肉桂挥发油β-环糊精包合物制备工艺优选

目的:优选肉桂挥发油β-环糊精(β-CD)包合物制备的最佳工艺条件,并考察促渗剂对药物渗透速率的影响。方法:按L_9(3~4)正交试验表进行试验,对影响饱和溶液的3个因素进行考察,以稳态透皮速率作为评价指标,优选处方组成。以SD♂大鼠皮肤为媒介,Franz单室扩散池为体外模型,用HPLC法测定透过皮肤的药物含量。结果:最佳包合工艺条件为挥发油:β-CD=1:5(mL:g),包合温度为50℃,搅拌2h。加入促渗剂二甲基亚砜、1,2-丙二醇后的增渗倍数分别为1.38、1.65倍。结论:本包合工艺简单、方便、实用,达到了改变肉桂挥发油剂型的目的。β-CD包合物有望成为肉桂新的经皮给药系统。

Optimizing the Inclusion Technology of Cinnamon Volatile Oil-β-cyclodextrin Inclusion Complex

OBJECTIVE:To optimize the inclusion technology of cinnamon volatile oii-β-cyclodextrin inclusion complex and to investigate the effects of the type of penetration enhancer on the permeation rate of inclusion compounds.METHODS: The experiment was carried out in accordance with L_9(3~4)orthogonal design table;the 3 factors affecting saturated solucion were investigated,and the formula was optimized with steady transdermal permeation rate as evaluation index.With the skin of SD male rat as media,the penetration experiments in vitro were performed on modified Franz diffusion cells.The amount of drug penetration concentration of inclusion compound was determined by HPLC.RESULTS:The optimized inclusion condi- tion was as follows:cinnamon oil:β-cyciodextrin=1:5(mL:g),stirring for 2 hour at 50℃;after addition of the penetration enhancers-DMSO and 1,2-trimethylene glycol,the enhancement ratios were 1.38 and 1.65 respectively(in ,some cases,the penetration rate was decreased).CONCLUSION:The inclusion technology is simple,convenient and practical,and by which transformation of dosage form of cinnamon volatile oil was achieved.β-CD inclusion compound is expected to become a new transdermal cinnamon delivery system.