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1. (WO2019063382) A METHOD FOR MODIFYING RELEASE OF A THERAPEUTICALLY ACTIVE AGENT FROM AN ELASTOMERIC MATRIX
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Pub. No.: WO/2019/063382 International Application No.: PCT/EP2018/075331
Publication Date: 04.04.2019 International Filing Date: 19.09.2018
IPC:
A61K 9/00 (2006.01) ,A61K 47/34 (2017.01) ,A61K 31/192 (2006.01) ,A61K 31/196 (2006.01) ,A61K 31/405 (2006.01) ,A61K 31/5415 (2006.01) ,A61K 47/02 (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
30
Macromolecular compounds
34
Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
185
Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19
Carboxylic acids, e.g. valproic acid
192
having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
185
Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19
Carboxylic acids, e.g. valproic acid
195
having an amino group
196
the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403
condensed with carbocyclic rings, e.g. carbazole
404
Indoles, e.g. pindolol
405
Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
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
54
having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
5415
ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
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
02
Inorganic compounds
Applicants:
BAYER OY [FI/FI]; Pansiontie 47 20210 Turku, FI
Inventors:
AHOLA, Manja; FI
HAKALA, Risto; FI
HARA, Piia; FI
KEINÄNEN, Antti; FI
KOROLAINEN, Henriikka; FI
PIHLAJA, Jyrki; FI
Agent:
BIP PATENTS; Alfred-Nobel-Str. 10 40789 Monheim am Rhein NRW, DE
Priority Data:
17193367.427.09.2017EP
18167014.212.04.2018EP
Title (EN) A METHOD FOR MODIFYING RELEASE OF A THERAPEUTICALLY ACTIVE AGENT FROM AN ELASTOMERIC MATRIX
(FR) PROCÉDÉ DE MODIFICATION DE LA LIBÉRATION D'UN AGENT THÉRAPEUTIQUEMENT ACTIF À PARTIR D'UNE MATRICE ÉLASTOMÈRE
Abstract:
(EN) The present invention relates to a method for modifying release of a therapeutically active agent from an elastomeric matrix, comprising providing a core comprising an elastomeric matrix and a therapeutically active agent; dipping the core to a coating solution of an elastomer, wherein the elastomer comprises 20-35 wt-% of a filler, calculated from the total amount of filler and elastomer; curing the dipped core to provide a coated core. In this method the dipping is provided as a continuous process by pulling the core through the coating solution, using a pulling speed suitable for providing a coating thickness of δ-ΙΟΟμιΐη; the filler is selected from silica, titanium dioxide, barium sulphate, carbon and mixtures thereof; the elastomer comprised in the core and the elastomer comprised in the coating solution are independently selected from poly(dimethyl) siloxanes, polyethylene vinyl acetates (EVAs), polyurethanes (PUs), polyhydroxyethyl methacrylates (PHEMAs) and polymethyl methacrylates (PMMAs).
(FR) La présente invention concerne un procédé de modification de la libération d'un agent thérapeutiquement actif à partir d'une matrice élastomère, comprenant le fait de se munir d'un noyau comprenant une matrice élastomère et un agent thérapeutiquement actif; le trempage du noyau dans une solution de revêtement d'un élastomère, l'élastomère comprenant de 20 à 35 % en masse d'une charge, calculés à partir de la quantité totale de charge et d'élastomère; le durcissement du noyau trempé pour obtenir un noyau enrobé. Dans ce procédé, le trempage est réalisé sous la forme d'un processus continu en tirant le noyau à travers la solution de revêtement, à l'aide d'une vitesse de traction adaptée à l'obtention d'une épaisseur de revêtement de δ-100 µm; la charge est choisie parmi la silice, le dioxyde de titane, le sulfate de baryum, le carbone et des mélanges de ceux-ci; l'élastomère compris dans le noyau et l'élastomère compris dans la solution de revêtement étant indépendamment choisis parmi les poly(diméthyl)siloxanes, les polyéthylène-acétates de vinyle (EVA), les polyuréthanes (PU), les polyméthacrylates d'hydroxyéthyle (PHEMA) et les polyméthacrylates de méthyle (PMMA).
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)