Liu Guoqiang, Dong Leilei, Lu Kuan, Liu Sisi, Zheng Yingying
Department of Pharmacy, The Third Hospital of Hebei Medical University, Shijiazhuang 050051, China.
The Third Hospital of Hebei Medical University, Shijiazhuang 050051, China.
Biomed Res Int. 2016;2016:1691579. doi: 10.1155/2016/1691579. Epub 2016 Aug 16.
Astragalus polysaccharide (APS) (used for intestinal protection) was added to formulate the Tongshu suppository to improve the pharmacokinetics of Aceclofenac, which were assessed in New Zealand rabbits using an orthogonal experimental design. The single-agent Aceclofenac was taken as the control formulation. The concentration-time and drug release curves were drawn, and T max (min), C max (μg·mL(-1)), AUC0→∞ , and MRT were compared using a pharmacokinetic systems program. The formulated Tongshu suppository had moderate hardness, a smooth surface with uniform color, and theoretical drug-loading rate of 8%. Its release rate was in accordance with the drug preparation requirements. The concentration-time curves and drug release curves revealed that the maximum concentrations (C max) were 4.18 ± 1.03 μg·mL(-1) and 3.34 ± 0.41 μg·mL(-1) for the Tongshu and Aceclofenac suppositories, respectively, showing statistically insignificant difference, while the peak times were 34.87 ± 4.69 min and 34.76 ± 6.34 min, respectively, also showing statistically insignificant difference. Compared with the Aceclofenac suppository, the relative bioavailability of the Tongshu suppository was 104.4%, and the difference between them was statistically insignificant. In this experiment, the Tongshu suppository was prepared using the hot-melt method. In vivo pharmacokinetic studies confirmed it had higher bioavailability than the Aceclofenac suppository.
将用于肠道保护的黄芪多糖（APS）添加到通舒栓中，以改善醋氯芬酸的药代动力学，采用正交试验设计在新西兰兔身上进行评估。以单药醋氯芬酸作为对照制剂。绘制浓度-时间曲线和药物释放曲线，并使用药代动力学系统程序比较Tmax（分钟）、Cmax（μg·mL-1）、AUC0→∞和MRT。所制备的通舒栓硬度适中，表面光滑、色泽均匀，理论载药率为8%。其释放速率符合药物制剂要求。浓度-时间曲线和药物释放曲线显示，通舒栓和醋氯芬酸栓的最大浓度（Cmax）分别为4.18±1.03μg·mL-1和3.34±0.41μg·mL-1，差异无统计学意义，而达峰时间分别为34.87±4.69分钟和34.76±6.34分钟，差异也无统计学意义。与醋氯芬酸栓相比，通舒栓的相对生物利用度为104.4%，两者差异无统计学意义。本实验中，通舒栓采用热熔法制备。体内药代动力学研究证实其生物利用度高于醋氯芬酸栓。
