Sustained release drug-resin complexes

Claim 2

An oral pharmaceutical composition in unit dosage form comprising irregularly shaped ion-exchange resin particles with an ion-­exchange capacity of less than about 6 meq/gram having particle sizes ranging from about 10 to about 500 microns, said particles having a pharmacologically active drug bound thereto wherein said drug comprises more than about 38% by weight of the drug-resin complex and wherein said drug-resin complex particles have been subsequently coated with from about 1.5% to about 25% by weight of the drug-resin complex of a water-permeable diffusion barrier and wherein said composition provides controlled release of said active drug.

Claim 3

A pharmaceutical composition according to Claim 1 wherein said irregularly shaped particles range from about 35 microns to about 150 microns.

Claim 4

A pharmaceutical composition according to Claim 2 wherein said irregularly shaped particles range from about 40 microns to about 80 microns.

Claim 5

A pharmaceutical composition according to Claim 3 wherein the ratio of pharmacologically-active drug to resin ranges from about 0.5:1 to about 1.5:1.

Claim 6

A pharmaceutical composition according to Claim 4 wherein the ratio of pharmacologically-active drug to resin ranges from about 0.8:1 to about 1.5:1.

Claim 7

A pharmaceutical composition according to Claim 5 wherein said pharmacologically-active drug is selected from the group consist­ing of dehydrocholic acid, diflunisal, ethacrynic acid, fenopro­fen, furosemide, gemfibrozil, ibuprofen, naproxen, phenytoin, probenecid, sulindac, theophylline, salicylic acid, acetylsali­cylic acid, acetophenazine, amitriptyline, amphetamine, benztro­pine, biperiden, bromodiphenhydramine, brompheniramine, carbinox­amine, chlorcyclizine, chlorpheniramine, chlorphenoxamine, chlor­promazine, clemastine, clomiphene, clonidine, codeine, cyclizine, cyclobenzaprine, cyproheptadine, desipramine, dexbrompheniramine, dexchlorpheniramine, dextroamphetamine, dextromethorphan, dicyclo­mine, diphemanil, diphenhydramine, doxepin, doxylamine, ergota­mine, fluphenazine, haloperidol, hydrocodone, hydroxychloroquine, hydroxyzine, hyoscyamine, imipramine, levopropoxyphene, maproti­line, meclizine, mepenzolate, meperidine, mephentermine, mesori­dazine, methadone, methdilazine, methscopolamine, methysergide, metoprolol, nortriptylene, noscapine, nylindrin, orphenadrine, papaverine, pentazocine, phendimetrazine, phentermine, phenylpro­panolamine, pyrilamine, tripelennamine, triprolidine, promazine, propoxyphene, propanolol, pseudoephedrine, pyrilamine, quinidine, scopolamine, dextromethorphan, chlorpheniramine, codeine, amino­caproic acid, aminosalicylic acid, hydromorphone, isoxsuprine, levorphanol, melphalan, morphine, nalidixic acid, and paraamino­salicylic acid and mixtures thereof.

Claim 8

A pharmaceutical composition according to Claim 6 wherein said resin particles have an ion-exchange capacity of less than about 5.5 meq./g.

Claim 9

A pharmaceutical composition according to Claim 7 wherein the ratio of pharmacologically-active drug to resin ranges from about 1:1 to about 1.5:1.

Claim 10

A pharmaceutical composition according to Claim 8 wherein said water-permeable diffusion barrier is selected from the group consisting of ethyl cellulose, methyl cellulose and mixtures thereof.

Claim 11

An oral pharmaceutical composition in unit dosage form comprising regularly shaped ion-exchange resin particles with an ion-exchange capacity of less than about 6 meq/gram having particle sizes ranging from about 10 to about 500 microns, said particles having a pharmacologically active drug bound thereto wherein said drug comprises more than about 30% by weight of the drug-resin complex and wherein said drug-resin complex particles have been subsequent­ly coated with from about 1.5% to about 25% by weight of the drug-resin complex of a water-permeable diffusion barrier and wherein said composition provides controlled release of said active drug.

Claim 12

An oral pharmaceutical composition in unit dosage form comprising regularly shaped ion-exchange resin particles with an ion-exchange capacity of less than about 6 meq/gram having particle sizes ranging from about 10 to about 500 microns, said particles having a pharmacologically active drug bound thereto wherein said drug comprises more than about 30% by weight of the drug-resin complex and wherein said drug-resin complex particles have been subsequent­ly coated with from about 1.5% to about 25% by weight of the drug-resin complex of a water-permeable diffusion barrier and wherein said composition provides controlled release of said active drug.

Claim 13

A pharmaceutical composition according to Claim 10 wherein said regularly shaped particles range from about 35 microns to about 150 microns.

Claim 14

A pharmaceutical composition according to Claim 11 wherein said regularly shaped particles range from about 40 microns to about 80 microns.

Claim 15

A pharmaceutical composition according to Claim 12 wherein the ratio of pharmacologically-active drug to resin ranges from about 0.4:1 to about 1.5:1.

Claim 16

A pharmaceutical composition according to Claim 13 wherein the ratio of pharmacologically-active drug to resin ranges from about 0.8:1 to about 1.5:1.

Claim 17

A pharmaceutical composition according to Claim 14 wherein said pharmacologically-active drug is selected from the group consist­ing of dehydrocholic acid, diflunisal, ethacrynic acid, fenopro­fen, furosemide, gemfibrozil, ibuprofen, naproxen, phenytoin, probenecid, sulindac, theophylline, salicylic acid, acetylsali­cylic acid, acetophenazine, amitriptyline, amphetamine, benztro­pine, biperiden, bromodiphenhydramine, brompheniramine, carbinox­amine, chlorcyclizine, chlorpheniramine, chlorphenoxamine, chlor­promazlne, clemastine, clomiphene, clonidine, codeine, cyclizine, cyclobenzaprine, cyproheptadine, desipramine, dexbrompheniramine, dexchlorpheniramine, dextroamphetamine, dextromethorphan, dicyclo­mine, diphemanil, diphenhydramine, doxepin, doxylamine, ergota­mine, fluphenazine, haloperidol, hydrocodone, hydroxychloroquine, hydroxyzine, hyoscyamine, imipramine, levopropoxyphene, maproti­line, meclizine, mepenzolate, meperidine, mephentermine, mesori­dazine, methadone, methdilazine, methscopolamine, methysergide, metoprolol, nortriptylene, noscapine, nylindrin, orphenadrine, papaverine, pentazocine, phendimetrazine, phentermine, phenylpro­panolamine, pyrilamine, tripelennamine, triprolidine, promazine, propoxyphene, propanolol, pseudoephedrine, pyrilamine, quinidine, scopolamine, dextromethorphan, chlorpheniramine, codeine, amino­caproic acid, aminosalicylic acid, hydromorphone, isoxsuprine, levorphanol, melphalan, morphine, nalidixic acid, and paraamino­salicylic acid and mixtures thereof.

Claim 18

A pharmaceutical composition according to Claim 15 wherein said resin particles have an ion-exchange capacity of less than about 5.5 meq./g.

Claim 19

A pharmaceutical composition according to Claim 16 wherein the ratio of pharmacologically-active drug resin ranges from about 1:1 to about 1.5:1.

Claim 20

A pharmaceutical composition according to Claim 17 wherein said water-permeable diffusion barrier is selected from the group consisting of ethyl cellulose, methyl cellulose and mixtures thereof.