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超临界辅助雾化法制备氨苄西林微粉

Ampicillin micronization by supercritical assisted atomization.

作者信息

Reverchon E, Della Porta G, Spada A

机构信息

Università di Salerno, Dipartimento di Ingegneria Chimica ed Alimentare, Via Ponte don Melillo, 84084 Fisciano (SA), Italy.

出版信息

J Pharm Pharmacol. 2003 Nov;55(11):1465-71. doi: 10.1211/0022357022043.

DOI:10.1211/0022357022043
PMID:14713356
Abstract

The micronization technique called supercritical assisted atomization (SAA) was used to produce ampicillin microparticles with controlled particle size and particle size distribution suitable for aerosol drug delivery. The process is based on the solubilization of supercritical CO2 in a liquid solution. The ternary mixture is then sprayed through a nozzle and, as a consequence of enhanced atomization, solid microparticles are formed. Water and organic solvents were tested with ampicillin to determine the influence of the solvent on the process mechanism. SAA process parameters were studied by testing different supercritical/liquid solvent flow ratios, ampicillin concentrations in the liquid solution and nozzle diameters. The effect of these parameters on morphology, particle size and particle size distribution of microparticles was analysed. Ampicillin particles suitable for aerosol delivery in the size range 1-5 microm were obtained using buffered water. Moreover, by varying the solute concentration, ampicillin particles in a narrower range (1-3 microm) than that usually suggested for aerosol deliverable drugs were obtained. This is an example of particle size tailoring by SAA.

摘要

一种名为超临界辅助雾化(SAA)的微粉化技术被用于制备具有可控粒径和粒径分布的氨苄青霉素微粒,这些微粒适用于气溶胶药物递送。该过程基于超临界二氧化碳在液体溶液中的溶解。然后将三元混合物通过喷嘴进行喷雾,由于雾化增强,形成了固体微粒。用氨苄青霉素对水和有机溶剂进行了测试,以确定溶剂对过程机制的影响。通过测试不同的超临界/液体溶剂流量比、液体溶液中氨苄青霉素的浓度和喷嘴直径,研究了SAA工艺参数。分析了这些参数对微粒形态、粒径和粒径分布的影响。使用缓冲水获得了粒径范围为1-5微米、适用于气溶胶递送的氨苄青霉素微粒。此外,通过改变溶质浓度,获得了比通常建议的可用于气溶胶递送药物的粒径范围更窄(1-3微米)的氨苄青霉素微粒。这是通过SAA进行粒径定制的一个例子。

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