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聚合物作为固体制剂药用辅料的应用。

Applications of Polymers as Pharmaceutical Excipients in Solid Oral Dosage Forms.

机构信息

Department of Chemical Engineering, Shenkar College of Engineering and Design, Ramat-Gan, Israel.

Department of Clinical Pharmacology, School of Pharmacy, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer-Sheva, Israel.

出版信息

Med Res Rev. 2017 Jan;37(1):52-97. doi: 10.1002/med.21403. Epub 2016 Aug 9.

Abstract

Over the last few decades, polymers have been extensively used as pharmaceutical excipients in drug delivery systems. Pharmaceutical polymers evolved from being simply used as gelatin shells comprising capsule to offering great formulation advantages including enabling controlled/slow release and specific targeting of drugs to the site(s) of action (the "magic bullets" concept), hence hold a significant clinical promise. Oral administration of solid dosage forms (e.g., tablets and capsules) is the most common and convenient route of drug administration. When formulating challenging molecules into solid oral dosage forms, polymeric pharmaceutical excipients permit masking undesired physicochemical properties of drugs and consequently, altering their pharmacokinetic profiles to improve the therapeutic effect. As a result, the number of synthetic and natural polymers available commercially as pharmaceutical excipients has increased dramatically, offering potential solutions to various difficulties. For instance, the different polymers may allow increased solubility, swellability, viscosity, biodegradability, advanced coatings, pH dependency, mucodhesion, and inhibition of crystallization. The aim of this article is to provide a wide angle prospect of the different uses of pharmaceutical polymers in solid oral dosage forms. The various types of polymeric excipients are presented, and their distinctive role in oral drug delivery is emphasized. The comprehensive know-how provided in this article may allow scientists to use these polymeric excipients rationally, to fully exploit their different features and potential influence on drug delivery, with the overall aim of making better drug products.

摘要

在过去的几十年中,聚合物已被广泛用作药物传递系统中的药物赋形剂。药用聚合物已经从简单地用作包含胶囊的明胶壳发展到具有很大的配方优势,包括能够控制/缓慢释放和将药物靶向作用部位(“神奇子弹”概念),因此具有重要的临床意义。口服固体制剂(例如片剂和胶囊)是最常见和方便的给药途径。在将具有挑战性的分子制成固体制剂时,药用聚合物赋形剂可以掩盖药物的不良物理化学性质,从而改变其药代动力学特征,以提高治疗效果。结果,可商购的合成和天然聚合物作为药物赋形剂的数量急剧增加,为各种困难提供了潜在的解决方案。例如,不同的聚合物可能允许增加溶解度,溶胀性,粘度,生物降解性,先进的涂层,pH 依赖性,粘膜附着力和抑制结晶。本文的目的是提供药用聚合物在固体制剂中的不同用途的广泛视角。介绍了各种类型的聚合物赋形剂,并强调了它们在口服药物传递中的独特作用。本文提供的全面知识可使科学家合理地使用这些聚合物赋形剂,充分利用它们在药物传递方面的不同特性和潜在影响,最终目的是生产更好的药物产品。

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