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[β-环糊精与羟丙基-β-环糊精对薄荷醇包合行为的差异]

[Difference in inclusion behavior of β-cyclodextrin and hydroxypropyl-β-cyclodextrin with menthol].

作者信息

Wan Guang-Wen, Xie Hui, Mao Chun-Qin, Tang Run-Qu, Yao Chao, Wang Zhuo

机构信息

School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.

School of Pharmacy, Guangxi University of Chinese Medicine, Nanning 530200, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2016 Sep;41(18):3336-3341. doi: 10.4268/cjcmm20161805.

Abstract

Volatile oils are important active components in traditional Chinese medicine, but their components are complicated and unstable. It is common to use cyclodextrin inclusion technique to improve the stability of volatile oils and make them easier to be prepared. At present, β-cyclodextrin (β-CD) is the most common inclusion material. The evaluation indicators for inclusion technique usually contain the inclusion rate and the oil content in the inclusion compound. However, the articles about the study on selecting inclusion materials for volatile oils were few. In this paper, menthol, the main active ingredient of mint volatile oil, was used as model drug, while β-CD and hydroxypropyl-β-cyclodextrin (HP-β-CD) were used as the inclusion materials. Inclusion equilibrium constant (K), solubilization ratio were investigated, and the results were combined with IR, DSC and TG to verify the formation of inclusion complexes. It turned out that in the range of 0-15 mmol•L⁻¹, the solubility of menthol was increased linearly with the increase of HP-β-CD concentration, with AL-type phase solubility diagram, K=3 188.62 L•mol⁻¹; in the range of 0-12.5 mmol•L⁻¹, the solubility of menthol was increased linearly with the increase of β-CD concentration, K=818.73 L•mol⁻¹. When the concentration was over 12.5 mmol•L⁻¹, the solubility of menthol appeared to be a negative deviation with the increase of β-CD concentration, with AN-type solubility diagram. The above results showed that the inclusion behavior was different between β-CD and HP-β-CD, laying a foundation for further study on inclusion complexes of volatile oil.

摘要

挥发油是中药中的重要活性成分,但其成分复杂且不稳定。采用环糊精包合技术提高挥发油的稳定性并使其更易于制剂化较为常见。目前,β-环糊精(β-CD)是最常用的包合材料。包合技术的评价指标通常包括包合率和包合物中的含油率。然而,关于挥发油包合材料选择的研究报道较少。本文以薄荷挥发油的主要活性成分薄荷醇为模型药物,以β-CD和羟丙基-β-环糊精(HP-β-CD)为包合材料,考察了包合平衡常数(K)、增溶倍数,并结合红外光谱(IR)、差示扫描量热法(DSC)和热重分析法(TG)对包合物的形成进行验证。结果表明,在0~15 mmol•L⁻¹范围内,薄荷醇的溶解度随HP-β-CD浓度的增加呈线性增加,呈AL型相溶解度图,K=3 188.62 L•mol⁻¹;在0~12.5 mmol•L⁻¹范围内,薄荷醇的溶解度随β-CD浓度的增加呈线性增加,K=818.73 L•mol⁻¹。当浓度超过12.5 mmol•L⁻¹时,薄荷醇的溶解度随β-CD浓度的增加出现负偏差,呈AN型溶解度图。上述结果表明β-CD与HP-β-CD的包合行为存在差异,为进一步研究挥发油包合物奠定了基础。

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