载药因子对利托那韦-介孔二氧化硅体系固态形态的影响

Tanweer AL-Dagamin, J. O'shea, A. Crean
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引用次数: 0

摘要

在用于提高水溶性差的药物的溶解度和溶出率的配方技术中,介孔二氧化硅给药系统显示出前景。将药物装载到二氧化硅上采用了一系列的工艺,溶剂基方法被广泛采用。本研究旨在了解药物浓度、溶剂和药物-二氧化硅比对药物在二氧化硅中的固态形态和非晶化的影响。以BCSⅱ类药物利托那韦为模型药物。使用溶剂蒸发法将利托那韦装入Syloid®244FP中。利托那韦的负载百分比是基于二氧化硅的整个比表面积暴露并可用于药物吸附的假设计算的。3种不同利托那韦浓度的乙醇溶液;25°C饱和溶解度分别为70%、32%和20%。利托那韦按1:1、1:2和1:3的利托那韦与二氧化硅的比例装入二氧化硅中。所有的系统包括利托那韦加载超过单层表面覆盖。采用DSC、PXRD、FT-IR和TGA对利托那韦- Syloid®244fp进行表征。结果表明,所有制备的利托那韦- syloid®244fp体系均含有非晶态的利托那韦。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The impact of drug-loading factors on the solid-state form of ritonavir-mesoporous silica systems
Among the formulation techniques used to enhance thesolubility and dissolution rate of poorly, aqueous-soluble drugs, mesoporoussilica drug delivery systems have shown promise. A range of processes areemployed to load drugs onto silica and solvent-based approaches are widelyemployed. This study aims to understand the influence of drug concentration insolvent and drug-silica ratio on drug solid-state form and amorphization withinsilica. Ritonavirwhich belongs to  BCS Class II was used asa model drug. Ritonavir wasloaded into Syloid®244FP using a solvent evaporationmethod. Ritonavir loading percentage was calculated based on the assumptionthat the entire specific surface area of silica is exposed and available fordrug adsorption.  Ethanolsolutions with 3 different ritonavir concentrations; 70%, 32% and 20% saturatedsolubility at 25°C were employed. Ritonavir was loaded into silica at 1:1, 1:2and 1:3 ritonavir:silica ratios.  Allsystems included ritonavir loaded beyond monolayer surface coverage. Ritonavir- Syloid®244 FP formulations were characterisedusing DSC, PXRD, FT-IR, and TGA. The results showed that all ritonavir-Syloid®244 FP systemsprepared contained ritonavir in a non-crystalline state.
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