# US 2025/0152579 A1 · Diketopiperazine Microparticles with Defined Specific Surface Areas

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- Number: US 2025/0152579 A1
- Document ID: US20250152579A1
- Status: Published application
- Kind: A1
- Application number: 19/022,095
- Filed: 2025-01-15
- Published: 2025-05-15
- Earliest claimed: 2009-06-12
- Assignees: MannKind Corporation
- Applicants: MannKind Corporation
- Inventors: Marshall L. Grant; Grayson W. Stowell; Paul Menkin; John J. Freeman, JR.
- Web page: https://patentgrep.com/patent/US20250152579A1

## CPC

- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 9/0075: {for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles}
- A61K 9/145: {with organic compounds}
- A61K 9/1617: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/1694: {resulting in granules or microspheres of the matrix type containing more than 5% of excipient}
- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- A61K 31/5575: having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
- A61K 38/193: {Colony stimulating factors [CSF]}
- A61K 38/28: Insulins
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61M 15/0028: {using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up}
- A61M 15/0091: {mechanically breath-triggered}
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/00: Drugs for disorders of the endocrine system
- C07D 241/08: with oxygen atoms directly attached to ring carbon atoms
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- 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)
- 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)}
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- Y10T: TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION

## Abstract

Disclosed herein are diketopiperazine microparticles having a specific surface area of less than about 67 m2/g. The diketopiperazine microparticle can be fumaryl diketopiperazine and can comprise a drug such as insulin.

## Claims

### Claim 1

A dry powder comprising diketopiperazine microparticles having a specific surface area of 35 m2/g to about 67 m2/g.

### Claim 2 (depends on 1)

The dry powder of claim 1, further comprising an active agent active agent.

### Claim 3 (depends on 2)

The dry powder of claim 2, wherein an active agent is vasoactive agent, a neuroactive agent, a an immunomodulating agent, a cytotoxic agent, an antibiotic, an antiviral agent, an antigen, and infectious agent, an inflammatory mediator, a hormone, or a cell surface antigen.

### Claim 4 (depends on 2)

The dry powder of claim 2, wherein an active agent is a prostaglandin.

### Claim 5 (depends on 2)

The dry powder of claim 2, wherein the prostaglandin is PG I2.

### Claim 6 (depends on 2)

The dry powder of claim 2, wherein the active agent is about 0.01% to about 20% of the weight of the microparticles.

### Claim 7 (depends on 1)

The dry powder of claim 1, wherein the diketopiperazine microparticles comprises 3,6-di(N-fumaryl-4-aminobutyl)-2,5-diketopiperazine; 2,5-diketo-3,6-di(4-succinylaminobutyl)piperazine; 2,5-diketo-3,6-di(4-glutarylaminobutyl)piperazine; or, 2,5-diketo-3,6-di(4-maleylaminobutyl)-piperazine.

### Claim 8

A dry powder for inhalation comprising microparticles of a diketopiperazine of the formula:
and a prostaglandin; wherein the microparticles have a specific surface area of 35 m2/g to about 67 m2/g.

### Claim 9 (depends on 8)

The dry powder of claim 8, wherein the prostaglandin is PG I2 or an analog thereof.

### Claim 10

A dry powder for inhalation comprising microparticles of a diketopiperazine of the formula:
and granulocyte macrophage colony stimulating factor; wherein the microparticles have a specific surface area of 35 m2/g to about 67 m2/g.

### Claim 11

A dry powder inhaler comprising a dry powder formulation comprising microparticles of a diketopiperazine having the formula:
wherein the FDKP microparticles have a specific surface area of less than about 67 m2/g and one or more than one active agents.

### Claim 12 (depends on 11)

The dry powder inhaler of claim 11, wherein the one or more active agents is a prostaglandin.

### Claim 13 (depends on 12)

The dry powder inhaler of claim 12, wherein the one or more active agent prostaglandin PG I2 or an analog thereof.

### Claim 14 (depends on 11)

The dry powder inhaler of claim 11 wherein the one or more active agent is granulocyte macrophage colony stimulating factor.