# US 2019/0167579 A1 · Itraconazole dry powders

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2019/0167579 A1
- Document ID: US20190167579A1
- Status: Published application
- Kind: A1
- Application number: 16/173,744
- Filed: 2018-10-29
- Published: 2019-06-06
- Earliest claimed: 2017-10-27
- Assignees: Pulmatrix Operating Company, Inc.
- Applicants: Pulmatrix Operating Company, Inc.
- Inventors: Jason M. Perry; Jean C. Sung; David L. Hava
- Web page: https://patentgrep.com/patent/US20190167579A1

## CPC

- A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles}
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 47/02: Inorganic compounds
- A61K 47/183: {Amino acids, e.g. glycine, EDTA or aspartame}
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 31/10: Antimycotics
- 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

In one aspect, a dry powder comprising respirable dry particles that comprise amorphous itraconazole in an amount of about 45% to about 75%, sodium sulfate in an amount of about 10% to about 55%, and optionally one or more other excipients, wherein all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%. In another aspect, a dry powder comprising respirable dry particles that comprise amorphous itraconazole in an amount of about 45% to about 55%, sodium chloride in an amount of about 30% to about 40%, and leucine in an amount of about 10% to about 20%, wherein all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%.

## Claims

### Claim 1

A dry powder comprising respirable dry particles that comprise amorphous itraconazole in an amount of about 45% to about 75%, sodium sulfate in an amount of about 10% to about 55%, and optionally one or more other excipients, wherein all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%.

### Claim 2 (depends on 1)

The dry powder of claim 1, wherein the one or more other excipients are selected from the group consisting of leucine, mannitol, or combinations thereof.

### Claim 3 (depends on 1)

The dry powder of claim 1, wherein the amorphous itraconazole is about 45% to about 55%.

### Claim 4

(canceled)

### Claim 5 (depends on 1)

The dry powder of claim 1, wherein the sodium sulfate is in an amount of about 30% to about 40%.

### Claim 6

(canceled)

### Claim 7 (depends on 1)

The dry powder of claim 1, wherein the one or more other excipients total about 5% to about 25%.

### Claim 8 (depends on 1)

The dry powder of claim 1, wherein the amorphous itraconazole is about 50%, the sodium sulfate is in an amount of about 35%, the one or more other excipients total about 15%.

### Claim 9 (depends on 1)

The dry powder of claim 1, wherein the one or more other excipients is leucine.

### Claim 10

(canceled)

### Claim 11

A dry powder comprising respirable dry particles that comprise amorphous itraconazole in an amount of about 45% to about 55%, sodium chloride in an amount of about 30% to about 40%, and leucine in an amount of about 10% to about 20%, wherein all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%.

### Claim 12

A dry powder comprising respirable dry particles that comprise amorphous itraconazole in an amount of about 50%, sodium chloride in an amount of about 35%, and leucine in an amount of about 15%, wherein all percentages are weight percentages on a dry basis and all the components of the respirable dry particles amount to 100%.

### Claim 13

(canceled)

### Claim 14

(canceled)

### Claim 15 (depends on 1)

The dry powder of claim 1, wherein the respirable dry particles have a volume median geometric diameter (VMGD) about 10 microns or less.

### Claim 16 (depends on 1)

The dry powder of claim 1, wherein the respirable dry particles have a volume median geometric diameter (VMGD) about 5 microns or less.

### Claim 17 (depends on 1)

The dry powder of claim 1, wherein the respirable dry particles have a tap density of about 0.2 g/cc or greater.

### Claim 18

(canceled)

### Claim 19 (depends on 1)

The dry powder of claim 1, wherein the dry powder has an MMAD of between about 1 micron and about 5 microns and a FPF of the total dose less than 3.4 microns of about 25% or more.

### Claim 20 (depends on 1)

The dry powder of claim 1, wherein the dry particles have a 1/4 bar dispersibility ratio (1/4 bar) of less than about 1.5 as measured by laser diffraction.

### Claim at position 21

21-24. (canceled)

### Claim 25 (depends on 1)

The dry powder of claim 1, wherein the dry powder is delivered to a patient with a capsule-based passive dry powder inhaler.

### Claim 26 (depends on 1)

The dry powder of claim 1, wherein the respirable dry particles have a capsule emitted powder mass of at least 80% when emitted from a passive dry powder inhaler that has a resistance of about 0.036 sqrt(kPa)/liters per minute under the following conditions; an inhalation flow rate of 30 LPM for a period of 3 seconds using a size 3 capsule that contains a total mass of 10 mg, said total mass consisting of the respirable dry particles, and wherein the volume median geometric diameter of the respirable dry particles emitted from the inhaler as measured by laser diffraction is 5 microns or less.

### Claim 27 (depends on 1)

A method for treating a fungal infection comprising administering to the respiratory tract of a patient in need thereof an effective amount of a dry powder of claim 1.

### Claim 28 (depends on 1)

A method for treating a fungal infection in a patient with asthma, cystic fibrosis or an immunocompromised patient comprising administering to the respiratory tract of the asthma or cystic fibrosis patient an effective amount of a dry powder of claim 1.

### Claim 29 (depends on 1)

A method for treating aspergillosis or allergic bronchopulmonary aspergillosis (ABPA) comprising administering to the respiratory tract of a patient in need thereof an effective amount of a dry powder of claim 1.

### Claim 30

(canceled)

### Claim 31 (depends on 1)

A method for treating or reducing the incidence or severity of an exacerbation of a respiratory disease comprising administering to the respiratory tract of a patient in need thereof an effective amount of a dry powder of claim 1, wherein the exacerbation is a fungal infection.

### Claim 32

(canceled)