阿维菌素/乙基纤维素载药纤维的制备及稳定性分析

doi:10.3969/j.issn.1000-2006.201711016

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南京林业大学学报（自然科学版） ›› 2018, Vol. 61 ›› Issue (06): 186-190.doi: 10.3969/j.issn.1000-2006.201711016

阿维菌素/乙基纤维素载药纤维的制备及稳定性分析

曾健勇¹,于颖颖¹,张方明¹,李大波²,张国财^1*

(1.东北林业大学林学院,黑龙江哈尔滨 150040; 2.红花尔基林业局,内蒙古呼伦贝尔 021112)

出版日期:2018-11-30 发布日期:2018-11-30
基金资助:
收稿日期2017-11-05 修回日期:2018-08-22
基金项目:中央高校基本科研业务费专项项目(2572017AA18); 中央财政林业科技推广示范资金项目(JLT[2016]13); 哈尔滨市应用技术研究与开发项目(2016RAXXJ035); 哈尔滨市科技创新人才项目(2017RALXJ010)
第一作者:曾健勇(zengjianyong123@163.com),博士生。*通信作者:张国财(zhang640308@126.com),教授。

Preparation and stability of avermectin-loaded ethylcellulose

ZENG Jianyong¹, YU Yingying¹, ZHANG Fangming¹, LI Dabo², ZHANG Guocai^1*

(1. School of Forestry, Northeast Forestry University, Harbin 150040, China; 2. Honghuaerji Forestry Bureau of Inner Mongolia, Hulunbeir 021112, China)

Online:2018-11-30 Published:2018-11-30

摘要/Abstract

摘要： 【目的】在农林害虫防治过程中阿维菌素(AVM)因光解性易造成药效损失,为此开发阿维菌素/乙基纤维素(AVM/EC)载药纤维,以制备工艺简单、成本低廉的AVM抗光解剂型。【方法】以乙基纤维素(EC)为载体,甲醇为溶剂,按AVM与EC质量比(m_AVM:m_EC)分别为1:10、1:8、1:6、1:4、1:2,采用溶剂共混-加水析出的方法制备AVM/EC载药纤维,并测定了载药纤维产率、AVM利用率、载药量、光稳定性及热贮稳定性,同时对AVM/EC载药纤维进行X射线衍射(XRD)分析。【结果】通过溶剂共混-加水析出法,可将AVM以无定形状态均匀地负载到EC中; 当m_AVM:m_EC为1:10～1:6时,载药纤维产率大于91. 85%,AVM利用率大于81. 18%,紫外光照射12 h光解率小于15. 80%,(54±2)℃热贮14 d后,89. 14%以上AVM未降解。【结论】通过溶剂共混-加水析出的方法制备AVM/EC载药纤维,可以将AVM以无定形状态均匀负载到EC中,提高AVM光稳定性及热贮稳定性,这可为AVM剂型开发提供新思路。

Abstract: 【Objective】The photolysis of avermectin(AVM)always reduces the effectiveness of its application in agricultural and forest pest control. Here, a simple and economical method was used to improve its photostability.【Method】Ethylcellulose(EC)was employed as the carrier, while methanol was employed as the solvent for this process. AVM and EC were mixed in mass ratios(m_AVM:m_EC)of 1:10, 1:8, 1:6, 1:4, and 1:2 to prepare a series of solutions. Five times the volume of distilled water was then added to the solutions to precipitate the AVM-loaded EC(AVM/EC). The yield, drug-loading rate, photostability, and thermostability of AVM/EC, as well as the utilization rate of AVM, were then determined. Additionally, X-ray diffraction(XRD)analysis was performed to characterize the AVM/EC samples.【Result】The method achieved a shapeless and uniform dispersal of AVM in EC. When the m_AVM:m_EC was increased from 1:10 to 1:6, the AVM/EC yield exceeded 91.85%, while the AVM utilization rate was higher than 81.18%. Additionally, a photodegradation rate of under 15.80% was observed after ultraviolet light exposure for 12 h, and an AVM degradation less than 10.86% was observed. These results were obtained after the AVM/EC was kept at(54 ± 2)℃ for 14 days.【Conclusion】The solvent blending-water addition precipitation method yielded a homogeneous structure of AVM/EC that improved the photostability and thermostability of AVM. Therefore, this method could be a potential approach for the preparation of AVM for incorporation into dosage forms.

中图分类号:

TQ450.6
S763

曾健勇,于颖颖,张方明,等. 阿维菌素/乙基纤维素载药纤维的制备及稳定性分析[J]. 南京林业大学学报（自然科学版）, 2018, 61(06): 186-190.

ZENG Jianyong, YU Yingying, ZHANG Fangming, LI Dabo, ZHANG Guocai. Preparation and stability of avermectin-loaded ethylcellulose[J].Journal of Nanjing Forestry University (Natural Science Edition), 2018, 61(06): 186-190.DOI: 10.3969/j.issn.1000-2006.201711016.

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阿维菌素/乙基纤维素载药纤维的制备及稳定性分析

Preparation and stability of avermectin-loaded ethylcellulose

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