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Last Updated: March 29, 2024

Claims for Patent: 10,376,587


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Summary for Patent: 10,376,587
Title:High capacity diketopiperazine microparticles and methods
Abstract: Disclosed herein are diketopiperazine microparticles having high capacity for adsorbing a drug or active agent. In particular, the diketopiperazine microparticle are formed using fumaryl diketopiperazine and can comprise a drug in large doses for the treatment of disease or disorders by pulmonary delivery via oral inhalation.
Inventor(s): Grant; Marshall (Newtown, CT), Menkin; Paul (Branford, CT), Stowell; Grayson W. (Cary, NC)
Assignee: MannKind Corporation (Valencia, CA)
Application Number:16/151,678
Patent Claims:1. A method of delivering a drug or an active agent to a patient in need thereof comprising administering to the patient in need thereof using a reusable inhaler an inhalable composition comprising a drug or active agent and diketopiperazine microparticles, each of the diketopiperazine microparticles comprising a plurality of structural domains, each of the plurality of structural domains comprising a nucleus surrounded by layers of a porous crystalline material, and each of the diketopiperazine microparticles have a mass-weighted average particle size of about 33,000 to about 216,000 voxels measured by X-ray tomography for particle sizes measuring from about 0.5 pm to about 4 pm in geometric diameter.

2. The method of claim 1, wherein said diketopiperazine is fumaryl diketopiperazine or 3,6-bis(N-fumaryl-4-aminobutyl)-2,5-diketopiperazine; or salt thereof.

3. The method of claim 1, wherein the diketopiperazine microparticles comprise structural domains ranging in number-weighted size from about 250 voxels to about 1,400 voxels.

4. The method of claim 1, wherein the diketopiperazine microparticles comprise structural domains ranging in voxel-weighted size from about 500 voxels to about 2,000 voxels.

5. The method of claim 1, wherein the diketopiperazine microparticles have a specific surface area greater than 70 m.sup.2/g.

6. The method according to claim 1, further comprising a surfactant.

7. The method according to claim 6, wherein said surfactant is polysorbate 80.

8. The method of claim 1, wherein said drug or active agent is a small organic molecule, peptide or protein, a lipid, or a nucleic acid molecule, or combinations thereof.

9. The method according to claim 1, wherein said active agent is insulin.

10. The method of claim 8, wherein said peptide or protein is insulin, parathyroid hormone, calcitonin, glucagon, glucagon-like peptide 1, oxyntomodulin, oxytocin, CCK-8, PYY3-36, ghrelin, vasoactive intestinal peptide, leuprolide, growth hormone, RGD (Arg-Gly-Assp) peptide, growth hormone releasing peptide, DDAVP (desamino-Cys-1, D-arg8) vasopressin peptide, cyclosporine, detirelex, somatostatin, interferon-.alpha., granulocyte colony stimulating factor, IgG, an analog or active fragment thereof.

11. The method of claim 8, wherein the small organic molecule is a neurotransmitter agonist, a neurotransmitter antagonist, a pain inhibitory agent, a vaccine, an anti-inflammatory agent, an anti-cancer agent, a cell receptor agonist molecule, cell receptor antagonist molecule, an immunosuppressant, a vasodilator, a statin or an anti-infective agent.

12. The method of claim 1, wherein the inhalable composition is in dry powder form.

13. A dry powder inhaler for use with the method according to claim 1, and wherein said inhalable composition is in dry powder form.

14. The dry powder inhaler of claim 13, wherein the inhalable composition is provided in a unit dose cartridge for using with a reusable inhaler.

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