# US 11,298,325 B2 · Pharmaceutical compositions of pimobendan

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- Number: US 11,298,325 B2
- Document ID: US11298325B2
- Status: Granted
- Kind: B2
- Application number: 17/097,039
- Filed: 2020-11-13
- Published: 2021-03-04
- Granted: 2022-04-12
- Earliest claimed: 2013-12-04
- Applicants: Boehringer Ingelheim Vetmedica GmbH
- Inventors: Péter Laczay
- Web page: https://patentgrep.com/patent/US11298325B2

## CPC

- A61K 9/5031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)}
- A61K 9/1641: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers}
- A61K 9/2081: {with microcapsules or coated microparticles according to A61K9/50}
- A61K 9/5015: {Organic compounds, e.g. fats, sugars}
- A61K 9/5089: {Processes}
- A61K 31/341: not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
- A61K 31/501: not condensed and containing further heterocyclic rings
- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K 31/585: containing lactone rings, e.g. oxandrolone, bufalin
- A61K 31/635: having a heterocyclic ring, e.g. sulfadiazine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61P 9/08: Vasodilators for multiple indications
- A61P 9/12: Antihypertensives
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- 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

A method for the preparation of a composition includes dispersing particulate pimobendan in a molten carrier matrix to form particles coated with the carrier matrix, where the molten carrier matrix includes one or more pharmaceutically acceptable carriers selected from a polyglycolized glyceride, a polyethylene glycol, and combinations thereof, atomizing the dispersion of coated particles, and cooling and collecting the coated particles from the atomized dispersion.

## Claims

### Claim 1

A method for the preparation of a composition, the process comprising:
dispersing particulate pimobendan in a molten carrier matrix to form particles coated with the carrier matrix, wherein the molten carrier matrix comprises one or more pharmaceutically acceptable carriers selected from the group consisting of a polyglycolized glyceride, a polyethylene glycol, and combinations thereof;
atomizing the dispersion of coated particles; and
cooling and collecting the coated particles from the atomized dispersion.

### Claim 2 (depends on 1)

The method of claim 1, wherein the particulate pimobendan has a mean particle size of less than 20 μm, the carrier matrix has a melting point from 40° C. to 80° C., and the dispersing is performed in a high shear mixer to obtain a homogenous suspension of the coated particles within the carrier matrix.

### Claim 3 (depends on 1)

The method of claim 1, wherein the carrier matrix comprises a polyglycolized glyceride.

### Claim 4 (depends on 1)

The method of claim 1, wherein the polyglycolized glyceride comprises a stearoyl macrogol-32 glyceride, a lauroyl macrogolglyceride or a stearoyl macrogolglyceride.

### Claim 5 (depends on 1)

The method of claim 1, wherein the polyethylene glycol has an average molecular weight of 1,500 to 20,000 g/mol, or an average molecular weight of 4,000 to 6,000 g/mol.

### Claim 6 (depends on 1)

The method of claim 1, wherein the polyethylene glycol comprises PEG 6000.

### Claim 7 (depends on 1)

The method of claim 1, wherein the atomizing the dispersion of coated particles is performed using an atomizer selected from the group consisting of a rotary atomizer, a pressure or pneumatic nozzle, a sonic nozzle, and combinations thereof.

### Claim 8 (depends on 1)

The method of claim 1, wherein the atomizing the dispersion of coated particles is performed using a two-fluid pressure or pneumatic nozzle atomization system fitted in a spray congealing/chilling apparatus and using atomizing gas pressures of 1 to 10 bar.

### Claim 9 (depends on 1)

The method of claim 1, wherein the cooling and collecting the coated particles from the atomized dispersion comprises applying a stream of cool air or an inert gas at a temperature of 0° to 30° C. from a spray apparatus to the coated particles within a cyclone separator or a bag filter.

### Claim 10 (depends on 9)

The method of claim 9, wherein the cool air or inert gas is applied at a temperature of 5° to 15° C., or at a temperature of 4° to 8° C.

### Claim 11 (depends on 1)

The method of claim 1, further comprising:
blending the cooled and collected coated particles with one or more additional components to form a blended mixture; and
compressing the blended mixture to form a tablet.

### Claim 12 (depends on 11)

The method of claim 11, wherein the one or more additional components comprises one or more additional active ingredients.