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由注射用载体制备的β-环糊精溶液和沉淀物的物理化学性质

Physicochemical properties of β-cyclodextrin solutions and precipitates prepared from injectable vehicles.

作者信息

Thurein Sai Myo, Lertsuphotvanit Nutdanai, Phaechamud Thawatchai

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.

Department of Pharmacognosy, University of Pharmacy, Mandalay, Myanmar.

出版信息

Asian J Pharm Sci. 2018 Sep;13(5):438-449. doi: 10.1016/j.ajps.2018.02.002. Epub 2018 Mar 16.

Abstract

β-Cyclodextrin (β-CyD) is cyclic oligosaccharide of a glucopyranose, containing a relatively hydrophobic central cavity and hydrophilic outer surface. However, the usefulness of β-CyD is limited owing to its low aqueous solubility whereas we found that its apparent high solubility was evident in some injectable solvents including 2-pyrrolidone (PYR), N-methyl pyrrolidone (NMP) and dimethyl sulfoxide (DMSO). Therefore, in the present study, the physicochemical properties of the 30-60% w/w β-CyD in PYR, NMP and DMSO were investigated such as viscosity, water resistant, matrix formation rate and syringeability. The higher the concentration of β-CyD resulted in the increased viscosity and the higher force and energy of syringeability. β-CyD in PYR gave the highest viscosity which contributed to the lowest syringeability while β-CyD in DMSO exhibited the highest syringeability. The β-CyD in DMSO and NMP exhibited the higher rate of matrix formation. β-CyD in PYR showed the highest water resistant for phase separation while β-CyD in NMP gave the faster de-mixing rate compared to that from PYR. The difference in physicochemical properties of β-CyD dried ppts studied by scanning electron microscope (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FT-IR) and thermogravimetric analysis (TGA) revealed that there was partial complexation of β-CyD with respective solvents. Both solution and precipitate characteristic properties will be useful for using β-CyD in further investigation as matrix material dissolved in the injectable vehicles as the forming gel for periodontitis treatment.

摘要

β-环糊精(β-CyD)是一种吡喃葡萄糖的环状寡糖,具有相对疏水的中心腔和亲水的外表面。然而,β-CyD的实用性因其低水溶性而受到限制,而我们发现其在一些可注射溶剂中表现出明显的高溶解性,包括2-吡咯烷酮(PYR)、N-甲基吡咯烷酮(NMP)和二甲基亚砜(DMSO)。因此,在本研究中,对30-60%w/w的β-CyD在PYR、NMP和DMSO中的物理化学性质进行了研究,如粘度、耐水性、基质形成速率和可注射性。β-CyD浓度越高,粘度增加,可注射性所需的力和能量越高。β-CyD在PYR中的粘度最高,导致可注射性最低,而β-CyD在DMSO中的可注射性最高。β-CyD在DMSO和NMP中表现出较高的基质形成速率。β-CyD在PYR中表现出最高的相分离耐水性,而β-CyD在NMP中的分层速率比PYR中的更快。通过扫描电子显微镜(SEM)、差示扫描量热法(DSC)、X射线衍射(XRD)、傅里叶变换红外光谱(FT-IR)和热重分析(TGA)研究的β-CyD干燥沉淀物的物理化学性质差异表明,β-CyD与各自的溶剂存在部分络合。溶液和沉淀的特性对于将β-CyD作为基质材料溶解在可注射载体中用作牙周炎治疗的形成凝胶的进一步研究将是有用的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d4b8/7032148/89db54946a2c/fx1.jpg

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