Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1985-05-14
1987-02-10
Roberts, Elbert L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
A61K 3156
Patent
active
046423052
DESCRIPTION:
BRIEF SUMMARY
The present invention is concerned with an eye drops composition containing estradiol-17beta in a dissolved or crystalline form for the treatment of chronic eye catarrh, that is chronic conjunctivitis simplex.
Chronic catarrh of the ocular conjunctiva is a condition common in middle-aged and elderly persons, especially in postmenopausal women (ages above about 45-50). Such a catarrh is apt to cause a great deal of discomfort to the patient. The eyes feel dry, "gritty" and irritated, which is a disagreeable condition, even though it does not really imply any serious damage to the eyes. As regards drug preparations for treating this condition, the preparations used up till now have generally been found to be inefficient. In certain cases some degree of alleviation may be obtained with agents having a weak cauterizing and/or decongestant effect. Also, ointments, having a lubrication effect, or viscous preparations capabel of forming a thin protective film over the eye may occasionally decrease the symptoms.
We have now found, in accordance with the present invention, that an effective means of treating chronic eye catarrh disorders is an eye drops composition containing estradiol17beta in a therapeutically active and physiologically acceptable amount.
Oral administration of estrogen has been suggested by Holly et al in Surv. Ophthalmol 22(2) (1977) 69-87 for treatment of keratoconjunctivitis sicca, that is a different type of eye disorder.
The hormone estradiol-17beta as a crystalline powder is almost insoluble in water. In our eye drops composition this hormone compound may be present in a crystalline, microcrystalline or dissolved state. We have found a suitable particle size to be one within the range of 1 to 25 micrometers, preferably 2 to 10 micrometers. The desired particle size and size distribution of the bulk of the particle mass, i.e. at least 90% thereof, can be obtained by mechanical working, such as e.g. grinding, followed by one or more screening steps. The mechanical procedure chosen should preferably be one that gives substantially smooth particle surfaces, to thus avoid frictional damage on the tissues of the eye. In view of the fact that there is only a very small space available in the conjunctiva for accommodating lacrimal fluid and eye drops, the amount of active compound, that can actually be administered, will depend largely on the concentration of the compound in the composition. The upper limit of concentration is set by the risk of an undesired increase of the hormone level in the blood, with a concomitant undersired systemic effect. In our experience this means, as applied to the case where estradiol-17beta is administered in a particulate form, that its concentration should not exceed about 0.05% by weight. A lower limit would be in this case around 0.005% by weight.
As mentioned above estradiol-17beta is almost insoluble in water, so, if this hormone is to be administered in a dissolved state, it has to be dissolved in a medium suitable therefor. Substances, which have been known for a long time to be solvents for steroid hormone compounds of this type, are for instance solutions of cyclodextrins. A number of cyclodextrin compounds have been described; for example, dimethyl beta-cyclodextrin is said to have advantageous properties for forming inclusion complexes with e.g. estrone (DE No. 3118218). It is imperative that the solvent chosen--whether this be a solution containing cyclodextrin, a derivative thereof or some other solvent--should be one, that does not to any substantial degree reduces the effect of the hormone. It is also imperative of course that neither the solvent nor the hormone-solvent complex should be liable to produce undersirable reactions in the eye. In these cases, preferred concentrations are within the range of from 0.001 to 0.01% by weight.
The composition according to the present invention is a sterile aqueous solution containing estradiol-17beta in a particulate or dissolved form. In addition the composition may contain such components as are known and co
REFERENCES:
patent: 4186184 (1980-01-01), Zaffaroni
hman Lena
Johansson Elof
Pharmacia AB
Philpitt Fred
Roberts Elbert L.
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