Vaculikova Eliska, Placha Daniela, Pisarcik Martin, Peikertova Pavlina, Dedkova Katerina, Devinsky Ferdinand, Jampilek Josef
Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, Brno 61242, Czech Republic.
Nanotechnology Centre, VSB-Technical University of Ostrava, 17. listopadu 15/2172, Ostrava 70833, Czech Republic.
Molecules. 2014 Nov 4;19(11):17848-61. doi: 10.3390/molecules191117848.
One approach for the enhancement of oral drug bioavailability is the technique of nanoparticle preparation. Risedronate sodium (Biopharmaceutical Classification System Class III) was chosen as a model compound with high water solubility and low intestinal permeability. Eighteen samples of risedronate sodium were prepared by the solvent evaporation technique with sodium dodecyl sulfate, polysorbate, macrogol, sodium carboxymethyl cellulose and sodium carboxymethyl dextran as nanoparticle stabilizers applied in three concentrations. The prepared samples were characterized by dynamic light scattering and scanning electron microscopy. Fourier transform mid-infrared spectroscopy was used for verification of the composition of the samples. The particle size of sixteen samples was less than 200 nm. Polysorbate, sodium carboxymethyl dextran and macrogol were determined as the most favourable excipients; the particle size of the samples of risedronate with these excipients ranged from 2.8 to 10.5 nm.
提高口服药物生物利用度的一种方法是纳米颗粒制备技术。选择阿仑膦酸钠(生物药剂学分类系统III类)作为具有高水溶性和低肠道渗透性的模型化合物。以十二烷基硫酸钠、聚山梨酯、聚乙二醇、羧甲基纤维素钠和羧甲基葡聚糖钠为纳米颗粒稳定剂,采用溶剂蒸发技术制备了18个阿仑膦酸钠样品,每种稳定剂应用三种浓度。通过动态光散射和扫描电子显微镜对制备的样品进行表征。采用傅里叶变换中红外光谱法验证样品的组成。16个样品的粒径小于200nm。聚山梨酯、羧甲基葡聚糖钠和聚乙二醇被确定为最有利的辅料;含有这些辅料的阿仑膦酸钠样品的粒径范围为2.8至10.5nm。