Technique Development in Improving the Solubility of Poorly Water Soluble Drugs (BCS II and IV): a Review Study

Muhamad Reza Pahlevi, Iyan Sopyan, Dolih Gozali
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Abstract

Orally active drugs are currently available on the market. API should have adequate solubility and permeability to enhance its therapeutic efficacy when administered orally and obtain optimum bioavailability. Almost 40% of New Chemical Entities had limited solubility or fell into BCS class II and IV. Our review aims to summarize and discuss the development of methods and characterization for increasing the solubility of poorly aqueous drugs from papers published in Google Scholar, NCBI, Science direct, Researchgate, and MDPI. We checked that the methods used such as solid dispersion, cocrystal formation, and coamorphous can increase the solubility of API which has an impact on increasing bioavailability. The successful formation of solid dispersions, cocrystals and coamorphs can be confirmed by the characterization of PXRD, DSC and SEM. In conclusion, drug solubility is an important aspect of pharmacological effects. Drugs with high solubility can provide fast solubility rates and high bioavailability, reducing the dose administered. Solid dispersion, cocrystals, and coamorphous techniques, have succeeded in increasing the solubility of BCS class II and IV drugs.
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提高难水溶性药物溶解度的技术进展(BCS II和IV):综述
目前市场上有口服活性药物。原料药应具有足够的溶解度和渗透性,以提高口服给药的疗效,并获得最佳的生物利用度。近40%的新化学实体具有有限的溶解度或属于BCS II和IV类。我们的综述旨在总结和讨论在Google Scholar, NCBI, Science direct, Researchgate和MDPI上发表的论文中提高差水药物溶解度的方法和表征的发展。我们检查了所使用的方法,如固体分散、共晶形成和共晶可以增加原料药的溶解度,从而提高生物利用度。通过PXRD、DSC和SEM的表征,证实了固体分散体、共晶和共晶的成功形成。总之,药物溶解度是药理作用的一个重要方面。具有高溶解度的药物可以提供快速的溶解度和高生物利用度,减少给药剂量。固体分散、共晶和共晶技术已经成功地提高了BCS II类和IV类药物的溶解度。
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