# US 9,750,696 B2 · Dissolution enhanced controlled drug delivery system for poorly water soluble drugs

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- Number: US 9,750,696 B2
- Document ID: US9750696B2
- Status: Granted
- Kind: B2
- Application number: 14/236,162
- Filed: 2012-08-01
- Published: 2015-06-25
- Granted: 2017-09-05
- Earliest claimed: 2011-08-01
- Assignees: Sun Pharmaceutical Industries Limited
- Applicants: Sandeep Kumar Vats; Kalaiselvan Ramaraju; Romi Barat Singh
- Inventors: Sandeep Kumar Vats; Kalaiselvan Ramaraju; Romi Barat Singh
- Web page: https://patentgrep.com/patent/US9750696B2

## CPC

- A61K 9/146: {with organic macromolecular compounds}
- A61K 9/1635: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/1641: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/2031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers}
- A61K 9/2045: {Polyamides; Polyaminoacids, e.g. polylysine}
- A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/4808: {characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release (capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084)}
- A61K 9/5042: {Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose}
- A61K 9/5078: {with drug-free core}
- A61K 31/41: having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K 31/546: containing further heterocyclic rings, e.g. cephalothin
- A61K 9/5047: {Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

The present invention relates to controlled-release pharmaceutical dosage forms comprising a solid dispersion of a poorly water-soluble or insoluble drug with improved solubility and thus improved dissolution in an aqueous medium. The invention further discloses a process of preparation of these controlled-release dosage forms.

## Claims

### Claim 1

A controlled-release pharmaceutical dosage form of a poorly water-soluble or insoluble drug comprising the solid dispersion of said drug, one or more of controlled-release material to slow the release of the drug, and one or more of pharmaceutically acceptable excipients; wherein the said solid dispersion comprises the said drug dispersed in polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer in a ratio of drug to graft copolymer at a weight by weight ratio of from 1:1 to 1:5.

### Claim 2 (depends on 1)

The controlled-release pharmaceutical dosage form of claim 1, wherein the dosage form is a matrix-type dosage form or a reservoir-type dosage form.

### Claim 3 (depends on 1)

The controlled-release pharmaceutical dosage form of claim 1, wherein the dosage form is in the form of hard or soft gelatin capsules, tablets, capsules, caplets, pills, granules or mini-tablets.

### Claim 4 (depends on 1)

The controlled-release pharmaceutical dosage form of claim 1, wherein the controlled-release material comprises hydrophilic polymers, hydrophobic polymers, water-swellable polymers, hydrophobic materials, or mixtures thereof.

### Claim 5 (depends on 4)

The controlled-release pharmaceutical dosage form of claim 4, wherein the amount of the controlled-release material comprises from about 2% to about 95% by weight of the dosage form.

### Claim 6 (depends on 1)

The controlled-release pharmaceutical dosage form of claim 1, wherein the pharmaceutically acceptable excipients comprise one or more of binders, fillers/diluents, disintegrants, anti-adherents, lubricants/glidants, plasticizers, coloring agents and flavoring agents.

### Claim 7

A process for the preparation of a controlled-release pharmaceutical dosage form of a poorly water-soluble or insoluble drug comprising the solid dispersion of said drug, one or more of controlled-release material to slow the release of the drug, and one or more of pharmaceutically acceptable excipients; wherein the said solid dispersion comprises said drug dispersed in polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer in a ratio of drug to graft copolymer at a weight by weight ratio of from 1:1 to 1:5; and wherein the process includes combining the solid dispersion, the controlled-release material and pharmaceutically acceptable excipient and processing into the dosage form using appropriate toolings.

### Claim 8 (depends on 1)

The controlled-release pharmaceutical dosage form of claim 1, wherein the controlled-release material slows the release of the drug to provide for release in a continuous manner.

### Claim 9 (depends on 8)

The controlled-release pharmaceutical dosage form of claim 8, wherein the controlled-release material releases the drug to provide for absorption in a continuous manner.

### Claim 10 (depends on 7)

The controlled-release pharmaceutical dosage form of claim 7, wherein the controlled-release material slows the release of the drug to provide for release in a continuous manner.

### Claim 11 (depends on 10)

The controlled-release pharmaceutical dosage form of claim 10, wherein the controlled-release material releases the drug to provide for absorption in a continuous manner.

### Claim 12 (depends on 2)

The controlled-release pharmaceutical dosage form of claim 2, wherein the dosage form is a reservoir-type dosage form comprising a core and a controlled release coating, and the core comprises the drug and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer.

### Claim 13 (depends on 12)

The controlled-release pharmaceutical dosage form of claim 12, wherein the controlled release coating comprises a polymer.

### Claim 14 (depends on 13)

The controlled-release pharmaceutical dosage form of claim 13, wherein the polymer comprises one or more of cellulose acetate, ethyl cellulose, polyamide, polyethylene, polyethylene terephthalate, polypropylene polyurethane, polyvinyl acetate, polyvinyl chloride, polyhydroxybutyrate, polyhydroxyvalerate, ethylene vinyl acetate copolymers, styrene-butadienestyrene copolymers, styrene-isoprene-styrene copolymers, and polylactic acid, polyglycolic acid and copolymers thereof, and mixtures thereof.