淫羊藿素氨基甲酸酯类前药及其制备方法和应用
CN119841798BActive Publication Date: 2026-07-17SHENYANG PHARMA UNIV
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- SHENYANG PHARMA UNIV
- Filing Date
- 2023-10-17
- Publication Date
- 2026-07-17
AI Technical Summary
Technical Problem
The poor water solubility and first-pass effect of ICT result in low bioavailability, and existing technological improvement methods have limitations, making it difficult to effectively improve its efficacy in clinical applications.
Method used
By introducing alkyl carbamate structures at the 3- or 7-position of ICT, carbamate prodrugs can be synthesized, increasing their solubility and metabolic stability, reducing phase II metabolism, and improving bioavailability.
Benefits of technology
It significantly improves the oral bioavailability of ICT, reduces the dosage, decreases toxic side effects, and provides a more efficient choice of anti-tumor drugs.
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Figure CN119841798B_ABST
Abstract
淫羊藿素氨基甲酸酯类前药及其制备方法和应用，属于制药领域，具体为式3‑N或7‑N所示淫羊藿素氨基甲酸酯类前药和其药学上可接受的盐，及其制备方法与用途。具体地，本发明通过将天然黄酮化合物淫羊藿素主要代谢位点(3位或7位羟基)，通过化学合成方法进行结构改造，在该位置引入适宜的基团，形成淫羊藿素氨基甲酸酯前药。此类氨基甲酸酯所采用的胺类为脂肪胺。氨基甲酸酯结构的存在，减小了淫羊藿素在SD大鼠中的Ⅱ相代谢，与淫羊藿素原料药相比，3‑N‑01前药的口服生物利用度显著提高，为最优前药，临床用药有希望能够降低给药剂量，提高患者顺应性，且有望为酚类药物口服生物利用度的提高提供一种有效策略。
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