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首页> 外文期刊>Current Bioactive Compounds >Amorphous Active Pharmaceutical Ingredients in Preclinical Studies: Preparation, Characterization, and Formulation
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Amorphous Active Pharmaceutical Ingredients in Preclinical Studies: Preparation, Characterization, and Formulation

机译：临床前研究中的无定形活性药物成分：制备，表征和配制

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摘要

A large number of the new pharmaceutical small molecules under development today are found to have poornwater solubility. This in turn may lead to low bioavailability, which can have a significant impact on the development ofnthe compound. Compounds with low bioavailability pose a greater challenge in early preclinical work involving animalnstudies, where obtaining maximum exposure is the primary goal especially in toxicology studies designed to establish thensafe dose.nFrom the standpoint of maximizing exposure, the amorphous phase is of great interest as pharmaceutical materials since itnis the most metastable state and as such offers the potential of higher solubility and better bioavailability. However, thenamorphous approach is not actively pursued in preclinical work owing to the tendency of the amorphous phase toncrystallize thereby neutralizing the solubility advantage. This review focuses on (i) methods to generate the amorphousnphase, (ii) methods to estimate the degree of crystallinity of the amorphous phase, (iii) methods to predict the stability ofnthe amorphous phase against crystallization, and (iv) choice of polymers carrier and formulation of the amorphous phasenfor preclinical studies.
机译：今天发现大量正在开发的新的药物小分子的水溶性差。反过来，这可能导致生物利用度低，这可能会对化合物的开发产生重大影响。具有低生物利用度的化合物在涉及动物研究的早期临床前工作中面临更大的挑战，在该研究中，获得最大暴露是主要目标，尤其是在旨在确定安全剂量的毒理学研究中。n从最大化暴露的角度来看，非晶态作为医药材料备受关注因为它具有最亚稳态，因此具有更高的溶解度和更好的生物利用度的潜力。然而，由于非晶态相结晶的趋势，从而抵消了溶解度的优势，因此在临床前工作中并未积极地采用非晶态方法。这篇综述着重于（i）产生非晶相的方法，（ii）估计非晶相结晶度的方法，（iii）预测非晶相对结晶稳定性的方法，以及（iv）聚合物载体的选择用于临床前研究的非晶相的配方和配方。

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