SUSTAINED RELEASE COMPOSITIONS

• US 20130230587A1
• Filed: 11/10/2010
• Published: 09/05/2013
• Est. Priority Date: 11/10/2010
• Status: Active Application

• Current Assignee: Rubicon Research Pvt. Ltd.
• Original Assignee: Rubicon Research Pvt. Ltd.
• Inventors: Pilgaonkar, Pratibha Sudhir, Rustomjee, Maharukh Tehmasp, Gandhi, Anikumar Surendrakumar
• Application Number:
  US13/884,652
• Publication Number:
  US 20130230587A1
• Time in Patent Office: Days
• US Class Current: 424/462
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/58 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
• CPC Class Codes: A61K 9/0002 Galenical forms characterised by the drug release technique; Application systems commanded by energy
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/0095 Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006
• CPC Class Codes: A61K 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61K 9/5047 Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 11/14 Antitussive agents

Abstract

Sustained release compositions comprising plurality of sustained release beads are disclosed. Particularly the sustained release beads comprise coated drug-resin complexes comprising drug-resin complexes of at least one active agent and at least one ion-exchange resin; coated with at least one release modifier.

Claims

1. ) A sustained release composition comprising plurality of sustained release beads comprising coated drug-resin complexes comprising:

a. drug-resin complex; and

b. release modifier coating.

2. ) The composition of claim 1 wherein the drug-resin complex comprises at least one active agent and at least one ion-exchange resin.

3. ) The composition of claim 2 wherein the active agent is an anti-tussive agent, an analgesic, an antihistamine, an expectorant, a mucolytic, a decongestant, an analeptic agent, an anesthetic agent, an anti-asthmatic, an anti-arthritic agent;

an anti-cancer agent, an anti-cholinergic agent, an anti-convulsant agent, an anti-depressant agent, an antidiabetic, an anti-helminthic agent, an anti-diarrheal agent;

an anti-epileptic, an anti-hyperlipidemic agent;

an antihypertensive, an antihypotensive, an anti-infective agent, an anti-inflammatory agent, a non-steroidal anti-inflammatory agent, an anti-emetic, an anti-migraine agent;

an anti-neoplastic agent, an anti-tubercular agent, an antibiotic, an antacid, an antiulcer agent;

an anti-Parkinsonism drug, an anti-pruritic agent, an antipsychotic agent, an anti-pyretic agent, an anti-spasmodic, an anti-viral agent, an anxiolytic agent, an appetite suppressant, an attention deficit hyperactivity disorder treating agent, a cardiovascular agent, a calcium channel blocker, an antianginal agent, a central nervous system agent, a beta-blocker, an antiarrhythmic agent, a bronchodilator, a central nervous system stimulant, a diuretic, a genetic material, a hormoholytic, a hypnotic, a hypercalcemic, a hypoglycemic agent, an immunosuppressive agent, an antimuscarinic, a genitourinary smooth muscle relaxant, a beta-agonist, a narcotic antagonist, nicotine, a nutritional agent, a parasympatholytic, a peptide drug, an antihemorrhoidal, a psychostimulant, a psychotropic, a mucolytic, a sedative, a laxative, a vitamin, a sialagogue, a steroid, a sympathomimetic, a tranquilizer, or a vasodilator or a combination thereof in the form of free base, free acid, pharmaceutically acceptable salt, prodrug, active metabolite, polymorph, solvate, hydrate, enantiomer, optical isomer, tautomer or racemic mixture thereof.

4. ) The composition of claim 2 wherein the active agent is dextromethorphan, hydrocodone, chlorpheniramine, phenylephrine, pseudoephedrine, codeine, morphine, dihydromorphone, oxycodone, dimenhydrinate, diphenhydramine, brompheniramine, cetirizine, levocetirizine, ambroxol, bromhexine, carbocisteine, domiodol, guaifenesin, hydroxyzine, dexbrompheniramine, fexofenadine, terfenadine, dexchlorpheniramine or combination thereof in the form of free base, free acid, pharmaceutically acceptable salt, prodrug, active metabolite, polymorph, solvate, hydrate, enantiomer, optical isomer, tautomer or racemic mixture thereof.

5. ) The composition of claim 2 wherein the ion exchange resin is a cation exchange resin or an anion exchange resin or combination thereof.

6. ) The composition of claim 2 wherein the cation exchange resin is a copolymer of methacrylic acid and divinylbenzene, a sodium polystyrene sulfonate resin, a sulfonated copolymer of styrene and divinylbenzene, a crosslinked polyacrylic acid resin, a polyacrylate resin, a crosslinked carboxylic acid resin, a crosslinked sulfonic acid resin, a crosslinked phosphonic acid resin, zeolite or a combination thereof.

7. ) The composition of claim 2 wherein the active agent and the ion exchange resin are present in a ratio of about 1:

0.1 to about 1;

20 in the drug-resin complex.

8. ) The composition of claim 1 wherein the release modifier coating comprises at least one release modifier, said release modifier being a water-insoluble release modifier, a water-soluble release modifier or a combination thereof.

9. ) The composition of claim 8 wherein the water-insoluble release modifier is a polymeric water-insoluble release modifier, a non-polymeric water-insoluble release modifier or a combination thereof.

10. ) The composition of claim 9 wherein the polymeric water-insoluble release modifier is polyvinyl acetate, polyvinyl chloride, polyvinyl carbonate, ethyl cellulose, nitrocellulose, vinylidene chloride-acrylonitrile copolymer, acrylonitrile-styrene copolymer, ethylene vinyl acetate, cellulose acetate, cellulose acetate phthalate, cellulose acetate butyrate, copolymer of vinyl pyrrolidone, hydroxypropylmethylcellulose phthalate, methacrylic acid copolymer, or methacrylate copolymer or a combination thereof.

11. ) The composition of claim 8 wherein the water-soluble release modifier is polyvinylpyrrolidone, poloxamer, guar gum, xanthan gum, gum arabic, tragacanthan, cellulose derivatives such as hydroxypropylmethylcellulose, hydroxypropyl cellulose, methylcellulose, and hydroxyethyl cellulose, carboxymethylethyl cellulose, hydroxyethylmethyl carboxymethyl cellulose, hydroxyethyl methyl cellulose, carboxymethyl cellulose, methylhydroxyethyl cellulose, or methylhydroxypropyl cellulose or a combination thereof.

12. ) The composition of claim 1 wherein the coated drug-resin complexes are present in the form of at least two populations of variably coated drug-resin complexes.

13. ) The composition of claim 12 wherein the variably coated drug-resin complexes comprise at least one population of drug-resin complexes coated with at least one release modifier from about 1% to about 25% by weight of the drug-resin complex;

and at least one population of drug-resin complexes coated with at least one release modifier from about 5% to about 75% by weight of the drug-resin complex.

14. ) The composition of claim 12 wherein the variably coated drug-resin complexes comprise at least one population of drug-resin complexes coated with at least one release modifier from about 1% to about 15% by weight of the drug-resin complex;

and at least one population of drug-resin complexes coated with at least one release modifier from about 15% to about 75% by weight of the drug-resin complex.

15. ) The composition of claim 1 wherein the sustained release composition comprising plurality of sustained release beads comprising coated drug-resin complexes comprising:

a. drug-resin complex comprising at least one active agent and at least one ion-exchange resin; and

b. release modifier coating;

wherein coated drug-resin complexes are present in the form of at least two populations of variably coated drug-resin complexes comprising at least one population of drug-resin complexes coated with at least one release modifier from about 1% to about 25% by weight of the drug-resin complex; and

at least one population of drug-resin complexes coated with at least one release modifier from about 5% to about 75% by weight of the drug-resin complex.

16. ) The composition of claim 1 wherein the sustained release beads further comprise at least one pharmaceutically acceptable excipient, said pharmaceutically acceptable excipient being a diluent, a stabilizer, or a release modifier or mixture thereof.

17. ) The composition of claim 1 wherein the sustained release composition is in the form of a liquid, a solid or a semisolid preparation;

said liquid preparation being suspension and said solid preparation being capsule, tablet, caplet, orally disintegrating tablet, dispersible tablet, dry suspension for reconstitution, granule, wafer or bite-dispersion tablet.

18. ) The composition of claim 1 wherein the sustained release composition further comprises at least one pharmaceutically acceptable excipient;

said pharmaceutically acceptable excipient being binder, disintegrant, superdisintegrant, diluent, salivating agent, surfactant, flavor, sweetener, colorant, souring agent, viscolizer, glidant, lubricant, solubilizer, stabilizer, suspending agent, preservative, cosolvent, anti-caking agent, or buffer or a combination thereof.

19. ) The composition of claim 1 wherein the sustained release composition further comprises an additional active agent.

20. ) The composition of claim 19 wherein the additional active agent is delivered in an immediate release or sustained release manner.