Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – 9,10-seco- cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
2000-10-03
2002-12-31
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
9,10-seco- cyclopentanohydrophenanthrene ring system doai
C514S168000, C514S474000, C514S912000
Reexamination Certificate
active
06500813
ABSTRACT:
TECHNICAL FIELD
The present invention relates to an ophthalmic composition and more specifically to an ophthalmic composition for treating patients suffering from intraocular inflammation, glaucoma and corneal degeneracy and for preventing any occurrence of hyperplasia of anterior ocular cells during the damaged tissue-healing process after operations thereof and/or for preventing, for instance, any reduction in transparency, any change in refractive power and any increase in intraocular pressure.
PRIOR ART
Rachitis is one of the osteopathy, and it has formerly been believed that the rachitis is closely related to the action of the sunlight. Thereafter, however, it has been found out that a certain vitamin is closely involved in the rachitis. This anti-rachitis vitamin is named vitamin D. Vitamin D
2
obtained by purifying vitamin D
1
which is a mixture with other isomers as well as vitamin D
3
discovered through the subsequent studies have widely been used in the treatments of many patients suffering from osteopathy such as rachitis, osteomalacia, osteoporosis, ostitis fibrous and osteosclerosis, malignant tumors such as breast cancer and carcinoma of large intestine, as well as dermatosis such as psoriasis. Vitamin D is an essential vitamin for the bone modeling and it is prescribed by the Ministry of Public Welfare of Japan that the required amount of this nutrient to be taken with foods is set at 200 IU (5 &mgr;g)/day. However, the required amount of the nutrient differs from that prescribed in foreign countries (i.e., 400 IU/day) because of the presence of vitamin D
3
which is produced in the skin by the action of ultraviolet light rays through sunbathing. In other words, it is necessary to take excess of vitamin D in case where sufficient sunbathing is not ensured. Vitamins D
2
to D
7
are classified as vitamins having rachitis-inhibitory activity, but presently used in the treatment of this disease are vitamin D
2
and vitamin D
3
having high physiological activity.
Vitamin D's are administered to patients per oral route or by injection. In case of skin diseases, they are also administered in the form of ointments. It has been known that the vitamin D undergoes a change in its molecular structure through the action of ultraviolet rays or in the liver and kidney and that it is thus converted into active vitamin D having high biological activities. It has been recognized that vitamin D's have not only calcium-regulatory effect, but also other biological activities since the discovery of the active vitamin D
3
, i.e., calcitriol (1&agr;,25-dihydroxy cholecalciferol) as a derivative of the cholecalciferol. As other derivatives or analogues of the cholecalciferol, there have been known, for instance, alpha-calcidol (1&agr;-monohydroxy cholecalciferol) and calcifedol (25-monohydroxy cholecalciferol). There have recently been known about 16 kinds of cholecalciferol derivatives. In addition, there have been developed several kinds of cholecalciferol analogues such as OCT (2-oxacalcitriol) and calcipotriol. The presence of active vitamin D receptors in cells have been discovered and there have been conducted studies on inhibition of cellular activities because of the ability of the active vitamin D's to control the production of various cytokines.
In the field of the ophthalmology, it has been known, as the symptoms caused due to vitamin deficiency, for instance, night blindness, Bitot's spots on conjunctiva, and xerophthalmia due to vitamin A deficiency; beriberi and weak eyesight because of vitamin B
1
deficiency; superficial punctate keratitis because of the vitamin B
2
deficiency (sometimes associated with retroocular neuropapillitis and optic atrophy); scorbutus due to the vitamin C deficiency (wherein there are often observed bleeding in eyelids, conjunctivae and retinae)
Dr. Ohashi et al. in Osaka University studied the inhibitory effect of vitamin D
3
against the expression of MHC class antigens in order to suppress any rejection observed during the keratoplasty and suggest that vitamin D
3
may serve to control the rejection of the transplantation of cornea (Bulletin of Ophthalmologic Society in Japan, 1990, Vol. 94, an extra edition, p. 250).
Japanese Un-Examined Patent Publication No. Hei 3-24016 discloses studies of cultivation of human glia cells wherein the ability of active vitamin D
3
to inhibit the proliferation of glia cells and also suggests that active vitamin D
3
may be applied to the treatment of patients suffering from proliferative retinopathy.
Japanese Examined Patent Publication No. Hei 4-43887 discloses that active vitamin D
3
is effective for the treatment of cataract such as congenital cataract, senile cataract, complicated cataract and diabetic cataract.
U.S. Pat. No. 5,254,538 discloses that vitamin D compounds are effective in healing of wounds and healing of a variety of ulcers.
The surgical operation with a scalpel has been employed for the correction of shortsightedness and astigmatisms, but this would adversely affect the visual power. For instance, the operated eye proceeds to the over correction after the operation and the incised site of the cornea becomes turbid or causes irregular reflection, which impair the visual acuity.
As laser device for operating cornea, there have been known an excimer laser and an Ho:YAG laser. The laser operations for cornea are divided into the operations for healing diseases and those for correcting the visual power.
Glaucoma is a disease in which a high intraocular pressure disease is caused due to excess production of the aqueous humor through the posterior chamber gonion or a trouble of flow paths for the aqueous humor in the anterior chamber gonion because of a certain intraocular disease and this leads to the visual field defect. Alternatively, the high intraocular pressure disease may sometimes be caused by a simple mechanical trouble of the flow paths for the aqueous humor in the anterior chamber gonion.
Corneal degeneracy (corneal dystrophy) is a disease in which heterogeneous proteins are mainly deposited on keratocytes due to the dysbolism of the corneal epithelial cells or keratocytes and this in turn leads to corneal haze/opacity. Examples of such corneal degeneracy include granular corneal degeneracy, porphyritic corneal degeneracy, cancellated corneal degeneracy, colloidal guttate corneal degeneracy, Schneider's corneal degeneracy and Francois' corneal degeneracy. On the other hand, corneal ulcer is a disease in which a collagenase is excessively produced by the corneal epithelial cells to thus form an ulcer. Accordingly, the corneal degeneracy and the corneal ulcer are quite different from one another in the etiological causes and clinical findings.
In a patient who has been subjected to an operation for incising the cornea using an excimer laser, there is observed, after the operation, the occurrence of hyperplasia of the cells at the inflamed corneal sites during the process for healing the damaged corneal tissues and further there are sometimes observed reduction in the degree of transparency and a change in the refractive power of the cornea due to the presence of cellular materials thus excessively produced. The normal corneal epithelium in general comprises about 5 layers, but when the traumatic injury reaches even the stroma of cornea and it is complicatedly damaged, the corneal epithelial cells covering the stroma may sometimes run up to about 10 layers. The damaged corneal cells undergo hyperplasia and produce metabolites such as collagen and proteins to thus restore the damaged tissue. The multilayered epithelium will return to the normal structure in the future, but the refractive power and the transparency of the cornea are influenced by the transient hyperplasia and the cellular materials produced by the epithelial cells as well as the stroma cells during the damaged tissue-healing process. Moreover, a steroid drug is administered after the operation for cornea using an excimer laser, but it has been known that this is accompanied by steroid
Ishii Yasuo
Itoh Seiji
Kita Kiyoshi
Mukai Katsuhiko
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