Abstract: An O/W emulsion composition comprising fluorometholone or clobetasone butyrate, a phospholipid, an oil, a nonionic water-soluble cellulose derivative, and water. The O/W composition has advantages that fluorometholone or clobetasone butyrate contained therein is highly bioavailable and that the solubility of fluorometholone or clobetasone butyrate and the concentration thereof present in the composition can be kept stable. Thus, this composition is usable for the treatment of various inflammatory diseases by the generalized or local administration thereof. It provides a drug which shows an anti-inflammatory activity equal or higher than that of commercially available eye drops comprising a suspension of such an active ingredient even when it is applied in a smaller dose than that of commercially available one and further provides a drug having excellent storability, which reduces apprehension of systemic side effects of fluorometholone or clobetasone butyrate when it is applied to the eyes.

Abstract: Ophthalmic compositions and methods of using the same to simultaneously treat eye surface inflammation and dry eye are disclosed. The ophthalmic preparation contains a tetracycline compound in aqueous solution. The preparation preferably further includes a balance of electrolytes sufficient to maintain or restore essentially normal levels of conjunctival mucus-containing goblet cells and corneal glycogen. These electrolytes can include potassium, chloride, bicarbonate, sodium, calcium, magnesium and phosphate.

Abstract: Methods for treating post-surgical formation of cataracts or posterior capsule opacification are disclosed. The methods utilize compositions containing certain compounds having an anti-inflammatory and anti-oxidant moiety covalently linked by and amide and ester bond.

Abstract: Aqueous ophthalmic preparations are provided and are intended to be instilled into the eye, or in which to pre soak or store an object to be inserted into the eye, such as a contact lens, an ointment, or a solid device to be inserted into the conjunctival sac. The preparations disclosed are utilized for the treatment of a tear film and ocular surface disorder known as keratoconjunctivitis sicca or dry eye syndrome. In general, the preparations of this invention are also effective for the relief of symptoms of eye irritation, such as those caused by dry environmental conditions or by contact lens wear. In accordance with the present invention, the ophthalmic preparation includes a mucin component, similar to that found at the normal human ocular surface and in one exemplary and preferred embodiment, the mucin is a transmembrane or surface mucin.

Abstract: HETE salts, the preparation of HETE salts, the preparation of stable and efficacious HETE compositions, HETE compositions and methods of use for treating dry eye are disclosed.

Abstract: A method and composition for altering a plausible sequence of pathological events in retinal ganglion cells associated with glaucoma, the sequence including membrane depolarization, influx of millimolar amounts of Na+ via non-inactivating Na+ chanels, and the lethal elevation of cell Ca2+ due to reversal of the Na+/Ca2+ exchanger. The method includes blocking, by administration of a selected composition, of associated, non-inactivating Na+ channels in retinal ganglion cells in order to limit Na+/Ca+ exchange in the retinal ganglion cells and prevent buildup of the Ca2+ level in the retinal ganglion cells to a lethal level. The results in a method of preventing retinal ganglion cell death, associated with glaucoma, by administering to the optic nerve of a mammal, a compound which blocks the non-inactivating sodium ion channels of the optic nerve.

Abstract: A method and composition for altering a plausible sequence of pathological events in retinal ganglion cells associated with glaucoma, the sequence including membrane depolarization, influx of millimolar amounts of Na+ via non-inactivating Na+ channels, and the lethal elevation of cell Ca2+ due to reversal of the Na+/Ca2+ exchanger. The method includes blocking, by administration of a selected composition, of associated, non-inactivating Na+ channels in retinal ganglion cells in order to limit Na+/Ca+ exchange in the retinal ganglion cells and prevent buildup of the Ca2+ level in the retinal ganglion cells to a lethal level. The results in a method of preventing retinal ganglion cell death, associated with glaucoma, by administering to the optic nerve of a mammal, a compound which blocks the non-inactivating sodium ion channels of the optic nerve.

Abstract: Topical ophthalmic anti-allergy drugs are identified by the extent of their interaction with a phospholipid model membrane. Disclosed are topically administrable ophthalmic formulations containing amphipathic anti-allergy compounds at concentrations such that the drugs have Surface Activity Ratings from about 2-11.

Abstract: An ophthalmic formulation is disclosed which reduces dilation in dim light and reduces redness.

Abstract: The invention relates to the use of tricyclic nitrogen heterocycles of general formula I as pharmaceutical compositions with an inhibitory effect on PDE IV, wherein the groups R1, R2 and R3 have the meanings given in the specification and claims.

Abstract: A nanoemulsion, the oil globules of which have an average size of less than 100 nm, comprising an anionic surfactant chosen from alkyl ether citrates and at least one oil having a molecular weight of greater than 400, the ratio by weight of the amount of oily phase to the amount of surfactant ranging from 2 to 10. The emulsion obtained is transparent and stable on storage. It can comprise large amounts of oil while retaining good transparency and while having good cosmetic properties. It can constitute a composition for topical use, a pharmaceutical composition or an ophthalmological composition. The invention also relates to the use of the nanoemulsion according to the invention in the cosmetics and dermatological fields, in particular for moisturizing the skin and/or mucous membranes, as well as for treating the hair, and in the ophthalmological field, as an eye lotion for treating the eyes.

Abstract: A device, methods and pharmaceutical compositions are disclosed for transnasal or transocular drug delivery to the central nervous system using a combination of electrotransport or phonophoresis with chemical permeation enhancers.

Abstract: A method for increasing or decreasing parasympathetic/cholinergic/ciliary tonic contraction in order to restore the resting portion of the eye and allow normal positive and negative accommodation includes administering to a myopic or hyperopic presbyope.

Abstract: A composition for treatment of bacterial infections of the eye is disclosed which comprises a lytic enzyme composition specific for the infecting bacteria, and a carrier for delivering said lytic enzyme. The carrier for delivering at least one lytic enzyme to the eye may be but is not limited to the use of an isotonic solution.

Abstract: The present invention relates to a neovascularization inhibitor comprising as the active ingredient N-(3,4-dimethoxycinnamoyl) anthranilic acid represented by the formula: or a pharmaceutically acceptable salt thereof, which has inhibitory effects on proliferation and chemotaxis of human microvascular endothelial cells and tube formation of human microvascular endothelial cells, and therefore, is useful as an agent for the prevention and treatment of diseases associated with neovascularization such as diabetic retino senile discoid macular degeneration, neovascular glaucoma and rheumatic arthritis.

Abstract: The ophthalmic composition of this invention are used for treatment of diabetic corneal lesion and/or for treatment of deteriorated corneal esthesia, which comprises, as an active ingredient, a compound represented by the general formula (I): wherein A and B are independently lower alkylene, X, Y, and Z are independently halogen, or a pharmacologically acceptable salt thereof. In addition, the ophthalmic composition of this invention are used for treatment of non-diabetic corneal lesion, for treatment of dry eye syndrome, and/or for treatment of hypolacrimation which comprises, as an active ingredient, an aldose reductase inhibitor. The ophthalmic compositions of this invention are effective for treatment of at least one disease selected among corneal lesion, deteriorated corneal esthesia, dry eye syndrome, and hypolacrimation.

Abstract: Isoquinolinesulfonyl compounds are used in ophthalmic compositions to treat glaucoma or other ischemic-borne ocular disorders such as retinopathies or optic neuropathies. These compounds vasodilate ocular blood vessels, lower IOP and prevent or reduce the progression of visual field loss.

Abstract: The present invention is directed to ophthalmic compositions containing a gelling amount of a combination of galactomannan polysaccharides and borates. The compositions gel or partially gel upon administration to the eye. The present invention also discloses methods of topical ophthalmic administration of the compositions of the eye.

Abstract: This invention relates to the compositions and methods for the treatment of corneal haze. The compositions and methods are particularly directed to the use of GAG synthesis inhibitors in the treatment of corneal haze.

Abstract: The present invention is directed to a method for the prophylactic treatment of cataract. The method involves the administration of a compound of Formula I wherein V, W and X are selected from the group consisting of hydro, hydroxyl, alkoxy, halo, an ester, an ether, a carboxylic acid group, a pharmaceutically acceptable salt of a carboxylic acid group, and —SR, in which R is hydrogen or an alkyl group, Y is selected from the group consisting of oxygen, sulfur, C(OH), and C═O, and Z is selected from the group consisting of hydro and C(O)OR1, wherein R1 is an alkyl, or an analogue or prodrug thereof or a pharmaceutically acceptable salt of any of the foregoing to an animal, such as a mammal, in particular a human, in an amount sufficient to treat cataracts prophylactically. The compound of Formula I is preferably genistein.

Abstract: The invention concerns an ophthalmic composition comprising a beta-blocker solution, said composition being obtained by dissolving in water beta-blocker in the presence of alginic acid and adding an alkaline base, to obtain a solution with the PH of 6 to 8. Said composition has a sustained duration of action.

Abstract: Low potency, preservative free sterile topical anti-inflammatory steroid compositions are to be applied to the area surrounding the eye. The compositions involve, for example, sterile gauze pads in a sterile package, as well as single-use capsules and tubes for dispensing the medicinal composition.

Abstract: The present invention is related to the use an ophthalmic composition comprising ketotifen in the preparation of an eye medicament for the treatment allergic conjunctivitis of contact lens wearers.

Abstract: Water soluable taurine derivatives, and methods of synthesizing, formulating, and using such taurine derivatives for treating or protecting the retina of a mammalian eye. The invention includes treatment methods which comprise contacting with the retinal tissue, a therapeutically effective amount of retinyliden tauret (3,7-dimethyl-9-(2,6,6-trimehyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraen-1-imido-(N-ethane sulfonic acid)). The invention also includes methods for synthesizing two (2) specific isomers of retinyliden tauret, namely (A) all-trans-[3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraen-1-imido-(N-ethane sulfonic acid)] and (B) 11-cis-[3,7-dimethyl-9-(2,6,6-trimehyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraen-1-imido-(N-ethane sulfonic acid)]. Also included are formulations and methods for administering such compounds to the retina of a mammalian eye to treat or prevent the progression of retinopathy.

Abstract: Medicinal compositions for treating eye diseases which contain as the active ingredient 2-alkynyladenosine derivatives having an acetylene union at the 2-position of adenine base. Having a long-lasting and remarkable effect of lowering ocular tension, these compositions are useful as remedies for eye diseases accompanying increased ocular tension or optic nerve failures, such as glaucoma and hypertonia oculi.

Abstract: A novel drug for improving the circulation in the optic nerve head, which comprises as an active ingredient Lomerizine (I): or a pharmaceutically acceptable acid addition salt. The optic nerve head circulation improving drug of this invention can increase the blood flow in the optic nerve head with no or little systemic side effects such as hypotensive activity or heart rate increasing activity and is useful particularly for the treatment of normal tension glaucoma.

Abstract: A pharmaceutical composition is provided which comprises an isotonic solution of an 0.02% mixture of di- and trisodim salts of echinochrome (Histochrome). It meets the requirements that apply to injectable formulations. Histochrome administration to human patients normalizes metabolic processes and eliminates inflammation in the retina, vascular membrane and cornea of the eye, improves trophic functions, reduces edema and accelerates epithelization.

Abstract: The instant invention provides a method of inhibiting the formation of metalloproteinase and its species, within the eyes of a patient inflicted with at least one form of retinitis characterized by the presence of metalloproteinase, through the administration of an effective dosage that includes an a tetracycline analog, its salts, conjugates or derivatives. In an alternate preferred embodiment of the invention, the dosage includes at least one other therapeutic substance in effective combination with a tetracyline analog.

Abstract: Macrolide compounds, such as the FK506 Substance and its related compounds, are provided for the prevention or treatment of eye diseases, particularly glaucoma. Composition containing such compounds is also disclosed.

Abstract: Use of flunarizine, a calcium channel blocking agent known for use as cerebral and peripheral vasodilator, in the treatment of glaucoma by topical administration. Differently from other calcium channel blockers already tested for use as antiglaucoma agents, flunarizine is highly active in lowering the intraocular pressure when administered by the topical ophthalmic route. The invention also comprises anti-glaucoma preparations containing flunarizine, or combinations of flunarizine with beta-blockers such as timolol.

Abstract: A pharmaceutical formulation may be prepared by a method comprising providing the active ingredient in solution in a pharmacologically-acceptable base and mixing the resulting solution with a pharmacologically-acceptable acid in an amount such that the formulation attains a pH in the range of from about 3.5 to about 8.5 to thereby precipitate out the active ingredients, a viscosity-enhancing agent having been incorporated in the formulation prior to or during the mixing with acid. The formulation is suitable for administration of a pharmacologically active ingredient which is sparingly soluble in water at a pH acceptable for administration, for example to the eye of the patient.

Abstract: Glutamate causes migration and proliferation of retinal pigment epithelium and/or glial cells, and glutamate antagonists can prevent, treat or reduce retinal pigment epithelium and/or glial migration and the subsequent development of proliferative vitreoretinopathy. Avoidance or management of proliferative vitreoretinopathy can be achieved by administering to the patient a compound capable of reducing glutamate-induced retinal cell migration in a concentration effective to reduce such migration.

Abstract: The present invention relates to a secondary cataract inhibitor comprising as the active ingredient N-(3,4-dimethoxy-cinnamoyl)anthranilic acid represented by the formula: or a pharmaceutically acceptable salt thereof, which has an inhibitory activity on posterior capsule opacification formation after cataract surgery and is useful for the prevention or treatment of secondary cataract.

Abstract: Topically administrable anti-allergy compositions comprising olopatadine and a polymeric quaternary ammonium preservative are suitable for use by patients wearing contact lenses.

Abstract: Proliferation of retinal pigment epithelium following surgery or trauma or resulting in ocular diseases associated with choroidal neovascularization, such as age related macular degeneration and histoplasmosis syndrome, is prevented by contacting retinal pigment epithelium cells with a therapeutic amount of a retinoic acid receptor (RAR agonist, preferably one with specific activity for retinoic acid receptors. Preferably the RAR agonist is also a potent antagonist of AP1-dependent gene expression. Alternatively, the proliferation of retinal pigment epithelium is ameliorated with a therapeutic amount of an AP-1 antagonist, alone or in combination with an RAR agonist. The drug can be administered by bolus injection into the vitreous cavity using a dosage from about 50 to 150 &mgr;g. Or by slow release from liposomes or an oil tamponade injected into the vitreous cavity. Formulations for preventing proliferation of retinal pigment epithelium are also provided.

Abstract: A controlled release medicament delivery system comprises a plasticized bioerodible polymer, such as a polyorthoester. Medicament desirably is entrapped in the plasticized polymer. The resulting delivery system is able to release the medicament in a controlled and sustained manner. The formulation is particularly advantageous for use as a once-a-day eyedrop. During preparation, the polymer may be heated to an elevated temperature for a sufficient time to substantially reduce its molecular weight.

Abstract: Ophthalmic composition for use in ocular surgery comprises an aqueous solution of sodium hyaluronate with a concentration within the range of 18-40 mg sodium hyaluronate/ml solution and the molecular mass of sodium hyaluronate being in the range of 1×106-10×106<M>r,M. In a method for conducting ocular surgery, the composition is introduced into the eye as a surgical aid. The composition may be used in a method for conducting cataract surgery.

Abstract: The present invention is directed to a biguanide-containing disinfecting solution containing tyloxapol in combination with a poloxamine for stabilizing the biguanide, which is especially useful for contact-lens solutions that provide enhanced disinfecting and enhanced cleaning efficacy. The method of the present invention comprises cleaning and disinfecting a contact lens with the above-described solution.

Abstract: The use of agents for blocking the synthesis of tyrosinase to prevent permanent pigmentation of the iris caused by melanin deposit induced by pharmacological treatments or by metabolic imbalance is described.

Abstract: Suspension formulations containing dexamethasone and ciprofloxacin are disclosed. The formulations contain a nonionic polymer, a nonionic surfactant and an ionic tonicity agent, but are physically stable and easily re-suspended. The formulations are intended for topical application to the eye, ear or nose.

Abstract: Phospholipid-HETE derivatives, compositions and methods of use are disclosed. The compounds are particularly useful for treating dry eye.

Abstract: Topically administrable aqueous solution compositions containing tobramycin and xanthan gum are disclosed. The solution compositions contain a buffering agent and a pH-adjusting agent in an amount sufficient to achieve a pH above 7.8 in order to minimize or avoid compatibility problems between tobramycin and xanthan gum.

Abstract: A method of increasing glutathione levels in mammalian cells comprising administering an oral bolus of encapsulated pharmaceutically stabilized glutathione in a rapidly dissolving formulation to a mammal on an empty stomach. Pharmaceutical formulations including glutathione are also disclosed.

Abstract: Pharmaceutical compositions and a method are disclosed for treating glaucoma and/or ocular hypertension in the mammalian eye by administering to the mammalian eye the pharmaceutical composition of the invention which contains as the active ingredient one or more compounds having calcium chelating activity. Examples of calcium chelating agents utilized in the pharmaceutical composition and method of treatment are: and lower alkyl and alkoxyalkyl esters thereof. Also disclosed are methods and compositions for delivering a drug within the cytoplasm of a cell having cell surface acetylcholinesterase or acetylcholinesterase receptors, wherein the compositions comprise an apolar prodrug joined to an acetylcholine ester or psuedoacetylcholine group.

Abstract: A preparation suitable for sustained and extended corneal analgesia and for repeated administration consisting of subanesthetic concentrations of lidocaine. A method for corneal analgesia by administering to a patient an ophthalmic analgesic solution containing lidocaine in subanesthetic 0.4% concentration.

Abstract: The invention relates to pharmaceutical compositions of antimicrobial effect as well as a process for the preparation thereof. The pharmaceutical compositions of the invention comprise zinc or cobalt hyaluronate associate (complex) as active ingredient in admixture with a carrier and/or other additives commonly used in the pharmaceutical industry.

Abstract: Methods of using prostaglandin agonists for the reduction of intraocular pressure, and accordingly glaucoma.

Abstract: Compositions and methods for the treatment of dry eye and related diseases utilizing EP4 receptor agonists are disclosed.

Abstract: A method is disclosed of preventing retinopathy of prematurity in a prematurely born neonate susceptible to developing retinopathy of prematurity, which comprises the step of parenterally administering to said prematurely born neonate, a therapeutically effective amount of a water-soluble, pharmaceutically effective salt of ibuprofen as an active ingredient to promote retinal and choroidal blood flow autoregulation in said neonate.

Abstract: Disclosed is the use of cloprostenol and fluprostenol analogues in combination with carbonic anhydrase inhibitors for the treatment of glaucoma and ocular hypertension and ophthalmic compositions therefor.