Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – 9,10-seco- cyclopentanohydrophenanthrene ring system doai
Patent
1998-02-12
2000-12-19
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
9,10-seco- cyclopentanohydrophenanthrene ring system doai
514912, A61K 3159
Patent
active
061628018
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
1. Field of Invention
This invention relates to ophthalmic or dermatological compositions for external use, and more specifically, to such external medicines when used for the purpose of mediating healing of injured ocular tissue or treating ophthalmic diseases with ophthalmic compositions containing vitamin D (ergocalciferol or cholecalciferol), or for the purpose of protecting ocular tissue or skin from harmful ultraviolet rays with ophthalmic or dermatological compositions containing vitamin D or vitamin K.
2. Description of the Related Art
Vitamin D2, which is refined from vitamin D1 containing other isomers and is highly antirachitic, and vitamin D3, which was researched after vitamin D2, are often used today for the treatment of patients suffering from rickets, osteomalacia, osteoporosis, osteatis fibrosa, osteosclerosis and other bone diseases, malignant tumors such as breast and colon cancers, and skin diseases such as psoriasis. In general, the term "vitamin D" by itself is used to refer to highly antirachitic vitamin D2 (ergocalciferol) and vitamin D3 (cholecalciferol).
In general, the ultraviolet (UV) light absorption spectra of vitamin D and active vitamin D have absorption maxima near 265 nm, with molar absorption coefficients of about 18,000. Their UV light absorption bands are in the 240-290 nm range. For example, ergocalciferol, 25-monohydroxyvitamin D2, 1alpha,25-dihydroxyvitamin D2, 24,25-dihydroxyvitamin D2 and others have UV light absorption spectra with maxima near 265 nm, and molar absorption coefficients of about 18,900. In addition to these vitamins, provitamin D and previtamin D also have similar UV light absorption spectra. The provitamins D ergosterol and 7-dehydrocholesterol have respective molar absorption coefficients of 11,000 and 10,920, and UV light absorption spectra with maxima at 271, 281 and 293 nm. The previtamins D pre-ergocalciferol and pre-cholecalciferol both have molar absorption coefficients of 9,000 and UV light absorption spectra with absorption maxima at 260 nm.
Therapeutic vitamin D is administered orally or by injection, and is applied to the skin as an active vitamin D ointment in the case of skin conditions. It is known that the molecular structure of vitamin D is altered in the liver and kidneys, converting it into biologically active vitamin D. Hitherto it has been thought that the topical human use of the vitamins D ergocalciferol or cholecalciferol was useless for the treatment of local tissue, as for the treatment of psoriasis, for example.
Since the discovery of calcitriol (1alpha,25-dihydroxycholecalciferol), an active form of vitamin D which is derived from cholecalciferol, it has come to be understood that vitamin D has physiological actions other than calcium regulation. Active vitamins D formed by hydroxylation of the C1 position of the A-ring of the sterol nucleus, side-chain C25 or both C1 and C25 include calcitriol (1alpha,25-dihydroxyvitamin D), 1alpha,24-dihydroxyvitamin D, alfacalcidol (1alpha-monohydroxyvitamin D), calcifediol (25-monohydroxyvitamin D), 1alpha,24,25-trihydroxyvitamin D, 1beta,25-dihydroxyvitamin D, oxacalcitriol, calcipotriol and KH1060. Analogues include dihydrotachysterol. It is now known that there are active vitamin D receptors in the cells, and the inhibition of cell activity is being studied since active vitamin D inhibits the production of a variety of cytokines.
The known ophthalmic symptoms of vitamin deficiency include nyctalopia, Bitot's spots of the conjunctiva and xerosis of the conjunctiva and cornea resulting from vitamin A deficiency, beriberi amblyopia resulting from vitamin B1 deficiency, and diffuse superficial keratitis, retrobulbar neuritis and optic atrophy occurring in cases of vitamin B2 deficiency, as well as hemorrhaging of the eyelid, conjunctiva and retina which are seen in cases of scurvy resulting from vitamin C deficiency.
Hyperplasia occurs in the cells of the keratitis site during the process of wound recovery in postoperative corneal surgery patients, and in s
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