β-环糊精包合技术在大蒜精油新剂型研究中的应用

APPLICATION OF β-CYCLODEXTRIN INCLUSION TECHNIQUE IN NEW DOSAGE FROM OF GARLIC ESSENTIAL OIL

采用电动搅拌法、高速组织捣碎机法和超声波法制备了大蒜精油-β-CYD包合物,运用正交设计法优选出制备包合物的最佳工艺条件为:大蒜精油:β-CYD=1:11.7(g/g),温度20±2℃。UV,IR,粉末X-射线衍射图谱表明包合前后光谱性质和X-射线衍射图谱均发生改变。 包合物小鼠灌胃给药的LD_(50)。为1280mg/kg,比未包合大蒜精油毒性明显降低。对实验性高脂血症大鼠的降脂实验表明,包合物能明显降低血清中TC、TG含量,提高HDL-C含量。也可降低肝脏中TC、TG含量而不影响大鼠肝重。

In order to reduce the pungent odour, increase patient accepta-bility, a new dosage form of garlic essential oil was developed by β-cyclodextrin (β-OYD) inclusion technique. Three methods, stirring, high-speed tissue homogenizer and ultrasonic vibration were used and the optimum conditions for preparation were set up by orthogonal tests. The ratio of garlic oil to β-CYD being 1:11.7 (W/W) when temperature being kept at 20 ± 2℃, The UV, IR spectra and powder X-ray diffraction pattern of physical mixture and inclusion compound were different, suggesting the formation of inclusion compound. The acute LD50 of ig inclusion, compound in mice was 1 280 mg/kg, significantly lower than that of raw garlic oil (600mg/kg). Suspensions of the inclusion compound at dose of 20mg·kg-1 (calculated as garlic oil) daily ig were given to rats of experimental hyperlipidemia. The results showed that inclusion compound could significantly decrease the serum level of TC, TC, increase the level of HDL-C. At the same time, both liver TO and TG could decrease significantly without influence the weight of liver.