一种托法替尼的自乳化纳米制剂及其制备方法
By preparing a self-emulsifying nanoformulation of tofacitinib and utilizing a specific combination of excipients, the pH-dependent solubility problem of tofacitinib was solved, achieving stable absorption and high bioavailability of the drug in the gastrointestinal tract, simplifying the production process, reducing production costs, and providing multiple forms of administration.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- CHONGQING UNIV
- Filing Date
- 2026-04-28
- Publication Date
- 2026-07-17
AI Technical Summary
Tofacitinib's solubility is significantly pH-dependent, leading to unstable blood drug concentrations. Existing technological improvements mainly target the salt form, which involves complex salt formation processes and degradation risks, making it difficult to effectively address the pH-dependent effects.
A self-emulsifying nano-formulation was prepared by combining tofacitinib free base with diethylene glycol monoethyl ether, polyoxyethylene 40 hydrogenated castor oil and glyceryl monocaprylate, avoiding the salt formation process, and using SEDDS technology to achieve rapid release and stable absorption of the drug in the gastrointestinal tract.
It improves the solubility and stability of tofacitinib, reduces pH-dependent effects, ensures stable absorption of the drug in the gastrointestinal tract, reduces production costs and inter-individual absorption differences, and provides multiple administration methods to improve patient convenience.
Smart Images
Figure CN122097264B_ABST