Method of use of polymers containing cross-linked azo bonds for releasing therapeutic agents into the lower gastrointestinal tract
AssigneesMedical College of Ohio, Bowling Green State University
InventorsMurray Saffran, Douglas C. Neckers
Life of this patent
Estimating the term…
Abstract
Polymers from ethylenically unsaturated monomers, cross-linked by a substituted or unsubstituted divinylazobenzene are useful as carriers or capsules for medicaments, which are degraded by the enzymes of the upper gastrointestinal tract or which must be transferred intact past the upper gastrointestinal tract, to deliver the medicament to the large intestine. Polymers containing monomeric units of the formula H.sub.2 C.dbd.CH--C.sub.6 H.sub.4 --N.dbd.N--M, wherein M is the residue of an amino-containing medicament, are useful as carriers for therapeutic agents or as therapeutic agents per se.
Claims41
A method for delivering to the large intestine of an animal a medicament normally destroyed by the digestive juices of the upper gastrointestinal tract, absorbed by the upper gastrointestinal tract or having an undesired effect on the upper gastrointestinal tract, which medicament is capable of being absorbed through the mucosa of the large intestine, comprising:
- (a) formulating the medicament into a unit dosage form;
- (b) coating the unit dosage form with a high molecular weight polymer from one or more ethylenically unsaturated monomers, cross-linked by a substituted or unsubstituted divinylazobenzene compound of the formula ##STR6## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of H, Cl, Br, I, NO.sub.2, NH.sub.2, RO, ArO, COOH or salts thereof, COOR, COOAr, CHO, COR, SO.sub.3 H or salts thereof, R or Ar and wherein R is an alkyl group of up to 18 carbon atoms and Ar is a mono- or bicyclic aryl group of up to 15 carbon atoms, in an amount sufficient to protect the unit dosage form from the action of digestive juices of the upper gastrointestinal tract to prevent the medicament from causing an adverse effect on the upper gastrointestinal tract or being absorbed therethrough;
- and
- (c) administering the thus-coated unit dosage form orally to the animal being given the medicament.
A method for delivering to the large intestine of an animal a medicament normally destroyed by the digestive juices of the upper gastrointestinal tract, having an undesired effect on the upper gastrointestinal tract or being absorbed therethrough, which medicament is capable of being absorbed through the mucosa of the large intestine, comprising:
- (a) formulating the medicament into a unit dosage form;
- (b) coating the unit dosage form with a high molecular weight polymer from one or more ethylenically unsaturated monomers, cross-linked by p,p'-divinylazobenzene, in an amount sufficient to protect the unit dosage form from the action of digestive juices of the upper gastrointestinal tract and to prevent the medicament from causing an adverse effect on the upper gastrointestinal tract or being absorbed therethrough;
- and
- (c) administering the thus-coated unit dosage form orally to the animal being given the medicament.
A method for delivering to the large intestine of an animal a medicament normally destroyed by the digestive juices of the upper gastrointestinal tract or a medicament having an undesired effect on the upper gastrointestinal tract or being absorbed therethrough, which medicament is capable of being absorbed through the mucosa of the large intestine, comprising:
- (a) formulating the medicament into a unit dosage form;
- (b) coating the unit dosage form with a high molecular weight polymer from one or more ethylenically unsaturated monomers, cross-linked by a substituted or unsubstituted divinylazobenzene compound of the formula ##STR7## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of H, Cl, Br, I, NO.sub.2, NH.sub.2, RO, ArO, COOH or salts thereof, COOR, COOAr, CHO, COR, SO.sub.3 H or salts thereof, R or Ar and wherein R is an alkyl group of up to 18 carbon atoms and Ar is a mono- or bicyclic aryl group of up to 15 carbon atoms, wherein at least some of the ethylenically unsaturated monomer is hydroxyethyl methacrylate, in an amount sufficient to protect the unit dosage form from the action of digestive juices of the upper gastrointestinal tract and to prevent the medicament from causing an adverse effect on the upper gastrointestinal tract and or being absorbed therethrough;
- and
- (c) administering the thus-coated unit dosage form orally to the animal being given the medicament.
A method for delivering to the large intestine of an animal a medicament normally destroyed by the digestive juices of the upper gastrointestinal tract, having an undesired effect on the upper gastrointestinal tract or being absorbed therethrough, which medicament is capable of being absorbed through the mucosa of the large intestine, comprising;
- (a) entrapping a unit dosage amount of the medicament in a high molecular weight polymer from one or more ethylenically unsaturated monomers, cross-linked by a substituted or unsubstituted divinylazobenzene compound of the formula ##STR8## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of H, Cl, Br, I, NO.sub.2, NH.sub.2, RO, ArO, COOH or salts thereof, COOR, COOAr, CHO, COR, SO.sub.3 H or salts thereof, R or Ar and wherein R is an alkyl group of up to 18 carbon atoms and Ar is a mono- or bicyclic aryl group of up to 15 carbon atoms, and
- (b) administering the thus-entrapped unit dosage amount of medicament orally to the animal being given the medicament.
A method of administering a medicament to the large gastrointestinal mucosa of an animal requiring medicament at that location, comprising
- (a) formulating the medicament into a unit dosage form;
- (b) coating the unit dosage form with a high molecular weight polymer from one or more ethylenically unsaturated monomers, cross-linked by a substituted or unsubstituted divinylazobenzene compound of the formula ##STR9## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of H, Cl, Br, I, NO.sub.2, NH.sub.2, RO, ArO, COOH or salts thereof, COOR, COOAr, CHO, COR, SO.sub.3 H or salts thereof, R or Ar and wherein R is an alkyl group of up to 18 carbon atoms and Ar is a mono- or bicyclic aryl group of up to 15 carbon atoms, in an amount sufficient to protect the unit dosage form from the action of digestive juices of the upper gastrointestinal tract;
- and
- (c) administering the thus-coated unit dosage form orally to the animal being given the medicament.
A method of administering a medicament to the large gastrointestinal mucosa of an animal requiring medicament at that location, comprising
- (a) formulating the medicament into a unit dosage form;
- (b) encapsulating the medicament in a high molecular weight polymer from one or more ethylenically unsaturated monomers, cross-linked by a substituted or unsubstituted divinylazobenzene compound of the formula ##STR10## wherein R.sub.1 and R.sub.2 are independently selected from the group consisting of H, Cl, Br, I, NO.sub.2, NH.sub.2, RO, ArO, COOH or salts thereof, COOR, COOAr, CHO, COR, SO.sub.3 H or salts thereof, R or Ar and wherein R is an alkyl group of up to 18 carbon atoms and Ar is a mono- or bicyclic aryl group of up to 15 carbon atoms, and
- (c) administering the thus-entrapped medicament orally to the animal to which the medicament is being administered.
A method of delivering a medicament to the large intestinal mucosa of an animal requiring medicament at that location, comprising
- (a) formulating a high molecular weight polymer from one or more ethylenically unsaturated monomers, containing in the polymer chain a plurality of monomer units of the formula
- H.sub.2 C.dbd.CH--C.sub.6 H.sub.4 --N.dbd.N--M
- wherein M is the residue of a medicament, whenever made by copolymerization of the ethylenically unsaturated monomer and H.sub.2 C.dbd.CH--C.sub.6 H.sub.4 --N.dbd.N--M in a unit dosage form, either alone or in admixture with one or more physiologically and pharmaceutically acceptable carriers and
- (b) administering the unit dosage form orally to the animal being given the medicament.
Dependencies are inferred from the claim text.