论文标题
直接从粉末筛选的多晶型筛选的微流体平台
Microfluidics platform for polymorph screening directly from powder
论文作者
论文摘要
我们描述了使用极少量的原材料的微流体平台，用于固相筛选。基于我们以前的溶解度测量设置，该设置直接从粉末生成饱和溶液，该平台不需要超过液滴结晶实验的溶液。该设置与大多数溶剂和分子兼容，而无需使用表面活性剂。使用这个微流体平台，我们首先测量了磺硫唑在水，异丙醇和乙腈中的溶解度。其次，我们使用低至30 mg的原材料对磺基二唑进行了多晶型筛选，以从80到10 {\ textDegree} c进行大量相同的冷却结晶实验。在提出的实验中，我们获得了硫唑的3个常规多晶型物。我们表明，这种经济的方法产生了有关给定多晶型物成核的可能性的可靠信息，可用于药物开发。
We describe a microfluidic platform for solid phase screening using extremely small quantities of raw materials. Based on our previous setup for solubility measurement that generates saturated solutions directly from powder, the platform requires no solution in excess of that used for the droplet-crystallization experiment. The setup is compatible with most solvents and molecules without using surfactant. Using this microfluidic platform, we first measured the solubility of Sulfathiazole in water, isopropanol, and acetonitrile. Second, we performed a polymorph screening of Sulfathiazole using as little as 30 mg of raw material, for numerous identical cooling crystallization experiments from 80 to 10{\textdegree}C. In the experiments presented, we obtained the 3 usual polymorphs of Sulfathiazole. We show that this economical approach yields reliable information on the probability of nucleation of a given polymorph, useful in pharmaceutical development.
