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吴茱萸碱磷脂复合物自乳化药物递送系统的制备、表征及胃黏膜
渗透性研究 Δ
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宋朔尧 1，2＊ ，杨贵前 ，陶 玲 ，沈祥春 ，张 环 ，李和蓉 ，王守莉 ，石惠云 ，刘 文 （1.贵州医科大学
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药学院，贵阳 550025；2.贵州省天然药物资源优效利用重点实验室，贵阳 550025）
中图分类号 R944 文献标志码 A 文章编号 1001-0408（2022）09-1056-06
DOI 10.6039/j.issn.1001-0408.2022.09.06
摘 要 目的 制备吴茱萸碱磷脂复合物自乳化药物递送系统（EVO-PC-SMEDDS），并对其进行表征及胃黏膜渗透性考察。方法
制备EVO-PC-SMEDDS，检测其粒径、多分散系数（PDI）和Zeta电位，并进行显微观察。考察该制剂在不同pH（1.2、2.0、4.0、7.0）模
拟胃液中的稳定性。测定该制剂的包封率和载药量，并进行体外释放考察。将大鼠胃黏膜组织和尤斯灌流室技术相结合，考察该
制剂的胃黏膜渗透性。结果 EVO-PC-SMEDDS 的粒径为（53.63±1.51）nm、PDI 为 0.217±0.017、Zeta 电位为（－12.20±0.15）
mV、包封率为（95.25±0.97）％、载药量为（19.30±1.21）mg/g。在透射电子显微镜下，EVO-PC-SMEDDS呈大小均匀的类球形乳
滴。稳定性实验结果显示，EVO-PC-SMEDDS在不同pH的模拟胃液中，粒径、PDI、Zeta电位均无明显变化，稳定性良好。体外释
放实验结果显示，与吴茱萸碱（EVO）原料药比较，EVO-PC-SMEDDS 的体外累积释放率提高了 6.83 倍，符合一级动力学释放模
型。胃黏膜渗透性实验结果显示，EVO-PC-SMEDDS的累积渗透转运量、渗透速率、渗透通量及累积渗透曲线下面积均高于EVO
原料药。结论 本研究成功制得EVO-PC-SMEDDS，且该制剂稳定性良好，可明显改善EVO的体外释放行为和胃黏膜渗透性。
关键词 自乳化药物递送系统；吴茱萸碱；表征；胃黏膜；释放
Preparation，characterization and gastric mucosal permeability of evodiamine phospholipid complex self-
microemulsifying drug delivery system
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SONG Shuoyao ，YANG Guiqian ，TAO Ling ，SHEN Xiangchun ，ZHANG Huan ，LI Herong ，WANG
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Shouli ，SHI Huiyun ，LIU Wen（1. School of Pharmacy，Guizhou Medical University，Guiyang 550025，China；
2. Guizhou Province Key Laboratory for Optimal Utilization of Natural Medicine Resources，Guiyang 550025，
China）
ABSTRACT OBJECTIVE To prepare and characterize evodiamine phospholipid complex self-microemulsifying drug delivery
system（EVO-PC-SMEDDS），and to investigate its gastric mucosal permeability. METHODS EVO-PC-SMEDDS was prepared，
and particle size，polydispersity（PDI）and Zeta potential were tested，and microscopic observation was carried out. The stability of
EVO-PC-SMEDDS in simulated gastric liquid with different pH（1.2，2.0，4.0，7.0）was investigated. The entrapment efficiency
and drug-loading amount of the preparation were determined，and the in vitro release was investigated. The gastric mucosal
permeability of EVO-PC-SMEDDS was studied by combining rat gastric mucosal tissue and Ussing Chamber technology.
RESULTS The particle size of EVO-PC-SMEDDS was （53.63 ± 1.51） nm，PDI and Zeta potential were 0.217 ± 0.017 and
（－12.20±0.15）mV，entrapment efficiency was（95.25±0.97）％ and drug-loading amount was（19.30±1.21）mg/g. EVO-PC-
SMEDDS exhibited a uniformly dispersed round spherical shape under transmission electron microscope. Stability experiments
showed that EVO-PC-SMEDDS exhibited no significant change in particle size，PDI and Zeta potential under the simulated gastric
fluid with different pH and showed excellent stability. Results of in vitro release test showed that compared with evodiamine
（EVO），in vitro accumulative release of EVO-PC-SMEDDS were enhanced 6.83-fold，which was in line with the first-order kinetic
release model. Results of gastric mucosal permeability showed that gastric mucosal permeation transport，permeation rate，
permeation flux and area under curve of cumulative permeability of EVO-PC-SMEDDS were higher than those of EVO，
respectively. CONCLUSIONS EVO-PC-SMEDDS is prepared
Δ 基 金 项 目：国 家 自 然 科 学 基 金 资 助 项 目（No.82060704，
No.81860706，No.81660666）；贵州省科技计划项目（No.黔科合基础 successfully and shows good stability. It could significantly
〔2018〕1016号，No.黔科合基础〔2019〕1024号） improve the release behavior and gastric mucosal permeability
＊硕士研究生。研究方向：药物新剂型与新技术。E-mail： of EVO.
15951083991@163.com KEYWORDS self-microemulsifying drug delivery system；
# 通信作者：教授，博士生导师。研究方向：药物新剂型与新技 evodiamine；characterization；gastric mucosal；release
术。电话：0851-86823742。E-mail：642771631@qq.com
·1056 · China Pharmacy 2022 Vol. 33 No. 9 中国药房 2022年第33卷第9期
