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1. WO2020116447 - SOLID DISPERSION OF POORLY SOLUBLE DRUG

Publication Number WO/2020/116447
Publication Date 11.06.2020
International Application No. PCT/JP2019/047231
International Filing Date 03.12.2019
IPC
A61K 31/426 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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425Thiazoles
4261,3-Thiazoles
A61K 9/14 2006.01
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
A61K 9/20 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
20Pills, lozenges or tablets
A61K 9/48 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
A61K 47/32 2006.01
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
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
A61K 47/38 2006.01
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
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
38Cellulose; Derivatives thereof
Applicants
  • 塩野義製薬株式会社 SHIONOGI & CO., LTD. [JP]/[JP]
Inventors
  • 佐久間 聡 SAKUMA Satoshi
Agents
  • 杉田 健一 SUGITA Ken-ichi
  • 渡部 秀昭 WATANABE Hideaki
Priority Data
2018-22732804.12.2018JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) SOLID DISPERSION OF POORLY SOLUBLE DRUG
(FR) DISPERSION SOLIDE DE MÉDICAMENT PEU SOLUBLE
(JA) 難溶性薬物の固体分散体
Abstract
(EN)
As a result of providing a solid dispersion containing (2E)-3-{2,6-dichloro-4-[(4-{3-[(1S)-1-(hexyloxy)ethyl]-2-methoxyphenyl}-1,3-thiazole-2-yl)carbamoyl]phenyl}-2-methyl-2-propenoic acid or a pharmaceutically acceptable salt thereof and a water-soluble polymer, the water solubility of the compound increases, and thus, the absorbability of the compound increases when orally administered.
(FR)
Selon l'invention, en conséquence de la fourniture d'une dispersion solide contenant de l'acide (2E)-3-{2,6-dichloro-4-[(4-{3-[(1S)-1-(hexyloxy)éthyl]-2-méthoxyphényl}-1,3-thiazol-2-yl)carbamoyl]phényl}-2-méthyl-2-propénoïque ou un sel pharmaceutiquement acceptable de ce dernier et un polymère soluble dans l'eau, la solubilité dans l'eau du composé augmente, et ainsi, l'absorbabilité du composé augmente lorsqu'il est administré par voie orale.
(JA)
(2E)-3-{2,6-ジクロロ-4-[(4-{3-[(1S)-1-(ヘキシルオキシ)エチル]-2-メトキシフェニル}-1,3-チアゾール-2-イル)カルバモイル]フェニル}-2-メチル-2-プロペン酸またはその製薬上許容される塩および水溶性高分子を含有する固体分散体の提供によって、当該化合物の水溶解度が増加し、経口投与における当該化合物の吸収性が増加する。
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