Resinate sustained release dextromethorphan composition

Claim 2

An antitussive pharmaceutical composition suitable for controlled, sustained release of dextromethorphan comprising (a) a sulfonated polystyrene resin in salt-form crosslinked with about 3% to about 10% by weight (based on the total resin) of cross-linking agent, said resin having an average particle size of at least 40 μm and less than 100 μm, (b) an effective amount of a pharmaceutically acceptable acid addition salt of dextromethorphan, which has been loaded onto said resin in a weight ratio of dextromethorphan-acid addition salt:resin of about 1:5 to about 1:10, and (c) at least one pharmaceutically acceptable adjuvant.

Claim 3

The composition of claim 1 wherein said cross-linking agent is a di or poly acrylate or methacrylate of a diol, a divinyl compounds, or a diallyl compound.

Claim 4

The composition of claim 1 wherein said cross-linking agent is divinyl benzene.

Claim 5

The composition of claim 1 wherein said resin is crosslinked with about 4% to about 8% by weight, based on the total of preloaded resin, of crosslinking agent.

Claim 6

The composition of claim 1 wherein the salt form of said resin is the sodium salt form and said resin is crosslinked with about 8% by weight of divinyl benzene, based on the total preloaded weight of resin.

Claim 7

The composition of claim 5 wherein said average particle size is about 50 μm to about 70 μm.

Claim 8

The composition of claim 5 wherein at least 95% of said resin particles are of said average particle size.

Claim 9

The composition of claim 5 wherein said dextromethorphan-acid addition salt is detromethorphan hydrobromide.

Claim 10

The composition of claim 8 wherein said dextromethorphan hydrobromide:resin ratio is about 1:6.

Claim 11

The composition of claim 8 wherein said resin is a sulfonated polystyrene homopolymer which is crosslinked with about 8% of divinyl benzene, based on the preloaded weight of resin.

Claim 12

The composition of claim 1 wherein said average particle size of said resin in dry state is between about 40 μm and about 80 μm.

Claim 13

The composition of claim 1 wherein said ratio is 1:5-1:8.

Claim 14

The composition of claim 12 wherein said ratio is about 1:6.

Claim 15

The composition of claim 1 wherein said adjuvants are selected from pharmaceutically acceptable solvents, thickeners, sweeteners, flavorings, colorings, and preservatives.

Claim 16

The composition of claim 14 wherein (a) said solvent is water or a hydroalcoholic solution; (b) said thickener is selected from lower alkyl cellulose ethers, hydroxy and carboxy derivatives thereof; bentonite, tragacanth; and acacia; (c) said sweetener is selected from artificial sweeteners, mono and disaccharides, and sugar alcohols; (d) said preservative is selected from lower alkyl paraben, propylene glycol, and sorbic acid.

Claim 17

The antitussive composition of claim 14 comprising ______________________________________ resinate anti-tussive effective amount tragacanth 0.3 g-1.5 g sorbitol 30 g-60 g artificial sweetener 0.05 g-0.2 g 1,2 propylene glycol 1 g-10 g paraben preservative 0.12 g-0.19 g sorbic acid 0.05 g-0.2 g solvent sufficient to make 100 ml ______________________________________

Claim 18

The anti-tussive composition of claim 16 comprising ______________________________________ resinate 2.10 g (dextromethorphan hydrobromide:resin = 1:6) tragacanth 1.00 g sorbitol 40.00 g saccharin sodium 0.1 g 1,2 propylene glycol 2.5 g methyl paraben 0.12 g propyl paraben 0.03 g sorbic acid 0.1 g water sufficient to make 100 ml ______________________________________

Claim 19

The composition of claim 16 further comprising additional active ingredients.

Claim 20

The composition of claim 18 wherein said additional active ingredients are selected from antihistamines, decongestants, demulcents, analgesics, and further antitussives.

Claim 21

A pharmaceutical composition according to claim 1 wherein the pharmaceutically acceptable acid addition salt of dextromethorphan is the hydrobromide addition salt of dextromethorphan.