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压缩口腔崩解片:辅料的演变和制剂策略。

Compressed orally disintegrating tablets: excipients evolution and formulation strategies.

机构信息

Aston University, Aston Pharmacy School , Aston Triangle, Birmingham B4 7ET , UK.

出版信息

Expert Opin Drug Deliv. 2013 May;10(5):651-63. doi: 10.1517/17425247.2013.769955. Epub 2013 Feb 7.

DOI:10.1517/17425247.2013.769955
PMID:23387409
Abstract

INTRODUCTION

Orally disintegrating tablets (ODTs) have emerged as one of the novel solid oral dosage forms with a potential to deliver a wide range of drug candidates to both paediatric and geriatric patient populations. Of the plethora of available technologies, compression of excipients offers a cost-effective and translatable methodology for the manufacture of ODTs.

AREAS COVERED

The review is a modest endeavour from the authors to assemble literature published over the last couple of decades on formulation development of compressed ODT. It describes the main ODT excipients used since the introduction of this dosage form in the 1990s and explores the switch from cellulose-based excipients towards sugar/polyols. Furthermore, it unfolds the key properties of ODT fillers, binders and disintegrants with an emphasis on their advantages and drawbacks. The review also provides a critical assessment of the various strategies employed for performance enhancement of compressed ODT with a focus on the underlying mechanisms for fast disintegration and acceptable mechanical strength.

EXPERT OPINION

Recent increase in the total number of compression-based technologies for ODT development promises to reduce the manufacturing cost of this dosage form in the future. However, some of the developed methods may affect the stability of tablets due to susceptibility to moisture, collapse of pores or the generation of less stable polymorphs which require rigorous testing prior to commercialization.

摘要

简介

口崩片(ODT)作为一种新型固体口服剂型,具有为儿科和老年患者群体提供广泛药物候选物的潜力,已逐渐兴起。在众多现有技术中,赋形剂的压缩为 ODT 的制造提供了一种具有成本效益和可转化的方法。

涵盖领域

作者进行了一项适度的努力,从已发表的文献中收集了过去二十年中有关压缩 ODT 制剂开发的信息。它描述了自 20 世纪 90 年代引入这种剂型以来使用的主要 ODT 赋形剂,并探讨了从基于纤维素的赋形剂向糖/多元醇的转变。此外,它还阐述了 ODT 填充剂、粘合剂和崩解剂的关键特性,重点介绍了它们的优缺点。该综述还对用于增强压缩 ODT 性能的各种策略进行了批判性评估,重点关注快速崩解和可接受的机械强度的潜在机制。

专家意见

最近用于 ODT 开发的基于压缩的技术总数增加,有望降低这种剂型的制造成本。然而,一些已开发的方法可能会因对水分的敏感性、孔塌陷或生成不太稳定的多晶型物而影响片剂的稳定性,这需要在商业化之前进行严格的测试。

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