Sustained release of methantheline

Claim 2

A SUSTAINED RELEASE ORAL INGESTION 26 HOUR METHANTHELINE ELUTING PHARMACEUTICAL COMPOSITION COMPRISING: A. A POLYMERIZED AND CURED MATRIX OF A WATER-INSOLUBLE BUT WATER-SWELLABLE HYDROPHILIC POLYMER OF A MONOMER MIXTURE CONSISTING ESSENTIALLY OF:

Claim 3

POLYMERIZABLE MONOESTER OF: A. AN ACID SELECTED FROM THE GROUP CONSISTING OF ACRYLIC ACID, METHACRYLIC ACID, AND MIXTURES THEREOF, AND B. A POLYHYDRIC ALCOHOL SELECTED FROM THE GROUP CONSISTING OF ETHYLENE GLYCOL, 1,3-PROPANEDIOL, DIETHYLENE GLYCOL, DIPROPYLENE GLYCOL, POLYETHYLENE GLYCOL, POLYPROPYLENE GLYCOL, 1,6-HEXAMETHYLENE GLYCOL, 1,4BUTANEDIOL, GLYCEROL, TRIMETHYLOL PROPANE, TRIMETHYLOLETHANE, PENTAERYTHRITOL, MANNITOL, SORBITOL, AND MIXTUES THEREOF,

Claim 4

POLYMERIZABLE MONOESTER OF: A. AN ACID SELECTED FROM THE GROUP CONSISTING OF ACRYLIC ACID, METHACRYLIC ACID, AND MIXTURES THEREOF, AND B. A POLYHYDRIC ALCOHOL SELECTED FROM THE GROUP CONSISTING OF ETHYLENE GLYCOL, 1,3-PROPANEDIOL, DIETHYLENE GLYCOL, DIPROPYLENE GLYCOL, POLYETHYLENE GLYCOL, POLYPROPYLENE GLYCOL, 1,6-HEXAMETHYLENE GLYCOL, 1,4BUTANEDIOL, GLYCEROL, TRIMETHYLOL PROPANE, TRIMETHYLOLETHANE, PENTAERYTHRITOL, MANNITOL, SORBITOL, AND MIXTUES THEREOF,

Claim 5

POLYMERIZABLE ETHYLENICALLY UNSATURATED AINO CONTAINING MONOMER SELECTED FROM THE GROUP CONSISTING OF DIACETONE ACRYLAMIDE, HYDROXY METHYLATED DIACETONE ACRYLAMIDE, AND MIXTURES THEREOF,

Claim 6

POLYMERIZABLE ETHYLENICALLY UNSATURATED AINO CONTAINING MONOMER SELECTED FROM THE GROUP CONSISTING OF DIACETONE ACRYLAMIDE, HYDROXY METHYLATED DIACETONE ACRYLAMIDE, AND MIXTURES THEREOF,

Claim 7

The composition of claim 1 wherein the monomer mixture contains from about 30 to about 70% by weight of (1); from about 30 to about 60% by weight of (2); from about 0.5 to about 2% by weight of (3); and from about 1 to about 75% by weight of (4) based upon the total weight of (1), (2), (3), and (4) in the monomer mixture.

Claim 8

polymerizable ethylenically unsaturated amino containing monomer selected from the group consisting of diacetone acrylamide, hydroxy methylated diacetone acrylamide, and mixtures thereof;

Claim 9

polymerizable ethylenically unsaturated amino containing monomer selected from the group consisting of diacetone acrylamide, hydroxy methylated diacetone acrylamide, and mixtures thereof;

Claim 10

ethylenically unsaturated acid selected from the group of acrylic acid, methacrylic acid, crotonic acid, and mixtures thereof; and

Claim 11

ethylenically unsaturated acid selected from the group of acrylic acid, methacrylic acid, crotonic acid, and mixtures thereof; and

Claim 12

ETHYLENICALLY UNSATURATED ACID SELECTED FROM THE GROUP OF ACRYLIC ACID, METHACRYLIC ACID, CROTONIC ACID, AND MIXTURES THEREOF, AND

Claim 13

ETHYLENICALLY UNSATURATED ACID SELECTED FROM THE GROUP OF ACRYLIC ACID, METHACRYLIC ACID, CROTONIC ACID, AND MIXTURES THEREOF, AND

Claim 14

The composition of claim 1 wherein the monomer mixture contains from about 30 to about 60% by weight of (1); from about 30 to about 60% by weight of (2); from about 1 to about 2% by weight of (3); and from about 5 to about 7.5% by weight of (4) based upon the total weight of (1), (2), (3), and (4) in the monomer mixture.

Claim 15

The composition of claim 1 wherein said monoester is selected from the group consisting of 2-hydroxy ethyl methacrylate, 2-hydroxy ethyl acrylate, 2-hydroxy propyl methacrylate, diethylene glycol monomethacrylate, diethylene glycol monoacrylate, 2-hydroxy propyl acrylate, 3-hydroxy propyl methacrylate, 3-hydroxy propyl acrylate, dipropylene glycol monomethacrylate, glyceryl methacrylate, pentaerythritol methacrylate, and mixtures thereof.

Claim 16

polymerizable diester selected from the group consisting of ethylene glycol diacrylate, ethylene glycol dimethacrylate, 1, 2-butylene dimethacrylate, 1,3-butylene dimethacrylate, 1,4-butylene dimethacrylate, propylene glycol diacrylate, propylene glycol dimethacrylate, diethylene glycol dimethacrylate, dipropylene glycol dimethacrylate, diethylene glycol diacrylate, dipropylene glycol diacrylate, tetraethylene glycol dimethacrylate, tetraethylene glycol diacrylate, and mixtures thereof; wherein the monomer mixture contains from about 30 to about 80% by weight of (1); from About 30 to about 60% by weight of (2); from about 0.5 to about 2% by weight of (3); and from about 0.5 to about 7.5% by weight of (4) based upon the total weight of (1), (2), (3), and (4) in the monomer mixture; B. said polymerized and cured matrix having been soaked for about 12 hours in isotonic saline solution containing per 5 ml of isotonic saline solution at least about 100 mg of methantheline bromide in an amount at least sufficient for the total dosage requirement adapted to gradually elute, upon oral ingestion during 26 hours of a treatment period; and thereby entrapping the methantheline bromide in said matrix.

Claim 17

polymerizable diester selected from the group consisting of ethylene glycol diacrylate, ethylene glycol dimethacrylate, 1, 2-butylene dimethacrylate, 1,3-butylene dimethacrylate, 1,4-butylene dimethacrylate, propylene glycol diacrylate, propylene glycol dimethacrylate, diethylene glycol dimethacrylate, dipropylene glycol dimethacrylate, diethylene glycol diacrylate, dipropylene glycol diacrylate, tetraethylene glycol dimethacrylate, tetraethylene glycol diacrylate, and mixtures thereof; wherein the monomer mixture contains from about 30 to about 80% by weight of (1); from About 30 to about 60% by weight of (2); from about 0.5 to about 2% by weight of (3); and from about 0.5 to about 7.5% by weight of (4) based upon the total weight of (1), (2), (3), and (4) in the monomer mixture; B. said polymerized and cured matrix having been soaked for about 12 hours in isotonic saline solution containing per 5 ml of isotonic saline solution at least about 100 mg of methantheline bromide in an amount at least sufficient for the total dosage requirement adapted to gradually elute, upon oral ingestion during 26 hours of a treatment period; and thereby entrapping the methantheline bromide in said matrix.

Claim 18

POLYMERIZABLE DIESTER SELECTED FROM THE GROUP CONSISTING OF ETHYLENE GYLCOL DIACRYLATE, ETHYLENE GLYCOL DIMETHACRYLATE, 1,2-BUTYLENE DIMETHACRYLATE, 1,3-BUTYLENE DIMETHACRYLATE, 1,4-BUTYLENE DIMETHACRYLATE, PROPYLENE GYCOL DIACRYLATE, PROPYLENE GLYCOL DIMETHACRYLATE, DIETHYLENE GLYCOL DIMETHACRYLATE, DIPROPYLENE GLYCOL DIMETHACRYLATE, DIETHYLENE GLYCOL DIACRYLATTE, DIPROPYLENE GLYCOL DIACRYLATE, TETRAETHYLENE GLYCOL DIMETHACRYLATE, TETRAETHYLENEGLYCOL DIACRYLATE, AND MIXTURES THEREOF, WHEREIN THE MONOMER MIXTURE CONTANS FROM ABOUT 30 TO ABOUT 80% BY WEIGHT OF (1), FROM ABOUT 30 TO ABOUT 60% BY WEIGHT OF (2), FROM ABOUT 0.5 TO ABOUT 2% BY WEIGHT OF (3), AND FROM ABOUT 0.5 TO ABOUT 7.5% BY WEIGHT OF (4) BASED UPON THE TOTAL WEIGHT OF .(1), (2), (3), AND (4) IN THE MONOMER MIXTURE, B. SAID POLYMERIZED AND CURED MATRIX HAVING BEEN SOAKED FOR ABOUT 12 HOURS IN ISOTONIC SALINE SOLUTION CONTAINING PER 5 ML OF ISOTONIC SALINE SOLUTION AT LEAST ABOUT 100 MG OF METHANTHLINE BROMIDE IN AN AMOUNT AT LEAST SUFFICIENT FOR THE TOTAL DOSAGE REQUIREMENT ADAPTED TO GRADUALLY ELUTE, UPON INGESTION DURING 26 HOURS OF A TREATMENT PERIOD, AND THEREBY ENTRAPPING THE METHANTHELINE BROMIDE IN SAID MATRIX.

Claim 19

POLYMERIZABLE DIESTER SELECTED FROM THE GROUP CONSISTING OF ETHYLENE GYLCOL DIACRYLATE, ETHYLENE GLYCOL DIMETHACRYLATE, 1,2-BUTYLENE DIMETHACRYLATE, 1,3-BUTYLENE DIMETHACRYLATE, 1,4-BUTYLENE DIMETHACRYLATE, PROPYLENE GYCOL DIACRYLATE, PROPYLENE GLYCOL DIMETHACRYLATE, DIETHYLENE GLYCOL DIMETHACRYLATE, DIPROPYLENE GLYCOL DIMETHACRYLATE, DIETHYLENE GLYCOL DIACRYLATTE, DIPROPYLENE GLYCOL DIACRYLATE, TETRAETHYLENE GLYCOL DIMETHACRYLATE, TETRAETHYLENEGLYCOL DIACRYLATE, AND MIXTURES THEREOF, WHEREIN THE MONOMER MIXTURE CONTANS FROM ABOUT 30 TO ABOUT 80% BY WEIGHT OF (1), FROM ABOUT 30 TO ABOUT 60% BY WEIGHT OF (2), FROM ABOUT 0.5 TO ABOUT 2% BY WEIGHT OF (3), AND FROM ABOUT 0.5 TO ABOUT 7.5% BY WEIGHT OF (4) BASED UPON THE TOTAL WEIGHT OF .(1), (2), (3), AND (4) IN THE MONOMER MIXTURE, B. SAID POLYMERIZED AND CURED MATRIX HAVING BEEN SOAKED FOR ABOUT 12 HOURS IN ISOTONIC SALINE SOLUTION CONTAINING PER 5 ML OF ISOTONIC SALINE SOLUTION AT LEAST ABOUT 100 MG OF METHANTHLINE BROMIDE IN AN AMOUNT AT LEAST SUFFICIENT FOR THE TOTAL DOSAGE REQUIREMENT ADAPTED TO GRADUALLY ELUTE, UPON INGESTION DURING 26 HOURS OF A TREATMENT PERIOD, AND THEREBY ENTRAPPING THE METHANTHELINE BROMIDE IN SAID MATRIX.

Claim 20

The composition of claim 1 wherein said monoester is 2-hydroxy ethyl methacrylate.

Claim 21

The composition of claim 1 wherein said polymerizable ethylenically unsaturated amino containing monomer is diacetone acrylamide.

Claim 22

The composition of claim 1 wherein said polymerizable ethylenically unsaturated amino containing monomer is hydroxy methylated diacetone acrylamide.

Claim 23

The composition of claim 1 wherein said ethylenically unsaturated acid is methacrylic acid.

Claim 24

The composition of claim 1 wherein said diester is tetraethylene glycol dimethacrylate.

Claim 25

The composition of claim 3 wherein said monoester is 2-hydroxy ethyl methacrylate; said polymerizable ethylenically unsaturated amino containing monomer is diacetone acrylamide; said unsaturated acid is methacrylic acid and said diester is tetraethylene glycol dimethacrylate.

Claim 26

The composition of claim 3 wherein said monoester is 2-hydroxy ethyl methacrylate, said amino containing monomer is hydroxy methylated diacetone acrylamide, said unsaturated acid is methacrylic acid and said diester is tetraethylene glycol dimethacrylate.