# US 12,178,819 B2 · DPP IV inhibitor formulations

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- Number: US 12,178,819 B2
- Document ID: US12178819B2
- Status: Granted
- Kind: B2
- Application number: 17/319,325
- Filed: 2021-05-13
- Published: 2021-08-26
- Granted: 2024-12-31
- Earliest claimed: 2006-05-04
- Assignees: Boehringer Ingelheim International GmbH
- Applicants: Boehringer Ingelheim International GmbH
- Inventors: Anja Kohlrausch; Patrick Romer; Gerd Seiffert
- Web page: https://patentgrep.com/patent/US12178819B2

## CPC

- A61K 31/522: having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
- A61K 9/2009: {Inorganic compounds}
- 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 9/2054: {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)}
- A61K 9/2813: {Inorganic compounds}
- A61K 9/2853: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)}
- A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/2893: {Tablet coating processes (mechanical aspects A61J3/06)}
- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/10: for osteoporosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets}
- 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 invention relates to pharmaceutical compositions of DPP IV inhibitors with an amino group, their preparation and their use to treat diabetes mellitus.

## Claims

### Claim 1

A pharmaceutical composition comprising as an active ingredient a DPP IV inhibitor compound of formula
in an amount of 5 mg, or a salt thereof, a first diluent, a second diluent, a binder, a disintegrant and a lubricant, wherein the first diluent is mannitol and the second diluent is pregelatinized starch
wherein the pharmaceutical composition comprises:
0.5-20% by weight of active ingredient
40-88% by weight of first diluent,
3-40% by weight of second diluent,
1-5% by weight of binder,
5-15% by weight of disintegrant, and
0.1-4% by weight of lubricant.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1, wherein the lubricant is talc, polyethylene glycol, calcium behenate, calcium stearate, hydrogenated castor oil, or magnesium stearate.

### Claim 3 (depends on 1)

The pharmaceutical composition of claim 1, wherein the binder is copovidone, hydroxypropyl methylcellulose (HPMC), hydroxypropylcellulose (HPC), or polyvinylpyrrolidone (Povidone).

### Claim 4 (depends on 1)

The pharmaceutical composition of claim 1, wherein the disintegrant is corn starch.

### Claim 5 (depends on 1)

The pharmaceutical composition of claim 1, wherein the first diluent is mannitol, the second diluent is pregelatinized starch, the binder is copovidone, the disintegrant is corn starch, and the lubricant is magnesium stearate.

### Claim 6 (depends on 1)

The pharmaceutical composition of claim 1 further comprising an additional disintegrant.

### Claim 7 (depends on 6)

The pharmaceutical composition of claim 6, wherein the additional disintegrant is crospovidone.

### Claim 8 (depends on 1)

The pharmaceutical composition of claim 1 further comprising a glidant.

### Claim 9 (depends on 8)

The pharmaceutical composition of claim 8, wherein the glidant is colloidal silicon dioxide.

### Claim 10 (depends on 1)

The pharmaceutical composition of claim 1 comprising
0.5-7% active ingredient
50-75% diluent 1,
5-15% diluent 2,
2-4% binder,
8-12% disintegrant, and
0.5-2% lubricant.

### Claim 11 (depends on 1)

The pharmaceutical composition according to claim 1 in the dosage form of a capsule, a tablet, or a film-coated tablet.

### Claim 12 (depends on 11)

The pharmaceutical composition of claim 11 comprising 2-4% film coat.

### Claim 13 (depends on 11)

The pharmaceutical composition of claim 11, wherein the film coat comprises a film-forming agent, a plasticizer, a glidant and optionally one or more pigments.

### Claim 14 (depends on 13)

The pharmaceutical composition of claim 13, wherein the film coat comprises hydroxypropylmethylcellulose (HPMC), polyethylene glycol (PEG), talc, titanium dioxide and iron oxide.

### Claim 15 (depends on 1)

The pharmaceutical composition of claim 1, wherein the binder is
copovidone, hydroxypropyl methylcellulose (HPMC), hydroxypropylcellulose (HPC), polyvinylpyrrolidon (povidone), pregelatinized starch, or low-substituted hydroxypropylcellulose (L-HPC).

### Claim 16 (depends on 1)

The pharmaceutical composition of claim 1, wherein the disintegrant is
corn starch, crospovidone, low-substituted hydroxypropylcellulose (L-HPC), or pregelatinized starch.

### Claim 17 (depends on 1)

The pharmaceutical composition of claim 1, wherein the lubricant is
talc, polyethyleneglycol, calcium behenate, calcium stearate, hydrogenated castor oil, or magnesium stearate.

### Claim 18 (depends on 1)

The pharmaceutical composition of claim 1, wherein
the binder is copovidone, hydroxypropyl methylcellulose (HPMC), hydroxypropylcellulose (HPC), polyvinylpyrrolidon (povidone), pregelatinized starch, or low-substituted hydroxypropylcellulose (L-HPC);
the disintegrant is corn starch, crospovidone, low-substituted hydroxypropylcellulose (L-HPC), or pregelatinized starch; and
lubricant is talc, polyethyleneglycol, calcium behenate, calcium stearate, hydrogenated castor oil, or magnesium stearate.

### Claim 19 (depends on 1)

The pharmaceutical composition of claim 1, wherein the DPP IV inhibitor compound is present in an amount 0.5-7.0% based on the total weight of DPP IV inhibitor, first diluent, second diluent, binder, disintegrant and lubricant.

### Claim 20 (depends on 1)

The pharmaceutical composition of claim 1, in the dosage form of a tablet, or a film-coated tablet.