新型配方中的环糊精和增溶技术:综述

Shraddha Todkar, S. Dhole, Tanuja Umate, N. Kulkarni
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引用次数: 0

摘要

使用环糊精有助于提高不同剂型的溶解度。被称为环糊精(CD)的寡糖类是由环状结合在一起的葡萄糖单元组成的。环糊精具有与药物分子结合成复合物的能力,无需进行分子修饰即可改善药物的理化性质。一般来说,药物-CD 复合物的化学计量为 1:1。然而,天然 CD 在水介质中具有自组装和形成聚集体的倾向,聚集体会降低 CD 的溶解度。人们可以通过形成衍生物来提高它们的络合能力和溶解度,但最终结果取决于取代的种类和程度。通过形成水溶性药物-CD 复合物,可以提高药物在生物膜上的渗透性。溶解度是指固体溶解到液相中形成均匀体系的特性。溶解度是在全身循环中获得适当药物浓度以产生最佳药理反应的关键因素。口服溶解度低的药物通常需要高剂量才能达到治疗血浆浓度。它们在水中的低溶解度是通过制剂创造新化学实体的主要问题之一。BCS 分类系统将这类药物归入第二类,其特点是渗透性高、溶解性差。要大大改善这些药物,可以使其生物利用度和溶解度更高。
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CYCLODEXTRIN IN NOVEL FORMULATIONS AND SOLUBILITY ENHANCEMENT TECHNIQUES: A REVIEW
Using cyclodextrin helps make different dosage forms more soluble. The oligosaccharide class known as cyclodextrins (CDs) is made up of glucose units bound together in a ring. CDs have the promising ability to assemble into complexes with drug molecules and improve their physicochemical properties without the need for molecular modifications. Generally, drug-CD complexes have a stoichiometry of 1:1. However, natural CDs have a tendency to self-assemble and form aggregates in aqueous media, which can reduce the solubility of the CDs by aggregating. One can increase their complexation capacity and solubility through derivative formation, but the final outcome depends on the kind and extent of substitution. Drug penetration through biological membranes can be improved by the formation of water-soluble drug-CD complexes. Solubility is the property of a solid dissolving into a liquid phase to form a homogenous system. Solubility is a crucial component in obtaining the right drug concentration in the systemic circulation for the optimal pharmacological response. Orally administered poorly soluble drugs often require high dosages to reach therapeutic plasma concentrations. Their low solubility in water is one of the primary problems with creating new chemical entities through formulation. The BCS classification system places these medications in class II, which is characterized by high permeability and poor solubility. To greatly improve these medications, it is possible to make them more bioavailable and soluble.
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