# US 10,117,940 B2 · DPI formulation containing sulfoalkyl ether cyclodextrin

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- Number: US 10,117,940 B2
- Document ID: US10117940B2
- Status: Granted
- Kind: B2
- Application number: 13/794,652
- Filed: 2013-03-11
- Published: 2013-08-01
- Granted: 2018-11-06
- Earliest claimed: 2004-04-23
- Assignees: CyDex Pharmaceuticals, Inc.
- Applicants: CyDex Pharmaceuticals, Inc.
- Inventors: James D. Pipkin; Gerold L. Mosher; Douglas B. Hecker
- Web page: https://patentgrep.com/patent/US10117940B2

## CPC

- A61K 47/40: Cyclodextrins; Derivatives thereof
- A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles}
- A61P 5/40: Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- Y10T 428/2982: Particulate matter [e.g., sphere, flake, etc.]
- 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
- Y10T: TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION

## Abstract

An inhalable dry powder formulation containing SAE-CD and an active agent is provided. The formulation is adapted for administration by DPI. The SAE-CD serves as a carrier rather than as an absorption enhancer. The average particle size of the SAE-CD is large enough to preclude (for the most part) pulmonary deposition thereof. Following release from the DPI device, the SAE-CD-containing particles dissociate from the active agent-containing particles in the buccal cavity or throat, after which the active agent-containing particles continue deeper into the respiratory tract. The physicochemical and morphological properties of the SAE-CD are easily modified to permit optimization of active agent and carrier interactions. Drugs having a positive, neutral or negative electrostatic charge can be delivered by DPI when SAE-CD is used as a carrier.

## Claims

### Claim 1

A composition, comprising solid particles that comprise sulfoalkylether cyclodextrin, wherein the composition comprises less than 8% by weight moisture, has a bulk density of 0.34 g/cc to 0.55 g/cc, and has a micro-flow fractal dimension analysis of about 1.0-1.2, wherein the composition is prepared by a process comprising a spray agglomeration of a feed solution using a spray drier apparatus to form agglomerated particles.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the composition comprises less than 6% by weight moisture.

### Claim 3 (depends on 1)

The composition of claim 1, wherein the composition comprises a CARR's index of about 10% to about 40%.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the composition comprises particles with a median particle diameter of about 25 microns to about 300 microns.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the composition comprises particles with a median particle diameter of about 175 microns to about 270 microns.

### Claim 6 (depends on 1)

The composition of claim 1, wherein the composition comprises a particle size distribution span of about 1.5 to about 2.9.

### Claim 7 (depends on 1)

The composition of claim 1, wherein the particles are agglomerates.

### Claim 8 (depends on 1)

The composition of claim 1, wherein the particles are aggregates.

### Claim 9 (depends on 1)

The composition of claim 1, wherein the particles are individual particles.

### Claim 10 (depends on 1)

The composition of claim 1, wherein the sufloalkyl ether cyclodextrin is a compound, or a mixture of compounds, of the Formula I:
wherein:
n is 4, 5, or 6;
R1, R2, R3, R4, R5, R6, R7, R8, and R9 are each, independently, —O— or a —O—(C2-C6 alkylene)-SO3− group, wherein at least one of R1 to R9 is independently the —O—(C2-C6 alkylene)-SO3− group; and
S1, S2, S3, S4, S5, S6, S7, S8, and S9, are each, independently, a pharmaceutically acceptable cation selected from the group consisting of H+, alkali metals, alkaline earth metals, ammonium ions and amine cations.

### Claim 11 (depends on 1)

A pharmaceutical composition comprising the composition of claim 1 and an active agent.

### Claim 12 (depends on 1)

A pharmaceutical dosage form comprising the composition of claim 1.

### Claim 13 (depends on 12)

The dosage form of claim 12, wherein the dosage form is a powder.

### Claim 14 (depends on 1)

The composition of claim 1, wherein the spray drier apparatus comprises a pressure nozzle; an inlet; an outlet; a fluid bed inlet; and a fluid product bed.

### Claim 15 (depends on 14)

The composition of claim 14, wherein the spray agglomeration comprises spraying the feed solution.

### Claim 16 (depends on 14)

The composition of claim 14, wherein the spray agglomeration comprises returning fines at the pressure nozzle.

### Claim 17 (depends on 1)

The composition of claim 1, wherein the composition has a micro-flow fractal dimension analysis of about 1.0-1.1.