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Last Updated: May 4, 2024

Claims for Patent: 8,586,103

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Summary for Patent: 8,586,103

Title:	Non-polymeric compositions for controlled drug delivery
Abstract:	The present invention provides a novel liquid composition suitable for in-situ formation of a depot system to deliver a bioactive substance in a controlled manner. The composition of the present invention comprises: (a) a hydrophobic non-polymeric carrier material; (b) a water miscible biocompatible organic solvent that dissolves the hydrophobic non-polymeric material; (c) an ionic complex that is formed between an amphiphilic molecule and a bioactive substance having a net charge at neutral pH in water. The present invention also provides a method of manufacturing and use of the composition thereof.
Inventor(s):	Li; Yuhua (Newark, DE), Guarino; Andrew (Newark, DE), Chien; Benjamin (Woodside, CA)
Assignee:	Foresee Pharmaceuticals, LLC (Newark, DE)
Application Number:	12/366,402
Patent Claims:	1. A liquid composition for sustained release of a bioactive substance, consisting essentially of: (a) sucrose acetate isobutyrate; (b) a solvent selected from the group consisting of acetone, benzyl alcohol, butylene glycol, caprolactam, caprolactone, dimethylsulfoxide, ethanol, ethyl acetate, ethyl lactate, glycerol, glycerol formal, glycofurol, tetraglycol, N-methyl-2-pyrrolidone, polyethylene glycol, methoxy polyethylene glycol, alkoxy polyethylene glycol, propylene carbonate, 2 pyrrolidone, triacetin and triethyl citrate; and (c) an ionic complex that is formed between a bioactive substance having a net charge at neutral pH in water and an amphiphilic molecule, wherein the amphiphilic molecule is selected from the group consisting of dialkyl ester sulfosuccinic acid, dioctyl sulfosuccinic acid, benzenesulfonic acid, camphorsulfonic acid, (+)-(1S)camphor-10-sulfonic acid, dodecylsulfuric acid, naphthalene-2-sulfonic acid, naphthalene-1,5-disulfonic acid, para-toluenesulfonic acid, cholesterol sulfuric acid and heptanesulfonic acid. 2. The composition of claim 1, wherein the bioactive substances are small molecules, macromolecules, peptides, proteins, or enzymes. 3. The composition of claim 1, wherein the molecular weight of the bioactive substance divided by the number of ionizable groups on the bioactive substance is greater than 100 daltons. 4. The composition of claim 1, wherein the bioactive substance is selected from the group consisting of 4-hydroxy-phenethylamine, methylamphetamine, amitriptyline, reboxetine, bupropion, mirtazapine, venlafaxine, duloxetine, fluoxetine, paroxetine, escitalopram, citalopram, sertraline, bromocriptine, pergolide, pramipexole, ropinirole, cabergoline, apomorphine, lisuride, doxorubicin, doxycyclin, diltiazam, cyclobenzaprine, bacitracin, noscapine, erythromycin, polymyxin, vancomycin, nortriptyline, quinidine, ergotamine, benztropine, verapamil, flunarizine, imipramine, gentamycin, kanamycin, neomycin, amoxicillin, amikacin, arbekacin, bambermycins, butirosin, dibekacin, dihydrostreptomycin, fortimicin, isepamicin, micronimicin, netilmicin, paromycin, ribostamycin, rapamycin, sisomicin, streptomycin and tobramycin, streptomycin and tobramycin, pyrimethamine, naltrexone, lidocaine, prilocalne, mepivacaine, bupivacaine, tetracaine, ropivacaine, and resperidone. 5. The composition of claim 1, wherein the bioactive substance is selected from the group consisting of oxytocin, vasopressin, adrenocorticotropic hormone, epidermal growth factor, platelet-derived growth factor, prolactin, luteinising hormone, luteinizing hormone releasing hormone, luteinizing hormone releasing hormone agonists, luteinizing hormone releasing hormone antagonists, growth hormones, growth hormone releasing factor, insulin, erythropoietin, somatostatin, glucagon, interleukin, interferon-.alpha., interferon-.beta., interferon-.gamma., gastrin, tetragastrin, pentagastrin, urogastrone, secretin, calcitonin, enkephalins, endorphins, angiotensins, thyrotropin releasing hormone, tumor necrosis factor, parathyroid hormone, nerve growth factor, granulocyte-colony stimulating factor, granulocyte macrophage-colony stimulating factor, macrophage-colony stimulating factor, heparinase, vascular endothelial growth factor, bone morphogenic protein, exenatide, renin, bradykinin, bacitracins, polymyxins, colistins, tyrocidine, gramicidins, cyclosporins, enzymes, cytokines, antibodies, vaccines, antibiotics, antibodies, glycoproteins, follicle stimulating hormone, kyotorphin, taftsin, thymopoietin, thymosin, thymostimulin, thymic humoral factor, serum thymic factor, colony stimulating factors, motilin, bombesin, dinorphin, neurotensin, cerulein, urokinase, kallikrein, angiotensin II, blood coagulation factor VII and IX, lysozyme, gramicidines, melanocyte stimulating hormone, thyroid hormone releasing hormone, thyroid stimulating hormone, pancreozymin, cholecystokinin, human placental lactogen, human chorionic gonadotrophin, protein synthesis stimulating peptide, gastric inhibitory peptide, vasoactive intestinal peptide, and platelet derived growth factor. 6. A liquid composition for sustained release of a bioactive substance, consisting essentially of: (a) sucrose acetate isobutyrate; (b) a solvent selected from the group consisting of acetone, benzyl alcohol, butylene glycol, caprolactam, caprolactone, dimethylsulfoxide, ethanol, ethyl acetate, ethyl lactate, glycerol, glycerol formal, glycofurol, tetraglycol, N-methyl-2-pyrrolidone, polyethylene glycol, methoxy polyethylene glycol, alkoxy polyethylene glycol, propylene carbonate, 2 pyrrolidone, triacetin and triethyl citrate; (c) an ionic complex that is formed between a bioactive substance having a net charge at neutral pH in water and an amphiphilic molecule, wherein the amphiphilic molecule is selected from the group consisting of dialkyl ester sulfosuccinic acid, dioctyl sulfosuccinic acid, benzenesulfonic acid, camphorsulfonic acid, (+)-(1S)camphor-10-sulfonic acid, dodecylsulfuric acid, naphthalene-2-sulfonic acid, naphthalene-1,5-disulfonic acid, para-toluenesulfonic acid, cholesterol sulfuric acid and heptanesulfonic acid; and (d) an additive selected from the group consisting of polylactides, polyglycolides, polycaprolactones, polyan hydrides, polyorthoesters, polydioxanones, polyacetals, polyketals, polycarbonates, polyphosphoesters, polyoxaesters, polyorthocarbonates, polyphosphazenes, succinates, poly(malic acid), poly(amino acids), polyvinylpyrrolidone, polyethylene glycol, polyhydroxycellulose, chitin, chitosan, and hyaluronic acid. 7. A liquid composition for sustained release of a bioactive substance, consisting essentially of: (a) sucrose acetate isobutyrate; (b) a solvent selected from the group consisting of acetone, benzyl alcohol, butylene glycol, caprolactam, caprolactone, dimethylsulfoxide, ethanol, ethyl acetate, ethyl lactate, glycerol, glycerol formal, glycofurol, tetraglycol, N-methyl-2-pyrrolidone, polyethylene glycol, methoxy polyethylene glycol, alkoxy polyethylene glycol, propylene carbonate, 2 pyrrolidone, triacetin and triethyl citrate; (c) an ionic complex that is formed between a bioactive substance having a net charge at neutral pH in water and an amphiphilic molecule, wherein the amphiphilic molecule is selected from the group consisting of dialkyl ester sulfosuccinic acid, dioctyl sulfosuccinic acid, benzenesulfonic acid, camphorsulfonic acid, (+)-(1S)camphor-10-sulfonic acid, dodecylsulfuric acid, naphthalene-2-sulfonic acid, naphthalene-1,5-disulfonic acid, para-toluenesulfonic acid, cholesterol sulfuric acid and heptanesulfonic acid; and (d) an additive selected from the group consisting of cysteine, methionine, d-alpha tocopherol acetate, dl-alpha tocopherol, ascorbyl palmitate, butylated hydroxyanidole, butylated hydroxyanisole, butylatedhydroxyquinone, butylhydroxyanisol, hydroxycomarin, butylated hydroxytoluene, cephalm, ethyl gallate, propyl gallate, octyl gallate, lauryl gallate, propylhydroxybenzoate, trihydroxybutyrophenone, dimethylphenol, ditertbutylphenol, vitamin E, and lecithin. 8. The composition of claim 1, wherein the bioactive substance is selected from the group consisting of doxorubicin, pramipexole, octreotide, and leuprolide. 9. The composition of claim 1, wherein the amphiphilic molecule is selected from the group consisting of dioctyl sulfosuccinic acid and dodecylsulfuric acid. 10. The composition of claim 1, wherein the ratio of sucrose acetate isobutyrate to solvent is from 50:50 to 95:5. 11. The composition of claim 1, wherein the ratio of sucrose acetate isobutyrate to solvent is from 70:30 to 90:10.

Details for Patent 8,586,103

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Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Microbix Biosystems Inc.	KINLYTIC	urokinase	For Injection	021846	01/16/1978	⤷ Try a Trial	2039-02-26
Nps Pharmaceuticals, Inc.	NATPARA	parathyroid hormone	For Injection	125511	01/23/2015	⤷ Try a Trial	2039-02-26
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

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