# US 11,077,099 B2 · Oral tablet formulation of lenalidomide

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- Number: US 11,077,099 B2
- Document ID: US11077099B2
- Status: Granted
- Kind: B2
- Application number: 16/341,682
- Filed: 2017-09-11
- Published: 2020-02-06
- Granted: 2021-08-03
- Earliest claimed: 2016-10-14
- Assignees: Samyang Holdings Corporation
- Applicants: Samyang Holdings Corporation
- Inventors: Sang Yeob Park; Hye Jung Lim; Sa Won Lee; Min Hyo Seo
- Web page: https://patentgrep.com/patent/US11077099B2

## CPC

- A61K 9/284: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone}
- A61K 31/454: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
- A61K 9/00: Medicinal preparations characterised by special physical form {(nuclear magnetic resonance contrast preparations or magnetic resonance imaging contrast preparations A61K49/18; preparations containing radioactive substances A61K51/12)}
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A61K 9/28: Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)}
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 35/00: Antineoplastic agents
- 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

## Abstract

The present disclosure relates to an oral tablet composition comprising lenalidomide and a method for preparing the same. More particularly, the present disclosure relates to a tablet-type composition and a method for preparing the same wherein the composition exhibits physicochemical equivalence with lenalidomide preparations of hard capsules, has the same pharmacological, therapeutic effect in non-clinical studies and bioequivalence studies, and also has improved ease of taking, handling, safety and the like.

## Claims

### Claim 1

An oral tablet composition, comprising:
lenalidomide as an active ingredient;
a diluent selected from the group consisting of sugars, sugar alcohols, celluloses, starches and mixtures thereof;
a disintegrant selected from the group consisting of croscarmellose sodium, sodium starch glyconate and mixtures thereof; and
a lubricant selected from the group consisting of magnesium stearate, calcium stearate, sodium stearyl fumarate and mixtures thereof;
wherein 3 to 30 parts by weight of the diluent, 0.1 to 2.5 parts by weight of the disintegrant and 0.03 to 0.75 part by weight of the lubricant per 1 part by weight of lenalidomide are comprised;
AUC (area under curve) is 140 to 7100 ng·hr/mL;
Cmax is 42 to 2100 ng/mL;
the disintegration time in a buffer solution of pH 1.2 is 2 to 10 minutes; and
the tablet is a direct compression tablet.

### Claim 2 (depends on 1)

The oral tablet composition according to claim 1, wherein a dissolution rate is 1 to 50% when measured at 2.5 minutes in 900 mL dissolution medium of pH 1.2 by a paddle method at 50 revolutions/min.

### Claim 3 (depends on 2)

The oral tablet composition according to claim 2, wherein the dissolution rate at 5 minutes is 10 to 95%.

### Claim 4 (depends on 1)

The oral tablet composition according to claim 1, wherein a hardness is 10 N to 300 N.

### Claim 5 (depends on 1)

The oral tablet composition according to claim 1, wherein a friability is less than 2%.

### Claim 6 (depends on 1)

The oral tablet composition according to claim 1, wherein the composition is in the form of a tablet and the tablet is coated with a coating agent.

### Claim 7 (depends on 6)

The oral tablet composition according to claim 6, wherein the coating layer is more than a single layer.

### Claim 8 (depends on 6)

The oral tablet composition according to claim 6, wherein a total thickness of the coating layer is no less than 1 μm.

### Claim 9 (depends on 6)

The oral tablet composition according to claim 6, wherein the coating agent is selected from the group consisting of polyvinylpyrrolidone, hydroxypropylmethylcellulose, carboxymethylcellulose and salts thereof, ethylcellulose, methylcellulose, hydroxyethylcellulose, ethylhydroxyethylcellulose, hydroxypropylcellulose, low-substituted hydroxypropylcellulose, polyvinyl alcohol, Macrogol polyvinylalcohol graft copolymer, polymer of acrylic acid and its salt, polymethacrylate, poly(butylmethacrylate, 2-dimethylaminoethyl methacrylate, methyl methacrylate) copolymer, vinylpyrrolidone-vinyl acetate copolymer, gelatin, guar gum, partially hydrolyzed starch, alginate, xanthan and mixtures thereof.

### Claim 10 (depends on 1)

The oral tablet composition according to claim 1, wherein the diluent is selected from the group consisting of lactose, cellulose powder, microcrystalline cellulose, silicified microcrystalline cellulose, starch, gelatinized starch, calcium carbonate, cyclodextrin, mannitol, maltitol, sorbitol, xylitol, lactose, dextrose, maltose, sucrose, glucose, fructose, maltodextrin, dextrates, dextrin and mixtures thereof.

### Claim 11 (depends on 1)

The oral tablet composition according to claim 1, wherein the composition is in the form of a tablet and the volume of the tablet is less than that of a size 0 capsule.