Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour, Egypt.
Department of Clinical & Hospital Pharmacy, Faculty of Pharmacy, Taibah University, AL-Madinah AL-Munawarah, Kingdom of Saudi Arabia.
Ther Deliv. 2020 Jul;11(7):447-464. doi: 10.4155/tde-2020-0042. Epub 2020 Jul 26.
To study the impact of various permeability enhancers on fexofenadine bioavailability. Furthermore, to predict the potential effect of Cremophor RH 40 on fexofenadine pharmacokinetics at higher doses using Biopharmaceutical Classification System criteria. The effect of the dose increase (60-360 mg) on the dissolution and permeability behavior of fexofenadine-Cremophor RH 40 formulations was studied in humans. The Biopharmaceutical Classification System criteria of the drug was determined. Cremophor RH 40 improved the dissolution and bioavailability of fexofenadine. The pharmacokinetics increased linearly with the dose increase. Absorption number (A) was significantly increased after addition of Cremophor RH 40 in comparison to an unprocessed drug. Similar A values were observed throughout the same dose range. The dose number (D) values were <1 whereas, all the dissolution number (D) values were >1 at the same dose level.
研究各种渗透增强剂对非索非那定生物利用度的影响。此外，根据生物药剂学分类系统标准，预测更高剂量的聚氧乙烯氢化蓖麻油（Cremophor RH 40）对非索非那定药代动力学的潜在影响。在人体中研究了剂量增加（60-360mg）对非索非那定-Cremophor RH 40 制剂的溶解和渗透行为的影响。确定了药物的生物药剂学分类系统标准。聚氧乙烯氢化蓖麻油（Cremophor RH 40）提高了非索非那定的溶解和生物利用度。药代动力学随剂量增加呈线性增加。与未加工药物相比，添加聚氧乙烯氢化蓖麻油（Cremophor RH 40）后吸收数（A）显著增加。在相同的剂量范围内观察到相似的 A 值。剂量数（D）值<1，而在相同剂量水平下，所有的溶解数（D）值>1。
