# US 2014/0150788 A1 · Dry Powder For Inhalation

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- Number: US 2014/0150788 A1
- Document ID: US20140150788A1
- Status: Published application
- Kind: A1
- Application number: 14/087,748
- Filed: 2013-11-22
- Published: 2014-06-05
- Earliest claimed: 2001-08-09
- Assignees: Jagotec AG
- Applicants: Jagotec AG
- Inventors: Manfred Keller; Rudi Mueller-Walz
- Web page: https://patentgrep.com/patent/US20140150788A1

## CPC

- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles}
- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/439: the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46)
- 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
- A61M 15/003: {using capsules, e.g. to be perforated or broken-up}
- A61M 15/0045: {using multiple prepacked dosages on a same carrier, e.g. blisters}
- A61M 15/0065: {Inhalators with dosage or measuring devices (A61M15/0028 takes precedence; dosage devices incorporated in aerosol cans B65D83/52)}
- A61M 2202/064: Powder
- 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)
- A61M: DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY (introducing media into or onto the bodies of animals A61D7/00; means for inserting tampons A61F13/26; devices for administering food or medicines orally A61J; containers for collecting, storing or administering blood or medical fluids A61J1/05); DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY (surgery A61B; chemical aspects of surgical articles A61L); DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR {(Electrotherapy, e.g. producing anaesthesia by the use of alternating or intermittent currents A61N1/36021)}

## Abstract

The present invention provides dry powder formulations for inhalation having improved moisture resistance such that the powders maintain a high fine particle dosage or fine particle fraction following storage under relatively extreme temperature and humidity conditions.

## Claims

### Claim 1

A dry powder inhaler, comprising
a) a multidose powder reservoir containing a dry powder comprising:
i) a pharmaceutically inactive carrier having particles of noninhalable particle size,
ii) a pharmaceutically active component comprising at least one finely divided pharmaceutically active compound having particles of inhalable particle size, and
iii) magnesium stearate as a pulverulent material present in an amount of 0.5 to 5% by weight, based on the total weight of the formulation; and
b) means for delivering metered doses of the pharmaceutically active compound for inhalation,
wherein said dry powder has a fine particle fraction (FPF) and a fine particle dose (FPD), said powder exhibiting improved stability of FPF and FPD following 4 to 10 days of storage at 40° C. and 75% relative atmospheric humidity compared to a reference lacking magnesium stearate as a pulverulent material.

### Claim 2 (depends on 1)

The dry powder inhaler of claim 1, wherein the pharmaceutically active compound is a hygroscopic compound capable of absorbing at least 0.5% by weight of its own weight of absorptively bound water when stored in air having a relative humidity of 50%.

### Claim 3 (depends on 1)

The dry powder inhaler of claim 1, wherein the pharmaceutically active compound is a hydrophilic compound having a wetting angle of less than 90°.

### Claim 4 (depends on 1)

The dry powder inhaler of claim 1, wherein the pharmaceutically active compound is a hydrophilic compound having a wetting angle of less than 70°.

### Claim 5 (depends on 1)

The dry powder inhaler of claim 1, wherein the magnesium stearate is present in an amount of 0.5% to 0.75% by weight, based on the total weight of the formulation.

### Claim 6 (depends on 1)

The dry powder inhaler of claim 1, wherein the carrier is selected from the group consisting of monosaccharides, disaccharides, sugar alcohols, polylactic acid and cyclodextrin.

### Claim 7 (depends on 1)

The dry powder inhaler of claim 1, wherein the carrier is selected from the group consisting of glucose, lactose monohydrate and trehalose.

### Claim 8 (depends on 1)

The dry powder inhaler of claim 1, wherein the formulation further comprises particles of micronized lactose monohydrate wherein at least 50% of the particles thereof have a maximum particle size of 10 um.

### Claim 9 (depends on 1)

The dry powder inhaler of claim 1, wherein the pharmaceutically active compound is formoterol or a pharmaceutically acceptable salt thereof.

### Claim 10 (depends on 1)

The dry powder inhaler of claim 1, wherein the pharmaceutically active compound is selected from the group consisting of formoterol fumarate, formoterol tartrate, ipratropium bromide and tiotropium bromide.

### Claim 11 (depends on 1)

The dry powder inhaler of claim 1, wherein the powder further comprises a second pharmaceutically active compound having particles of inhalable size.

### Claim 12 (depends on 1)

The dry powder inhaler of claim 1, wherein the pharmaceutically active component comprises a) a member selected from the group consisting of formoterol fumarate, formoterol tartrate, levalbuterol sulfate and salmeterol xinafoate, and b) a corticosteroid.

### Claim 13 (depends on 1)

The inhaler of claim 1, wherein the pharmaceutically active component does not comprise salbutamol sulfate, salmeterol xinafoate, or beclomethasone dipropionate.