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1. WO2021204883 - PHARMACEUTICAL COMPOSITION FOR TREATING INFLAMMATORY BOWEL DISEASES

Publication Number WO/2021/204883
Publication Date 14.10.2021
International Application No. PCT/EP2021/059076
International Filing Date 07.04.2021
IPC
A61K 9/16 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders
16Agglomerates; Granulates; Microbeadlets
A61K 31/443 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
443containing a five-membered ring with oxygen as a ring hetero atom
A61P 1/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
Applicants
  • CVASTHERA [FR]/[FR]
  • INSTITUT MINES TELECOM [FR]/[FR]
Inventors
  • SABLAYROLLES, Sylvie
  • LE GRAND, Bruno
  • RÉ, Maria Ines
  • PERRON, Antoine
Agents
  • IPSIDE
Priority Data
FR200349608.04.2020FR
Publication Language French (FR)
Filing Language French (FR)
Designated States
Title
(EN) PHARMACEUTICAL COMPOSITION FOR TREATING INFLAMMATORY BOWEL DISEASES
(FR) COMPOSITION PHARMACEUTIQUE POUR LE TRAITEMENT DES MALADIES INFLAMMATOIRES INTESTINALES
Abstract
(EN)
The invention relates to a pharmaceutical composition suitable for oral administration, containing as active ingredient a compound chosen from the group consisting of vorapaxar, vorapaxar isomers, atopaxar and 3,2-(chlorophenyl)-1-[4-(4-fluorobenzyl)piperazin-1-yl]propenone, and pharmaceutically acceptable salts thereof. This composition contains particles comprising a core containing a mixture of the active ingredient and of a substance capable of inhibiting recrystallisation of the active ingredient at a pH which has become greater than or equal to 5; and a pH-dependent, controlled-release coating layer covering said core, said coating layer being formed of a gastro-resistant coating agent and being porous.
(FR)
L'invention concerne une composition pharmaceutique convenant à une administration par voie orale, contenant en tant que principe actif un composé choisi dans le groupe constitué du vorapaxar, des isomères du vorapaxar, de l'atopaxar, de la 3-2-(chloro-phényl)-1-[4-(4-fluoro-benzyl)-pipérazin-1-yl]- propénone et de leurs sels pharmaceutiquement acceptables. Cette composition contient des particules comprenant un cœur contenant un mélange du principe actif et d'une substance apte à inhiber la recristallisation du principe actif à un pH devient supérieur ou égal à 5; et une couche d'enrobage à libération contrôlée pH-dépendante recouvrant ledit cœur, ladite couche d'enrobage étant formée d'un agent d'enrobage gastro-résistant et étant poreuse.
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