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喷雾干燥无定形复合颗粒的压缩行为及压片能力

Compression behaviour and tablet-forming ability of spray-dried amorphous composite particles.

作者信息

Berggren Jonas, Frenning Göran, Alderborn Göran

机构信息

Department of Pharmacy, Uppsala University, Box 580, SE-751 23 Uppsala, Sweden.

出版信息

Eur J Pharm Sci. 2004 Jun;22(2-3):191-200. doi: 10.1016/j.ejps.2004.03.008.

Abstract

The aim of this study was to investigate the compression behaviour and tablet-forming ability of spray-dried amorphous two- and three-component composite particles. Particles of lactose alone, two-component particles of lactose and PVP, and three-component particles of lactose, PVP and a small amount of polysorbate 80 were prepared by spray-drying. Two qualities of PVP with different molecular weights were used for the preparation of both types of particles. The particles were characterised with respect to permeametry surface area, moisture content, particle and bulk density, glass transition and crystallisation temperature, and heat of crystallisation. The tablet tensile strength of the different particles formed at a series of applied pressures was determined and compression parameters were derived from the Heckel and Kawakita equations. The presence of PVP gave particles that were less prone to deform permanently during compression while the presence of surfactant gave particles that were less able to form tablets. In conclusion, the compression behaviour and tablet-forming ability of spray-dried amorphous lactose can be modulated by the addition of stabilising polymers or surfactants to the spray feed solution.

摘要

本研究的目的是研究喷雾干燥无定形二元和三元复合颗粒的压缩行为和压片能力。通过喷雾干燥制备了单独的乳糖颗粒、乳糖与聚乙烯吡咯烷酮(PVP)的二元颗粒以及乳糖、PVP和少量聚山梨酯80的三元颗粒。两种不同分子量的PVP用于制备这两种类型的颗粒。对颗粒的渗透率表面积、水分含量、颗粒密度和堆密度、玻璃化转变温度和结晶温度以及结晶热进行了表征。测定了在一系列施加压力下形成的不同颗粒的片剂抗张强度,并从赫克尔(Heckel)方程和川北(Kawakita)方程推导压缩参数。PVP的存在使颗粒在压缩过程中不易发生永久变形,而表面活性剂的存在使颗粒形成片剂的能力降低。总之,通过向喷雾进料溶液中添加稳定聚合物或表面活性剂,可以调节喷雾干燥无定形乳糖的压缩行为和压片能力。

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