Combined novel approach to enhance the solubility and Intestinal absorption: A recent review

Ambuj Dubey, B. Patel, S. Parmar
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Abstract

For oral pharmaceutical products to achieve high bioavailability and minimal variability, the API must dissolve and be stable in the GI media as well as sufficiently absorb at pertinent sites in the large intestine and small intestine. The possibility for API absorption from any dosage form is determined by an important biopharmaceutical parameter known as regional intestine effective permeability. For effective estimation of the manufacturing potential of a dosage form, it is especially crucial to understand the quantity of drug absorption from the human large intestine. Drug development is difficult because enhancing a drug's solubility, dissolution, and bioavailability is challenging. Among the four classes of the biopharmaceutical classification system (BCS) major work has been done on the low soluble drugs. In recent years poor solubility has been a major challenge for pharmaceutical scientists and a lot of experimental works are ongoing. Changing polymorphic forms by different new approaches and increase in the surface area is a widely used and comparatively simple method for increasing solubility and making the drug more bioavailable. For achieving the desired effects, permeability (intestinal absorption) is also playing an important role like solubility, but the focus of scientists is less on the permeability enhancement of low permeable drugs in respect of solubility. Sometimes it has been tried but with very limited success. The objective of this paper to provide a comprehensive review on improving solubility, release and intestinal absorption of low soluble and low permeable drugs with a combined novel approach of solubility and absorption enhancement. The ability to produce high soluble and high permeable drugs will grow significantly in the coming years and this will help to grow the revenue of the innovators as well as generic pharmaceutical companies. Keywords: Absorption, Bioavailability, Dissolution, Duodenum, Gastrointestinal tract, Gastrointestinal transit time, Gastroretention, Milling, Permeability, Poorly water-soluble drug(s), Polymer(s), Solvent evaporation, Spray drying
结合新方法提高溶解度和肠道吸收:最近的综述
口服药物产品要达到高生物利用度和最小可变性,原料药必须在胃肠道介质中溶解和稳定,并在大肠和小肠的相关部位充分吸收。任何剂型的原料药吸收的可能性是由一个重要的生物制药参数决定的,即区域肠道有效通透性。为了有效地估计一种剂型的生产潜力,了解人体大肠对药物的吸收量尤为重要。药物开发是困难的,因为提高药物的溶解度、溶解度和生物利用度是具有挑战性的。在生物药物分类系统的四大类中,低溶性药物是研究的重点。近年来,溶解度差一直是制药科学家面临的主要挑战,许多实验工作正在进行中。通过不同的新途径改变多晶形态和增加表面面积是一种广泛使用的相对简单的方法,可以提高药物的溶解度,提高药物的生物利用度。为了达到预期的效果,通透性(肠吸收)和溶解度一样也起着重要的作用,但在溶解度方面,科学家对低通透性药物的通透性增强关注较少。有时已经尝试过,但收效甚微。本文就利用增强溶解度和吸收相结合的新方法改善低溶性和低渗透药物的溶解度、释放和肠道吸收作一综述。在未来几年,生产高可溶性和高渗透性药物的能力将显著增长,这将有助于创新者和仿制药公司增加收入。关键词:吸收,生物利用度,溶解,十二指肠,胃肠道,胃肠传递时间,胃潴留,研磨,渗透性,低水溶性药物,聚合物,溶剂蒸发,喷雾干燥
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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