Osthole奈米粒子之製備及其性質探討

Preparation and characterization of osthole nanoparticles

洪珮雯(Pei-Wen Hung)

指導教授 ： 蔡東榮

高雄醫學大學/藥學院/藥學研究所/碩士(2005年)

摘要

已有許多化合物從蛇床子藥材中分離出來，蛇床子素(osthole)為主成分，是一水難溶性藥物。本實驗之目的為osthole奈米粒子之製備及其性質探討。使用柱層層析方法及超臨界流體萃取方法萃取蛇床子中的osthole，並比較這兩種萃取方法。應用23 複因子實驗設計法評估osthole最佳超臨界流體萃取條件，並利用界面聚合方法製備osthole奈米膠囊分子及熱均質法製備osthole固體脂質奈米粒子。
萃取結果顯示，使用柱層層析方法之蛇床子素萃取量(32.11 mg/g)比超臨界流體萃取方法之蛇床子素萃取量(5.36 mg/g)多，而壓力250 bar，溫度40℃，添加co-solvent (ethanol)之條件為osthole之最佳超臨界流體萃取條件。以正己烷和乙酸乙酯純化蛇床子萃取物，並利用質譜儀和核磁共振儀之光譜來鑑定osthole之結構，結果顯示，分子量為244，和osthole之分子式C15H16O3 一致。
Osthole奈米膠囊分子和osthole固體脂質奈米粒子之平均粒徑大小分別為200 nm及100 nm，藥品包埋率分別為67.44% 和62.35%。示差掃瞄熱分析（DSC）結果顯示，osthole是以非晶型狀態存在奈米製劑中，而體外溶離試驗方面，osthole奈米膠囊分子和osthole固體脂質奈米粒子之釋離情形相似，其溶離釋出較慢，具有緩釋的效果。

關鍵字

蛇床子素 ； 奈米粒子

並列摘要

Many compounds had been isolated from Cnidium monnier. Osthole is a major one, but it is a poor solubility drug. The objective of this study was preparation and characterization of osthole nanoparticles. Column chromatography had been compared with supercritical fluid extraction (SFE), for the extraction of osthole from the fruits of Cnidium monnier (L.) Cusson. 23 factorial design was used to optimize SFE conditions for osthole. Osthole nanocapsules were prepared by interfacial polymerization method and osthole solid lipid nanoparticles were prepared by hot homogenization technique.
The extraction results showed that the yield extracted by column chromatography (32.11 mg/g) was higher than the yield extracted by SFE (5.36 mg/g). SFE experimental data showed that the most effective extraction amount of osthole was performed at 250 bar, 40℃, and with co-solvent (ethanol). The extract was purified with n-hexane and ethyl acetate. The structural identification of osthole was carried out by MS, 1H-NMR and 13C-NMR spectra. It showed that the molecular ion at m/z 244, which was in agreement with the molecular formula C15H16O3 of osthole.
The mean particle size of osthole nanocapsules and osthole-SLN were 200 nm and 100 nm. The entrapment efficiency of osthole nanocapsules and osthole-SLN were 67.44% and 62.35%. Differential scanning calorimetry (DSC) was performed in order to characterize the physical state of osthole in nanocapsules and SLN. The DSC results showed that osthole was presented in an amorphous state in nanocapsules and SLN. The release profiles obtained were similar for osthole nanocapsules and osthole-SLN. The release rate of osthole from nanocapsules and SLN were slower than osthole solution. This results showed that osthole nanocapsules and osthole-SLN had slow- release effect.

並列關鍵字

osthole ； nanoparticles

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