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作者

Bi, Yanping Xiao, Deli Ren, Shuai Bi, Shuyan Wang, Jianzhu Li, Fei

作者单位

Graduate School, Taishan Medical University, No. 619, Changcheng Road, Tai’an 271016, People’s Republic of China School of Pharmaceutical Sciences, Taishan Medical University, No. 619, Changcheng Road, Tai’an 271016, People’s Republic of China Key Laboratory of Drug Quality Control and Pharmacovigilance, Ministry of Education, China Pharmaceutical University, Nanjing 210009, People’s Republic of China Department of Ultrasound, Zibo Hospital of PKU Healthcare Industry Group, No. 2, Xishanwu Street, Zibo 255069, People’s Republic of China

刊名

Journal of Pharmaceutical Sciences

年份

2017

卷号

Vol.106 No.10

页码

3150-3155

ISSN

0022-3549

关键词

amorphous cocrystals dissolution rate microspheres nanotechnology porosity silica

摘要

Coamorphous systems have gained success in stabilizing amorphous drugs and improving their solubility and dissolution. Here we proposed to confine a binary mixture of drug and coformer within nanopores to obtain a nanoconfined coamorphous system. For proving feasibility of this proposal, a poorly water-soluble drug and a frequently used pharmaceutical CF were loaded into nanopores of mesoporous silica microspheres. The solid state of NCA system was characterized by differential scanning calo...更多

Coamorphous systems have gained success in stabilizing amorphous drugs and improving their solubility and dissolution. Here we proposed to confine a binary mixture of drug and coformer within nanopores to obtain a nanoconfined coamorphous system. For proving feasibility of this proposal, a poorly water-soluble drug and a frequently used pharmaceutical CF were loaded into nanopores of mesoporous silica microspheres. The solid state of NCA system was characterized by differential scanning calorimetry, X-ray powder diffraction, infrared spectrum, and solid-state nuclear magnetic resonance. With large numbers of nanopores, mesoporous silica microspheres appear to be a feasible carrier to transform a cocrystal system into coamorphism by nanoscale confinement. Benefiting from both nanoscale confinement and CF, the NCA system of ibuprofen achieved synchronic increase in dissolution properties and physical stability. Consequently, the NCA strategy is effective in achieving coamorphous state and offers a promising alternative for formulating poorly water-soluble drugs.收起

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