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1. WO2020210722 - FORMULATION FOR ORAL DELIVERY OF PROTEINS, PEPTIDES AND SMALL MOLECULES WITH POOR PERMEABILITY

Publication Number WO/2020/210722
Publication Date 15.10.2020
International Application No. PCT/US2020/027800
International Filing Date 10.04.2020
IPC
A61K 38/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 9/08 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
08Solutions
A61K 9/10 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
A61K 47/14 2017.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
08containing oxygen
14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 31/4545 2006.01
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
445Non-condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
4545containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61K 38/03
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
03Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
A61K 39/395
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
39Medicinal preparations containing antigens or antibodies
395Antibodies
A61K 47/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
08containing oxygen, ; e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/34
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 9/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
08Solutions
Applicants
  • R.P. SCHERER TECHNOLOGIES, LLC [US]/[US]
  • BIOHAVEN PHARMACEUTICAL HOLDING COMPANY LTD. [US]/[US]
Inventors
  • PLASSAT, Vincent
  • HILBOLD, Benoit
  • GALUS, Aurélia
  • POINTEAUX, Thomas
  • MEISSONNIER, Julien
  • DUBOWCHIK, Gene M.
  • CONWAY, Charles M.
Agents
  • VOGLER, Nathan
  • BOCKMAN, Jonathan
Priority Data
62/832,50811.04.2019US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) FORMULATION FOR ORAL DELIVERY OF PROTEINS, PEPTIDES AND SMALL MOLECULES WITH POOR PERMEABILITY
(FR) FORMULATION POUR L'ADMINISTRATION PAR VOIE ORALE DE PROTÉINES, DE PEPTIDES ET DE PETITES MOLÉCULES À FAIBLE PERMÉABILITÉ
Abstract
(EN)
The present disclosure is directed to a pharmaceutical formulation intended for oral delivery of synthetic or natural poorly permeable calcitonin gene-related peptide (CGRP) inhibitors or salts/solvates thereof having a therapeutic activity. The pharmaceutical formulation can include a synthetic or natural poorly permeable CGRP inhibitors or salt or solvate thereof in an amount 0.01-10 wt.% of the total weight of the formulation; a lipophilic phase comprising triglycerides of fatty acids in an amount of 50-80 wt.% of the total weight of the formulation; and at least one lipophilic surfactant comprising partial esters of polyol and fatty acids in an amount of about 10-50 wt.% of the total weight of the formulation.
(FR)
La présente invention concerne une formulation pharmaceutique destinée à l'administration par voie orale d'inhibiteurs du peptide lié au gène de la calcitonine (CGRP), faiblement perméables, synthétiques ou naturels, ou de sels/solvates de ceux-ci ayant une activité thérapeutique. La formulation pharmaceutique peut comprendre des inhibiteurs du CGRP faiblement perméables, synthétiques ou naturels, ou un sel ou un solvate de ceux-ci, en une proportion de 0,01 à 10 % en poids du poids total de la formulation ; une phase lipophile comprenant des triglycérides d'acides gras en une proportion de 50 à 80 % en poids du poids total de la formulation ; et au moins un tensioactif lipophile comprenant des esters partiels de polyol et d'acides gras en une proportion d'environ 10 à 50 % en poids du poids total de la formulation.
Latest bibliographic data on file with the International Bureau