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为什么甘露醇作为固体制剂中的药用辅料越来越受欢迎?

Why is mannitol becoming more and more popular as a pharmaceutical excipient in solid dosage forms?

机构信息

Merck KGaA , Darmstadt , Germany.

出版信息

Pharm Dev Technol. 2014 May;19(3):257-62. doi: 10.3109/10837450.2013.775154. Epub 2013 Mar 26.

Abstract

Various fillers/binders which are applied for the formulation of solid oral dosage forms are assessed for their benefits and drawbacks, including lactose, sorbitol, mannitol, microcrystalline cellulose and calcium hydrogen phosphate dihydrate. A focus of this work was to evaluate the application of mannitol in comparison to other common fillers/binders as it was observed that this excipient is gaining more and more attention in pharmaceutical formulation development and production. While one of the main advantages of conventional fillers/binders such as lactose, microcrystalline cellulose and calcium hydrogen phosphate dihydrate is their low price level, mannitol excels regarding its physicochemical characteristics such as a low hygroscopicity, a strong inertness towards both the API and the patient's body, its good compactibility and the ability to produce extremely robust tablets. Additionally, the suitability of mannitol for the emerging formulation technology of orally disintegrating tablets is pointed out. In summary, it is emphasized that the selection of the filler/binder is highly individual, depending, for example, on the preferred characteristics of the final solid dosage form, the applied API and the available budget. However, mannitol exhibits many strong advantages which can be expected to result in a more widespread application in the near future.

摘要

各种用于制备固体制剂的填充剂/粘合剂,包括乳糖、山梨糖醇、甘露醇、微晶纤维素和磷酸氢钙二水合物,都需要评估其优缺点。这项工作的重点是评估甘露醇的应用,与其他常见的填充剂/粘合剂相比,因为人们发现这种赋形剂在药物制剂开发和生产中越来越受到关注。虽然乳糖、微晶纤维素和磷酸氢钙二水合物等传统填充剂/粘合剂的主要优点之一是价格低廉,但甘露醇在物理化学特性方面表现出色,如吸湿性低、对 API 和患者身体具有很强的惰性、可压性好,以及能够生产出极其坚固的片剂。此外,还指出甘露醇适用于新兴的口腔崩解片制剂技术。总之,强调选择填充剂/粘合剂是高度个体化的,取决于例如最终固体制剂的首选特性、应用的 API 和可用的预算。然而,甘露醇具有许多优势,预计在不久的将来会有更广泛的应用。

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