目的 采用星点设计-响应面法优选细梗香草总皂苷自微乳处方。方法 在溶解度考察、配伍试验与三元相图绘制的基础上,以乳化时间、平均粒径及Zeta电位为评价指标,采用星点设计-响应面法筛选细梗香草总皂苷自微乳的最佳处方,并对细梗香草总皂苷自微乳的理化性质进行考察。结果 细梗香草总皂苷自微乳最佳处方为油酸乙酯-Kolliphor RH40-Transcutol=12.93∶57.25∶29.82,其平均粒径、多分散指数、Zeta电位、载药量分别为23.0 nm、0.160、-20.28 mV、10.52 mg·g-1。结论 星点设计-响应面法所建数学模型预测性好,可用于优化细梗香草总皂苷自微乳。
Abstract
OBJECTIVE To optimize the formulation of self-microemulsion containing total saponins from Lysimachia capillipes by central composite design-response surface methodology. METHODS Based on the study of solubility, compatibility test and ternary phase diagram, central composite design-response surface methodology was adopted to optimize the best prescription with the emulsifying time, particle size, and Zeta pontential as indexes, physicochemical properties of this self-microemulsion were also determined. RESULTS Optimum formulation was 12.93% of ethyl oleate, 57.25% of Kolliphor RH40, 29.82% of Transcutol. The a verage particle size, polydispersity index, Zeta pontential and drug loading of self-microemulsion containing total saponins from Lysimachia capillipes were 23.0 nm,0.160,-20.28 mV and 10.52 mg·g-1.CONCLUSION With good predictability, this METHODS can be used for the formulation optimization of self-microemulsion loaded total saponins from Lysimachia capillipes.
关键词
总皂苷 /
细梗香草 /
自微乳 /
配伍实验 /
三元相图 /
星点设计-响应面法
{{custom_keyword}} /
Key words
total saponin /
Lysimachia capillipes /
self-microemulsion /
compatibility test /
ternary phase diagram /
central composite design-response surface methodology
{{custom_keyword}} /
中图分类号：
R944
{{custom_clc.code}}
({{custom_clc.text}})
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
参考文献
[1] Editorial board of National Chinese Medicine Administration《Chinese Materia Medica》. Chinese Materia Medica(中华本草)[M]. Shanghai:Shanghai Science and Technology Press,1999:53-56.
[2] XU Y, RONG Y M, LIU X B. Studies on the antitumor activity of the total saponins of Lysimachia capillipes [J]. Chin Pharmacol Bull(中国药理学通报),2012,28(4):545-549.
[3] FEI Z H, CHEN Y L, MA S L, et al. Capillipes inhibits proliferation and induces apoptosis of human lung cancer H460 cells [J]. Zhejiang Med J(浙江医学),2014,36(9):742-746.
[4] CHENG Z Z. The metabolism and pharmacokinetics of capilliposide B and capilliposide C in Lysimachia capillipes Hemsl extract[D]. Huazhong University Science Technol, 2015.
[5] ZHOU W, LI X F, XIANG Z Y, et al. Combined application of self micro-emulsifying drug delivery system and liquidsolid compact technique in insoluble traditional Chinese medicine formulaticn [J]. Pharm Clin Chin Mater Med(中药与临床), 2016,7(2):87-89.
[6] DOKANIA S,JOSHI A K.Self-microemulsifying drug delivery system (SMEDDS)--challenges and road ahead[J].Drug Deliv,2015,22(6):675-690.
[7] SUN D D, XU X G, SHENG L S, et al. Optimization of self-microemulsion drug delivery system of ursolic acid by central composite design/response surface methodology [J]. China J Exp Tradit Med Form(中国实验方剂学杂志),2013,19(8):46-50.
[8] YANG P F,DING L P,CAI X L, et al. Optimization of prescription and evaluation of quality and security of ginkgolide B self-microemulsifying drug delivery system[J].China J Exp Tradit Med Form(中国实验方剂学杂志), 2013,19(12):26-33.
[9] WANG Z J, HU R F, WANG G K, et al. Optimization of self-microemulsifying drug delivery system of naringenin by Box-Behnken design and response surface method[J].Chin Tradit Herb Drugs(中草药), 2014,45(17):2461-2466.
[10] LEVIN V A, DOLGINOW D, LANDAHL H D, et al. Relationship of octanol/water partition coefficient and molecular weight to cellular permeability and partitioning in s49 lymphoma cells[J]. Pharm Res, 1984, 1(6):259-266.
[11] PAN X, XIE Q Q, LI H C. Simultaneous determination of three flavonoids in Fructus Ponciri Trifoliatae Immaturi by HPLC [J]. Chin J Pharm Anal(药物分析杂志),2015,35(4):666-669.
[12] ZHONG L Q, HE C L, MIAO X D, et al. Simultaneous determination of isofraxidin, rosmarinic acid and chlorogenic acid in Shenghong Qingyan Buccal tablets by HPLC [J]. Strait Pharm J(海峡药学),2016,28(10):48-51.
[13] GU J, LI H, QIN K M, et al. Determination of the equilibrium solubility and apparent oil/water partition coefficients of liquiritigenin using HPLC [J]. Chin J Pharm Anal(药物分析杂志), 2013, 63(8):1293-1297.
{{custom_fnGroup.title_cn}}
脚注
{{custom_fn.content}}
基金
福建省引导性项目资助(2015Y0066)
{{custom_fund}}
PDF(2188 KB)
