Poorly aqueous soluble active pharmaceutical ingredients are highly risky development candidates and remain a concern of pharmaceutical industries in drug discovery and development processes. Pharmaceutical industries are putting significant efforts into the target identification and lead candidate development using combinatorial chemistry. About 40% of compounds arising from combinatorial screening are poorly water soluble. Pharmaceutical industries evolved over this challenge by coming up with reproducible and scalable particle size reduction or by identifying alternate morphs. Another important area where pharmaceutical industries are working is solid dispersion technology. With the emergence of the hot-melt extrusion and spray drying approach, many molecules have been brought to the market using solid dispersion technology from the discovery phase by improving bioavailability and thereby efficacy. Although the solid solution technology in the last 60 years evolved from eutectic mixtures, solid dispersions using water-soluble polymers, and enteric polymers especially hydroxypropyl methylcellulose acetate succinate (HPMCAS), still there is no preformulation tool to identify correct polymer or polymer combination at the early stage of development. Thus, this leads to the urgent need to focus on the design and development of third-generation solid dispersions for the unmet needs of the industries and society.

中文翻译：

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固体分散技术的发展：使用醋酸羟丙基甲基纤维素琥珀酸酯提高溶解度：神话还是现实？

水溶性差的活性药物成分是高风险的开发候选者，并且仍然是制药行业在药物发现和开发过程中关注的问题。制药行业正在使用组合化学在目标识别和先导候选开发方面投入巨大努力。组合筛选产生的大约 40% 的化合物水溶性差。制药行业通过提出可重现和可扩展的粒径减小或通过识别替代形态来克服这一挑战。制药行业的另一个重要领域是固体分散技术。随着热熔挤出和喷雾干燥方法的出现，通过提高生物利用度和功效，许多分子从发现阶段就使用固体分散技术推向市场。尽管过去 60 年中的固溶体技术从低共熔混合物、使用水溶性聚合物的固体分散体和肠溶聚合物特别是醋酸琥珀酸羟丙基甲基纤维素 (HPMCAS) 发展而来，但仍然没有预配制工具来识别正确的聚合物或聚合物组合。发展的早期阶段。因此，这导致迫切需要专注于第三代固体分散体的设计和开发，以满足行业和社会未满足的需求。使用水溶性聚合物和肠溶聚合物特别是醋酸琥珀酸羟丙基甲基纤维素 (HPMCAS) 的固体分散体，在开发的早期阶段仍然没有预配制工具来识别正确的聚合物或聚合物组合。因此，这导致迫切需要专注于第三代固体分散体的设计和开发，以满足行业和社会未满足的需求。使用水溶性聚合物和肠溶聚合物特别是醋酸琥珀酸羟丙基甲基纤维素 (HPMCAS) 的固体分散体，在开发的早期阶段仍然没有预配制工具来识别正确的聚合物或聚合物组合。因此，这导致迫切需要专注于第三代固体分散体的设计和开发，以满足行业和社会未满足的需求。