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1. (WO2018222922) PRECIPITATION RESISTANT SMALL MOLECULE DRUG FORMULATIONS
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Pub. No.: WO/2018/222922 International Application No.: PCT/US2018/035473
Publication Date: 06.12.2018 International Filing Date: 31.05.2018
IPC:
A61K 9/00 (2006.01) ,A61K 47/14 (2017.01) ,A61K 47/16 (2006.01) ,A61K 47/20 (2006.01) ,A61K 47/22 (2006.01) ,A61K 9/08 (2006.01) ,A61K 31/5513 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
08
containing oxygen
14
Esters of carboxylic acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
16
containing nitrogen
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
20
containing sulfur
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
22
Heterocyclic compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
08
Solutions
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
55
having seven-membered rings, e.g. azelastine, pentylenetetrazole
551
having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
5513
1,4-Benzodiazepines, e.g. diazepam
Applicants:
XERIS PHARMACEUTICALS, INC. [US/US]; 180 N. LaSalle Street Suite 1800 Chicago, Illinois 60601, US
Inventors:
PRESTRELSKI, Steven J.; US
SANDOVAL, Michael A.; US
SLOAT, Brian R.; US
Agent:
LANDRUM, Charles P.; US
Priority Data:
62/514,47402.06.2017US
Title (EN) PRECIPITATION RESISTANT SMALL MOLECULE DRUG FORMULATIONS
(FR) FORMULATIONS DE MÉDICAMENTS À PETITE MOLÉCULE RÉSISTANTES À LA PRÉCIPITATION
Abstract:
(EN) Embodiments of the invention are directed to formulations that provide a solution to the problem of small molecule (e.g., diazepam) precipitation at the injection site when administered as a highly-concentrated formulation. In certain aspects the formulations include at least one surfactant in a non-aqueous formulation, which prevents small molecule precipitation and improves the bioavailability of the drug by enhancing absorption into the systemic circulation.
(FR) Des modes de réalisation de la présente invention concernent des formulations qui apportent une solution au problème de la précipitation de petites molécules (par exemple, le diazépam) au niveau du site d’injection lorsqu’elles sont administrées sous la forme d’une formulation hautement concentrée. Dans certains aspects, les formulations comprennent au moins un tensioactif dans une formulation non aqueuse, qui empêche la précipitation de petites molécules et améliore la biodisponibilité du médicament en augmentant l’absorption dans la circulation systémique.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)