Composition containing a substance showing a topical effect on the eye, and a method of preparing the same

Claim 2

CONTRIBUTES TO PREVENTING MECHANICAL IRRITATION OF THE EYE AS A RESULT OF THE SHAPED BODY AND PREVENTS THE BODY FROM REMAINING IN A SPECIFIC POSITION IN THE EYE CAVITY, SINCE IT ENABLES THE UNIT TO CHANGE POSITION WITHIN THE CAVITY.

Claim 3

A composition according to claim 1, wherein the aliphatic monoalcohol is 1-tridecanol, 1-hexadecanol, 1-octadecanol or 1-dodecanol or mixtures thereof.

Claim 4

forms a diffusion barrier for the drug or drugs for glaucoma therapy and therewith prevents a topical overdose with subsequent accompanying irritation, and

Claim 5

forms a diffusion barrier for the drug or drugs for glaucoma therapy and therewith prevents a topical overdose with subsequent accompanying irritation, and

Claim 6

FORMS A DIFFUSION BARRIER FOR THE DRUG OR THE DRUGS FOR GLAUCOMA THERAPY AND THEREWITH PREVENT A TOPICAL OVERDOSE WITH SUBSEQUENT ACCOMPANYING IRRITATION, AND

Claim 7

FORMS A DIFFUSION BARRIER FOR THE DRUG OR THE DRUGS FOR GLAUCOMA THERAPY AND THEREWITH PREVENT A TOPICAL OVERDOSE WITH SUBSEQUENT ACCOMPANYING IRRITATION, AND

Claim 8

forms a diffusion barrier for the drug or drugs for glaucoma therapy and therewith prevents a topical overdose with subsequent accompanying irritation, and

Claim 9

forms a diffusion barrier for the drug or drugs for glaucoma therapy and therewith prevents a topical overdose with subsequent accompanying irritation, and

Claim 10

forms a diffusion barrier for the drug or drugs for glaucoma therapy and therewith prevents a topical overdose with subsequent accompanying irritation, and

Claim 11

forms a diffusion barrier for the drug or drugs for glaucoma therapy and therewith prevents a topical overdose with subsequent accompanying irritation, and

Claim 12

forms a diffusion barrier for the drug or drugs for glaucoma therapy and therewith prevents a topical overdose with subsequent accompanying irritation, and

Claim 13

forms a diffusion barrier for the drug or drugs for glaucoma therapy and therewith prevents a topical overdose with subsequent accompanying irritation, and

Claim 14

is free from difficulties with vision caused by ointment spread to the corneus tunic of the eye.

Claim 15

is free from difficulties with vision caused by ointment spread to the corneus tunic of the eye.

Claim 16

is free from difficulties with vision caused by ointment spread to the corneus tunic of the eye.

Claim 17

is free from difficulties with vision caused by ointment spread to the corneus tunic of the eye.

Claim 18

is free from difficulties with vision caused by ointment spread to the corneus tunic of the eye.

Claim 19

is free from difficulties with vision caused by ointment spread to the corneus tunic of the eye.

Claim 20

A composition according to claim 1 wherein the solid shaped body has a largest dimension lying between the limits 2 and 20 mm.

Claim 21

IS FREE FROM DIFFICULTIES WITH VISION CAUSED BY OINTMENT SPREAD TO THE CORNEUS TUNIC OF THE EYE.

Claim 22

IS FREE FROM DIFFICULTIES WITH VISION CAUSED BY OINTMENT SPREAD TO THE CORNEUS TUNIC OF THE EYE.

Claim 23

is free from difficulties with vision caused by ointment spread to the corneus tunic of the eye.

Claim 24

is free from difficulties with vision caused by ointment spread to the corneus tunic of the eye.

Claim 25

A composition according to claim 1 wherein the solid shaped body has a largest dimension lying between the limits 6 and 16 mm.

Claim 26

A composition according to claim 1 wherein at least one surface of the solid shaped body is convex.

Claim 27

A composition according to claim 1 wherein the drug for glaucoma therapy comprises pilocarpine, adrenalide, physostigmine or synstigmine or salts thereof, either separately or in combination.

Claim 28

A composition according to claim 1 wherein the substance showing a mydriatic effect is metaoxedrin or atropin or therapeutically acceptable salts thereof.

Claim 29

A composition in the form of a solid lens-shaped body having at least one curved surface and softly rounded corners which is adapted for insertion into the cavity between the eye and surrounding tissue, said shaped body retaining its shape during the whole time of use and containing a substance having a topical effect on the eye, which composition comprises a mixture of a. 10 - 45 percent of at least one lipophilic substance having a melting point of 37* - 75*C and being selected from the group consisting of higher hydrocarbons, waxes, fats and mixtures thereof, b. 10 - 30 percent of at least one water-soluble or water-swellable polymer in solid, finely-divided form and being selected from the group consisting of dextran, lower hydroxy-alkyl dextran, carboxymethyl dextran, lower hydroxy-alkyl cellulose, lower alkyl cellulose, carboxy-methyl cellulose, polyvinyl alcohol, dextrin, starch, polyvinyl pyrrolidone and polyalkylene glycols, the particle size of the solid polymer being less than approximately 150 microns. c. 0.5 - 20 percent of at least one substance having a topical effect on the eye, being in solid, finely-divided form with a particle size less than approximately 150 microns, and being selected from the group consisting of drugs for glaucoma therapy and substances showing a mydriatic effect, d. 10 - 50 percent of at least one member of the group consisting of aliphatic monoalcohols having 13 - 22 carbon atoms to serve as stabilizer for the mixture, the percentages relating to percent by weight calculated on the total weight of the mixture, whereby when said solid shaped body is inserted in an eye cavity and comes into contact with tear fluid, the polymer set forth in (b) which comes into contact with the tear fluid dissolves into a viscous solution or gel-like envelope that acts as a lubricating envelope, which, in cooperation with the shape of the unit

Claim 30

A composition in the form of a solid lens-shaped body having at least one curved surface and softly rounded corners which is adapted for insertion into the cavity between the eye and surrounding tissue, said shaped body retaining its shape during the whole time of use and containing a substance having a topical effect on the eye, which composition comprises a mixture of a. 10 - 45 percent of at least one lipophilic substance having a melting point of 37* - 75*C and being selected from the group consisting of higher hydrocarbons, waxes, fats and mixtures thereof, b. 10 - 30 percent of at least one water-soluble or water-swellable polymer in solid, finely-divided form and being selected from the group consisting of dextran, lower hydroxy-alkyl dextran, carboxymethyl dextran, lower hydroxy-alkyl cellulose, lower alkyl cellulose, carboxy-methyl cellulose, polyvinyl alcohol, dextrin, starch, polyvinyl pyrrolidone and polyalkylene glycols, the particle size of the solid polymer being less than approximately 150 microns. c. 0.5 - 20 percent of at least one substance having a topical effect on the eye, being in solid, finely-divided form with a particle size less than approximately 150 microns, and being selected from the group consisting of drugs for glaucoma therapy and substances showing a mydriatic effect, d. 10 - 50 percent of at least one member of the group consisting of aliphatic monoalcohols having 13 - 22 carbon atoms to serve as stabilizer for the mixture, the percentages relating to percent by weight calculated on the total weight of the mixture, whereby when said solid shaped body is inserted in an eye cavity and comes into contact with tear fluid, the polymer set forth in (b) which comes into contact with the tear fluid dissolves into a viscous solution or gel-like envelope that acts as a lubricating envelope, which, in cooperation with the shape of the unit

Claim 31

In the art of medicating the eye with ophthalmic medication the improvement which consists of the step of placing beneath one eyelid a solid lens-shaped body having at least one curved surface and softly rounded corners which is adapted for insertion into the cavity between the eye and surrounding tissue, said shaped body retaining its shape during the whole time of use and containing a substance having a topical effect on the eye, which composition comprises a mixture of a. 5 - 60 percent of at least one lipophilic substance having a melting point of 37* - 75*C and being selected from the group consisting of higher hydrocarbons, waxes, fats and mixtures thereof, b. 5 - 40 percent of at least one water-soluble or water-swellable polymer in solid, finely divided form and being selected from the group consisting of dextran, lower hydroxy-alkyl dextran, carboxymethyl dextran, lower hydroxy-alkyl cellulose, lower alkyl cellulose, carboxy-methyl cellulose, poLyvinyl aclochol, dextrin, starch, polyvinyl pyrrolidone and polyalkylene glycols, the particle size of the solid polymer being less than approximately 150 microns, c. 0.05 - 30 percent of at least one substance having a topical effect on the eye, being in solid, finely-divided form, with a particle size less than approximately 150 microns, and being selected from the group consisting of drugs for glaucoma therapy and substances showing a mydriatic effect, d. 10 - 80 percent of at least one member of the group consisting of aliphatic monoalcohols having 13 - 22 carbon atoms, to serve as stabilizer for the mixture, the percentages relating to percent by weight calculated on the total weight of the mixture, whereby when said solid shaped body is inserted in an eye cavity and comes into contact with tear fluid, the polymer set forth in (b) which comes into contact with the tear fluid dissolves into a viscous solution or gel-like envelope that acts as a lubricating envelope, which, in cooperation with the shape of the unit

Claim 32

In the art of medicating the eye with ophthalmic medication the improvement which consists of the step of placing beneath one eyelid a solid lens-shaped body having at least one curved surface and softly rounded corners which is adapted for insertion into the cavity between the eye and surrounding tissue, said shaped body retaining its shape during the whole time of use and containing a substance having a topical effect on the eye, which composition comprises a mixture of a. 5 - 60 percent of at least one lipophilic substance having a melting point of 37* - 75*C and being selected from the group consisting of higher hydrocarbons, waxes, fats and mixtures thereof, b. 5 - 40 percent of at least one water-soluble or water-swellable polymer in solid, finely divided form and being selected from the group consisting of dextran, lower hydroxy-alkyl dextran, carboxymethyl dextran, lower hydroxy-alkyl cellulose, lower alkyl cellulose, carboxy-methyl cellulose, poLyvinyl aclochol, dextrin, starch, polyvinyl pyrrolidone and polyalkylene glycols, the particle size of the solid polymer being less than approximately 150 microns, c. 0.05 - 30 percent of at least one substance having a topical effect on the eye, being in solid, finely-divided form, with a particle size less than approximately 150 microns, and being selected from the group consisting of drugs for glaucoma therapy and substances showing a mydriatic effect, d. 10 - 80 percent of at least one member of the group consisting of aliphatic monoalcohols having 13 - 22 carbon atoms, to serve as stabilizer for the mixture, the percentages relating to percent by weight calculated on the total weight of the mixture, whereby when said solid shaped body is inserted in an eye cavity and comes into contact with tear fluid, the polymer set forth in (b) which comes into contact with the tear fluid dissolves into a viscous solution or gel-like envelope that acts as a lubricating envelope, which, in cooperation with the shape of the unit

Claim 33

Medication according to claim 9 wherein the solid shaped body has a largest dimension lying between the limits 2 and 20 mm.

Claim 34

Medication according to claim 9 wherein the solid shaped body has a largest dimension lying between the limits 6 and 16 mm.

Claim 35

Medication according to claim 9 wherein at least one surface of the solid shaped body is convex.

Claim 36

Medication according to claim 9 wherein the drug for glaucoma theraphy comprises pilocarpine, adrenaline, physostigmine or synstigmine or salts thereof, either separately or in combination.

Claim 37

Medication according to claim 9 wherein the substance showing a mydriatic effect is metaoxedrin or atropin or therapeutically acceptable salts thereof.

Claim 38

In the art of medicating the eye with opthalmic medication the improvement which consists of the step of placing beneath one eyelid a solid lens-shaped body having at least one curved surface and softly rounded corners which is adapted for insertion into the cavity between the eye and surrounding tissue, said shaped body retaining its shape during the whole time of use, and containing a substance having a topical effect on the eye, which composition comprises a mixture of a. 10 - 45 percent of at least one lipophilic substance having a melting point of 37* - 75*C and being selected from the group consisting of higher hydrocarbons, waxes, fats or mixtures thereof, b. 10 - 30 percent of at least one water-soluble or waterswellable polymer in solid, finely-divided form and being selected from the group consisting of dextran, lower hydroxy-alkyl dextran, carboxymethyl dextran, lower hydroxy-alkyl cellulose, lower alkyl cellulose, carboxy-methyl cellulose, polyvinyl alcohol, dextrin, starch, polyvinyl pyrrolidone and polyalkylene glycols, the particle size of the polymer being less than approximately 150 microns, c. 0.5 - 20 percent of at least one substance having a topical effect on the eye, being in solid, finely-divided form, with a particle size less than approximately 150 microns, and being selected from the group consisting of drugs for glaucoma therapy and substances showing a mydriatic effect, d. 10 - 60 percent of at least one member of the group consisting of aliphatic monoalcohols having 13 - 22 carbon atoms, to serve as stabIlizer for the mixture, the percentages relating to percent by weight calculated on the total weight of the mixture, whereby when said solid shaped body is inserted in an eye cavity and comes into contact with tear fluid, the polymer set forth in (b) which comes into contact with fluid dissolves into a viscous solution or gel-like envelope that acts as a lubricating envelope, which, in cooperation with the shape of the unit

Claim 39

In the art of medicating the eye with opthalmic medication the improvement which consists of the step of placing beneath one eyelid a solid lens-shaped body having at least one curved surface and softly rounded corners which is adapted for insertion into the cavity between the eye and surrounding tissue, said shaped body retaining its shape during the whole time of use, and containing a substance having a topical effect on the eye, which composition comprises a mixture of a. 10 - 45 percent of at least one lipophilic substance having a melting point of 37* - 75*C and being selected from the group consisting of higher hydrocarbons, waxes, fats or mixtures thereof, b. 10 - 30 percent of at least one water-soluble or waterswellable polymer in solid, finely-divided form and being selected from the group consisting of dextran, lower hydroxy-alkyl dextran, carboxymethyl dextran, lower hydroxy-alkyl cellulose, lower alkyl cellulose, carboxy-methyl cellulose, polyvinyl alcohol, dextrin, starch, polyvinyl pyrrolidone and polyalkylene glycols, the particle size of the polymer being less than approximately 150 microns, c. 0.5 - 20 percent of at least one substance having a topical effect on the eye, being in solid, finely-divided form, with a particle size less than approximately 150 microns, and being selected from the group consisting of drugs for glaucoma therapy and substances showing a mydriatic effect, d. 10 - 60 percent of at least one member of the group consisting of aliphatic monoalcohols having 13 - 22 carbon atoms, to serve as stabIlizer for the mixture, the percentages relating to percent by weight calculated on the total weight of the mixture, whereby when said solid shaped body is inserted in an eye cavity and comes into contact with tear fluid, the polymer set forth in (b) which comes into contact with fluid dissolves into a viscous solution or gel-like envelope that acts as a lubricating envelope, which, in cooperation with the shape of the unit