Abstract: Compounds of formula I ##STR1## and compounds of formula Ia ##STR2## and their physiologically tolerated salts, processes for their preparation and drugs and cosmetics prepared therefrom.

Abstract: This invention relates to an intraocular irrigating composition containing a compound of the following formula or a pharmacologically acceptable salt thereof ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a methyl group.The glutathione derivative contained in the intraocular irrigating solution of this invention is not only effective in protecting the intraocular tissues on the occasion of ophthalmic surgery but effectively inhibits precipitation of the calcium contained. Therefore, the intraocular irrigating solution of this invention is very stable and can be used with advantage in various kinds of ophthalmic surgery such as cataract surgery and transplantation of the cornea, iris and vitreous body.

Abstract: A device for pinpoint application of micro-quantities of a pharmacologically suitable composition to the outer hard coat of the eye, comprises a micro-container with a fixation element. The micro-container comprises a bore whose aperture is adapted to contact the eye surface, and the fixation element is adapted for reversibly adhering to the eye surface.

Abstract: A carboxyvinyl polymer having Newtonian viscosity, ophthalmic preparations containing the polymer, a process for preparing the polymer, and a vehicle for ophthalmic preparations containing the polymer. By using the polymer in a vehicle, an ophthalmic preparation having a low viscosity and a desirable permeability of a drug can be obtained.

Abstract: Reversibly gelling aqueous and oil emulsions are disclosed which can be modified to incorporate oil soluble pharmaceutical compounds for delivery to physiological systems in a soluble form and which undergo significant changes in viscosity in response to substantially simultaneous changes in both temperature and pH. The compositions are formed of relatively low concentrations of a stable combination of at least one pH-sensitive reversibly gelling polymer, at least one temperature-sensitive reversibly gelling polymer and at least one organic oil. The compositions can be formulated to exhibit a sol-gel transition over a wide range of conditions and viscosities and may be modified to incorporate a pharmaceutical compound for utilization as droppable or injectable drug delivery systems which will gel following administration to a physiological system for the sustained delivery of such pharmaceutical compounds.

Abstract: Low-tension glaucoma is treated by topical administration to the eye of an amount of a calcium channel blocking agent effective to increase blood flow to the optic nerve head. Calcium channel blocking agents of Class I are especially useful, and among these a preferred agent is verapamil hydrochloride.

Abstract: Ischemic disorders of the retina and associated tissues of the posterior segment of the eye are treated by topical administration to the eye of an amount of a calcium channel blocking agent effective to increase blood flow to those tissues. Calcium channel blocking agents of Class I are especially useful, and among these a preferred agent is verapamil hydrochloride.

Abstract: Disclosed is a sustained release liquid aqueous ophthalmic delivery system and a method of providing a slow and sustained release of ophthalmic treating agents to the eye of a mammal which comprises administering to the eye of a said mammal an effective amount of a homogeneous liquid aqueous ophthalmic pharmaceutical composition, of pH between about 3.0 and about 6.2, which is adminstrable in drop form and which comprises an ophthalmically effective concentration of a said ophthalmic treating agent and about 0.05% to about 10% by weight of the polymer chitosan; said polymer consisting essentially of(A) monomeric .beta.(1.fwdarw.4)-D-glucosamine linked units and of(B) monomeric .beta.(1.fwdarw.

Abstract: A topical composition comprising an amount of a carbonic anhydrase inhibitor and an amount of .beta.-cyclodextrin derivative effective in increasing the bioavailability of the carbonic anhydrase inhibitor when coadministered topically to the eye.

Abstract: Double-substituted, water-soluble, cellulose ethers substituted with a cationic substituent and a hydrophobic substituent are disclosed. The levels of substitution for the cationic substituent and the hydrophobic substituent can provide enhanced properties when used in personal care compositions, such as, for example, enhanced substantivity, saline capability and low irritation potential to mucosal linings.

Abstract: An ophthalmologic gel is disclosed having a viscosity in the range of about 10,000 to about 50,000 mPa.s and comprising (1) about 0.05 to about 3% by weight of one or more polyacrylates and (2) about 0.1 to about 10% by weight one or more water-soluble, physiologically compatible polymers selected from the group consisting of polyvinyl alcohol, dextran, and mixtures thereof.

Abstract: Aqueous solutions for treating inflammations of the eye, comprising: from about 0.03-3 weight percent of piroxicam; an effective amount of a buffer; from about 0 to about 1 weight percent of a wetting agent; from about 0 to about 5 weight percent of a pH adjusting agent; from about 0 to about 5 weight percent of a tonicity agent; an effective amount of a preservative; from about 0 to about 3 weight percent of a demulcent polymer; from about 0 to about 40 weight percent of a complexing agent; and from about 0 to about 0.1 weight percent of a stabilizer; and having a pH between about 7 and about 10.

Abstract: Cationic polysaccharide polymers and anionic therapeutic agents delivery systems are disclosed which have been found to be substantive to mucosal surfaces. The present delivery system is well suited for the delivery of anionic ophthalmic pharmaceuticals.

Abstract: A method for measuring precorneal tear film stability and diagnosing dry and wet eye conditions. The method comprises stressing baseline visual acuity with the installation of a predetermined ophthalmic preparation and measuring the time to recover normal visual acuity. Once baseline visual acuity is regained and sustained, the Lacrimal Equilibration Time (LET) is recorded. LET measures the quality of precorneal tear film stability and is related to the degree of dry and wet eye condition.

Abstract: Aqueous ophthalmic compositions containing water-soluble borate-polyol complexes are useful in aqueous ophthalmic compositions containing polyvinyl alcohol. These compositions provide the benefits of a borate buffering system, such as enhanced antimicrobial activity, without the problems associated with the use of borate and pol, such as formation of borate-polyvinyl alcohol complexes which are water-insoluble.

Abstract: A composition for treating a Sjoegren syndrome disease is disclosed. The composition comprising derivative of spirooxathiolane-quinuclidine of the following formula (I), ##STR1## wherein Z is .dbd.CR.sup.1 R.sup.2, wherein R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen, alkyl, cyclopentyl, cyclohexyl, aryl, diarylmethylol, or alkyl which may be substituted by one or more aryl groups, or an acid addition salt thereof, or an acid addition salt thereof, as an effective component. Especially effective is an administration of a hydrochloric acid addition salt of 2-methylspiro(1,3-oxathiolane-5,3')quinuclidine.

Abstract: An ophthalmologic composition therapeutic in the treatment of dry eye syndrome is disclosed. The composition is comprised of a minimally soluble salt of calcium that has been finely divided into particles having a mean diameter of 10 to 60 microns. The calcium salt particles are suspended within a pharmacologically acceptable carrier such as petrolatum or physiological saline. The composition is delivered to the ocular surface in an amount and for a time sufficient to alleviate the symptoms of dry eye.

Abstract: A method for treating a body condition comprising introducing an aqueous solution of a water soluble polyether polyurethane into said body condition.

Abstract: Reversibly gelling aqueous compositions are disclosed which undergo significant changes in viscosity in response to substantially simultaneous changes in both temperature and pH. The compositions are formed of relatively low concentrations of a stable combination of at least one pH-sensitive reversibly gelling polymer and at least one temperature-sensitive reversibly gelling polymer. The compositions can be formulated to exhibit a sol-gel transition over a wide range of conditions and viscosities and may be modified to incorporate a pharmaceutical compound for utilization as droppable or injectable drug delivery systems which will gel following administration to a physiological system for the sustained delivery of such pharmaceutical compounds.

Abstract: Disclosed is a liquid ophthalmic composition of unique rheological and lubricating properties comprising, inter alia, a polyanionic polymer for use as a long lasting artificial tear. Also disclosed is a method of treatment comprising topically administering the composition when indicated for relief of dry eye syndrome, foreign body sensation, burning, hyperemia, corneal staining, and the like.

Abstract: Two solutions capable of gel formation are simultaneously or successively applied to the mucous membrane of the eye for the purpose of treating diseases of the eye.

Abstract: An ophthalmic formulation comprising a salt of sepazonium or a similar imidazolium compound as a preservative is provided.

Abstract: Lightly crosslinked polymers, preferably ones prepared by suspension or emulsion polymerizing at least about 90% by weight of a carboxyl-containing monoethylenically unsaturated monomer such as acrylic acid with from about 0.1% to about 5% by weight of a polyfunctional, and preferably difunctional, crosslinking agent such as divinyl glycol (3,4-dihydroxy-1,5-hexadiene), having a particle size of not more than about 50 .mu.m in equivalent spherical diameter, when formulated with an ophthalmic medicament, e.g., fluorometholone, into suspensions in aqueous medium in which the amount of polymer ranges from about 0.1% to about 6.5% by weight, based on the total weight of the aqueous suspension, the pH is from about 3.0 to about 6.

Abstract: The invention relates to the use of dodecyl-dimethyl-(2 phenoxyethyl)-ammonium bromide as an antimicrobial agent to be a preservative for ophthalmic drug solutions, in disinfecting solutions, as well as in preservatives for aqueous ocular solutions for contact lenses.

Abstract: Vitronectin produces very high therapeutic effects upon injuries of the corneal epithelium. When applied to lesions of the corneal epithelium in the form of eye drops, Vitronectin induces rapid cure of the lesions with regeneration of normal cells. Moreover Vitronectin can be sterilized by autoclaving.

Abstract: Glycosaminoglycan polysulfates (GAGPS) have been found to be useful in ophthalmic medications in the prevention and treatment of eye injuries. Particularly useful are GAGPS having a molecular weight in the range of 5,000-20,000 daltons. GAGPS-containing ophthalmic medications are usefully combined with an antibiotic in the treatment of ocular fungal or bacterial infections or with an antibiotic in the treatment of fungal or bacteria infections or with an anti-glaucoma agent, such as pilocarpine or epinephrine, in the treatment of glaucoma. Also, of particular usefulness are GAGPS solutions or dispersions used to enhance healing after corneal abrasion or surgical insult.

Abstract: Disclosed is an ophthalmic gel composition of unique rheological and lubricating properties comprising, inter alia, a carboxy vinyl polymer (carbomer) for use as a long lasting artificial tear. Also disclosed is a method of treatment comprising totally administering the composition when indicated for relief of dry eye syndrom, foreign body sensation, burning, hyperemia, corneal straining, and the like.

Abstract: This invention relates to an improved viscoelastic fluid or gel for use in surgery and other therapies which consists of polyethylene oxide in selected concentrations not to exceed approximately 15% (15,000 ppm), contained in a physiologic balanced salt solution. The PEO may also be used in conjunction with viscosity enhancers which also act as heat stabilizers such as methylcellulose and its derivatives, polyvinyl pyrrolidone of polyvinyl alcohol or in conjunction with elasticizes such as low molecular weight polyethylene glycols or polypropylene glycols or in conjunction with gelation modifiers. These mixtures may be modified to increase retention time in the body by crosslinking with the use of material like dimethyl urea.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or methyl, A is an ethylene or methylene radical which is unsubstituted or substituted by methyl, hydroxyl or oxo, L is a saturated or unsaturated five-membered or six-membered heterocyclic structure which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.6 -alkyl, or C.sub.1 -C.sub.4 -alkanoyl and has from 1 to 3 heteroatoms from the group consisting of N, O and S, the second and third heteroatoms being a nitrogen atom,R.sup.3 is hydrogen, a hydroxy or C.sub.1 -C.sub.6 -alkoxy group,R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen or methoxy,R.sup.5 is hydrogen or methoxy or tert-butyl,R.sup.6 is hydrogen, methyl, nitrile or a C.sub.2 -C.sub.10 -ketal group or the radical --CHR.sup.7 OR.sup.8 --CHR.sup.7 --NR.sup.9 R.sup.10, --COR.sup.11, --SR.sup.12, ##STR2## in which R.sup.7 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.8 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.

Abstract: Improved healing of wounds, particularly wounds of the eye, such as keratorefractive surgical incisions, is obtained by coating the wound surfaces with a solution containing a protein crosslinking compound such as dimethyl pimelimidate dihydrochloride, followed by treatment with a composition containing an extracellular matrix material such as fibronectin, a biologically active fragment or an analog thereof.

Abstract: The present invention contemplates a treatment for ocular inflammation.More particularly, one aspect of the present invention relates to a method of reducing, inhibiting or preventing ocular inflammation in a mammal which comprises administering to said mammal an effective amount of matrine or a derivative thereof.Another aspect of the present invention is directed to a pharmaceutical composition useful in reducing, inhibiting or preventing ocular inflammation in a mammal comprising an effective amount of matrine or a derivative thereof and a pharmaceutically acceptable carrier.Yet another aspect of the present invention contemplates a method of inducing ocular analgesia and a pharmaceutical composition useful for same.

Abstract: The present invention concerns a pharmaceutical and/or cosmetic composition designed to be applied on the skin or the mucosae, characterized in that it contains Rhamsan gum.

Abstract: This invention relates to an improved viscoelastic fluid or gel for use in surgery and other therapies which consists of polyethylene oxide in selected concentrations not to exceed approximately 15% (15,000 ppm), contained in a physiologic balanced salt solution. The PEO may also be used in conjunction with viscosity enhancers which also act as heat stabilizers such as methyl cellulose and its derivatives, polyvinyl pyrrolidone or polyvinyl, alcohol or in conjunction with elasticizers such as low molecular weight polyethylene glycols or polypropylene glycols or in conjunction with gelation modifiers. These mixtures may be modified to increase retention time in the body by crosslinking with the use of materials like dimethylol urea.

Abstract: An ophthalmic solution comprising 0.1 to 0.9 % volume of povidone iodine in association with a suitable ophthalmic carrier. The solution is useful in treating various ophthalmic disorders such as follicular conjunctivitis and giant papillary conjunctivitis resulting from reaction to contact lenses, cosmetics and allergies among others. It is also useful in the treatment of ocular dryness resulting from post menopausal stage and from Sjogren's disease.

Abstract: Topical ophthalmic compositions containing microfine particles of one or more retinoids are described. The compositions are useful in the treatment of dry eye syndrome and related ophthalmic surface disorders and as ocular lubricants. A method of treating dry eye syndrome and related ophthalmic surface disorders and a method of providing topical ocular lubrication using these compositions are also described.

Abstract: An ophthalmic surgical procedure wherein the anterior or posterior chamber of the eye is filled with viscoelastic space-filling and ocular tissue protective surgical material, the improvement comprising the utilization therein of a composition particularly adapted for use as an ophthalmic viscoelastic surgical material in the anterior or posterior chamber of the eye consisting of an aqueous solution containing from about 1.5% to about 25%, by weight, of a physiologically acceptable, water-soluble polyvinylpyrrolidone polymer or polyvinylpyrrolidone copolymer, having a molecular weight greater than 500,000, said aqueous solution having a viscosity greater than about 5,000 centipoises, measured at 25.degree. C. using a Brookfield viscometer.

Abstract: The invention disclosed is a composition and method for the slow sustained ocular delivery of a prophylactic agent contained in liposome vesicles. The liposome vesicles are composed of phospholipid and cholesterol in a molar ratio of phospholipid to cholesterol of 8:2 to 1:1. Preferably, stearylamine is included in the liposome composition.

Abstract: An inventive method for preventing ultraviolet radiation exposure to the outer tissues of mammalian eyes is disclosed. In particular, the composition containing about 0.3%-0.4% hydroxypropylmethylcellulose in the form of either an eyedrop solution or an ointment is applied to the eyes prior to exposure to UV radiation.

Abstract: An ophthalmic preparation and a method for preparing the ophthalmic preparation is described. The ophthalmic preparation has an enhanced ability to permit essentially normal maintenance of ocular surface mucus-containing goblet cells while present in the eye.

Abstract: There is provided a stable, ophthalmic aqueous composition for topical administration, comprising (a) acetazolamide and either (b) a pre-formed, pharmaceutically acceptable, aqueous gel or (c) an aqueous gel-forming liquid capable of forming a pharmaceutically acceptable gel in situ when applied topically to a patient; said composition having a pH of less than 5.0.

Abstract: A synergistic combination of an aqueous solution of a partially hydrolyzed poly(vinyl acetate) and a fully hydrolyzed poly(vinyl acetate), i.e. poly(vinyl alcohol), exhibiting a low surface tension at the water-air interface, while forming a completely wettable absorbed layer over hydrophobic solids. The combination is used as part of an ophthalmic solution including a hydrophilic low viscosity polymer, poly(N-glucose) or poly(N-vinyl pyrrolidone) with higher than normal oncotic pressure in a physiologically compatible electrolytic solution base. The formulation is effective in treating the two major underlying causes of the dry eye syndrome; ocular surface disorder and tear film abnormalities resulting in tear film instability. It can also be effective as an aqueous vehicle for topically used ophthalmic drugs or nutrients.

Abstract: A method and preparation for the stimulation of tear secretion. The method involves topically applying to the ocular surface melanocyte stimulating hormones, and their active precursors, derivatives, and fragments which activate melanotropin receptors of lacrimal gland tissue. The preparation contains a melanocyte stimulating hormone, and a vehicle for a melanocyte stimulating hormone and may also contain an ophthalmic preservative.

Abstract: The present invention relates to a pharmaceutical composition intended for contacting with a physiological liquid characterized in that said composition is intended to be administered as a non-gelled liquid form and is intended to gel in situ, this composition containing at least one polysaccharide in aqueous solution, of the type which undergoes liquid-gel phase transition gelling in situ under the effect of an increase in the ionic strength of said physiological liquid.

Abstract: The present invention provides a method of treating an aqueous-deficient dry eye state in a patient suffering therefrom, which method includes the step of administering cyclosporin topically to the patient's eye. The cyclosporin is administered as a solution, suspension or ointment in a pharmaceutically acceptable excipient.

Abstract: Topical ophthalmic compositions containing one or more retinoids selected from the group consisting of near and remote analogues and derivatives of retinoic acid are described. Six classes of ophthalmic vehicles suitable as carriers for the retinoids are also described. The compositions are useful in the treatment of dry eye syndrome and related ophthalmic surface disorders and as ocular lubricants. A method of treating dry eye syndrome and related ophthalmic surface disorders and a method of providing topical ocular lubrication using these compositions are also described.

Abstract: Ophthalmic compositions useful as tear stimulants when topically applied to the eye for effective treatment of dry eye syndrome.

Abstract: A liposome composition useful in the treatment of dry eye. The composition includes an aqueous suspension of liposomes whose lipid composition preferably includes about 70-85 mole percent of hydrogenated phosphatidylcholine, and 15-30 mole percent of benzyldimethylstearylammonium chloride. The suspension is stable on storage at room temperature for several months.

Abstract: A novel mutant microorganism Streptococcus zooepidemicus HA-116 ATCC 39920, has been produced. The microorganism produces large amounts of high molecular weight hyaluronic acid. The invention provides a method of obtaining such microorganisms.The invention also concerns a method of obtaining sodium hyaluronate which comprises growing with vigorous agitation a microorganism of the genus Streptococcus under appropriate conditions in a suitable nutrient medium containing a sugar component as a carbon source. The sugar component is present in a substantially constant concentration between 0.2 and 10 grams per liter. The medium has a substantially constant pH between about 6.0 and 7.5 and includes a substantially constant magnesium ion concentration above 0.05 grams per liter. The sodium hyaluronate excreted into the medium by the organism is purified using methods involving precipitation, redissolving and reprecipitating the hyaluronate.

Abstract: An ophthalmic preparation and a method for preparing the ophthalmic preparation is described. The ophthalmic preparation has an enhanced ability to permit essentially normal maintenance of ocular surface mucus-containing goblet cells while present in the eye.

Abstract: An ophthalmic solution for improving the exchange of fluid in the area outside a hydrogel contact lens with the fluid in the area underneath the hydrogel contact lens comprising:(a) 0.0005% by weight to an amount of a hydrogel contact lens flattening agent equivalent to 330 milliosmoles/kg;(b) an amount of a viscosity enhancing agent sufficient to cause the composition to have a Brookfield relative viscosity of 3 to 50 cps; and(c) an amount of an ionic salt sufficient to render the solution substantially isotonic.The invention also includes a method for improving the exchange of fluid in the area outside a hydrogel contact lens with the fluid in the area underneath the hydrogel contact lens in a human eye comprising adding to said eye an effective amount of such ophthalmic solutions.