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载有缬沙坦-香草醛二元共无定形系统的介孔硅粒子的溶解性能增强。

Enhanced dissolution of valsartan-vanillin binary co-amorphous system loaded in mesoporous silica particles.

机构信息

a Riphah Institute of Pharmaceutical Sciences , Riphah International University , Islamabad , Pakistan.

b Department of Pharmacy , Quaid-i-Azam University , Islamabad , Pakistan.

出版信息

J Microencapsul. 2019 Jan;36(1):10-20. doi: 10.1080/02652048.2019.1579265. Epub 2019 Apr 8.

Abstract

The study was aimed to prepare a co-amorphous system of valsartan (VAL) with vanillin (VAN) for improving its solubility and dissolution followed by its confinement in mesoporous silica particles (MSPs) to stabilise the co-amorphous system and prevent its recrystallization. Amorphous VAL and VAN were obtained through quench-cooling and VAL/VAN binary co-amorphous system (VAL/VAN-CAS) was prepared through solvent evaporation technique. The particle size and morphology of VAL/VAN-CAS-MSPs were studied using scanning electron microscopy (SEM) and solid-state characterisation was performed by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD). The dissolution was investigated by dialysis bag diffusion method. SEM analysis revealed irregular shaped VAL/VAN-CAS-MSPs with a size range of 5-25 μm, while outcomes of DSC and XRPD confirmed the formation of VAL/VAN-CAS. The dissolution profiles demonstrated a significantly increased dissolution in first 60 minutes from VAL/VAN-CAS (∼68%) and VAL/VAN-CAS-MSPs (∼76%) compared to powder VAL (∼25%).

摘要

这项研究旨在制备缬沙坦(VAL)与香草醛(VAN)的共无定形系统,以提高其溶解度和溶解率,随后将其限制在介孔硅粒子(MSPs)中,以稳定共无定形系统并防止其再结晶。通过骤冷法获得无定形 VAL 和 VAN,通过溶剂蒸发技术制备 VAL/VAN 二元共无定形系统(VAL/VAN-CAS)。通过扫描电子显微镜(SEM)研究了 VAL/VAN-CAS-MSPs 的粒径和形貌,并通过差示扫描量热法(DSC)和 X 射线粉末衍射(XRPD)进行了固态特性研究。通过透析袋扩散法研究了溶解情况。SEM 分析显示,VAL/VAN-CAS-MSPs 呈不规则形状,粒径范围为 5-25μm,而 DSC 和 XRPD 的结果证实了 VAL/VAN-CAS 的形成。溶解曲线表明,与粉末 VAL(约 25%)相比,VAL/VAN-CAS(约 68%)和 VAL/VAN-CAS-MSPs(约 76%)在前 60 分钟内的溶解率显著提高。

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