A simple blending with α-glycosylated naringin produce the enhancement of solubility and absorption of pranlukast hemihydrate
A simple blending with α-glycosylated naringin produce the enhancement of solubility and absorption of pranlukast hemihydrate
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与 α-糖基化柚皮苷简单混合可增强普仑司特半水合物的溶解度和吸收
DOI：
10.1016/j.ijpharm.2019.118490
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发表时间：
2019
期刊：
影响因子：
--
通讯作者：
Y. Tozuka
中科院分区：
文献类型：
--
作者：
H. Uchiyama;K. Kadota;A. Nakanishi;M. Tandia;Y. Tozuka
针对水溶性极低的模型药物普仑司特半水合物 (PLH)，研究了新开发的 α-糖基化柚皮苷 (Naringin-G) 作为增溶剂的可能性。与 PLH 晶体和含有其他添加剂（如 α-糖基化芦丁 (Rutin-G) 和十二烷基硫酸钠 (SDS)）的 PM 相比，PLH/柚皮苷-G 的物理混合物 (PM) 增加了 PLH 的溶解度。柚皮苷-G 不会降低表面张力，而 SDS 显示出表面活性特性和临界胶束浓度。 PLH 的表观溶解度与柚皮苷-G 的浓度成比例增加，对于 SDS 也类似，表明恒定量的柚皮苷-G 分子与 PLH 分子相互作用。与高浓度柚皮苷-G 溶液（10%（w/v））接触后，Caco-2 细胞活力没有变化。当与柚皮苷-G 一起给药时，大鼠动物模型中 PLH 的口服吸收得到改善。 PLH/柚皮苷-G PM 的血浆浓度-时间曲线下面积值比单独 PLH 晶体高 2.2 倍。总之，这些结果表明新合成的柚皮苷-G 将成为一种有前途的增溶剂，作为表面活性剂的替代品。
The possibility of newly developed α-glycosylated naringin (Naringin-G) as a solubilizing agent was investigated against pranlukast hemihydrate (PLH), a model drug with extremely low water solubility. The physical mixtures (PMs) of PLH/Naringin-G increased the solubility of PLH compared with PLH crystals and PMs with other additives, such as α-glycosylated rutin (Rutin-G) and sodium dodecyl sulfate (SDS). Naringin-G did not decrease the surface tension, whereas SDS showed a surface-active property and critical micelle concentration. The apparent solubility of PLH increased in proportion to the concentration of Naringin-G, and similarly for SDS, indicating that constant amounts of Naringin-G molecules interacted with PLH molecules. There was no change in the Caco-2 cell viability following contact with a high concentration of Naringin-G solution (10% (w/v)). The oral absorption of PLH in a rat animal model was improved when administrated with Naringin-G. The value for the area under plasma concentration–time curve from PMs of PLH/Naringin-G was 2.2 times higher than that from PLH crystals alone. Together, these results suggested that newly synthesized Naringin-G would be a promising solubilizing agent as an alternative to surfactants.