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首页> 外文期刊>Crystal growth & design >Maintaining supersaturation in aqueous drug solutions: Impact of different polymers on induction times
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Maintaining supersaturation in aqueous drug solutions: Impact of different polymers on induction times

机译：维持药物水溶液中的过饱和度：不同聚合物对诱导时间的影响

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摘要

The use of polymeric additives is an increasingly common approach for inhibiting crystallization from the supersaturated solutions used to enhance the delivery of poorly water-soluble drugs. Maintaining supersaturation by employing polymeric additives depends on their ability to inhibit nucleation and crystal growth. In solution crystallization, nucleation initiates the process of crystallization, and therefore adequate control over crystallization from supersaturated solutions cannot be achieved without understanding the mechanism of nucleation inhibition by polymers. In this study, the effectiveness of a group of chemically diverse polymers, including several recently synthesized cellulose derivatives, on induction times in aqueous solutions was quantified. Nucleation was quantified by measuring the induction time for the appearance of particulates from unseeded desupersaturation experiments for three model pharmaceutical compounds: celecoxib, efavirenz, and ritonavir. Induction times in the absence of the polymers varied from approximately 2 min for celecoxib to 2 h for ritonavir. Some polymers were found to extend induction times by up to a factor of 5-6 at the highest supersaturations tested. The effectiveness of the various polymers appeared to depend on the hydrophobicity of the polymer relative to that of the drug. The hydrophobicity of the polymer most likely influences the ability of the polymer to form polymer-solute interactions relative to polymer-solvent and polymer-polymer interactions. Polymer-solute interactions would be expected to hinder the reorganization of a cluster of solute molecules into an ordered crystal structure.
机译：聚合物添加剂的使用是抑制从用于增强水溶性差的药物的递送的过饱和溶液中结晶的越来越普遍的方法。通过使用聚合物添加剂保持过饱和取决于它们抑制成核和晶体生长的能力。在溶液结晶中，成核作用引发结晶过程，因此，如果不了解聚合物抑制成核的机理，就无法实现对过饱和溶液结晶的充分控制。在这项研究中，量化了一组化学上多样化的聚合物（包括几种最近合成的纤维素衍生物）对水溶液中诱导时间的有效性。通过测量三种模型药物化合物（塞来昔布，依法韦仑和利托那韦）的非种子去饱和度实验中出现颗粒的诱导时间，可以量化成核作用。在不存在聚合物的情况下，诱导时间从塞来昔布大约2分钟到利托那韦2小时不等。发现某些聚合物在测试的最高过饱和度下可以将诱导时间延长至5-6倍。各种聚合物的有效性似乎取决于聚合物相对于药物的疏水性。聚合物的疏水性最有可能影响聚合物形成相对于聚合物-溶剂和聚合物-聚合物相互作用的聚合物-溶质相互作用的能力。预期聚合物-溶质相互作用会阻碍溶质分子簇重组为有序晶体结构。

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