Powder bed packing and API content homogeneity of granules in single drop granule formation
Powder bed packing and API content homogeneity of granules in single drop granule formation
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单滴颗粒形成过程中颗粒的粉末床填充和 API 含量均匀性
DOI：
10.1016/j.powtec.2020.02.039
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发表时间：
2020
影响因子：
5.2
通讯作者：
Emady, Heather N.
中科院分区：
文献类型：
--
作者：
Gao, Tianxiang;Singaravelu, Arun S.S.;Oka, Sarang;Ramachandran, Rohit;Štepánek, František;Chawla, Nikhilesh;Emady, Heather N.
研究了药物混合物在静态粉末床上的单滴颗粒形成，以考察疏水性和初级粒度分布对粉末床堆积结构和所形成颗粒中活性药物成分（API）含量均匀性的影响。颗粒的形成机制，液滴渗透时间，颗粒形态和内部结构已在粗微晶纤维素（MCC）和细对乙酰氨基酚（APAP）的混合物中进行了研究。当APAP量增加（减小粒度和增加疏水性）时，液滴渗透时间增加，形成机制从铺展转变为隧道化，颗粒尺寸变小，并且颗粒的内部孔隙率降低（Gao等人，2018年）。在目前的研究中，单滴造粒MCC和APAP的混合物具有不同的粒径的形成机制和颗粒形态进行了研究。此外，通过X射线显微CT表征了粉末床的堆积结构，并通过紫外-可见光谱法测量了API含量均匀性。结果表明，在粗MCC和细APAP混合物中，当APAP含量为25%时，混合物内部结构变得不均匀，在粉床和颗粒中均出现了致密聚集体区域，在此区域内发生了由铺展向隧道化的转变。细粉床中颗粒的含量均匀性比粗粉床中颗粒的含量均匀性要差得多（表明实际值与理论值之间存在差异）。当APAP在粉末床中的比例较高（高于50%）时，这种含量差异变得更大。这是以前观察到的其他研究人员（Nguyen等人，2010），并归因于成分的优先润湿。认为粉床的一次粒径比疏水性对形成机理、颗粒内部结构和含量均匀性的影响更大。
Single drop granule formation on a static powder bed of pharmaceutical mixtures was studied to investigate the effects of hydrophobicity and primary particle size distribution on the powder bed packing structure and the content homogeneity of active pharmaceutical ingredient (API) in granules formed. The granule formation mechanisms, drop penetration time, granule morphology and internal structure have been previously investigated in a mixture of coarse microcrystalline cellulose (MCC) and fine acetaminophen (APAP). When the APAP amount increased (decreasing particle size and increasing hydrophobicity), drop penetration time increased, formation mechanisms transitioned from Spreading to Tunneling, the granules became smaller in size, and the internal porosity of the granules decreased (Gao et al., 2018). In the current study, single drop granulation on mixtures of MCC and APAP with different particle sizes were investigated for formation mechanisms and granule morphology. Additionally, the powder bed packing structure was characterized by X-ray micro-CT and the API content uniformity was measured by UV–vis spectrometry. It was found that in the mixture made from coarse MCC and fine APAP, the internal structure became heterogeneous and there were dense aggregate regions in both the powder bed and granules from 25% APAP proportion, where the transition from Spreading to Tunneling occurs. The content uniformities of granules from fine powder beds are much more compromised (indicating a discrepancy between the actual value and theoretical value) than those from coarse powder beds. This content discrepancy becomes much larger when the APAP proportion in the powder bed is higher (above 50%). This was previously observed by other researchers (Nguyen et al., 2010) and was attributed to the preferential wetting of the ingredients. It is believed that the primary particle size of the powder bed is more significant than the hydrophobicity in affecting the formation mechanism, granule internal structure, and content uniformity.
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