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反气相色谱法在有限稀释条件下对药物粉末表面能的表征。

Characterising surface energy of pharmaceutical powders by inverse gas chromatography at finite dilution.

机构信息

Faculty of Pharmacy and Pharmaceutical Sciences, Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.

出版信息

J Pharm Pharmacol. 2012 Sep;64(9):1337-48. doi: 10.1111/j.2042-7158.2012.01533.x. Epub 2012 May 9.

Abstract

OBJECTIVES

The objectives of this project were the use of surface energy distributions in: distinguishing the effects of magnesium stearate on the surface energy of lactose processed by two methods: mixing in a Turbula and mechanofusion; characterising surface energy of materials before and after micronisation; and understanding surface energy changes of micronised lactose before and after storage at high relative humidity (RH).

METHODS

Heptane, octane and nonane were used to determine nonpolar surface energy, and dichloromethane and ethyl acetate were used to determine polar surface energy in inverse gas chromatography at finite dilution.

KEY FINDINGS

The total surface energy of lactose decreased more after mechanofusion with magnesium stearate than mixing in Turbula. The nonpolar surface energy of indometacin increased while polar and total surface energies decreased after micronisation. The nonpolar, polar and total surface energies and work of cohesion of micronised lactose decreased after storage at 75% RH for three months.

CONCLUSIONS

The surface energy distributions determined at finite dilution successfully distinguished and revealed more information than infinite dilution on surface energy changes in materials undergoing different pharmaceutical processes such as mixing, mechanofusion, micronisation and storage at high RH.

摘要

目的

本项目的目的是利用表面能分布:区分硬脂酸镁对通过两种方法(在 Turbula 中混合和机械融合)加工乳糖的表面能的影响;在微粉化前后对材料的表面能进行表征;并了解高相对湿度(RH)储存前后微粉化乳糖的表面能变化。

方法

在有限稀释的反气相色谱法中,使用庚烷、辛烷和壬烷来测定非极性表面能,使用二氯甲烷和乙酸乙酯来测定极性表面能。

主要发现

硬脂酸镁经机械融合后,乳糖的总表面能比在 Turbula 中混合后下降更多。米诺环素经微粉化后,非极性表面能增加,极性和总表面能降低。在 75%RH 下储存三个月后,微粉化乳糖的非极性、极性和总表面能以及内聚功降低。

结论

在有限稀释下确定的表面能分布成功地区分并揭示了更多信息,比在无限稀释下更能反映材料在不同制药工艺(如混合、机械融合、微粉化和高 RH 储存)中表面能变化的信息。

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