Study on formability of solid nanosuspensions during nanodispersion and solidification: I. Novel role of stabilizer/drug property
Study on formability of solid nanosuspensions during nanodispersion and solidification: I. Novel role of stabilizer/drug property
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固体纳米混悬剂纳米分散和固化过程中的形成性研究：一、稳定剂/药物性质的新作用
DOI：
10.1016/j.ijpharm.2013.06.050
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发表时间：
2013-09-15
影响因子：
5.8
通讯作者：
Wang, Chang-Hong
中科院分区：
文献类型：
--
作者：
Yue, Peng-Fei;Li, Yu;Wang, Chang-Hong
到目前为止，很少或根本没有人尝试从药物性质和稳定剂的特性方面来了解固体纳米悬浮剂在纳米分散和固化过程中的可行性。为了建立药物化合物和稳定剂在纳米分散和固化过程中的物理化学性质对固体纳米悬浮液产生影响的知识库，首先对8种结构不同的药物化合物在3种浓度下对10种不同的稳定剂进行了比较研究。合成聚合物(HPMC、PVP K30、CMS-Na和MC)在纳米分散过程中表现出较差的稳定性能(平均成功率为10%)，但在冷冻和冷冻干燥过程中使用较高浓度的聚合物表现出较好的稳定性。同时，在纳米分散过程中，表面活性剂基团的影响更加明显。然而，表面活性剂稳定的固体纳米悬浮液在冷冻和冷冻干燥过程中以设定的浓度使用时，成型性最差。从药物性质的角度来看，药物的表面疏水性和结合能决定了固体纳米悬浮液在纳米分散和固化过程中的成形性。润湿指数(K)和Delta E与形成稳定的固体纳米悬浮液的可行性直接相关，这可以给出一种处方设计策略，从哪里可以得到具有一系列性质的候选药物和稳定剂。(C)2013爱思唯尔B.V.保留所有权利。
Few or no attempts have been made so far to understand the feasibility of solid nanosuspension formulation during nanodispersion and solidification in terms of drug properties and stabilizer characterizations. In order to establish a knowledge base about the effect of physicochemical property of drug compounds and stabilizers on solid nanosuspension production during nanodispersion and solidification, a comparative study was firstly performed on 10 different stabilizers at 3 concentrations for 8 structurally different drug compounds. Synthetic polymers (HPMC, PVP K30, CMS-Na and MC) displayed a poor stabilizing performance (10% success rate on average) during nanodispersion, but polymers showed better potential when higher concentrations was applied during freezing and lyophilization. Meanwhile, an effect for the surfactants group was even more pronounced during nanodispersion. However, the solid nanosuspension stabilized by surfactants showed the worst formability potential when be applied in setted concentrations during freezing and lyophilization. From the point of view of drug property, it was found that the surface hydrophobicity and cohesive energy of drug, were responsible for the formability of the solid nanosuspension during nanodispersion and solidification. Wetting index (k) and Delta E were concluded to have a direct correlation on the feasibility of formation of a stable solid nanosuspension, which can give a formulation design strategy from where candidate drugs and stabilizers with a set of properties. (c) 2013 Elsevier B.V. All rights reserved.