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CRYSTENGCOMM · 2021 ·Vol. 23 ·期 46 ·8027-8032 · IF 3.545

Polymorph control of 5-fluorouracil during a ball milling process

Fenghua Chen,Jie Fan,Xiuzhi Chen,Yanping Li,Chengfeng Liang,Shizhao Ren,Rongrong Xue

Polymorph control of 5-fluorouracil (5-FU) was achieved by ball milling. Form II was synthesized through one-step neat grinding of raw 5-FU (RFU), and Form III (a new polymorph) was obtained by neat grinding RFU twice. Forms II and III of 5-FU were prepared separately through ball milling with different amounts of ethanol as an additive at the same period without influencing each other.

CAS / MDL: 51-21-8

研究领域: 药物化学 · 制药工程

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JOURNAL OF CRYSTAL GROWTH · 2018 · IF 1.742

A new polymorph of fenofibrate prepared by polymer-mediated crystallization

Xiangjun Shi,Yinghua Shao,Xiaoxia Sheng

The polymer-mediated crystallization is an effective means to control the drug crystal. This project was focusing on a new form of Fenofibrate (Form IV) obtained by polymer-mediated crystallization. Medical polymer materials such as Hydroxy Propyl Methyl Cellulose (HPMC), Sodium Carboxyl Methyl Cellulose (CMC-Na) and Polyvinylpyrrolidone (PVP) were tested in this study. The powder X-ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA) and Fourier Transform Infrared Spectroscopy (FTIR) were used to differentiate the new form and other known forms. Material studio was applied to solve structures of Form IV. These polymorphic forms present different physicochemical properties. The crystallization conditions of Form IV were also detected. The study disclosed the Form IV has a low melting point of 65 °C and it is more stable compared with other metastable forms. This new form was proved to be more soluble in 0.5% tween-80 solution, which suggested it has highly potential to generate medicinal crystal.

研究领域: 药学 · 材料科学 · 晶体化学

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Polymorph control of 5-fluorouracil during a ball milling process

A new polymorph of fenofibrate prepared by polymer-mediated crystallization