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槲皮素纳米混悬剂的制备及其性能研究
  • ISSN号:1674-5515
  • 期刊名称:《现代药物与临床》
  • 时间:0
  • 分类:R944[医药卫生—药剂学;医药卫生—药学]
  • 作者机构:[1]黑龙江中医药大学药学院,黑龙江哈尔滨150040, [2]中国医学科学院药用植物研究所,北京100193
  • 相关基金:国家国际科技合作专项(2008DFA31070);黑龙江中医药大学重点实验室开放课题(2013kf04)
中文摘要:

目的:制备高载药量、小粒径的槲皮素纳米混悬剂,并进行性质考察。方法采用纳米沉淀–高压均质法制备,以粒径分布、药载比、稳定性为指标对处方和工艺进行优化,并对最优处方进行体外性质考察。结果以超声注入联合高压均质法制备,最佳处方为TPGS为稳定剂、DMF为有机试剂,药载比为5∶1;最佳工艺条件为低温10℃超声、200 MPa、循环5次。制备得到的槲皮素纳米混悬剂粒径为(173.21±0.90) nm,电位为(?19.02±0.15) mV,载药量为(80.40±1.44)%,包封率为(96.41±1.72)%。药物在纳米粒中以结晶状态存在,能够体外缓释36 h。结论利用TPGS可制备高载药量、小粒径的槲皮素纳米混悬剂,其体外具有明显缓释作用,解决了槲皮素水溶性差的难题,具有较好的应用前景。

英文摘要:

Objective To prepare Quercetin Nanosuspensions with high drug-loading capacity and small particle size, and study their behaviors in vitro.Methods Quercetin Nanosuspensions were prepared using nano-precipitation and high-pressure homogenization method. The formulation and preparation process were optimized using particle size distribution, drug loading capacity, and stability of samples as evaluating indicators, and then the propertiesin vitro of optimal sample were studied.Results Ultrasonic injection and high-pressure homogenization was selected as optimal method. The optimal prescription included using TPGS as the stabilizer with the drug-stabilizer ratio of 5:1, DMF as the organic reagent. The optimal preparation was as following: ultrasonic processing was under 10℃, the homogenization pressure was 200 MPa, and cycles were 5 times. The prepared Quercetin Nanosuspensions had average diameter (173.21 ± 0.90) nm and Zeta potential (?19.02 ± 0.15) mV. Drug-loading content was calculated to be (80.40±1.44) % and the entrapment efficiency was determined to be (96.41±1.72)%. Quercetin was in the same form of crystalline in Quercetin Nanosuspensions as in the bulk quercetin. Quercetin could release in a sustained release manner during 36 h.Conclusion Using the polymer TPGS, Quercetin Nanosuspensions with high drug-loading and small size sustained released are prepared, and it has obviously in vitrosustained released effect, which dissolves poor water solubility of quercetin, and has good prospect of application.

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期刊信息
  • 《现代药物与临床》
  • 中国科技核心期刊
  • 主管单位:天津市委
  • 主办单位:天津药物研究院 中国药学会
  • 主编:邹美香
  • 地址:天津市鞍山西道308号
  • 邮编:300193
  • 邮箱:dc@tipress.com
  • 电话:022-23006823
  • 国际标准刊号:ISSN:1674-5515
  • 国内统一刊号:ISSN:12-1407/R
  • 邮发代号:
  • 获奖情况:
  • 国内外数据库收录:
  • 美国化学文摘(网络版),英国农业与生物科学研究中心文摘,波兰哥白尼索引,美国剑桥科学文摘,中国中国科技核心期刊
  • 被引量:6060