Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
2000-01-05
2002-05-28
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C514S912000
Reexamination Certificate
active
06395721
ABSTRACT:
FIELD OF THE INVENTION
The herein disclosed invention finds applicability in ophthalmology and dermatology. More specifically, the invention relates to compositions for application to inflamed tissue surrounding the eye.
BACKGROUND OF THE INVENTION
Pruritic, inflamed eyelids are a common clinical presentation to the dermatologist and ophthalmologist. Common causes of eyelid dermatitis are atopic dermatitis, contact dermatitis, contact urticaria, seborrheic dermatitis and psoriasis. An important treatment for each of these conditions is the use of topical corticosteroids. The ideal formulation for eyelid dermatitis treatment is not currently available.
Several ophthalmic ointments are disclosed in Chemical Abstracts:
Sirbu et al—Chemical Abstracts Vol. 100: abstract 56870; (1982) discloses a veterinary ophthalmic ointment for treating keratconjunctivitis containing hydrocortisone, lidocaine, lanolin and white petrolatum.
Dorsey—Chemical Abstracts Vol. 110 abstract 121459e (1989) shows a corticosteroid composition containing a corticosteroid, peppermint oil, urea, lanolin, propylene glycol and petrolatum used to treat eczematous dermatitis.
Tuomi et al—Chemical Abstracts Vol. 114 abstract 192384v (1990) teaches corticosteroid formulations containing hydrocortisone and propylene glycol creams.
Zilberman et al—Chemical Abstracts Vol. 84 abstract 140734b teaches an eye ointment containing hydrocortisone, kanamycin, lanolin and petrolatum, paraffin and paraffin oil.
Maistrello et al—Chemical Abstracts Vol. 80 abstract 22968a (1974) teach corticosteroids for application to the eye.
While the prior art teaches the application of corticosteroids to the eye, the prior art fails to teach sterile, non-preserved low potency corticosteroid ointments applied to the eye.
The inventors do not profess to be the first to dispense a sterile medication, for example, sterile ampoules are conventional dispensing means. However, the invention is directed to the novel means of applying for dermatitis of the eye a single dosage lower potency steroid ointment in a sterile preservative free ointment base.
SUMMARY OF THE INVENTION
This invention has as an object the preparation of ophthalmic ointments which do not inflame the delicate tissue surrounding the eye.
Another object is the preparation of ophthalmic ointments which do not produce an allergic response.
A further object is to produce simple formulations of sterile, preservative-free lower potency corticosteroid ophthalmic ointments.
A further object is to produce an easy to package and easy to use ophthalmic composition.
A still further object of this invention is to produce a sterile, preservative-free low-potency topical steroid ophthalmic product.
These and other objects of the present invention will become apparent from a reading of the following specification.
This invention contemplates the use of lower potency anti-inflammatory steroids. Steroid compositions have been rated on a scale of 1 to 7, with 7 being the least potent. (In this regard see Cornell and Stoughton, Dermatol. Clin. Vol. 2 (1984), pages 397-409 and Stoughton and Cornell, Semin. Dermatol Vol. 6 (1987, pages 72-76). The fluorinated steroids are generally rated among the most potent steroids, for example, Betamethasone and Clobetasol. Among the least potent steroids are non-fluorinated steroids, for example, desonide, cortisone, hydrocortisone, hydrocortisone butyrate, hydrocortisone valerate and aldomethasone diproprionate.
Because the skin around the eye is sensitive, non-fluorinated steroids will be used because fluorinated steroids would tend to adversely affect the skin around the eyes.
At times, higher concentrations of steroids may unduly irritate the skin around the eye and lower concentrations of steroid, e.g., 1% or even less, are at times contemplated by this invention.
In its broadest sense the disclosed invention is directed to a lower potency, preservative free anti-inflammatory steroid in a simple ointment base. The composition is designed to be therapeutically effective, while at the same time minimizing or eliminating any potential adverse side effects; particularly the skin around the eyes.
The anti-inflammatory steroids of this invention are classes 3-7 and preferably 4-7 topical steroids. The super fluorinated steroids (classes 1 and 2) tend to be too potent and irritating to the eye. In addition, super fluorinated steroids (classes 1 and 2) are not desirable for use because these steroids, after long use, tend to cause cataracts and accelerate glaucoma.
The thin structure of the eyelid and proximity to the eye make higher potency (super fluorinated) steroids less than ideal for the treatment of eyelid dermatitis. Further, high potency steroids increase the risk to the skin, for example, thinning and atrophy. In addition, high potency steroids increase the risk to the eye of cataract formation and glaucoma. Preserved medications increase the risk of both contact allergy and direct toxic effects to the eyelid and the eye. Currently available commercial preparations of corticosteroid ointments marketed for ophthalmic use, are not preservative-free, and are all generally high potency fluorinated steroids. Commercial dermatologic preparations, while available as low potency non-fluorinated corticosteroid are preserved and non-sterile.
Among the prescribed corticosteroid ophthalmic ointment preparations are dexamethasone sodium phosphate (AK-Dex by Akorn Pharmaceuticals, Decadron Sterile Ophthalmic Petrolatum by Merck and Maxidex by Alcon) and fluoromethalone ophthalmic ointment (FML S.O.P. by Allergan). The above ophthalmic preparations are fluorinated. (See the Ophthalmic PDR, 1995)
Dermatologic formulations available as low potency non-fluorinated corticosteroids include various strengths of hydrocortisone base or acetate, which are all non-sterile and preserved. These and other low potency topical steroid preparations are listed in the Monthly Prescribing Reference, January 1996. The current invention is intended to overcome the shortcomings of the presently available corticosteroid formulations.
The current invention would fulfill an important niche for some of the more common oculo-dermal problems confronting both the ophthalmologist and dermatologist, as well as the primary care physician. The present invention is expected to provide a new therapeutic modality for the clinician.
There exists a major crisis in topical formulation of corticosteroids for the treatment of acute and chronic diseases of the skin around the eyes. There is no preservative free, hypoallergenic, sterile preparation available to treat common and uncommon dermatosis present in the periocular region. The concern is that the periocular or eyelid skin is one of the thinnest, and most sensitive areas of the human body and cannot withstand currently available commercial topical corticosteroid formulations as they contain noxious preservatives and alcohols that adversely affect the very condition that is to be treated. In addition to the lack of preservative free topical steroids for periocular use, there are no pure topical steroids that are sterile. Dermatitis, such as seborrheic dermatitis (a very common disorder currently treated), if treated with the currently commercially available preparations could induce an irritant affect due to their preservatives or introduce an infection into the eye due to their non-sterile nature.
The skin of the eyelids is the thinnest in the body as described in Ophthalmology Principles and Concepts—author F. W. Newell—fourth edition—1978—(pages 49 and 50)The C. V. Mosby Company.
The inventors have found that, in view of the special sensitivity of the skin around the eye, a particularly mild ointment, based together with a low potency steroid preparation provide the ideal vehicle and medicament for application to the skin around the eye. In view of the particular sensitivity of the skin around the eye to allergic influences, the disclosed invention avoids the use of preservatives. Because of skin-sensitivity around the eye, applicants have limited the nu
Martin Neil F.
Robinson Howard N.
Bloom Leonard
Bloom Leonard
Fay Zohreh
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