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首页> 外文期刊>Crystal growth & design >Impact of Bile Salts on Solution Crystal Growth Rate and Residual Supersaturation of an Active Pharmaceutical Ingredient
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Impact of Bile Salts on Solution Crystal Growth Rate and Residual Supersaturation of an Active Pharmaceutical Ingredient

机译：胆汁盐对活性药物成分溶液晶体生长速率及残留过饱和度的影响

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摘要

Supersaturating formulations have become a popular approach to address the issue of inadequate aqueous solubility for small molecules. Given that prevention of nucleation may not be always possible, it is of particular interest to control crystal growth from supersaturated solutions in order to maximize the extent of oral absorption of therapeutic agents. Bile salts are endogenous surfactants that are present in biorelevant dissolution media and can have direct impact on the in vivo performance of therapeutic agents due to their presence in the gastrointestinal tract. In this study, an in situ common history seeding method was implemented to provide seeds that better mimic crystals formed from aqueous supersaturated solutions. By forming seeds in situ and then regenerating supersaturation, we were able to probe the influence of biorelevant bile salts on telaprevir crystal growth rates and secondary nucleation. The extent of growth inhibition was found to vary with bile salt chemistry and aggregation level. It was also noted that sodium taurocholate and sodium taurochenodeoxycholate inhibited secondary nucleation of telaprevir from highly supersaturated solutions. The impact of bile salts on crystal growth and secondary nucleation is of relevance for improved understanding of precipitation kinetics of supersaturating dosage forms.
机译：超饱和制剂已成为一种流行的方法，以解决小分子的水溶性不足的问题。鉴于预防成核可能并不总是可能的，对来自超饱和溶液的晶体生长特别感兴趣，以最大限度地提高治疗剂的口服吸收程度。胆汁盐是在Biorelevant溶解介质中存在的内源性表面活性剂，并且由于它们在胃肠道中存在而导致治疗剂的体内性能直接影响。在该研究中，实施了原位常见的历史播种方法，以提供种子，以提供由过饱和溶液水溶液形成的更好的模拟晶体。通过原位形成种子然后再生过饱和度，我们能够探测Biorelevant胆汁盐对TelaPrevir晶体生长率和次生成核的影响。发现生长抑制程度随胆汁盐化学和聚集水平而变化。还注意到，牛磺酸钠和牛磺酸钠抑制来自高度超饱和溶液的Teladrevir的次要成核。胆汁盐对晶体生长和次要成核的影响是有关改善对超饱和剂型的降水动力学的理解的相关性。

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