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使用中孔碳酸镁提高塞来昔布在模拟肠细胞膜模型中的传递

Increasing the Transport of Celecoxib over a Simulated Intestine Cell Membrane Model Using Mesoporous Magnesium Carbonate.

机构信息

Division of Nanotechnology and Functional Materials, Department of Materials Science and Engineering, Uppsala University, P.O. Box 534, SE-751 21 Uppsala, Sweden.

Drug Delivery, Department of Pharmacy, Uppsala University, P.O. Box 580, SE-751 23 Uppsala, Sweden.

出版信息

Molecules. 2021 Oct 21;26(21):6353. doi: 10.3390/molecules26216353.

Abstract

In the current work, mesoporous magnesium carbonate (MMC) was used to suppress crystallization of the poorly soluble drug celecoxib (CXB). This resulted in both a higher dissolution rate and supersaturation of the substance in vitro as well as an increased transfer of CXB over a Caco-2 cell membrane mimicking the membrane in the small intestine. The CXB flux over the cell membrane showed a linear behavior over the explored time period. These results indicate that MMC may be helpful in increasing the bioavailability and obtaining a continuous release of CXB, and similar substances, in vivo. Neusilin US2 was used as a reference material and showed a more rapid initial release with subsequent crystallization of the incorporated CXB in the release media. The presented results form the foundation of future development of MMC as a potential carrier for poorly soluble drugs.

摘要

在目前的工作中,介孔碳酸镁(MMC)被用于抑制难溶性药物塞来昔布(CXB)的结晶。这导致药物在体外的溶解速率和过饱和度更高,并且在模拟小肠中细胞膜的 Caco-2 细胞膜上的 CXB 转移增加。细胞膜上的 CXB 通量在探索的时间段内呈线性行为。这些结果表明,MMC 可能有助于提高生物利用度,并在体内获得 CXB 和类似物质的持续释放。N 中空硅石 US2 被用作参考材料,显示出更快的初始释放,随后在释放介质中掺入的 CXB 结晶。所呈现的结果为 MMC 作为难溶性药物潜在载体的未来发展奠定了基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/865f/8588146/3b7d192a4396/molecules-26-06353-g001.jpg

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