations thereof. Under such circumstances, there has been proposed a method in which fluorometholone is included in dimethyl-.beta.-cyclodextrin to thus enhance the solubility thereof in water [Japanese Un-Examined Patent Publication (hereinafter referred to as "J. P. KOKAI") No. Sho 59-130900] and a method in which clobetasone butyrate is included in heptakis(2,6-di-O-methyl)-.beta.-cyclodextrin to thus enhance the solubility thereof in water(J. P. KOKAI No. Sho 61-129115), but such methods have not yet been put into practical use.
On the other hand, there have been disclosed O/W emulsion compositions each of which comprises a drug, an oil, a phospholipid and a surfactant (J. P. KOKAI No. Hei 5-186333 and WO 94/05298) as prior arts concerning vehicles for instilled drugs hardly soluble in water 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.
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REFERENCES:
patent: 4419352 (1983-12-01), Cox et al.
patent: 4670185 (1987-06-01), Fujiwara et al.
patent: 4789667 (1988-12-01), Makino et al.
Hirata Reiko
Maeda Makoto
Nagoshi Kaei
Naito Yoshikazu
Oguma Touru
Dees Jos,e G.
Shelborne Kathryne E.
Wakamoto Pharmaceutical Co., Ltd.
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