Hot melt granulation of coarse pharmaceutical powders in a spouted bed
Hot melt granulation of coarse pharmaceutical powders in a spouted bed
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DOI：
10.1016/j.powtec.2008.08.004
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发表时间：
2009-02-13
影响因子：
5.2
通讯作者：
Freitas, Luis A. P.
中科院分区：
文献类型：
--
作者：
Borini, G. B.;Andrade, T. C.;Freitas, Luis A. P.
描述了在顶部喷雾喷动床中对粗药粉进行热熔造粒。底物是含有或不含对乙酰氨基酚的乳糖-聚乙烯吡咯烷酮颗粒作为药物模型。用作粘合剂的聚乙二醇（MW，4000）通过双流体喷嘴雾化到床上。造粒实验遵循 2(3) 因子设计，在中心点重复三次，并通过改变喷嘴垂直位置、雾化空气流速和粘合剂进料速率来进行。通过颗粒的药学特性（如尺寸分布、堆积密度和振实密度、卡尔指数、豪斯纳比和压片特性）对其进行评估。方差分析表明，颗粒尺寸受PEG进料速率和雾化气压的影响，显着性水平分别为1.0%和5.0%。分别，但喷嘴到基质床的距离并不显着。喷雾条件还影响颗粒流动和固结特性。通过卡尔指数和豪斯纳比率来衡量。测量的密度、卡尔指数和豪斯纳比证明颗粒的流动性和固结特性足以满足药物加工和压片的要求。用含对乙酰氨基酚的颗粒制备的片剂在体外溶出试验中显示出良好的性能和足够的释放曲线。结果表明喷射床适用于药物粗粉的热熔造粒。 (C) 2008 Elsevier B.V. 保留所有权利。
The hot melt granulation of a coarse pharmaceutical powder in a top spray spouted bed is described. The substrate was lactose-polyvinylpyrrolidone particles containing or not acetaminophen as a drug model. Polyethylene glycol (MW, 4000) used as binder was atomized onto the bed by a two-fluid spray nozzle. The granulation experiments followed a 2(3) factorial design with triplicates at the center point and were carried out by varying the spray nozzle vertical position, the atomizing air flow rate and the binder feed rate. Granules were evaluated by their pharmacotechnical properties like size distribution, bulk and tapped densities, Carr index, Hausner ratio and tableting characteristics. Analysis of variance showed that granule sizes were affected by the PEG feed rate and atomizing air pressure at the significance levels of 1.0 and 5.0%. respectively, but spray nozzle distance to the substrate bed was not significant. The spray conditions also affected granule flow and consolidation properties. measured by the Carr index and Hausner ratio. Measured densities, Carr indexes and Hausner ratios proved that granules flowability and consolidation properties are adequate for pharmaceutical processing and tableting. Tablets prepared with acetaminophen-containing granules showed good properties and adequate release profiles in in vitro dissolution tests. The results indicate the suitability of spouted beds for the hot melt granulation of pharmaceutical coarse powders. (C) 2008 Elsevier B.V. All rights reserved.