该栓剂含有一种活性药物成分的复合物——由甲氟喹和青蒿琥酯与咪唑酸沸石骨架衍生的离子液体（API-IL）

IF 13.2 1区工程技术 Q1 ENGINEERING, CHEMICAL

Chemical Engineering Journal Pub Date : 2025-10-10 DOI:10.1016/j.cej.2025.169534

Chen Chen, Xinlu Li, Weixia Zhu, Yu Chen, Jie Tang, Shun Yao

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引用次数: 0

摘要

本研究旨在开发一种含有活性药物成分离子液体（API-IL）与金属有机骨架配合物的新型栓剂。作为联合治疗COVID-19的两种著名抗病毒药物，盐酸甲氟喹（MQ）与青蒿琥酯（Art）联合治疗后转化为api - il，以提高治疗效果。采用熔点测试、傅里叶变换红外光谱（FT-IR）、质子核磁共振（1H NMR）和质谱（MS）对合成的[MQ][Art]进行了表征。此外，[MQ][Art]表现出更好的水溶性、稳定性和pH值，促进了治疗效果，同时最大限度地减少了给药期间对肠道的刺激。随后，将[MQ][Art]加入到ZIF-8分子筛中，进一步增强稳定性，达到控释效果。结合ZIF-8与API-IL相互作用能的计算研究，综合表征证实了[MQ][Art]在ZIF-8上的成功结合。研究了栓剂的制备方法；在所测试的9种栓剂碱中，波洛沙莫为基础的栓剂具有均匀的质量，适宜的硬度和溶化时间，同时在[MQ][Art]上具有控释作用。经过10 h的累积释放率测试达到90 %。最后，含有[MQ][Art]@ZIF-8的poloxamer基栓剂表现出良好的质量均匀性，平均药物含量为11.4 mg /栓剂，平均位移值为2.59。此外，还检测了体内释放过程，以证明所开发系统的有效性。综上所述，api - il与ZIF-8联合用于治疗COVID-19的栓剂通过改善溶解度和稳定性提高了治疗效果，同时还提供了对MQ和Art的控释效果。

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The suppository containing a complex of active pharmaceutical ingredient-ionic liquid (API-IL) derived from mefloquine and artesunate with Zeolitic imidazolate framework-8

This study aimed to develop a new suppository containing the complex of active pharmaceutical ingredient-ionic liquid (API-IL) and metal organic framework. As two famous drugs with anti-virus activities for the combination therapy of COVID-19, mefloquine (MQ) hydrochloride and artesunate (Art) were combined and then transformed to API-ILs to enhance therapeutic effects. The synthesized [MQ][Art] was characterized using melting point tests, Fourier transform infrared spectrum (FT-IR), proton nuclear magnetic resonance (¹H NMR), and mass spectroscopy (MS). Furthermore, [MQ][Art] exhibited improved water solubility, stability and pH values, which promoted treatment effectiveness while minimizing intestinal irritation during administration. Subsequently, [MQ][Art] was incorporated into Zeolitic imidazolate framework-8 (ZIF-8) to further enhance stability and achieve a controlled release effect. Combined with computational studies on interactive energy between ZIF-8 and API-IL, comprehensive characterizations confirmed the successful incorporation of [MQ][Art] on ZIF-8. The preparation method of suppositories was then investigated; among the 9 tested suppository bases, poloxamer-based suppositories demonstrated uniform quality with suitable hardness and melting time while also exhibiting a controlled release effect on [MQ][Art]. After 10 h of cumulative release rate testing reached 90 %. Finally, the poloxamer-based suppository containing [MQ][Art]@ZIF-8 showed good quality uniformity with an average drug content of 11.4 mg per suppository and an average displacement value of 2.59. Besides that, the in vivo release process was detected to demonstrate the effectiveness of the developed system. In conclusion, the combination of API-ILs with ZIF-8 in suppositories designed for COVID-19 treatment enhances therapy effectiveness by improving solubility and stability while also providing controlled release effects on MQ and Art.

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来源期刊

Chemical Engineering Journal 工程技术-工程：化工

CiteScore

21.70

自引率

9.30%

发文量

6781

审稿时长

2.4 months

期刊介绍： The Chemical Engineering Journal is an international research journal that invites contributions of original and novel fundamental research. It aims to provide an international platform for presenting original fundamental research, interpretative reviews, and discussions on new developments in chemical engineering. The journal welcomes papers that describe novel theory and its practical application, as well as those that demonstrate the transfer of techniques from other disciplines. It also welcomes reports on carefully conducted experimental work that is soundly interpreted. The main focus of the journal is on original and rigorous research results that have broad significance. The Catalysis section within the Chemical Engineering Journal focuses specifically on Experimental and Theoretical studies in the fields of heterogeneous catalysis, molecular catalysis, and biocatalysis. These studies have industrial impact on various sectors such as chemicals, energy, materials, foods, healthcare, and environmental protection.