# US 2017/0281631 A1 · Pharmaceutical formulation of palbociclib and a preparation method thereof

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- Number: US 2017/0281631 A1
- Document ID: US20170281631A1
- Status: Published application
- Kind: A1
- Application number: 15/613,853
- Filed: 2017-06-05
- Published: 2017-10-05
- Earliest claimed: 2016-03-29
- Assignees: Shenzhen HLK Pharmaceuticals Co., Ltd.
- Applicants: Shenzhen HLK Pharmaceuticals Co., Ltd.
- Inventors: Zeren WANG; Jun XU; Long QU
- Web page: https://patentgrep.com/patent/US20170281631A1

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 9/145: {with organic compounds}
- A61K 9/146: {with organic macromolecular compounds}
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- 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)}
- A61P 35/00: Antineoplastic agents
- C07D 471/04: Ortho-condensed systems
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention belongs to the pharmaceutical field, and in particular, it relates to a pharmaceutical formulation of palbociclib and a preparation method thereof. The pharmaceutical formulation comprises palbociclib, an acidic auxiliary material, and optionally a hydrophilic high-molecular material, which has better solubility and in vitro dissolution property as compared with the conventional formulation and can be used for enhancing in vivo absorption and bioavailability of palbociclib.

## Claims

### Claim 1

A pharmaceutical formulation of palbociclib, comprising a palbociclib free base or a pharmaceutically acceptable salt thereof and an acidic auxiliary material, wherein the acidic auxiliary material is one or more selected from the group consisting of tartaric acid, fumaric acid, succinic acid, citric acid, lactic acid and malic acid, and wherein a mass ratio of the acidic auxiliary material to palbociclib is from 0.2:1 to 5:1.

### Claim 2 (depends on 1)

The pharmaceutical formulation according to claim 1, wherein the palbociclib free base or the salt thereof is a solid and has a particle size of 20 μm or less.

### Claim 3 (depends on 1)

The pharmaceutical formulation according to claim 1, wherein the mass ratio of the acidic auxiliary material to palbociclib is from 0.5:1 to 2:1.

### Claim 4 (depends on 1)

The pharmaceutical formulation according to claim 1, which is a tablet or capsule.

### Claim 5 (depends on 4)

The pharmaceutical formulation according to claim 4, wherein the tablet or capsule has a dosage of from 25 mg to 500 mg.

### Claim 6 (depends on 5)

The pharmaceutical formulation according to claim 5, wherein the tablet or capsule has a dosage of from 50 mg to 150 mg.

### Claim 7

A solid dispersion of palbociclib, comprising a palbociclib free base or a pharmaceutically acceptable salt thereof, an acidic auxiliary material and a hydrophilic high-molecular material.

### Claim 8 (depends on 7)

The solid dispersion according to claim 7, wherein the acidic auxiliary material is selected from one or more pharmaceutically acceptable organic acids and optionally one or more pharmaceutically acceptable inorganic acids.

### Claim 9 (depends on 8)

The solid dispersion according to claim 8, wherein the pharmaceutically acceptable organic acid is selected from the group consisting of tartaric acid, fumaric acid, succinic acid, citric acid, lactic acid, malic acid, aliphatic sulfonic acid and aromatic sulfonic acid, and the pharmaceutically acceptable inorganic acid is selected from the group consisting of hydrochloric acid, sulfuric acid and phosphoric acid.

### Claim 10 (depends on 9)

The solid dispersion according to claim 9, wherein the aliphatic sulfonic acid is selected from the group consisting of methanesulfonic acid, ethanesulfonic acid and isethionic acid, and the aromatic sulfonic acid is selected from the group consisting of benzenesulfonic acid and p-toluenesulfonic acid.

### Claim 11 (depends on 7)

The solid dispersion according to claim 7, wherein the hydrophilic high-molecular material is one or more selected from the group consisting of povidone K30, copovidone VA64, Soluplus, hydroxypropylmethylcellulose E5, hydroxypropylmethylcellulose acetate succinate, hydroxypropyl-β-cyclodextrin and sulfobutyl ether-β-cyclodextrin.

### Claim 12 (depends on 7)

The solid dispersion according to claim 7, wherein the mass ratio of the hydrophilic high-molecular material to palbociclib is from 0.1:1 to 10:1, and the mass ratio of the acidic auxiliary material to palbociclib is from 0.2:1 to 5:1.

### Claim 13 (depends on 12)

The solid dispersion according to claim 12, wherein the mass ratio of the hydrophilic high-molecular material to palbociclib is from 1:1 to 3:1, and the mass ratio of the acidic auxiliary material to palbociclib is from 0.5:1 to 2:1.

### Claim 14 (depends on 1)

A method for the preparation of a pharmaceutical formulation according to claim 1, comprising: mixing an API of palbociclib with a pharmaceutically acceptable acidic auxiliary material; or pulverizing the API of palbociclib to control the particle size at 20 μm or less, and then mixing with the acidic auxiliary material; or adding the acidic auxiliary material to the API, mixing and co-pulverizing to control the particle size at 20 μm or less.

### Claim 15 (depends on 7)

A method for the preparation of a solid dispersion according to claim 7, comprising: mixing an API of palbociclib with an acidic auxiliary material, adding a solvent for dissolving or dispersing, adding a hydrophilic high-molecular material, dissolving or dispersing evenly, and removing the solvent by heating.

### Claim 16 (depends on 15)

The method for the preparation according to claim 15, wherein the concentration of the API of palbociclib in the solvent is up to 50 mg/ml or more.

### Claim 17 (depends on 1)

Use of a pharmaceutical formulation according to claim 1 in the manufacture of a medicament for the treatment of breast cancer.