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载体辅料的聚合物包衣改变干粉吸入疗法中粘附药物的气溶胶性能。

Polymer coating of carrier excipients modify aerosol performance of adhered drugs used in dry powder inhalation therapy.

机构信息

Respiratory Technology, Woolcock Institute of Medical Research, 431 Glebe Point Road, Glebe, NSW 2037, Australia.

出版信息

Int J Pharm. 2012 Nov 15;438(1-2):150-9. doi: 10.1016/j.ijpharm.2012.08.036. Epub 2012 Sep 1.

Abstract

The potential of excipient coating to enhance aerosol performance of micronized drugs in carrier excipient-drug blends, used in dry powder inhalers, was investigated. Both EC (ethyl cellulose) and PVP (polyvinylpyrrolidone) were used as coating agents. Carriers were prepared via sieve fractioning followed by spray drying, with and without polymer additive. Each uncoated and coated carrier salbutamol sulphate (SS) blended systems were evaluated for particle size, morphology, drug carrier adhesion and aerosolisation performance, after blending and storage for 24h. All carrier-based systems prepared had similar particle sizes and morphologies. The surface chemistries of the carriers were significantly different, as was drug-carrier adhesion and aerosolisation performance. Particle adhesion between SS and aerosol performance (fine particle fraction; FPF) followed the rank: PVP coated>un-coated>EC coated lactose. This rank order could be attributed to the surface energy measured by contact goniometry and related to the chemistry of lactose and each polymer. Storage did not significantly affect aerosol performance, however a rank increase in mean FPF value was observed for uncoated and EC coated lactose. Finally, the net electrostatic charge across the aerosol cloud indicated that the EC coated lactose transferred less charge to SS particles. The performance of each carrier system could be attributed to the carrier surface chemistry and, in general, by careful selection of the coating polymer, drug-carrier adhesion, electrostatic charge and aerosol performance could be controlled.

摘要

研究了赋形剂涂层在干粉吸入器中载体-药物混合物中微米化药物气溶胶性能的潜在增强作用。使用乙基纤维素 (EC) 和聚乙烯吡咯烷酮 (PVP) 作为涂层剂。载体通过筛分分馏和喷雾干燥制备,有和没有聚合物添加剂。在混合和储存 24 小时后,对未经涂层和涂层的沙丁胺醇硫酸盐 (SS) 混合系统进行粒径、形态、药物载体附着力和雾化性能评估。所有基于载体的系统都具有相似的粒径和形态。载体的表面化学性质明显不同,药物载体附着力和雾化性能也不同。SS 与气溶胶性能(细颗粒分数;FPF)之间的颗粒附着力依次为:PVP 涂层>未涂层>EC 涂层乳糖。这种顺序可以归因于通过接触测角法测量的表面能,以及与乳糖和每种聚合物的化学性质有关。储存不会显著影响气溶胶性能,但是未涂层和 EC 涂层乳糖的平均 FPF 值的等级增加。最后,气溶胶云中的净静电荷表明 EC 涂层乳糖向 SS 颗粒传递的电荷较少。每个载体系统的性能可归因于载体表面化学性质,并且通常通过仔细选择涂层聚合物,可以控制药物-载体附着力、静电荷和气溶胶性能。

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