Crystalline inclusion complexes formed between the drug diflunisal and block copolymers
Crystalline inclusion complexes formed between the drug diflunisal and block copolymers
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药物二氟尼柳和嵌段共聚物之间形成的结晶包合物
DOI：
10.1016/j.cclet.2017.04.001
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发表时间：
2017-06
影响因子：
9.1
通讯作者：
Xu Jun
中科院分区：
文献类型：
--
作者：
Zhong Zhi;Yang Xiaotong;Fu Xiao-Bin;Yao Ye-Feng;Guo Bao-Hua;Huang Yanbin;Xu Jun
药物的固体形式在优化药物的物理化学性质方面起着核心作用，新的固体形式将提供更多的选择来实现药物的理想药学特征。最近，已经发现某些药物与多种类型的线性聚合物形成结晶包合物（IC），代表药物固体的一个新的子类别。本研究以二氟尼柳（DIF）为模型药物主体，将药物/聚合物IC的客体从均聚物扩展到聚乙二醇（PEG）和聚己内酯（PCL）的嵌段共聚物。客体共聚物中嵌段长度对DIF IC的形成、热稳定性和溶解行为有显著影响。虽然PEG嵌段几乎不能单独包含，但当PCL嵌段足够长时，它确实可以包含在DIF IC中。PCL嵌段长度的增加产生具有改善的热稳定性的IC晶体。DIF/嵌段共聚物IC的溶出曲线表现出随着PCL嵌段长度的增加而逐渐降低的水溶解度和溶出速率。这些结果证明了使用药物/聚合物IC以可预测和可控制的方式调节药物的所需药物特性的可能性。
The solid form of drugs plays a central role in optimizing the physicochemical properties of drugs, and new solid forms will provide more options to achieve the desirable pharmaceutical profiles of drugs. Recently, certain drugs have been found to form crystalline inclusion complexes (ICs) with multiple types of linear polymers, representing a new subcategory of pharmaceutical solids. In this study, we used diflunisal (DIF) as the model drug host and extended the guest of drug/polymer ICs from homopolymers to block copolymers of poly(ethylene glycol) (PEG) and poly(ε-caprolactone) (PCL). The block length in the guest copolymers showed a significant influence on the formation, thermal stability and dissolution behavior of the DIF ICs. Though the PEG block could hardly be included alone, it could indeed be included in the DIF ICs when the PCL block was long enough. The increase of the PCL block length produced IC crystals with improved thermal stability. The dissolution profiles of DIF/block copolymer ICs exhibited gradually decreased aqueous solubility and dissolution rate with the increasing PCL block length. These results demonstrate the possibility of using drug/polymer ICs to modulate the desired pharmaceutical profiles of drugs in a predictable and controllable manner.
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药物分子二氟尼柳与多种线型聚合物形成结晶包合物
影响因子：
3.8
作者：
Zhong Zhi;Guo Canxiong;Yang Xiaotong;Guo Baohua;Xu Jun;Huang Yanbin
通讯作者：
Huang Yanbin
影响因子：
5.5
作者：
N. Vasanthan;I. D. Shin;Lei Huang;S. Nojima;A. Tonelli
通讯作者：
N. Vasanthan;I. D. Shin;Lei Huang;S. Nojima;A. Tonelli
PEG分子量对灰黄霉素-PEG结晶包合物热稳定性和溶解行为的影响
影响因子：
5.8
作者：
Yang, Xiaotong;Zhong, Zhi;Huang, Yanbin
通讯作者：
Huang, Yanbin
影响因子：
3.8
作者：
Schultheiss, Nate;Newman, Ann
通讯作者：
Newman, Ann
影响因子：
120.1
作者：
Gardner, CR;Walsh, CT;Almarsson, Ö
通讯作者：
Almarsson, Ö