Pharmaceutics Department, Faculty of Pharmacy, Helwan University, Cairo, Egypt.
International Center for Bioavailability, Pharmaceutical and Clinical Research (ICBR), Cairo, Egypt.
Drug Dev Ind Pharm. 2020 May;46(5):762-774. doi: 10.1080/03639045.2020.1753062. Epub 2020 Apr 20.
The development of nanosuspension for targeted delivery of glibenclamide as hypoglycemic agent to the lung in an inhaler dosage form. Glibenclamide nanosuspension formulations were prepared using Box-Behnken design to investigate the effect of independent factors on the dependent variables, Fourier-transform Infrared spectroscopy, Differential Scanning Calorimetry, evaluation of glibenclamide nanosuspension inhaler and hypoglycemic efficacy were performed to determine glibenclamide nanosuspension inhaler effect. The results revealed that the mean particle sizes of the prepared nanosuspension ranged from 0.216 to 0.856 µm, zeta potential from +9 to +16 mV, the solubility ranged from 43% to 75%, the mass median aerodynamic diameter was 2.34 µm and the glucose level in rat was significantly reduced by about 60%. These results confirmed that glibenclamide nanosuspension inhaler enhance hypoglycemic effectiveness and reduce adverse effect of glibenclamide, opening up new dosage form in Diabetes mellitus treatment.
将格列本脲制成纳米混悬剂，作为一种吸入剂型的肺部靶向递药的降血糖药物。采用 Box-Behnken 设计制备格列本脲纳米混悬剂配方，考察各独立因素对各因变量的影响。采用傅里叶变换红外光谱、差示扫描量热法、评价格列本脲纳米混悬剂吸入剂和降血糖效果来确定格列本脲纳米混悬剂吸入剂的效果。结果表明，所制备的纳米混悬剂的平均粒径范围为 0.216 至 0.856 µm，zeta 电位范围为+9 至+16 mV，溶解度范围为 43%至 75%，质量中值空气动力学直径为 2.34 µm，大鼠血糖水平显著降低约 60%。这些结果证实，格列本脲纳米混悬剂吸入剂增强了降血糖效果，降低了格列本脲的不良反应，为糖尿病治疗开辟了新的剂型。
