Wanawongthai C, Pongpeerapat A, Higashi K, Tozuka Y, Moribe K, Yamamoto K
Graduate School of Pharmaceutical Sciences, Chiba University, Chiba, Japan.
Int J Pharm. 2009 Jul 6;376(1-2):169-75. doi: 10.1016/j.ijpharm.2009.04.034. Epub 2009 May 3.
Nanoparticles of a poorly water-soluble drug, probucol, have been obtained by co-grinding with PVP and SDS. The purpose of this study was to investigate the effect of the alkyl chain length of sodium alkyl sulfates (CnS, n=6, 8, 12, 16 and 18) on probucol nanoparticle formation. From the results of particle size determination and quantitative measurement of nanoparticle fraction of probucol by HPLC, it was found that the alkyl chain length of the sodium alkyl sulfate affected the probucol nanoparticle formation. The efficiency, based on the quantitative determination of nanoparticles, was in the order: C18S>C16S>C12S>C8S>C6S. Probucol nanoparticles of less than 800 nm were effectively produced (more than 95%) with the increase of the amount of surfactants. (13)C solid-state NMR of co-ground mixtures showed a new peak originating from the probucol interaction with PVP together with the existence of probucol crystal peaks. Excess amounts of surfactants were expected to play an important role for stabilizing the probucol nanoparticles in the suspension via the electrostatic repulsive effect.
通过与聚乙烯吡咯烷酮（PVP）和十二烷基硫酸钠（SDS）共同研磨，制备了难溶性药物普罗布考的纳米颗粒。本研究旨在考察烷基硫酸钠（CnS，n = 6、8、12、16和18）的烷基链长度对普罗布考纳米颗粒形成的影响。通过粒径测定结果以及用高效液相色谱法（HPLC）对普罗布考纳米颗粒部分进行定量测量发现，烷基硫酸钠的烷基链长度影响了普罗布考纳米颗粒的形成。基于纳米颗粒的定量测定，效率顺序为：C18S > C16S > C12S > C8S > C6S。随着表面活性剂用量的增加，有效制备出了粒径小于800 nm的普罗布考纳米颗粒（超过95%）。共研磨混合物的碳-13（¹³C）固态核磁共振显示，除了存在普罗布考晶体峰外，还有一个源自普罗布考与PVP相互作用的新峰。预计过量的表面活性剂通过静电排斥作用，在稳定悬浮液中的普罗布考纳米颗粒方面发挥重要作用。
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