Formation of fine drug particle by cogrinding with cyclodextrins. Part II. The influence of moisture condition during cogrinding process on fine particle formation.
Formation of fine drug particle by cogrinding with cyclodextrins. Part II. The influence of moisture condition during cogrinding process on fine particle formation.
复制标题
通过与环糊精共研磨形成细小的药物颗粒。
DOI：
10.1016/s0378-5173(03)00409-5
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发表时间：
2003
影响因子：
5.8
通讯作者：
Keiji. Yamamoto
中科院分区：
文献类型：
--
作者：
A. Wongmekiat;Y. Tozuka;T. Oguchi;Keiji. Yamamoto
本研究的目的是探讨共研磨过程中的水分条件对药物微粒形成的影响。以环糊精（CD）：普仑司特（Pranlukast）半水合物（Pranlukast）摩尔比为2：1，在不同的湿度条件下进行共研磨，并研究了Pranlukast亚微米颗粒的形成。在共磨过程中的水分含量显着影响细颗粒的形成。当与α-CD、β-CD或γ-CD共研磨时，超过90%的普仑司特负载转化为亚微米颗粒，其中每个CD系统含有特定量的水。环糊精的微粒形成被认为是环糊精特有的现象，因为当使用d-甘露醇、乳糖或微晶纤维素（MCC）作为共研磨添加剂时，不能形成亚微米颗粒。此外，发现细颗粒形成的出现和消失是可逆的，这取决于研磨过程中水的存在。
The purpose of this study was to investigate the effect of moisture condition during cogrinding process on fine drug particle formation. Cogrinding of cyclodextrins (CDs) and pranlukast (PRK) hemihydrate was performed in various moisture conditions at a mixing molar ratio of 2:1 (CDs:PRK) and the formation of PRK submicron particle was investigated. The moisture content in the cogrinding process significantly affected the fine particle formation. More than 90% of pranlukast loaded transformed to submicron particles when coground with α-CD, β-CD or γ-CD containing the specific amount of water for each CD system. Fine particle formation of PRK was considered as a particular phenomenon to cyclodextrins, since the submicron particles could not be formed when d-mannitol, lactose or microcrystalline cellulose (MCC) was used as a cogrinding additive. Moreover, the appearance and disappearance of fine particle formation was found to be reversible depending on the existence of water during the grinding process.