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第 36 卷第 6 期 精 细 化 工 Vol.36, No.6
201 9 年 6 月 FINE CHEMICALS June 2019

医药与日化原料
甲氨蝶呤插层 MgAl-LDH 复合物的制备与释药性能

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梁 良 ，任 锦 ，徐常青 ，代 军 ，李东霖
（1. 九江学院 分析测试中心，江西 九江 332005；2. 九江学院 药学与生命科学学院，江西 九江 332005）
摘要：以 Mg(NO 3 ) 2 ·6H 2 O 和 Al(NO 3 ) 3 ·9H 2 O 为主要原料，采用共沉淀联合水热合成法制备了甲氨蝶呤插层镁铝
层状双氢氧化物复合物（MTX-LDH），通过正交实验分析了主要工艺条件对 MTX-LDH 复合物载药率、粒径及
其分散性的影响。结果表明：当反应温度为 60 ℃、Mg(NO 3 ) 2 ·6H 2 O 和 Al(NO 3 ) 3 ·9H 2 O 的投入量分别为 2.67 和
1.33 mmol、MTX 和聚乙二醇 400 加入量分别为 0.20 mmol 和 15 mL 时，复合产物单分散性良好，粒径均值为
175.6 nm，载药率达 18.90%。利用 FTIR、XRD、TG 以及 TEM 对样品结构、热力学性质和微观形貌进行了测
定。重点考察了 MTX-LDH 复合物在不同 pH 缓冲溶液中的释药性能，表明其具备 pH 响应型释放特性，在 pH=5.8
的弱酸环境中缓释效果良好，12 h 累积释药率为 93.7%，并通过热力学释药模型确定其缓释机理为层板溶蚀与
置换扩散并存的缓释机制。
关键词：层状双氢氧化物；甲氨蝶呤；粒径；载药率；缓释性能；医药原料
中图分类号：O614; TB33 文献标识码：A 文章编号：1003-5214 (2019) 06-1166-07

Preparation and Release Properties of Methotrexate
Intercalated MgAl-LDH Composites

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LIANG Liang , REN Jin , XU Chang-qing , DAI Jun , LI Dong-lin
（1. Analytical and Testing Center, Jiujiang University, Jiujiang 332005, Jiangxi, China; 2. School of Pharmacy and
Life Sciences, Jiujiang University, Jiujiang 332005, Jiangxi, China）
Abstract: Methotrexate intercalated Mg-Al layered double hydroxide composites (MTX-LDH) were
prepared via combination of coprecipitation and hydrothermal synthesis by using Mg(NO 3) 2·6H 2O and
Al(NO 3) 3·9H 2O as main materials. The effects of main technological conditions on the drug loading rate,
particle size and particle size dispersion of MTX-LDH were analyzed by orthogonal experiments. The
results showed that the composites had good monodispersity with an average particle size of 175.6 nm, and
exhibited high drug loading rate of 18.90% when the reaction temperature was 60 ℃, and the amount of
Mg(NO 3 ) 2 ·6H 2 O, Al(NO 3 ) 3 ·9H 2 O, MTX and polyethylene glycol 400 were 2.67 mmol, 1.33 mmol, 0.20 mmol
and 15 mL, respectively. The structure, thermodynamic properties and micro-morphology of the samples
were studied by FTIR, XRD, TG and TEM. The release properties of MTX-LDH particles in different pH
buffer solutions were investigated. The results indicated that the composites had pH-responsive release
characteristics and good sustained release properties in weak acid environment (pH=5.8), and the
cumulative release rate at 12 h was up to 93.7%. Moreover, the release mechanism of laminate dissolution
coexisting with displacement diffusion was confirmed by the thermodynamic release model.
Key words: layered double hydroxides; methotrexate; particle size; drug loading rate; sustained
release property; drug materials
Foundation items: National Natural Science Foundation of China (81860631), Scientific Research Fund of
Jiangxi Provinical Health Commission (20195633)

收稿日期：2018-11-07; 定用日期：2019-02-21; DOI: 10.13550/j.jxhg.20180820
基金项目：国家自然科学基金项目（81860631）；江西省卫健委科研项目（20195633）
作者简介：梁 良（1986—），男，硕士，实验师，E-mail：liangliangrj@126.com。联系人：任 锦（1986—），女，博士，讲师，E-mail：
yanjiushengrj@126.com。