WO2025200966 - PALIPERIDONE COCRYSTAL, AND PREPARATION AND USE THEREOF
National phase entry is expected:
Publication Number
WO/2025/200966
Publication Date
02.10.2025
International Application No.
PCT/CN2025/080572
International Filing Date
04.03.2025
Title **
[English]
PALIPERIDONE COCRYSTAL, AND PREPARATION AND USE THEREOF
[French]
COCRISTAL DE PALIPÉRIDONE, PRÉPARATION ET UTILISATION CORRESPONDANTES
[Chinese]
一种帕利哌酮共结晶体及其制备和应用
Applicants **
CHANGZHOU NO.4 PHARMACEUTICAL FACTORY CO. LTD
Inventors
SHEN, Zheng
GE, Jilong
Priority Data
202410385077.9
29.03.2024
CN
Application details
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International Searching Authority |
CNIPA
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| Recordal of a Change of the Applicant's Name/Address |
Change of Applicant's Name and Address
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| Type of Assignment |
The Standard Agent's Assignment
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| Applicant's Legal Status |
Legal Entity
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| Entry into National Phase under |
Chapter I
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| Patent Delivery |
Send the Letters Patent by Courier
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| Translation |
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 1575 | |
| EPO | Filing, Examination, Granting | 11598 | |
| Japan | Filing, Examination, Granting | 2015 | |
| South Korea | Filing, Examination, Granting | 1796 | |
| USA | Filing, Examination, Granting | 4740 |
Total:
21,724
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Abstract[English]
The present invention provides a paliperidone cocrystal, and a preparation method therefor and a use thereof. The cocrystal former of the paliperidone cocrystal is nicotinic acid. The paliperidone cocrystal is obtained by dissolving paliperidone and nicotinic acid in an aqueous organic solvent and then evaporating to dryness under reduced pressure. The paliperidone cocrystal of the present invention has high purity and stable quality, is suitable for commercial storage, has greatly improved solubility and dissolution rate, and is more suitable for the development of paliperidone preparations.[French]
La présente invention concerne un cocristal de palipéridone, un procédé de préparation associé et une utilisation correspondante. L'agent de formation du cocristal du cocristal de palipéridone est l'acide nicotinique. Le cocristal de palipéridone est obtenu par dissolution de palipéridone et d'acide nicotinique dans un solvant organique aqueux, puis par évaporation à sec sous pression réduite. Le cocristal de palipéridone selon la présente invention présente une pureté élevée et une qualité stable, est approprié pour un stockage commercial, présente une solubilité et une vitesse de dissolution considérablement améliorées et est plus approprié pour la mise au point de préparations de palipéridone.[Chinese]
本发明提供一种帕利哌酮共结晶体及其制备方法和应用，所述帕利哌酮共结晶体的共晶配体是烟酸，通过将帕利哌酮与烟酸在一种含水有机溶剂中溶解，再通过减压蒸干获得。本发明的帕利哌酮共结晶体纯度高，质量稳定，宜于商业存储，且溶解度和溶出速率得到极大的提升，更适用于帕利哌酮制剂的开发。