Strategies for improving hydrophobic drugs solubility and bioavailability

Krishna R. Gupta, Monali R Dakhole, Ketki S Jinnawar, Milind J Umekar
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Abstract

Nowadays various drugs synthesized by various computational drug designs as well as various drugs have complex structure. Due to their complex structure, higher molecular weight which will increases solubility issues. Solubility is the most important and challenging task for researchers. Bioavailability and absorption of a drug depends on solubility of drug and thus we achieve pharmacological response. But poor aqueous solubility is a rate limiting step in bioavailability which made drug development more difficult. Drugs having low bioavailability require to be administered at a higher dose to achieve desired drug concentration in the systemic circulation and reach the target site. Thus, instead of getting desired effects drug produces side effects in the gastrointestinal tract. Hence, with the advancement of chemical science, the need of development of pharmaceutical technologies is also increasing. New techniques have been developed with a focus on enhancement of the solubility and oral bioavailability of poorly water-soluble drugs. The present review focuses on new technologies which are being used to resolve solubility issue of poorly soluble drugs which is the rate limiting step in bioavailability.
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提高疏水药物溶解度和生物利用度的策略
目前,通过各种计算药物设计合成的各种药物以及各种药物具有复杂的结构。由于其结构复杂,分子量较高,会增加溶解度的问题。溶解度是研究人员最重要和最具挑战性的任务。药物的生物利用度和吸收取决于药物的溶解度,因此我们获得药理学反应。但水溶解度差是生物利用度的限速步骤,使药物开发更加困难。生物利用度低的药物需要以更高的剂量给药,才能在体循环中达到所需的药物浓度并到达靶部位。因此,药物在胃肠道中产生副作用,而不是得到预期的效果。因此,随着化学科学的进步,对制药技术发展的需求也越来越大。新技术的发展重点是提高水溶性差药物的溶解度和口服生物利用度。本文综述了目前用于解决难溶性药物溶解度问题的新技术,这是生物利用度的限速步骤。
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