HRP20230551T1 - Formulacije kapsula - Google Patents
Formulacije kapsula Download PDFInfo
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- HRP20230551T1 HRP20230551T1 HRP20230551TT HRP20230551T HRP20230551T1 HR P20230551 T1 HRP20230551 T1 HR P20230551T1 HR P20230551T T HRP20230551T T HR P20230551TT HR P20230551 T HRP20230551 T HR P20230551T HR P20230551 T1 HRP20230551 T1 HR P20230551T1
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- solid solution
- ionic surfactant
- capsule
- solution capsule
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- 239000007963 capsule composition Substances 0.000 title claims 2
- 239000002775 capsule Substances 0.000 claims 34
- 239000006104 solid solution Substances 0.000 claims 28
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 18
- 239000002736 nonionic surfactant Substances 0.000 claims 17
- 239000002904 solvent Substances 0.000 claims 16
- 238000002844 melting Methods 0.000 claims 12
- 230000008018 melting Effects 0.000 claims 12
- 229940125904 compound 1 Drugs 0.000 claims 10
- 201000010099 disease Diseases 0.000 claims 9
- 208000035475 disorder Diseases 0.000 claims 9
- 229940057838 polyethylene glycol 4000 Drugs 0.000 claims 9
- 229920001030 Polyethylene Glycol 4000 Polymers 0.000 claims 8
- 238000000034 method Methods 0.000 claims 8
- SHBUUTHKGIVMJT-UHFFFAOYSA-N Hydroxystearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OO SHBUUTHKGIVMJT-UHFFFAOYSA-N 0.000 claims 6
- 239000012458 free base Substances 0.000 claims 6
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerol Substances OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 6
- 229940072106 hydroxystearate Drugs 0.000 claims 6
- 230000007935 neutral effect Effects 0.000 claims 6
- -1 polyoxyethylene Polymers 0.000 claims 6
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 5
- 238000010438 heat treatment Methods 0.000 claims 5
- 239000008118 PEG 6000 Substances 0.000 claims 4
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 4
- 229920002560 Polyethylene Glycol 3000 Polymers 0.000 claims 4
- 229920002562 Polyethylene Glycol 3350 Polymers 0.000 claims 4
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 claims 4
- 239000004359 castor oil Substances 0.000 claims 4
- 235000019438 castor oil Nutrition 0.000 claims 4
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims 4
- 208000029574 C3 glomerulopathy Diseases 0.000 claims 3
- 208000005777 Lupus Nephritis Diseases 0.000 claims 3
- 206010047115 Vasculitis Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 208000002557 hidradenitis Diseases 0.000 claims 3
- 201000007162 hidradenitis suppurativa Diseases 0.000 claims 3
- 208000027134 non-immunoglobulin-mediated membranoproliferative glomerulonephritis Diseases 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000000243 solution Substances 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 2
- 229920002511 Poloxamer 237 Polymers 0.000 claims 2
- 229920002517 Poloxamer 338 Polymers 0.000 claims 2
- 229920002535 Polyethylene Glycol 1500 Polymers 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- 229930195729 fatty acid Natural products 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- 150000004665 fatty acids Chemical class 0.000 claims 2
- 229940099472 immunoglobulin a Drugs 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 201000008383 nephritis Diseases 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- 229920001993 poloxamer 188 Polymers 0.000 claims 2
- 229940044519 poloxamer 188 Drugs 0.000 claims 2
- 229920001992 poloxamer 407 Polymers 0.000 claims 2
- 229940044476 poloxamer 407 Drugs 0.000 claims 2
- 229940066675 ricinoleate Drugs 0.000 claims 2
- WBHHMMIMDMUBKC-QJWNTBNXSA-M ricinoleate Chemical compound CCCCCC[C@@H](O)C\C=C/CCCCCCCC([O-])=O WBHHMMIMDMUBKC-QJWNTBNXSA-M 0.000 claims 2
- 239000004094 surface-active agent Substances 0.000 claims 2
- VUYXVWGKCKTUMF-UHFFFAOYSA-N tetratriacontaethylene glycol monomethyl ether Chemical compound COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO VUYXVWGKCKTUMF-UHFFFAOYSA-N 0.000 claims 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 102000005590 Anaphylatoxin C5a Receptor Human genes 0.000 claims 1
- 108010059426 Anaphylatoxin C5a Receptor Proteins 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010011091 Coronary artery thrombosis Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000024869 Goodpasture syndrome Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000004852 Lung Injury Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 208000010718 Multiple Organ Failure Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 206010034277 Pemphigoid Diseases 0.000 claims 1
- 241000721454 Pemphigus Species 0.000 claims 1
- 229920002538 Polyethylene Glycol 20000 Polymers 0.000 claims 1
- 229920002594 Polyethylene Glycol 8000 Polymers 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010038563 Reocclusion Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010051379 Systemic Inflammatory Response Syndrome Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010069363 Traumatic lung injury Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010052568 Urticaria chronic Diseases 0.000 claims 1
- 206010053648 Vascular occlusion Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000024376 chronic urticaria Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 208000002528 coronary thrombosis Diseases 0.000 claims 1
- 230000001086 cytosolic effect Effects 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 239000007902 hard capsule Substances 0.000 claims 1
- 230000002949 hemolytic effect Effects 0.000 claims 1
- 208000030603 inherited susceptibility to asthma Diseases 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 208000012947 ischemia reperfusion injury Diseases 0.000 claims 1
- 231100000515 lung injury Toxicity 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 208000029744 multiple organ dysfunction syndrome Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- 208000004235 neutropenia Diseases 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical compound C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 claims 1
- 229920002523 polyethylene Glycol 1000 Polymers 0.000 claims 1
- 230000002980 postoperative effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- WBHHMMIMDMUBKC-XLNAKTSKSA-N ricinelaidic acid Chemical compound CCCCCC[C@@H](O)C\C=C\CCCCCCCC(O)=O WBHHMMIMDMUBKC-XLNAKTSKSA-N 0.000 claims 1
- 229960003656 ricinoleic acid Drugs 0.000 claims 1
- FEUQNCSVHBHROZ-UHFFFAOYSA-N ricinoleic acid Natural products CCCCCCC(O[Si](C)(C)C)CC=CCCCCCCCC(=O)OC FEUQNCSVHBHROZ-UHFFFAOYSA-N 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 230000003582 thrombocytopenic effect Effects 0.000 claims 1
- 230000008736 traumatic injury Effects 0.000 claims 1
- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 208000021331 vascular occlusion disease Diseases 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4833—Encapsulating processes; Filling of capsules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/40—Cyclodextrins; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
Claims (22)
1. Formulacija kapsule čvrste otopine koja sadrži Spoj 1 kao slobodnu bazu, u njenom neutralnom obliku ili u obliku farmaceutski prihvatljive soli
[image]
i nosač koji sadrži
najmanje jedan ne-jonski surfaktant koji ima vrijednost hidrofilno-lipofilne ravnoteže (HLB) od najmanje 10, i
najmanje jedan solubilizator topljiv u vodi koji ima točku topljenja na ili iznad 37° C.
2. Kapsula čvrste otopine prema patentnom zahtjevu 1, pri čemu:
(a) nosač sadrži oko 97 do 99% po masi od ukupne mase punjenja navedene kapsule čvrste otopine, poželjno pri čemu nosač sadrži oko 98% po masi od ukupne mase punjenja navedene kapsule čvrste otopine; ili
(b) kapsula čvrste otopine sadrži oko 1 do 3% Spoja 1 po masi od ukupne mase punjenja navedene kapsule čvrste otopine, poželjno pri čemu kapsula čvrste otopine sadrži oko 2% Spoja 1 po masi od ukupne mase punjenja navedene kapsule čvrste otopine.
3. Kapsula čvrste otopine prema patentnim zahtjevima 1 ili 2, pri čemu ukupna masa nosača sadrži odnos 30:70 do 65:35, poželjno odnos 35:65 do 65:35 najmanje jednog ne-jonskog surfaktanta koji ima vrijednost hidrofilno-lipofilne ravnoteže (HLB) od najmanje 10 prema najmanje jednom solubilizatoru topljivom u vodi koji ima temperaturu topljenja na ili iznad 37° C.
4. Kapsula čvrste otopine prema patentnom zahtjevu 1 ili 2, pri čemu ukupna masa nosača sadrži odnos 40:60 do 60:40, poželjno odnos 45:55 do 55:45 najmanje jednog ne-jonskog surfaktanta koji ima vrijednost hidrofilno-lipofilne ravnoteže (HLB) od najmanje 10 prema najmanje jednom solubilizatoru topljivom u vodi koji ima temperaturu topljenja na ili iznad 37° C.
5. Kapsula čvrste otopine prema patentnom zahtjevu 1 ili 2, pri čemu ukupna masa nosača sadrži odnos oko 50:50, najmanje jednog ne-jonskog surfaktanta koji ima vrijednost hidrofilno-lipofilne ravnoteže (HLB) od najmanje 10 prema najmanje jednom solubilizatoru topljivom u vodi koji ima temperaturu topljenja na ili iznad 37° C.
6. Kapsula čvrste otopine prema bilo kojem od patentnih zahtjeva 1 do 5, pri čemu:
(a) najmanje jedan ne-jonski surfaktant koji ima vrijednost HLB od najmanje 10 sadrži polioksietilenski derivat masne kiseline koja sadrži od oko 8 do 22 atoma ugljenika, poželjno pri čemu je masna kiselina ricinoleinska kiselina; ili
(b) najmanje jedan ne-jonski surfaktant koji ima vrijednost HLB od najmanje 10 je polioksietilen hidrogenizovano ricinusovo ulje ili polioksietilen ricinusovo ulje; ili
(c) najmanje jedan ne-jonski surfaktant koji ima vrijednost HLB od najmanje 10 je makrogol- 40-glicerol hidroksistearat ili makrogolglicerol ricinoleat.
7. Kapsula čvrste otopine prema bilo kojem od patentnih zahtjeva 1 do 5, pri čemu najmanje jedan ne-jonski surfaktant koji ima vrijednost HLB od najmanje 10 je makrogol-40-glicerol hidroksistearat.
8. Kapsula čvrste otopine prema bilo kojem od patentnih zahtjeva 1 do 7, pri čemu:
(a) najmanje jedan solubilizator topljiv u vodi koji ima temperaturu topljenja na ili iznad 37° C bira se iz grupe koja se sastoji od PEG-1000, PEG-1500, PEG-1540, PEG-2000, PEG-3000, PEG- 3350, PEG-4000, PEG- 6000, PEG-8000, PEG-10000, PEG-20000, poloksamera 188, poloksamera 237, poloksamera 338 i poloksamera 407, poželjno izabranih iz grupe koja se sastoji od PEG-1540, PEG-2000, PEG-3000, PEG-3350, PEG-4000, PEG-6000
9. Kapsula čvrste otopine prema bilo kojem od patentnih zahtjeva 1 do 7, pri čemu najmanje jedan solubilizator topljiv u vodi koji ima temperaturu topljenja na ili iznad 37° C je PEG-4000.
10. Kapsula čvrste otopine prema bilo kojem od patentnih zahtjeva 1 do 5, pri čemu najmanje jedan ne-jonski surfaktant koji ima vrijednost HLB od najmanje 10 je makrogol-40-glicerol hidroksistearat i najmanje jedan solubilizator topljiv u vodi koji ima temperaturu topljenja na ili iznad 37° C je PEG- 4000.
11. Kapsula čvrste otopine prema bilo kojem od patentnih zahtjeva 1 do 10, pri čemu:
(a) ukupna masa punjenja navedene kapsule čvrste otopine je od oko 130 mg do 900 mg, poželjno oko 500 mg; ili
(b) veličina kapsule bira se iz grupe koja se sastoji od #00, #0, #1, #2, #3, #4, ili #5, poželjno pri čemu veličina kapsule je #0; ili
(c) kapsula je tvrda kapsula.
12. Postupak pripreme kapsule čvrste otopine koja sadrži Spoj 1 kao slobodnu bazu, u njenom neutralnom obliku ili u obliku farmaceutski prihvatljive soli
[image]
i nosač koji sadrži
najmanje jedan ne-jonski surfaktant koji ima vrijednost hidrofilno-lipofilne ravnoteže (HLB) od najmanje 10, i
najmanje jedan solubilizator topljiv u vodi koji ima točku topljenja na ili iznad 37° C;
pri čemu navedeni postupak obuhvaća
(a) topljenje nosača;
(b) kombiniranje istopljenog nosača dobivenog u koraku (a) sa Spojem 1 da bi se stvorila otopina lijeka;
(c) inkapsuliranje otopine lijeka u oblogu kapsule; i
(d) hlađenje inkapsulirane otopine lijeka da bi se stvorila kapsula čvrste otopine koja sadrži Spoj 1.
13. Postupak prema patentnom zahtjevu 12, pri čemu:
1) korak (a) obuhvaća zagrijavanje nosača do temperature od oko 50° do 85° C; ili
2) korak (a) obuhvaća
(i) zagrijavanje najmanje jednog ne-jonskog surfaktanta koji ima vrijednost HLB od najmanje
10 da bi se stvorio istopljeni surfaktant;
(ii) zagrijavanje najmanje jednog solubilizatora topljivog u vodi da bi se stvorio istopljeni solubilizator; i
(iii) kombiniranje istopljenog solubilizatora s istopljenim surfaktantom da bi se stvorio istopljeni nosač;
poželjno pri čemu korak (i) obuhvaća zagrijavanje najmanje jednog ne-jonskog surfaktanta koji ima vrijednosti HLB od najmanje 10 do temperature od oko 50° do 70° C, i/ili korak (ii) obuhvaća zagrijavanje najmanje jednog solubilizatora topljivog u vodi do temperature od oko 80 do 85° C.
14. Postupak prema patentnom zahtjevu 12 ili 13, pri čemu:
(a) najmanje jedan ne-jonski surfaktant koji ima vrijednost HLB od najmanje 10 je polioksietilen hidrogenizirano ricinusovo ulje ili polioksietilen ricinusovo ulje; ili
(b) najmanje jedan ne-jonski surfaktant koji ima vrijednost HLB od najmanje 10 je makrogol-40- glicerol hidroksistearat ili makrogolglicerol ricinoleat, poželjno makrogol-40-glicerol hidroksistearat; ili
(c) najmanje jedan solubilizator topljiv u vodi koji ima temperaturu topljenja na ili iznad 37° C izabran iz grupe koja se sastoji od PEG-1500, PEG-1540, PEG-2000, PEG-3000, PEG-3350, PEG- 4000, PEG-6000, poloksamera 188, poloksamera 237, poloksamera 338 i poloksamera 407, poželjno izabran iz grupe koja se sastoji od PEG-1540, PEG-2000, PEG-3000, PEG-3350, PEG- 4000, i PEG-6000, poželjnije je PEG-4000.
15. Postupak prema patentnom zahtjevu 12 ili 13, pri čemu najmanje jedan ne-jonski surfaktant koji ima vrijednost HLB od najmanje 10 je makrogol-40-glicerol hidroksistearat i najmanje jedan solubilizator topljiv u vodi je polietilen glikol 4000 (PEG-4000).
16. Kapsula čvrste otopine koja sadrži Spoj 1 kao slobodnu bazu, u njenom neutralnom obliku ili u obliku farmaceutski prihvatljive soli
[image]
i nosač koji sadrži
najmanje jedan ne-jonski surfaktant koji ima vrijednost hidrofilno-lipofilne ravnoteže (HLB) od najmanje 10, i
najmanje jedan solubilizator topljiv u vodi koji ima točku topljenja na ili iznad 37° C;
navedena kapsula čvrste otopine može se dobiti prema postupku iz bilo kojeg od patentnih zahtjeva 12 do 15.
17. Kapsula čvrste otopine prema bilo kojem od patentnih zahtjeva 1 do 11 ili 16, pri čemu Spoj 1 je slobodna baza, u njenom neutralnom obliku.
18. Kapsula čvrste otopine prema bilo kojem od patentnih zahtjeva 1 do 11 ili 16 do 17 za upotrebu u postupku za liječenje pojedinca koji pati od ili je podložan bolesti ili poremećaju koji uključuju patološku aktivaciju C5a receptora, pri čemu postupak obuhvaća davanje pojedincu efikasne količine kapsule čvrste otopine.
19. Kapsula čvrste otopine za upotrebu prema patentnom zahtjevu 18, pri čemu:
(a) bolest ili poremećaj je zapaljenska bolest ili poremećaj, poželjno pri čemu se bolest ili poremećaj bira iz grupe koja se sastoji od neutropenije, sepse, septičkog šoka, Altheimerove (Alzheimer) bolesti, multiple skleroze, moždanog udara, zapaljenske bolesti crijeva, starosne degeneracije makule, kroničnog opstruktivnog poremećaja pluća, zapaljenja povezanog s opekotinama, povrede pluća, osteoartritisa, atopijskog dermatitisa, kronične urtikarije, ishemijsko-reperfuzione povrede, akutnog respiratornog distres sindroma, sindroma sistemskog inflamatornog odgovora, sindroma višestruke disfunkcije organa, odbacivanja presađenog tkiva, raka i hiperakutnog odbacivanja presađenih organa; ili
(b) bolest ili poremećaj je kardiovaskularni ili cerebrovaskularni poremećaj, poželjno pri čemu se bolest ili poremećaj bira iz grupe koja se sastoji od infarkta miokarda, koronarne tromboze, vaskularne okluzije, postoperativne vaskularne reokluzije, arteroskleroza, traumatske povrede centralnog nervnog sistema i ishemijske bolesti srca; ili
(c) bolest ili poremećaj je autoimuni poremećaj, poželjno pri čemu se bolest ili poremećaj bira iz grupe koja se sastoji od reumatodinog artritisa, C3 glomerulopatije (C3G), hidradenitis suppurativa (HS), sistemski eritematozni lupus, Gijen-Bareovog (Guillain-Barre) sindroma, pankreatitisa, lupusnog nefritisa, lupusnog glomerulonefritisa, psorijaze, imunoglobulin A (IgA) nefropatije, Kronove (Crohn) bolesti, vaskulitisa, sindroma iritabilnog creva, dermatomiozitisa, multiple skleroze, bronhijalne astme, pemfigusa, pemfigoida, skleroderme, mijastenije gravis, autoimunih hemolitičkih i trombocitopeničnih stanja, Gudpasturovog (Goodpasture) sindroma, imunskog vaskulitisa, odbacivanja presađenog tkiva i hiperakutnog odbacivanja presađenih organa; ili
(d) bolest ili poremećaj je patološka posljedica povezana s grupom koja se sastoji od inzulin zavisnog dijabetesa, melitusa, lupusne nefropatije, Heymanovog (Heyman) nefritisa, membranoznog nefritisa, glomerulonefritisa, reakcija osjetljivosti na kontakt, i zapaljenja koje je posljedica kontakta krvi s umjetnim površinama; ili
(e) bolest ili poremećaj se bira iz grupe koja se sastoji od vaskulitisa povezanog s antineutrofilnim citoplazmatskim antitijelom (ANCA), C3 glomerulopatije, hidradenitis suppurativa, i lupusnog nefritisa.
20. Jedinična doza kapsule koja sadrži oko 2,6 mg do 25,2 mg Spoja 1 kao slobodne baze, u svom neutralnom obliku
[image]
(Spoj 1)
i nosač koji sadrži
najmanje jedan ne-jonski surfaktant koji ima vrijednost hidrofilno-lipofilne ravnoteže (HLB) od najmanje 10, i
najmanje jedan solubilizator topljiv u vodi koji ima točku topljenja na ili iznad 37° C.
21. Jedinična doza kapsule prema patentnom zahtjevu 20, pri čemu:
(a) jedinična doza kapsule sadrži oko 2,6 mg do 18 mg, poželjno oko 10 mg, Spoja 1 kao slobodne baze, u njenom neutralnom obliku; i/ili
(b) ukupna masa punjenja navedene kapsule čvrste otopine je od oko 130 mg do 900 mg.
22. Komplet koji sadrži jednu ili više kapsula čvrste otopine prema bilo kojem od patentnih zahtjeva 1 do 11, 16 ili 17, ili jednu ili više pojedinačnih doznih jedinica prema patentnom zahtjevu 20 ili 21.
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| US201862773848P | 2018-11-30 | 2018-11-30 | |
| PCT/US2019/063547 WO2020112961A1 (en) | 2018-11-30 | 2019-11-27 | Capsule formulations |
| EP19889873.6A EP3886820B8 (en) | 2018-11-30 | 2019-11-27 | Capsule formulations |
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| HRP20230551T1 true HRP20230551T1 (hr) | 2023-08-18 |
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| US (2) | US20200170957A1 (hr) |
| EP (2) | EP4233850A3 (hr) |
| JP (1) | JP7342124B2 (hr) |
| KR (1) | KR102586747B1 (hr) |
| CN (1) | CN113164403A (hr) |
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| WO2023225533A1 (en) * | 2022-05-19 | 2023-11-23 | Dow Global Technologies Llc | Use of peg-based interpolymer complexes for improved solubilization of bcs class ii drugs |
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| AR038681A1 (es) * | 2002-02-14 | 2005-01-26 | Solvay Pharm Bv | Formulacion oral de solucion solida de una sustancia activa pobremente soluble en agua |
| KR20070084531A (ko) | 2004-11-24 | 2007-08-24 | 머크 앤드 캄파니 인코포레이티드 | 치환된 아미드의 경구 투여용 액체 및 반고체 약제학적제형 |
| DE102005053066A1 (de) | 2005-11-04 | 2007-05-10 | Basf Ag | Verwendung von Copolymeren als Solubilisatoren für in Wasser schwerlöslichen Verbindungen |
| WO2010075257A1 (en) | 2008-12-22 | 2010-07-01 | Chemocentryx, Inc. | C5ar antagonists |
| PE20130198A1 (es) * | 2010-03-10 | 2013-03-24 | Abbvie Bahamas Ltd | Composiciones solidas |
| PL2585064T3 (pl) * | 2010-06-24 | 2017-09-29 | Chemocentryx, Inc. | Antagoniści C5AR |
| US9034858B2 (en) * | 2010-11-30 | 2015-05-19 | Lipocine Inc. | High-strength testosterone undecanoate compositions |
| EA037895B1 (ru) | 2014-02-05 | 2021-06-02 | Лек Фармасьютикалз Д.Д. | Твердые фармацевтические композиции антагонистов рецепторов андрогенов |
| CN113121415A (zh) | 2014-09-29 | 2021-07-16 | 凯莫森特里克斯股份有限公司 | 制备C5aR拮抗剂的方法和中间体 |
| BR112018014222A2 (pt) | 2016-01-14 | 2018-12-11 | Chemocentryx, Inc. | método de tratamento da glomerulopatia c3 |
| MX2018011831A (es) | 2016-04-04 | 2019-02-13 | Chemocentryx Inc | Antagonistas solubles de receptor de c5aa(c5ar). |
| WO2018184739A1 (en) | 2017-04-03 | 2018-10-11 | Inflarx Gmbh | Treatment of inflammatory diseases with inhibitors of c5a activity |
| US10376595B2 (en) * | 2017-04-03 | 2019-08-13 | Inflarx Gmbh | Treatment of inflammatory diseases with inhibitors of C5a activity |
| EP3703687A4 (en) | 2017-10-30 | 2021-04-07 | ChemoCentryx, Inc. | DEUTERATED COMPOUNDS USED AS IMMUNOMODULATORS |
| WO2019089534A1 (en) | 2017-10-31 | 2019-05-09 | Chemocentryx, Inc. | C5aR INHIBITOR REDUCTION OF URINARY sCD163 |
| MX2020013166A (es) | 2018-06-07 | 2021-03-29 | Chemocentryx Inc | Dosificación y efecto del antagonista de c5a con la vasculitis asociada con anca. |
| WO2020112961A1 (en) | 2018-11-30 | 2020-06-04 | Chemocentryx, Inc. | Capsule formulations |
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