Fluorometholone ophthalmic suspension

Details Fluorometholone ophthalmic suspension Fluorometholone ophthalmic suspension

2000-07-13

2001-09-11

Criares, Theodore J. (Department: 1617)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

C514S912000

Reexamination Certificate

active

06288049

ABSTRACT:

TECHNICAL FIELD
The present invention relates to improved compositions of an ophthalmic suspension containing fluorometholone, which is an anti-inflammatory synthetic adrenocorticosteroid, as an active ingredient.
BACKGROUND ART
Fluorometholone is a drug to be used for medical treatment as an anti-inflammatory steroid and is particularly widely used in the form of eye drops. Since fluorometholone is a drug which is hardly soluble in water, it is practically used in the form of ophthalmic suspensions. Since drugs are not dissolved in ophthalmic suspensions, it is necessary to shake the eye drop bottle in order to redisperse uniformly the settling and aggregating drug when the ophthalmic suspensions are used. Accordingly, a method of facilitating the redispersion is used wherein a nonionic surfactant such as polysorbate 80 is added to the ophthalmic suspensions.
The ophthalmic suspensions of fluorometholone are designed to improve redispersibility of the drug as mentioned above, but it is desirable to improve further the ophthalmic suspensions so that the redispersibility is much elevated and the drug can readily be dispersed uniformly. In the ophthalmic suspensions, it is also likely that the drug having been in a uniform dispersion state in preparation forms aggregates during preservation and the drug does not completely return to the original uniform dispersion state although the eye drops are shaken (irreversible aggregate formation). Accordingly, it is also desirable to improve the ophthalmic suspensions so as to reduce this aggregate formation.
SUMMARY OF THE INVENTION
As a result of precise studies to solve these problems, it was found that fluorometholone ophthalmic suspensions which are more excellent in redispersibility and hardly form aggregates are obtained by adding a nonionic surfactant and a cellulosic polymer. The nonionic surfactant works to improve the redispersibility of a drug, but it was difficult to prevent the drug sufficiently from forming aggregates with only the nonionic surfactant. As a result of studies of additives which reduce the aggregate formation of the drug, the cellulosic polymer was found to be appropriate. The cellulosic polymer exists among settled and concentrated drug particles and lowers contact frequencies of the particles, and thereby reducing the drug aggregation. However, adding only the cellulosic polymer causes problems that bubbles attached to the eye drop bottle are hard to remove and the redispersibility of the drug is lowered. The inventors found that it is possible to compensate for disadvantages of the nonionic surfactant and the cellulosic polymer and to develop advantages thereof by using these two in combination, and completed the present invention.
Studying also appropriate amounts of the nonionic surfactant and the cellulosic polymer, it was found that the amount of the nonionic surfactant is preferably 0.0001 to 0.5%, more preferably 0.001 to 0.1%, and the amount of the cellulosic polymer is preferably 0.0001 to 0.003%, more preferably 0.0005 to 0.002%. All percentages in the present invention mean W/V (%).
In general, the fluorometholone ophthalmic suspensions are used for medical treatment at a concentration of 0.02 to 0.1%. Accordingly, conducting the present invention, it is also preferable to prepare suspensions at this concentration, but the concentration is not limited to this range. The ophthalmic suspension of the present invention can be produced according to procedure of commercially available fluorometholone ophthalmic suspensions. Examples of the nonionic surfactant to be used in the present invention are polysorbate 80, polyoxyethylene hydrogenated castor oil, polyoxyethylene castor oil, polyoxyl 40 stearate and the like. Examples of the cellulosic polymer are hydroxypropylmethylcellulose, methylcellulose, hydroxypropylethylcellulose and the like. Additives widely used for an ophthalmic formulation, namely, a preservative such as benzalkonium chloride, an tonicity agent such as sodium chloride, a stabilizing agent such as disodium edetate, a buffer such as sodium hydrogenphosphate and the like, may be added to the ophthalmic suspension of the present invention besides the essential components, if necessary. The pH of the ophthalmic suspension can be preferably between 4 and 8, but it is not limited if pH is in a range widely used for an ophthalmic formulation.


REFERENCES:
patent: 5149693 (1992-09-01), Cagle et al.
patent: 59-130900 (1984-07-01), None
patent: 1-213228 (1989-08-01), None
patent: 8-295622 (1996-11-01), None
patent: 10-36253 (1998-02-01), None
patent: 11-29463 (1999-02-01), None

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