PHARMACEUTICAL FORMULATIONS CONTAINING MICROPARTICLES OR NANOPARTICLES OF A DELIVERY AGENT
This invention relates to microparticles and/or nanoparticles containing a delivery agent and/or an active agent. This invention also relates to pharmaceutical formulations and solid dosage forms, including controlled release solid dosage forms of active agent and a delivery agent.
1 - 11 . (canceled)
12 . A pharmaceutical formulation comprising particles having a median particle size of less than about 999 micrometers, the particles comprising a delivery agent and an active agent.
13 - 16 . (canceled)
17 . The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 45 to about 150 micrometers.
18 . The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 150 to about 250 micrometers.
19 . The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 250 to about 425 micrometers.
20 . The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 425 to about 850 micrometers.
21 . The pharmaceutical formulation of claim 12 , wherein the particles have a median particle size of about 100 to about 1000 nanometers.
22 . The pharmaceutical formulation of claim 21 , wherein the particles have a median particle size of about 500 to about 1000 nanometers.
23 - 38 . (canceled)
39 . The pharmaceutical formulation of claim 12 , wherein the delivery agent compound is selected from N-(8-[2-hydroxybenzoyl]amino)caprylic acid, N-(10-[2-hydroxybenzoyl]-amino)decanoic acid, 8-(2-hydroxy-4-methoxybenzoylamino)octanoic acid, 8-(2-hydroxy-5-chlorobenzoylamino)-octanoic acid, 4-[(2-hydroxy-4-chlorobenzoyl)-amino]butanoic acid, and pharmaceutically acceptable salts thereof.
40 . The pharmaceutical formulation of claim 12 , wherein the delivery agent compound is N-(8-[2-hydroxybenzoyl]-amino)caprylic acid or a pharmaceutically acceptable salt thereof.
41 . The pharmaceutical formulation of claim 12 , wherein the delivery agent compound is N-(10-[2-hydroxybenzoyl]-amino)decanoic acid or a pharmaceutically acceptable salt thereof.
42 . The pharmaceutical formulation of claim 12 , wherein the delivery agent compound is 4-[(2-hydroxy-4-chloro-benzoyl)-amino]butanoic acid or a pharmaceutically acceptable salt thereof.
43 . The pharmaceutical formulation of claim 12 , wherein the active agent is selected from proteins, polypeptides, peptides, hormones, and polysaccharides.
44 . The pharmaceutical formulation of claim 12 , wherein the active agent is selected from the following, including synthetic, natural or recombinant sources thereof: growth hormones; growth hormone releasing hormones; growth hormone releasing factor, interferons; interleukin-1; interleukin-2; insulin, optionally having counter ions including zinc, sodium, calcium and ammonium; insulin-like growth factor; heparin; calcitonin; erythropoietin; atrial naturetic factor; antigens; monoclonal antibodies; somatostatin; protease inhibitors; adrenocorticotropin, gonadotropin releasing hormone; oxytocin; leutinizing-hormone-releasing-hormone; follicle stimulating hormone; glucocerebrosidase; thrombopoietin; filgrastim; prostaglandins; cyclosporin; vasopressin; cromolyn sodium; vancomycin; desferrioxamine; bisphosphonates; parathyroid hormone; anti-migraine agents; glucagon-like peptide 1 (GLP-1); antimicrobials; vitamins; analogs, fragments, mimetics or polyethylene glycol (PEG)-modified derivatives of these compounds; or any combination thereof.
45 . The pharmaceutical formulation of claim 12 , wherein the active agent is insulin.
46 - 49 . (canceled)
50 . A solid dosage unit form comprising the pharmaceutical formulation of claim 12 .
51 - 56 . (canceled)
57 . A method of treating diabetes in a mammal in need thereof, comprising administering to the animal a therapeutic effective amount of a pharmaceutical formulation of claim 12 .
58 . The method of claim 57 , wherein the delivery agent compound is 4-[(2-hydroxy-4-chloro-benzoyl)-amino]butanoic acid or a pharmaceutically acceptable salt thereof.
59 . A method of treating impaired glucose tolerance, early stage diabetes, or late stage diabetes or achieving glucose homeostasis in humans, comprising administering a therapeutic effective amount of a pharmaceutical formulation of claim 12 .
60 . (canceled)
61 . A method of treating a human diabetic patient comprising orally administering to the human diabetic patient on a chronic basis a therapeutic effective amount of a pharmaceutical formulation of claim 12 .
62 - 94 . (canceled)