鱼腥草挥发油HPCD包合物肠用温敏凝胶的制备  

Preparation of thermosensitive intestinal gels of Houttuynia cordata volatile oils HPCD inclusion compound

作　　者：张壮丽[1] 赵晓丹 王纪芬 赵志鸿[1] 张小俊[1] 王桂芳[1] ZHANG Zhuang-li;ZHAO Xiao-dan;WANG Ji-fen;ZHAO Zhi-hong;ZHANG Xiao-jun;WANG Gui-fang(Institute of Medical and Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450052, China;College of Pharmaceutical Sciences,Zhengzhou University, Zhengzhou 450001, China)

机构地区：[1]河南省(郑州大学)医药科学研究院,河南郑州450052 [2]郑州大学药物研究院,河南郑州450001

出　　处：《中成药》2018年第5期1060-1064,共5页Chinese Traditional Patent Medicine

基　　金：河南省高等学校重点科研项目资助计划(18A360005);河南省医药科学研究院基本业务费科研项目(YYYJK201710)

摘　　要：目的制备鱼腥草挥发油羟丙基-β-环糊精(HPCD)包合物肠用温敏凝胶。方法冷溶法制备凝胶,以泊洛沙姆407、泊洛沙姆188用量为影响因素,相变温度为评价指标,星点设计-效应面法优化处方。以甲基正壬酮为指标成分,无膜溶出法和透析袋法分别考察凝胶溶出率与体外释放率,再通过高温(40、60℃)、低温(4℃)、强光[(4 500±500)lx]、加速(3个月)试验评价其稳定性。结果最佳条件为P407用量20.61%,P188用量3.03%,相变温度36.5℃。在30~150 min时,HPCD包合物凝胶累积溶出率高于挥发油凝胶,在150~210 min时趋于一致,但前者累积释放率(0~50 h)一直高于后者。所得凝胶在低温下稳定性良好;高温、强光、加速下其外观、性状(高温除外)、p H均较稳定,但甲基正壬酮含有量明显降低。结论鱼腥草挥发油HPCD包合物肠用温敏凝胶应在低温(4℃)下保存。AIM To prepare the thermosensitive intestinal gels of Houttuynia cordata Thunb volatile oils hydroxypropyl-β-cyclodextrin（ HPCD） inclusion compound. METHODS For the gels prepared by cold dissolving method,poloxamer 407 consumption and poloxamer 188 consumption were taken as influencing factors,together with phase transition temperature as an evaluation index,central composite design-response surface method was applied to optimizing the formulation. With 2-undecanone as an index component,the gels＇ dissolution rate and in vitro release rate were investigated by non-membrane dissolution method and dialysis bag method respectively,whose stability was then evaluated by high temperature（ 40,60 ℃）,low temperature（ 4 ℃）,strong light[（4 500 ± 500） lx]and acceleration（three months） tests. RESULTS The optimal conditions were determined to be 20. 61% for P407 consumption and 3. 03% for P188 consumption,the phase transition temperature was36. 5 ℃. Within the time range of 30-150 min,the HPCD inclusion compound gels exhibited higher accumulative dissolution rate than the volatile oils gels,which tended to be consistent in 150-210 min,but the former exhibited higher accmulative release rate（0-50 h） than the latter all the time. The obtained gels showed good stability at low temperature,whose appearance,characteristic（ except for high temperature） and p H were stable at high temperature,strong light and acceleration with obviously decreased 2-undecanone content. CONCLUSION The thermosensitive intestinal gels of Houttuynia cordata Thunb volatile oils HPCD inclusion compound should be stored at low temperature（4 ℃）.

关 键 词：鱼腥草挥发油 HPCD包合物 肠用温敏凝胶 甲基正壬酮 星点设计-效应面法 冷溶法 

分 类 号：R944[医药卫生—药剂学]