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提高卡洛芬溶解度:ZnAl-LDH 混合化合物的合成。

Improving the Carprofen Solubility: Synthesis of the ZnAl-LDH Hybrid Compound.

机构信息

Department of Chemistry, University of Pavia, viale Taramelli 16, Pavia 27100, Italy.

Department of Drug Sciences, University of Pavia, via Taramelli 12, Pavia 27100, Italy.

出版信息

J Pharm Sci. 2018 Jan;107(1):267-272. doi: 10.1016/j.xphs.2017.09.019. Epub 2017 Oct 5.

Abstract

The development of efficient strategies for drug delivery is considerably desired. Indeed, often several issues such as the drug solubility, the control of the drug release rate, the targeted delivery of drugs, the drug bioavailability, and the minimization of secondary effects still present great obstacles. Different methodologies have been proposed, but the use of nano-hybrids compounds that combine organic and inorganic substances seems particularly promising. An interesting inorganic host is the layered double hydroxide (LDH) with a sheets structure and formula M M (OH) yHO (M = Zn, Mg; M = Al; A = nitrates, carbonates, chlorides). The possibility to exchange these counterions with drug molecules makes these systems ideal candidates for the drug delivery. In this article, we synthesize by co-precipitation method the hybrid compound Carprofen-ZnAl-LDH. Carprofen, a poorly soluble anti-inflammatory drug, could also benefit of the association with a natural antacid such as LDH, to reduce the gastric irritation after its administration. Through X-ray diffraction and Fourier-transformed infrared spectroscopy (FT-IR), we could verify the effective drug intercalation into LDH. The dissolution tests clearly demonstrate a significant improvement of the drug release rate when carprofen is in the form of hybrid compound.

摘要

开发有效的药物输送策略是非常需要的。事实上,通常存在多个问题,例如药物溶解度、药物释放速率的控制、药物的靶向输送、药物的生物利用度以及最小化副作用等,这些问题仍然是巨大的障碍。已经提出了不同的方法,但使用将有机和无机物质结合在一起的纳米杂化化合物似乎特别有前途。一种有趣的无机主体是具有片状结构和化学式[M M (OH)] (A) yHO 的层状双氢氧化物(LDH)(M = Zn、Mg;M = Al;A = 硝酸盐、碳酸盐、氯化物)。这些抗衡离子可以与药物分子交换,这使得这些系统成为药物输送的理想候选物。在本文中,我们通过共沉淀法合成了布洛芬-ZnAl-LDH 杂化化合物。布洛芬是一种溶解度较差的抗炎药,与 LDH 等天然抗酸剂结合使用也可以减少给药后的胃刺激。通过 X 射线衍射和傅里叶变换红外光谱(FT-IR),我们可以验证药物有效插入 LDH。溶解试验清楚地表明,当布洛芬以杂化化合物的形式存在时,药物释放速率显著提高。

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