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首页> 外文期刊>Organic process research & development >A Process for the Formation of Nanocrystals of Active Pharmaceutical Ingredients with Poor Aqueous Solubility in a Nanoporous Substrate
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A Process for the Formation of Nanocrystals of Active Pharmaceutical Ingredients with Poor Aqueous Solubility in a Nanoporous Substrate

机译：在纳米多孔基质中水溶性差的活性药物成分纳米晶体的形成方法

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摘要

A potential process for the formation of nanocrystals of the poorly soluble drug, ibuprofen, within a nanoporous material is demonstrated. Nanocrystalline ibuprofen (IBP) is prepared at <= 106 nm by adding a solution containing IBP to particles of controlled pore glass (CPG) within a column so that the pores contain IBP solution. The imbibed particles of CPG are then rinsed with a minimal amount of solvent to remove excess solution at the surface of CPG, and a flow of air within the column is used to evaporate the solvent, resulting in crystallization of IBP within the pores of CPG. Crystallinity is determined using X-ray powder diffraction. MP is confirmed as being in the nanosize range by observation of a negative shift in the melting point measured by differential scanning calorimetry, and loading of IBP nanocrystals within the pores (% w/w) is determined by thermogravimetric analysis. Parameters were investigated for the process and demonstrate that an increase in percentage loading is achieved with increasing solution concentration and with increasing solvent viscosity. Loading of IBP within CPG was also found to be very sensitive to the volume of rinse solvent used. It is shown that rinsing with a minimal amount of solvent is necessary to avoid the significant presence of bulk micron-sized surface crystals. In vitro dissolution profiles, performed in water, demonstrate the significant dissolution rate increase offered by nanocrystalline IBP relative to bulk micron-sized crystals or even formulated tablets of IBP.
机译：证明了在纳米多孔材料中形成难溶性药物布洛芬纳米晶体的潜在方法。纳米晶布洛芬（IBP）可通过将含有IBP的溶液添加到柱内受控孔玻璃（CPG）的颗粒中以使孔中包含IBP溶液的方式在<= 106 nm处制备。然后将吸收的CPG颗粒用最少量的溶剂冲洗，以去除CPG表面的过量溶液，并使用色谱柱内的空气流蒸发溶剂，从而使CBP孔内的IBP结晶。使用X射线粉末衍射测定结晶度。通过观察通过差示扫描量热法测得的熔点的负位移来确认MP在纳米尺寸范围内，并且通过热重分析确定在孔内的IBP纳米晶体的负载（％w / w）。研究了该工艺的参数，结果表明，随着溶液浓度的增加和溶剂粘度的增加，负载百分率的增加。还发现CPG中IBP的装载量对所用冲洗溶剂的量非常敏感。结果表明，需要用最少量的溶剂冲洗才能避免大量存在的微米级表面晶体的存在。在水中进行的体外溶出曲线表明，相对于块状微米级晶体甚至是IBP制成的片剂，纳米晶IBP所提供的溶出速率显着提高。

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