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菊粉的表面活性剂衍生物(Inutec® SP1)是高载药量固体分散体的优良载体。

Surface-active derivative of inulin (Inutec® SP1) is a superior carrier for solid dispersions with a high drug load.

机构信息

Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, 9713 AV Groningen, the Netherlands.

出版信息

J Pharm Sci. 2011 Jun;100(6):2333-42. doi: 10.1002/jps.22471. Epub 2011 Jan 19.

Abstract

The aim of this study was to compare the applicability of inulin, its surface-active derivative (Inutec® SP1), and polyvinylpyrrolidone (PVP) as carriers in high drug load solid dispersions (SDs) for improving the dissolution rate of a range of lipophilic drugs (diazepam, fenofibrate, ritonavir, and efavirenz). The SDs were prepared by spray freeze-drying. Scanning electron microscopy showed that the obtained samples were highly porous spherical particles. Modulated differential scanning calorimetry showed that the drugs incorporated in these carriers were fully or partially amorphous. The solubility of the drugs in solutions of the different carriers was increased in an order: inulin 2.3 kDa < PVP K30  ≪ Inutec® SP1. The dissolution behavior of SD tablets was evaluated. Inutec® SP1-based SD tablets showed the best performance followed by PVP- and inulin-based SD tablets. The superior dissolution behavior of the drugs from Inutec® SP1-based SDs could be ascribed to its surface-active nature. In addition, Inutec® SP1-based SD tablets gave good physical stability at 20 °C/45% relative humidity (RH) and 40 °C/75% RH for 3 months.

摘要

本研究旨在比较菊粉、其表面活性剂衍生物(Inutec® SP1)和聚乙烯吡咯烷酮(PVP)作为载体在高载药量固体分散体(SD)中应用的适用性,以提高一系列亲脂性药物(地西泮、非诺贝特、利托那韦和依非韦伦)的溶解速率。SD 通过喷雾冷冻干燥制备。扫描电子显微镜显示,所得样品为高度多孔的球形颗粒。调制差示扫描量热法表明,这些载体中包封的药物完全或部分呈无定形。药物在不同载体溶液中的溶解度按以下顺序增加:菊粉 2.3 kDa < PVP K30 ≪ Inutec® SP1。评估了 SD 片剂的溶解行为。基于 Inutec® SP1 的 SD 片剂表现出最好的性能,其次是基于 PVP 和菊粉的 SD 片剂。基于 Inutec® SP1 的 SD 中药物的优越溶解行为可归因于其表面活性剂性质。此外,基于 Inutec® SP1 的 SD 片剂在 20°C/45%相对湿度(RH)和 40°C/75%RH 下 3 个月具有良好的物理稳定性。

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