Sustained release of methantheline

Claim 2

A SUSTAINED RELEASE ORAL INGESTION 24 HOUR METHANTHELINE ELUTING PHARMACEUTICAL COMPOSITION COMPRISING: A. POLYMERIZED AND CURED MATRIX OF WATER-INSOLUBLE BUT WATER-SWELLABLE HYDROPHILIC POLYMER OF A MONOMER MIXTURE CONTAINING:

Claim 3

POLYMERIZABLE MONOESTER OF A MEMBER SELECTED FROM THE GROUP CONSISTING OF ACRYLIC ACID, METHACRYLIC ACID, AND MIXTURES THEREOF, AND A POLYHYDRIC ALCOHOL,

Claim 4

POLYMERIZABLE MONOESTER OF A MEMBER SELECTED FROM THE GROUP CONSISTING OF ACRYLIC ACID, METHACRYLIC ACID, AND MIXTURES THEREOF, AND A POLYHYDRIC ALCOHOL,

Claim 5

A POLYMERIZABLE SULFUR CONTAINING MATERIAL SELECTED FROM THE GROUP CONSISTING OF VINYL SULFONIC ACID, VINYLPROPANE SULFONIC ACID, STYRENE SULFONIC ACIDS, ALKALI METAL SALTS THEREOF, AMMONIUM SALTS THEREOF, AND MIXTURES THEREOF, AND

Claim 6

A POLYMERIZABLE SULFUR CONTAINING MATERIAL SELECTED FROM THE GROUP CONSISTING OF VINYL SULFONIC ACID, VINYLPROPANE SULFONIC ACID, STYRENE SULFONIC ACIDS, ALKALI METAL SALTS THEREOF, AMMONIUM SALTS THEREOF, AND MIXTURES THEREOF, AND

Claim 7

a polymerizable sulfur containing material selected from the group consisting of vinyl sulfonic acid, vinylpropane sulfonic acid, styrene sulfonic acids; alkali metal salts thereof; ammonium salts thereof; and mixtures thereof; and

Claim 8

a polymerizable sulfur containing material selected from the group consisting of vinyl sulfonic acid, vinylpropane sulfonic acid, styrene sulfonic acids; alkali metal salts thereof; ammonium salts thereof; and mixtures thereof; and

Claim 9

The composition of claim 1 wherein said polymerizable monoester is a monoester of a member selected from the group consisting of acrylic acid, methacrylic acid, and mixtures thereof; and 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, 1,4-butanediol, glycerol, trimethylol propane, trimethylolethane, pentaerythritol, mannitol, and sorbitol.

Claim 10

polymerizable diester of a member selected from the group consisting of acrylic acid, methacrylic acid, and mixtures thereof; and a polyhydric alcohol; and wherein the monomer mixture contains from about 25 to about 44.4% by weight of (1); from about 5 to about 30% by weight of (2); and from about 0.5 to about 25.2% by weight of (3) based upon the total weight of (1), (2), and (3) in the monomer mixture; and 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 100.5 mg of methantheline bromide in an amount sufficient for the total dosage requirement adapted to gradually elute methantheline upon oral ingestion during 24 hours of a treatment period; and thereby the methantheline bromide being entrapped in said matrix.

Claim 11

polymerizable diester of a member selected from the group consisting of acrylic acid, methacrylic acid, and mixtures thereof; and a polyhydric alcohol; and wherein the monomer mixture contains from about 25 to about 44.4% by weight of (1); from about 5 to about 30% by weight of (2); and from about 0.5 to about 25.2% by weight of (3) based upon the total weight of (1), (2), and (3) in the monomer mixture; and 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 100.5 mg of methantheline bromide in an amount sufficient for the total dosage requirement adapted to gradually elute methantheline upon oral ingestion during 24 hours of a treatment period; and thereby the methantheline bromide being entrapped in said matrix.

Claim 12

The composition of claim 1 wherein said polymerizable 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-hyroxy propyl acrylate, dipropylene glycol monomethacrylate, glyceryl methacrylate, and pentaerythritol methacrylate.

Claim 13

POLYMERIZABLE DIESTER OF MEMBER SELECTED FROM THE GROUP CONSISTING OF ACRYLIC ACID, METHACRYLIC ACID, AND MIXTURES THEREOF, AND A POLYHYDRIC ALCOHOL, AND WHEREIN THE MONOMER MIXTURE CONTAINS FROM ABOUT 25 TO ABOUT 44.4% BY WEIGHT OF (1), FROM ABOUT 5 TO ABOUT 30% BY WEIGHT OF (2), AND FROM ABOUT 0.5 TO ABOUT 25.25% BY WEIGHT OF (3) BASED UPON THE TOTAL WEIGHT OF (1), (2), AND (3) IN THE MONOMER MIXTURE, AND 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 ABOUT100.5 MG OF METHANTHLINE BROMIDE IN AN AMOUNT SUFFICIENT FOR THE TOTAL DOSAGE REQUIREMENT ADAPTED TO GRADUALLY ELUTE METHNTHELINE UPON ORAL INGESTION DURING 24 HOURS OF A TREATMENT PERIOD, AND THEREBY THE METHANTHELINE BROMIDE BEING ENTRAPPED IN SAID MATRIX.

Claim 14

POLYMERIZABLE DIESTER OF MEMBER SELECTED FROM THE GROUP CONSISTING OF ACRYLIC ACID, METHACRYLIC ACID, AND MIXTURES THEREOF, AND A POLYHYDRIC ALCOHOL, AND WHEREIN THE MONOMER MIXTURE CONTAINS FROM ABOUT 25 TO ABOUT 44.4% BY WEIGHT OF (1), FROM ABOUT 5 TO ABOUT 30% BY WEIGHT OF (2), AND FROM ABOUT 0.5 TO ABOUT 25.25% BY WEIGHT OF (3) BASED UPON THE TOTAL WEIGHT OF (1), (2), AND (3) IN THE MONOMER MIXTURE, AND 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 ABOUT100.5 MG OF METHANTHLINE BROMIDE IN AN AMOUNT SUFFICIENT FOR THE TOTAL DOSAGE REQUIREMENT ADAPTED TO GRADUALLY ELUTE METHNTHELINE UPON ORAL INGESTION DURING 24 HOURS OF A TREATMENT PERIOD, AND THEREBY THE METHANTHELINE BROMIDE BEING ENTRAPPED IN SAID MATRIX.

Claim 15

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

Claim 16

The composition of claim 1 wherein said diester is 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 glcyol dimethacylate, and tetraethylene glycol diacrylate.

Claim 17

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

Claim 18

The composition of claim 1 wherein said polymerizable sulfur-containing material is selected from the group consisting of styrene sulfonic acids, ammonium salts thereof, alkali metal salts thereof; and mixtures thereof.

Claim 19

The composition of claim 7 wherein the styrene sulfonic acid is p-toluene sulfonic acid.

Claim 20

The composition of claim 1 wherein said polymerizable sulfur-containing material is sodium p-toluene sulfonic acid.

Claim 21

The composition of claim 1 wherein the monomer mixture contains from about 35 to about 44.4% by weight of (1); from about 5 to about 30% by weight of (2); and from about 1 to about 25.2% by weight of (3) based upon the total weight of (1), (2), and (3) in the monomer mixture.

Claim 22

The composition of claim 1 wherein 1. said polymerizable monoester is a monoester of a member selected from the group consisting of acrylic acid, methacrylic acid, and mixtures thereof; and 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, 1,4-butanediol, glycerol, trimethylol propane, trimethylolethane, pentaerythritol, mannitol, and sorbitol; wherein said polymerizable sulfur-containing material is selected from the group consisting of styrene sulfonic acids, ammonium salts thereof, alkali metal salts thereof, and mixtures thereof; and wherein said diester (3) is 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, and tetraethylene glycol diacrylate.

Claim 23

The composition of claim 11 wherein said polymerizable 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, and pentaerythritol methacrylate; and wherein the styrene sulfonic acid is p-toluene sulfonic acid.

Claim 24

The composition of claim 12 wherein the monomer mixture contains from about 35 to about 44.4% by weight of (1); from about 5 to about 30% by weight of (2); and from about 1 to about 25.2% by weight of (3) based upon the total weight of (1), (2), and (3) in the monomer mixture.

Claim 25

The composition of claim 1 wherein said monoester (1) is 2-hydroxy ethyl methacrylate; said sulfur-containing monomer (2) is sodium p-toluene sulfonic acid; and said diester (3) is tetraethylene glycol dimethacrylate.

Claim 26

The composition of claim 14 wherein the monomer mixture contains from about 35 to about 44.4% by weight of (1); from about 5 to about 30% by weight of (2); and from about 1 to about 25.2% by weight of (3) based upon the total weight of (1), (2), and (3) in the monomer mixture.