Tanaka Akiko, Furubayashi Tomoyuki, Yamasaki Hitomi, Takano Katsuko, Kawakami Mayuko, Kimura Shunsuke, Inoue Daisuke, Katsumi Hidemasa, Sakane Toshiyasu, Yamamoto Akira
IEEE Trans Nanobioscience. 2016 Dec;15(8):798-803. doi: 10.1109/TNB.2016.2612682. Epub 2017 Jan 4.
For nasal drug absorption, powder formulations can be expected to provide many advantages. The first aim of this study was to examine drug absorption following nasal administration of powder formulations in rats. Pharmaceutical excipients are typically added to most powder formulations. The second aim was to investigate the change in nasal drug absorption of powder formulations in the presence of sodium carboxymethyl cellulose (CMC-Na). Model drugs used were norfloxacin (NFX), warfarin (WF), and piroxicam (PXC). The absorption from bulk powders is different from that of solutions. The absorption of PXC and WF from powder formulations was enhanced compared to those of the other solutions, while that of NFX, which has a low solubility, was decreased, suggesting that the nasal absorption of many drugs, except poorly soluble drugs, is enhanced when they are administered as powder formulations. CMC-Na enhanced the absorption of NFX and PXC. The presence of CMC-Na slightly decreased the absorption of WF. In vitro transepithelial transport from the powder formulation was not affected by the presence of CMC-Na. Furthermore, the nasal retention of the powder formulation was significantly increased in the presence of CMC-Na. In conclusion, the nasal absorption of many drugs, except those that are poorly soluble, can be increased by administering them as a powder formulation and the nasal absorption of the formulation is enhanced further in the presence of CMC-Na.
对于鼻腔给药吸收而言,粉末制剂有望具备诸多优势。本研究的首要目的是考察大鼠鼻腔给予粉末制剂后的药物吸收情况。大多数粉末制剂通常会添加药用辅料。第二个目的是研究在羧甲基纤维素钠(CMC-Na)存在的情况下粉末制剂鼻腔药物吸收的变化。所使用的模型药物为诺氟沙星(NFX)、华法林(WF)和吡罗昔康(PXC)。来自散装粉末的吸收与溶液的吸收不同。与其他溶液相比,PXC和WF从粉末制剂中的吸收增强,而溶解度低的NFX的吸收降低,这表明许多药物(除难溶性药物外)以粉末制剂给药时鼻腔吸收会增强。CMC-Na增强了NFX和PXC的吸收。CMC-Na的存在使WF的吸收略有降低。粉末制剂的体外跨上皮转运不受CMC-Na存在的影响。此外,在CMC-Na存在的情况下,粉末制剂的鼻腔滞留显著增加。总之,许多药物(除难溶性药物外)以粉末制剂给药可增加鼻腔吸收,并且在CMC-Na存在的情况下制剂的鼻腔吸收会进一步增强。