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1. WO2011140194 - OPHTHALMIC COMPOSITION

Publication Number WO/2011/140194
Publication Date 10.11.2011
International Application No. PCT/US2011/035147
International Filing Date 04.05.2011
IPC
A61K 31/74 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
74Synthetic polymeric materials
CPC
A61K 31/138
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines
135having aromatic rings ; , e.g. ketamine, nortriptyline
138Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61K 31/382
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
382having six-membered rings, e.g. thioxanthenes
A61K 31/433
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
433Thidiazoles
A61K 31/4704
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
47Quinolines; Isoquinolines
47042-Quinolinones, e.g. carbostyril
A61K 31/5377
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
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/542
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
54having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
542ortho- or peri-condensed with heterocyclic ring systems
Applicants
  • SENJU USA, INC. [US]/[US] (AllExceptUS)
  • INOUE, Jun [JP]/[US] (UsOnly)
  • SHAH, Tapan [IN]/[US] (UsOnly)
Inventors
  • INOUE, Jun
  • SHAH, Tapan
Agents
  • SCHMID, Amy, E.
Priority Data
12/774,41905.05.2010US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) OPHTHALMIC COMPOSITION
(FR) COMPOSITION OPHTALMIQUE
Abstract
(EN)
The present invention provides an ophthalmic composition comprising a hyperbranched polyester. The ophthalmic compositions may also comprise carbonic anhydrase inhibitors, wherein the hyperbranched polyester increases the aqueous solubility of the carbonic anhydrase inhibitor, and increases corneal permeation of the active agent. The ophthalmic compositions may also comprise non-ionic surfactants, such as PEG, Polysorbate, HPMC or HEC, and beta-blockers,such as Carteolol, Levobunolol, Betaxolol, Metipranolol, Timolol or Propranolol. The concentration of the hyperbranched polyester in the ophthalmic formulation should be less than or equal to 4% (w/v) in order to avoid any cytotoxic effects on human corneal cells and thus the eye irritation.
(FR)
L'invention concerne une composition ophtalmique comprenant un polyester hyperramifié. Les compositions ophtalmiques peut également comprendre des inhibiteurs d'anhydrase carbonique, dans lesquels le polyester hyperramifié accroît la solubilité aqueuse de l'inhibiteur d'anhydrase carbonique, ainsi que la perméation cornéenne de l'agent actif. Les compositions ophtalmiques peuvent également comprendre des tensio-actifs non ioniques, tels que PEG, polysorbate, HPMC ou HEC, et des bêta-bloquants, tels que cartéolol, lévobunolol, bétaxolol, métipranolol, timolol ou propranolol. La concentration du polyester hyperramifié dans la formulation ophtalmique devrait être inférieure ou égale à 4% (p/v) afin d'éviter tout effet cytotoxique sur les cellules cornéennes et par conséquent l'irritation de l'oeil.
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