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1. WO2022006946 - IBUPROFEN IATRIC FIBER SUSPENSION AND PREPARATION METHOD THEREFOR

Publication Number WO/2022/006946
Publication Date 13.01.2022
International Application No. PCT/CN2020/102252
International Filing Date 16.07.2020
IPC
A61K 9/10 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
10Dispersions; Emulsions
A61K 47/32 2006.1
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 2006.1
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
A61K 47/30 2006.1
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
A61K 47/06 2006.1
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
A61K 47/26 2006.1
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
26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
Applicants
  • 江苏四环生物制药有限公司 JIANGSU SIHUAN BIOENGINEERING PHARMACEUTICAL CO., LTD [CN]/[CN]
Inventors
  • 丁月萍 DING, Yueping
  • 江永红 JIANG, Yonghong
  • 徐益明 XU, Yiming
  • 陶冬梅 TAO, Dongmei
  • 袁菊凤 YUAN, Jufeng
Agents
  • 无锡华源专利商标事务所(普通合伙) WUXI HUAYUAN PATENT AND TRADEMARK AGENCY (GENERAL PARTNERSHIP)
Priority Data
202010651960.X08.07.2020CN
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) IBUPROFEN IATRIC FIBER SUSPENSION AND PREPARATION METHOD THEREFOR
(FR) SUSPENSION DE FIBRES IATRIQUES D'IBUPROFÈNE ET SON PROCÉDÉ DE PRÉPARATION
(ZH) 一种布洛芬药物纤维混悬剂及其制备方法
Abstract
(EN) Disclosed in the present invention are an ibuprofen iatric fiber suspension and a preparation method therefor, falling within the technical field of sustained-release medicaments. The ibuprofen iatric fiber suspension is prepared according to the present invention, which can prolong the half-life period of ibuprofen to 6.926 h and the time to peak Tmax to 2.5 h, can reduce the peak concentration Cmax to 19.51 μg·mL -1, and has an obvious in vivo sustained-release effect. The preparation method provided by the present invention has a high production efficiency and the production cost is reduced; and the whole process can be carried out in a glass reaction kettle, the parameters are easy to control, and the process is fundamentally not influenced by external conditions.
(FR) La présente invention concerne une suspension de fibres iatriques d'ibuprofène et son procédé de préparation, tombant dans le domaine technique des médicaments à libération prolongée. La suspension de fibres iatriques d'ibuprofène est préparée selon la présente invention, qui peut prolonger la période de demi-vie de l'ibuprofène à 6,926 h et le temps jusqu'au pic Tmax à 2,5 h, peut réduire le pic de concentration Cmax à 19,51 μg·mL-1, et présente un effet de libération prolongée in vivo évident. Le procédé de préparation selon la présente invention présente un rendement de production élevé et le coût de production est réduit; et l'ensemble du procédé peut être mis en œuvre dans un autoclave de réaction en verre, les paramètres sont faciles à contrôler, et le procédé n'est fondamentalement pas influencé par des conditions externes.
(ZH) 本发明公开了一种布洛芬药物纤维混悬剂及其制备方法,属于缓释药剂技术领域。本发明制备了一种布洛芬药物纤维混悬剂,其能够将布洛芬的半衰期延长至6.926h,达峰时间Tmax延长至2.5h,峰浓度Cmax降低至19.51μg·mL -1,具有明显的体内缓释效果。本发明提供的制备方法在生产效率高的同时,降低了生产成本,且整个过程都能在玻璃反应釜中进行,容易控制参数,且基本不受外界条件影响。
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