固体分散体技术作为制备改性释放剂型的配方策略:综述。

Kaushika Patel, Shreeraj Shah, Jaymin Patel
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引用次数: 6

摘要

溶解度限制生物利用度是影响新化学实体配方发展的关键参数之一。因此,有效药物成分的溶解度增强技术是制约药品开发的主要因素。固体分散(SD)是改善溶解度的首选方法,最终可能有助于提高生物利用度。长期以来,非晶固体分散体(ASD)一直是改善溶解度的首选方法,但近二十年来,ASD方法已与不同的修饰释放方法相结合,以提高SD的稳定性和位点特异性,以掌握与此类剂型相关的特定优势。目前,SD技术不仅可以提高溶解度和有限的生物利用度,而且可以根据SD载体的选择和合适的技术,与其他方法结合,根据需要修改制剂的药物释放谱。这篇综述涵盖了所有这些配方的全面概述,其中SD技术用于双重目的,而不仅仅是提高溶解度的唯一目的。SD方法已经成功地应用于一些难溶性草药,并且在该领域仍有很大的进步空间。本综述将提供改良释药配方的SD技术领域的广泛成果,并描述SD的现状和未来前景。药物在常规载体内分散形成的SD增加了溶解度、溶出率和生物利用度;而第四代疏水载体则提供了控释(CR)或缓释(SR)的优势,并增强了SD的稳定性。在另一个前沿领域,pH依赖性载体使SD能够实现位点特异性或延迟释放(DR)特征。
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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Solid dispersion technology as a formulation strategy for the fabrication of modified release dosage forms: A comprehensive review.

Solubility limited bioavailability is one of the crucial parameters that affect the formulation development of the new chemical entities. Thus the major constraint in the pharmaceutical product development is the suitable solubility enhancement technique for Active Pharmaceutical Ingredient. Solid dispersion (SD) is an established and preferred method for improving the solubility which ultimately may be helpful to enhance bioavailability. For long period of time Amorphous solid dispersion (ASD) have been preferred for improving solubility, but since last two decades, ASD approach have been combined with different modified release approaches to improvise the stability and site specificity of SD to grasp a hold over the specific advantages associated with such dosage forms. It is an established fact now that the SD technique not only improves solubility limited bioavailability, but it may be combined with other approaches to modify the drug release profile from the formulation as per the requirement based on the apt selection of SD carriers and suitable technology. This review covers the comprehensive overview of all such formulations where SD technology is used to serve dual purpose rather than only the sole purpose of solubility enhancement. The SD approach has been successfully implemented for some of the poorly soluble herbal drugs and still there is a vast scope of advancement in that area. The current review will provide a broad outcome in the area of SD technology for modified release formulations along with the description of current status and future prospective of SD. The SD formed by dispersing drug within the conventional carrier to form ASD increases solubility, dissolution rate and bioavailability; whereas fourth generation hydrophobic carriers provide added advantage of controlled release (CR) or sustained release (SR) profile along with enhanced stability of SD. On the other frontier, pH dependant carriers enable the SD to achieve site specificity or delayed release (DR) profile.

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