丹参素异丙酯经鼻吸收的影响因素  

Influencing factors in nasal absorption of isopropyl 3-( 3,4-dihydroxyphenyl )-2-hydroxypropanoate

作　　者：韩姣姣[1] 曲秦 吕卓 王玥月[1] 郑晓晖[1] 张亚军[1] 

机构地区：[1]西北大学生命科学学院,陕西西安710069 [2]陕西新药技术研究开发中心,陕西西安710075 [3]陕西省食品药品检验所,陕西西安710065

出　　处：《中成药》2015年第1期74-78,共5页Chinese Traditional Patent Medicine

基　　金：陕西省科技统筹创新工程计划(2013KTCQ03-15);陕西省教育厅科学研究计划(2013JK0812)

摘　　要：目的探究丹参素异丙酯的经鼻吸收特性及影响因素。方法采用大鼠鼻腔循环灌流法,考察丹参素异丙酯鼻腔给药的吸收性能,以及溶液p H值、吸收促进剂和P-gp抑制剂对吸收的影响。结果丹参素异丙酯质量浓度在100~1 000μg/m L范围内,鼻黏膜的最大吸收速度常数为5.2×10-3/min;溶液p H对鼻腔吸收速度常数无显著影响;0.50%、1.00%β-环糊精和2.00%泊洛沙姆能显著提高鼻腔吸收（P〈0.05）,0.25%~1.00%去氧胆酸钠和0.50%~2.00%吐温-80对丹参素异丙酯的鼻腔吸收无明显影响;0.10%维拉帕米可提高丹参素异丙酯的鼻腔吸收（P〈0.05）。结论丹参素异丙酯能够透过鼻黏膜吸收;β-环糊精维拉帕米可提高丹参素异丙酯的鼻腔吸收速度常数。AIM To explore the characteristics of isopropyl 3-（ 3,4-dihydroxyphenyl）-2-hydroxypropanoate（ IDHP） for nasal absorption and its influencing factors. METHODS The rat nasal cavity recirculating perfusion method was employed to regulate IDHP nasal absorption. And the influence given to the nasal mucosa for the absorption by p H value,the enhancer and P-gp inhibitors were examined. RESULTS In a concentration range of100-1 000 μg / m L,the largest nasal absorption rate constant of IDHP was 5. 2 × 10-3min-1. The p H value of IDHP solution made no change to the absorption. β-cyclodextrin（ 0. 50% and 1. 00%） and poloxamer（ 2. 00%）markedly improved nasal absorption rate（ P 〈 0. 05）,but sodium deoxycholate（ 0. 25%-1. 00%） and tween-80（ 0. 5%-2. 00%） were unaffected. In addition,0. 10% verapamil increased the constant for absorption rate.CONCLUSION IDHP can be absorbed through the nasal mucosa,and suitable β-cyclodextrin and verapamil can help to increase the constant value for nasal IDHP absorption rate.

关 键 词：鼻腔循环灌流法 丹参素异丙酯 鼻腔吸收速度常数 影响因素 Β-环糊精 维拉帕米 

分 类 号：R969.1[医药卫生—药理学]