# US 7,744,924 B2 · Venlafaxine formulations and methods of preparing the same

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- Number: US 7,744,924 B2
- Document ID: US7744924B2
- Status: Granted
- Kind: B2
- Application number: 11/675,831
- Filed: 2007-02-16
- Published: 2007-06-14
- Granted: 2010-06-29
- Earliest claimed: 2003-12-30
- Assignees: Actavis Group HF.
- Inventors: Grant Heinicke
- Web page: https://patentgrep.com/patent/US7744924B2

## CPC

- A61K 9/2095: {Tabletting processes}
- A61K 9/1676: {having a drug-free core with discrete complete coating layer containing drug (adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921)}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- 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

A method of forming a multi-particulate dosage form using rotary granulation is described in which polyethylene oxide is employed as s binder in a rotary granulation process. A multi-particulate oral dosage form comprises a plurality of pellets, the pellets comprising a core having disposed thereon a core composition layer. The core composition layer comprises venlafaxine and a binder, wherein the binder comprises a polyethylene oxide. In other embodiments, the binder comprises a 1:2:1 bis (butyl methacrylate-co-(2-dimethylaminoethyl)methacrylate-co-methyl methacrylate.

## Claims

### Claim 1

A multi-particulate oral dosage form, comprising a plurality of pellets, the pellets comprising a core having disposed thereon a core composition layer, the core composition layer comprising an admixture of venlafaxine and a binder, wherein the binder comprises polyethylene oxide, wherein the polyethylene oxide has an average molecular weight of about 100,000 to about 6,000,000, and wherein a ratio of polyethylene oxide to venlafaxine is about 1:30 to about 1:5.

### Claim 2 (depends on 1)

The multi-particulate oral dosage form of claim 1, wherein the binder comprises about 0.2 wt % to about 12 wt % of the total weight of the core and the core composition layer.

### Claim 3 (depends on 1)

The multi-particulate oral dosage form of claim 1, comprising about 10 wt % to about 98 wt % of the core, about 2 wt % to about 85 wt % of the venlafaxine, and about 0.1 wt % to about 20 wt % of the binder, all based on the total weight of the core and the core composition layer.

### Claim 4 (depends on 3)

The multi-particulate oral dosage form of claim 3, comprising about 10 wt % to about 70 wt % of the venlafaxine, based on the total weight of the core and the core composition layer.

### Claim 5 (depends on 1)

The multi-particulate oral dosage form of claim 1, further comprising an additional coating layer, wherein the additional coating layer is a controlled-release coating, a seal coating, or a combination of one or more of the foregoing coatings.

### Claim 6 (depends on 1)

The multi-particulate dosage form of claim 1, wherein the core is an inert sphere.

### Claim 7 (depends on 6)

The multi-particulate dosage form of claim 6, wherein the inert sphere comprises nonpareils, sugar spheroids, microcrystalline cellulose spheres, spheres made of microcrystalline cellulose and one or more sugars, or a combination of one or more of the foregoing cores.

### Claim 8 (depends on 1)

The multi-particulate dosage form of claim 1, wherein the inert sphere is a sugar sphere.

### Claim 9 (depends on 1)

The multi-particulate dosage form of claim 1, wherein the core composition layer further comprises a plasticizer.

### Claim 10

A multi-particulate oral dosage form, comprising a plurality of pellets, the pellets comprising an inert sphere core having disposed thereon a core composition layer, the core composition layer comprising an admixture of venlafaxine, a plasticizer, and a binder, wherein the binder comprises a 1:2:1 (butyl methacrylate-co-(2-dimethylaminoethyl)methacrylate-co-methyl methacrylate).

### Claim 11 (depends on 10)

The multi-particulate oral dosage form of claim 10, wherein the ratio of binder to venlafaxine in the core composition layer is about 1:30 to about 1:5.

### Claim 12 (depends on 10)

The multi-particulate oral dosage form of claim 10, wherein the binder comprises about 0.2 wt % to about 12 wt % of the total weight of the core and the core composition layer.

### Claim 13 (depends on 10)

The multi-particulate oral dosage form of claim 10, comprising about 10 wt % to about 98 wt % of the core, about 2 wt % to about 85 wt % of the venlafaxine, and about 0.1 wt % to about 20 wt % of the binder, all based on the total weight of the core and the core composition layer.

### Claim 14 (depends on 13)

The multi-particulate oral dosage form of claim 13, comprising about 10 wt % to about 70 wt % of the venlafaxine, based on the total weight of the core and the core composition layer.

### Claim 15 (depends on 1)

The multi-particulate oral dosage form of claim 1, further comprising an additional coating layer, wherein the additional coating layer is a controlled-release coating, a seal coating, or a combination of one or more of the foregoing coatings.

### Claim 16 (depends on 10)

The multi-particulate dosage form of claim 10, wherein the inert sphere is a sugar sphere.

### Claim 17 (depends on 1)

A method of making a multi-particulate oral dosage form, of claim 1 comprising mixing venlafaxine, a binder comprising polyethylene oxide, and a dispersing agent to form a coating mixture, and
atomizing the coating mixture in the presence of a plurality of cores in a fluidized bed with a rotor-disk granulator to produce a plurality of pellets, the pellets comprising the core having disposed thereon a core composition layer comprising the venlafaxine and the binder.