摘要
制备刺五加总苷微乳,优化其处方和制备工艺并进行质量评价,通过在体单向肠灌流模型考察自微乳给药系统对刺五加总苷的吸收特性。以伪三元相图面积大小为考察指标,对油相、质量比(K_(m))、转数、药物浓度进行单因素考察,利用D-最优混料设计法以粒径为考察指标进行工艺优化,并对外观、形态、粒径等进行考察,以刺五加苷B、刺五加苷E为指标,测定其在微乳中的质量浓度。结果表明,刺五加总苷微乳的最优处方为水相20.8%,棕榈酸异丙酯31.2%,大豆磷脂与无水乙醇(K_(m)=1∶1)为48.0%。通过透射电镜观察其形态呈圆整的球状乳滴,分散均匀,微乳类型为油包水型。室温下,pH为5.19,折光率为1.4165,平均粒径(26.47±0.04)nm,多分散性指数(PDI)0.118±0.03,刺五加苷B、刺五加苷E的质量分数分别为0.0389、0.1664 mg·mL^(-1)。初步稳定性研究表明,30 d内溶液澄清透明,不分层,含量基本无变化,稳定性良好。与刺五加总苷相比,制备成微乳后在各肠段的吸收均显著提高,在回肠吸收效果最好,为刺五加进一步开发和利用奠定基础。
Following the preparation of Acanthopanax senticosus total saponins microemulsion,the formulation and preparation technology were optimized and the quality was evaluated.The absorption characteristics of A.senticosus total saponins microemulsion by the self-microemulsifying drug delivery system(SMEDDS)were investigated in the unidirectional intestinal perfusion model in vivo.The oil phase,mass ratio(K_(m)),number of revolutions,and drug concentration were subjected to single-factor investigation with the area of pseudo-ternary phase diagram as the index.The process was optimized by D-optimal mixture design with the particle size as the index,and then the appearance,morphology,and particle size were investigated.The mass concentrations of eleutherosides B and E in the microemulsion were determined.The results showed that the optimum formulation of A.senticosus total saponins microemulsion was determined as follows:20.8%of water phase,31.2%of isopropyl palmitate,and 48.0%of soybean phospholipid and absolute ethanol(K_(m)=1∶1).As revealed by the observation under a transmission electron microscope,the microemulsion exhibited homogeneous dispersion and was a spherical emulsion droplet in the water-in-oil type.At room temperature,the pH value was 5.19,the refractive index 1.4165,the average particle size(26.47±0.04)nm,and the polydispersity index(PDI)0.118±0.03.The content of the eleutherosides B and E was 0.0389 and 0.1664 mg·mL^(-1),respectively.The preliminary stability study showed that the solution was clear and transparent within 30 d,without stratification or content change,indicating good stability.The absorption of microemulsion in each intestinal segment was significantly improved as compared with that of the A.senticosus total saponins,with the best absorption effect detected in the ileum,which has laid a foundation for further development and utilization of A.senticosus.
作者
张宇航
高寒
徐伟
邱智东
贾艾玲
ZHANG Yu-hang;GAO Han;XU Wei;QIU Zhi-dong;JIA Ai-ling(Key Laboratory of Traditional Chinese Medicine Active Ingredients of Ministry of Education,School of Pharmaceutical Sciences,Changchun University of Chinese Medicine,Changchun 130117,China;State Key Laboratory of Characteristic Chinese Medicine Resources in Southwest China,School of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2022年第12期3233-3241,共9页
China Journal of Chinese Materia Medica
基金
吉林省科技发展计划项目(20200602034ZP)
吉林省教育厅科学技术研究项目(JJKH20210987KJ)。
关键词
刺五加总苷
微乳
伪三元相图
D-最优混料设计
肠吸收
Acanthopanax senticosus total saponins
microemulsion
pseudo-ternary phase diagram
D-optimal mixture design
intestinal absorption
