纳米级片状羧甲基木薯淀粉作为固体分散体的赋形剂。
Nano-sized flake carboxymethyl cassava starch as excipient for solid dispersions.
机构信息
College of Chemistry and Materials Engineering, Wenzhou University, Wenzhou 325027, China.
出版信息
Int J Pharm. 2012 Feb 28;423(2):435-9. doi: 10.1016/j.ijpharm.2011.12.014. Epub 2011 Dec 17.
Nano-sized excipients were used in solid dispersions (SD) to enhance the dissolution rate of poorly water-soluble drug in this study. Nano-sized flake carboxymethyl cassava starch (CMCS) was firstly synthesized under ultrasonic irradiation. Then acetylsalicylic acid (ASA) was selected as water insoluble drug model to prepare solid dispersions using three different kinds of excipients. SD1 was prepared using native cassava starch as carrier. SD2 and SD3 were prepared using nano-sized CMCS (degree substitution, DS=1.15, 100-400 nm) and micro-sized CMCS (DS=0.36, 8-28 μm), respectively. These solid dispersions were characterized by powder X-ray diffractometry, scanning electron micrographs and dissolution. The results suggested that the SD2 prepared by nano-sized CMCS had much better dispersion capability for the drug than the other two solid dispersions. And the dissolution rate of SD2 was considerably higher than that of pure drug. These results indicated that the nanoscale CMCS was a kind of good carrier for solid dispersion to improve the solubility of poorly water-soluble drugs.
在本研究中，纳米级辅料被用于固体分散体（SD）中，以提高难溶性药物的溶解速率。首先在超声辐射下合成纳米片状羧甲基木薯淀粉（CMCS）。然后选择乙酰水杨酸（ASA）作为水不溶性药物模型，使用三种不同的辅料制备固体分散体。SD1 是使用天然木薯淀粉作为载体制备的。SD2 和 SD3 分别使用纳米级 CMCS（取代度，DS=1.15，100-400nm）和微米级 CMCS（DS=0.36，8-28μm）制备。通过粉末 X 射线衍射、扫描电子显微镜和溶解度对这些固体分散体进行了表征。结果表明，与其他两种固体分散体相比，由纳米级 CMCS 制备的 SD2 对药物具有更好的分散能力。并且 SD2 的溶解速率明显高于纯药物。这些结果表明纳米级 CMCS 是一种用于改善难溶性药物溶解度的固体分散体的良好载体。
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