Pharmaceutical composition containing cyclosporin in admixture with α-

Claim 2

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of at least one cyclosporin in admixture with an amount of a functional derivative of α-cyclodextrin sufficient to solubilise the cyclosporin in water, wherein the α-cyclodextrin derivative is selected from the group consisting of α-cyclodextrin esters, α-cyclodextrin ethers, aminoalkylated derivatives of α-cyclodextrin, salts of α-cyclodextrin with a sulfur-containing acid, carboxyalkylated derivatives of α-cyclodextrin, addition compounds of α-cyclodextrin with a monosaccharide, addition compounds of α-cyclodextrin with a disaccharide, polymers comprising α-cyclodextrin in their main chain and polymers comprising α-cyclodextrin pendant on their main chain.

Claim 3

The composition of claim 1, wherein the weight ratio of said cyclosporin to said α-cyclodextrin derivative is from 1:0.5 to 1:1000.

Claim 4

The composition of claim 1, wherein the weight ratio of said cyclosporin to said α-cyclodextrin derivative is from 1:1 to 1:200.

Claim 5

The composition of claim 1, wherein the α-cyclodextrin derivative is selected from the group consisting of acetylated α-cyclodextrin, methylated α-cyclodextrin, aminoethyl-α-cyclodextrin, α-cyclodextrin sulfate and maltosylated α-cyclodextrin.

Claim 6

The composition of claim 1, wherein said cyclosporin is selected from the group consisting of cyclosporin A, cyclosporin B, cyclosporin D and cyclosporin G.

Claim 7

The composition of claim 1, wherein said α-cyclodextrin derivative is a α-cyclodextrin ester in which some or all of the hydroxy groups in the glucose units are acylated and the acyl groups are derived from an acid selected from the group consisting of (a) a carboxylic acid, said carboxylic acid selected from the group consisting of acetic acid, propionic acid, butyric acid, valeric acid, isovaleric acid, pivalic acid, fumaric acid, succinic acid, citric acid, tartaric acid, oxalic acid and maleic acid; (b) a sulfonic acid, said sulfonic acid selected from the group consisting of methanesulfonic acid, trifluoromethane sulfonic acid, ethanesulfonic acid, benzenesulfonic acid and p-toluene sulfonic acid; and (c) an amino acid, said amino acid selected from the group consisting of glutamic acid and aspargic acid.

Claim 8

The composition of claim 1, wherein said α-cyclodextrin derivative is an ether derivative wherein the ether moiety is an alkyl group having 1 to 4 carbon atoms.

Claim 9

The composition of claim 1, wherein said α-cyclodextrin derivative is an aminoalkylated derivative of α-cyclodextrin wherein the alkyl group has 1 to 4 carbon atoms.

Claim 10

The composition of claim 8, wherein the aminoalkylated derivative of α-cyclodextrin is selected from the group consisting of aminomethyl-α-cyclodextrin and aminoethyl-α-cyclodextrin.

Claim 11

The composition of claim 1, wherein said α-cyclodextrin derivative is a carboxyalkylated derivative having an alkyl group with 1 to 4 carbon atoms.

Claim 12

The composition of claim 10, wherein said carboxyalkylated derivative is selected from the group consisting of carboxymethyl-α-cyclodextrin, carboxyethyl-α-cyclodextrin and carboxypropyl-α-cyclodextrin.

Claim 13

The composition of claim 1, wherein said α-cyclodextrin derivative is an addition compound of α-cyclodextrin comprising a monosaccharide or a disaccharide which is condensed with a hydroxy group of an α-cyclodextrin derived from maltose, glucose, fructose, galactose, sucrose or lactose.

Claim 14

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of at least one cyclosporin in admixture with an amount of α-cyclodextrin sufficient to solubilise the cyclosporin in water.

Claim 15

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of at least one cyclosporin in admixture with an amount of α-cyclodextrin sufficient to solubilise the cyclosporin in water.

Claim 16

The composition of claim 13, wherein the weight ratio of said cyclosporin to said α-cyclodextrin is from 1:0.5 to 1:1000.

Claim 17

The composition of claim 13, wherein the weight ratio of said cyclosporin to said α-cyclodextrin is from 1:1 to 1:200.

Claim 18

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of at least one cyclosporin and α-cyclodextrin or a functional derivative thereof dissolved in water, the amount of α-cyclodextrin or said functional derivative thereof being sufficient to solubilise the cyclosporin in the water, wherein the α-cyclodextrin derivative is selected from the group consisting of α-cyclodextrin esters, α-cyclodextrin ethers, aminoalkylated derivatives of α-cyclodextrin, salts of α-cyclodextrin with a sulfur-containing acid, carboxyalkylated derivatives of α-cyclodextrin, addition compounds of α-cyclodextrin with a monosaccharide, addition compounds of α-cyclodextrin with a disaccharide, polymers comprising α-cyclodextrin in their main chain and polymers comprising α-cyclodextrin pendant on their main chain.

Claim 19

A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of at least one cyclosporin and α-cyclodextrin or a functional derivative thereof dissolved in water, the amount of α-cyclodextrin or said functional derivative thereof being sufficient to solubilise the cyclosporin in the water, wherein the α-cyclodextrin derivative is selected from the group consisting of α-cyclodextrin esters, α-cyclodextrin ethers, aminoalkylated derivatives of α-cyclodextrin, salts of α-cyclodextrin with a sulfur-containing acid, carboxyalkylated derivatives of α-cyclodextrin, addition compounds of α-cyclodextrin with a monosaccharide, addition compounds of α-cyclodextrin with a disaccharide, polymers comprising α-cyclodextrin in their main chain and polymers comprising α-cyclodextrin pendant on their main chain.

Claim 20

The composition of claim 16, wherein the weight ratio of said cyclosporin to said α-cyclodextrin or derivative thereof is from 1:0.5 to 1:1000.

Claim 21

The composition of claim 16, wherein the weight ratio of said cyclosporin to said α-cyclodextrin or derivative thereof is from 1:1 to 1:200.

Claim 24

The method of claim 19, wherein said cyclosporin and said α-cyclodextrin or derivative thereof are administered in admixture.

Claim 25

The method of claim 19, wherein said cyclosporin and said α-cyclodextrin or derivative thereof are administered separately, but essentially simultaneously.

Claim 26

The method of claim 19, wherein the α-cyclodextrin derivative is selected from the group consisting of acetylated α-cyclodextrin, methylated α-cyclodextrin, aminoethyl-α-cyclodextrin, α-cyclodextrin sulfate and maltosylated α-cyclodextrin.

Claim 27

The method of claim 19, wherein the weight ratio of said cyclosporin to said α-cyclodextrin or derivative thereof is from 1:0.5 to 1:1000.

Claim 28

The method of claim 19, wherein the weight ratio of said cyclosporin to said α-cyclodextrin or derivative thereof is from 1:1 to 1:200.

Claim 29

The method of claim 19, wherein the administering is orally, by injection, or as eyedrops.

Claim 32

The method of claim 26, wherein the weight ratio of said cyclosporin to said α-cyclodextrin is from 1:1 to 1:200.

Claim 33

A pharmaceutical composition comprising (a) a pharmaceutically acceptable carrier, (b) a pharmaceutically effective amount of cyclosporin A or a mixture of cyclosporin A with at least one other cyclosporin in admixture with (c) an amount of a functional derivative of α-cyclodextrin sufficient to solubilise said cyclosporin in water, wherein the α-cyclodextrin derivative is selected from the group consisting of α-cyclodextrin esters, α-cyclodextrin ethers, aminoalkylated derivatives of α-cyclodextrin, salts of α-cyclodextrin with a sulfur-containing acid, carboxyalkylated derivatives of α-cyclodextrin, addition compounds of α-cyclodextrin with a monosaccharide, addition compounds of α-cyclodextrin with a disaccharide, polymers comprising α-cyclodextrin in their main chain and polymers comprising α-cyclodextrin pendant on their main chain.

Claim 34

A pharmaceutical composition comprising (a) a pharmaceutically acceptable carrier, (b) a pharmaceutically effective amount of cyclosporin A or a mixture of cyclosporin A with at least one other cyclosporin in admixture with (c) an amount of a functional derivative of α-cyclodextrin sufficient to solubilise said cyclosporin in water, wherein the α-cyclodextrin derivative is selected from the group consisting of α-cyclodextrin esters, α-cyclodextrin ethers, aminoalkylated derivatives of α-cyclodextrin, salts of α-cyclodextrin with a sulfur-containing acid, carboxyalkylated derivatives of α-cyclodextrin, addition compounds of α-cyclodextrin with a monosaccharide, addition compounds of α-cyclodextrin with a disaccharide, polymers comprising α-cyclodextrin in their main chain and polymers comprising α-cyclodextrin pendant on their main chain.

Claim 35

A pharmaceutical composition comprising (a) a pharmaceutically acceptable carrier, (b) a pharmaceutically effective amount of cyclosporin A or a mixture of cyclosporin A with at least one other cyclosporin in admixture with (c) an amount of α-cyclodextrin sufficient to solubilise said cyclosporin in water.

Claim 36

A pharmaceutical composition comprising (a) a pharmaceutically acceptable carrier, (b) a pharmaceutically effective amount of cyclosporin A or a mixture of cyclosporin A with at least one other cyclosporin in admixture with (c) an amount of α-cyclodextrin sufficient to solubilise said cyclosporin in water.

Claim 39

The method of claim 30, wherein the administering is orally, by injection, or as eyedrops.

Claim 42

The method of claim 32, wherein the administering is orally, by injection, or as eyedrops.