李家政, 富雪丹, 张兰, 刘鑫, 肖婉, 宁青, 张振海, 鞠建明. 多孔二氧化硅吸附和环糊精包合对桂皮醛释放和药动学的影响J. 药学学报, 2025, 60(7): 2324-2341. DOI: 10.16438/j.0513-4870.2024-1088
引用本文: 李家政, 富雪丹, 张兰, 刘鑫, 肖婉, 宁青, 张振海, 鞠建明. 多孔二氧化硅吸附和环糊精包合对桂皮醛释放和药动学的影响J. 药学学报, 2025, 60(7): 2324-2341. DOI: 10.16438/j.0513-4870.2024-1088
LI Jia-zheng, FU Xue-dan, ZHANG Lan, LIU Xin, XIAO Wan, NING Qing, ZHANG Zhen-hai, JU Jian-ming. Effect of porous silica adsorption and β-cyclodextrin inclusion on the release and pharmacokinetics of trans-cinnamaldehydeJ. Acta Pharmaceutica Sinica, 2025, 60(7): 2324-2341. DOI: 10.16438/j.0513-4870.2024-1088
Citation: LI Jia-zheng, FU Xue-dan, ZHANG Lan, LIU Xin, XIAO Wan, NING Qing, ZHANG Zhen-hai, JU Jian-ming. Effect of porous silica adsorption and β-cyclodextrin inclusion on the release and pharmacokinetics of trans-cinnamaldehydeJ. Acta Pharmaceutica Sinica, 2025, 60(7): 2324-2341. DOI: 10.16438/j.0513-4870.2024-1088

多孔二氧化硅吸附和环糊精包合对桂皮醛释放和药动学的影响

Effect of porous silica adsorption and β-cyclodextrin inclusion on the release and pharmacokinetics of trans-cinnamaldehyde

  • 摘要: 探讨不同固化方式对桂皮醛(trans-cinnamaldehyde, CA) 的体外释放和药动学的影响。采用多孔二氧化硅吸附和β-环糊精包合对CA进行固化和表征, 测定释放度, 并对SD大鼠进行药动学研究。通过差示扫描量热法、X射线衍射分析和傅里叶变换红外光谱等分析技术验证了两种固化物的成功制备。在pH值为1.2、4.5和6.8的条件下, 两种固化方式均能显著提高CA的累积释放度, 多孔二氧化硅吸附加速了CA的初期体外释放, 大鼠的Cmax有所提高, AUC0-∞显著增加, β-环糊精包合可以延缓CA的初期体外释放, 大鼠体内Cmax明显降低, AUC0-∞显著增加。所有动物实验经江苏省中西医结合医院动物伦理委员会批准(伦理号: AEWC-20220815-230)。上述结果表明, 相对于CA, 多孔二氧化硅吸附可以提高CA的初期释放和AUC0-∞, β-环糊精包合CA则在一定程度上延缓了CA的初期释放, 降低了Cmax, 提高了AUC0-∞

     

    Abstract: This study investigates the effects of various curing methods on the dissolution, in vitro release, and pharmacokinetics of trans-cinnamaldehyde (CA). CA was cured and characterized using porous silica adsorption and β-cyclodextrin inclusion. The dissolution and release profiles were determined, followed by conducting comprehensive pharmacokinetic studies in SD rats. The successful preparation of the two cures was verified by analytical techniques such as differential scanning calorimetry, X-ray diffraction analysis, and Fourier transform infrared spectroscopy. Both curing methods significantly increased the cumulative dissolution and cumulative release of CA at pH 1.2, 4.5 and 6.8. In comparison to free CA, the use of porous silica adsorption not only enhanced the in vitro release of CA but also significantly increased its Cmax and the AUC0-∞ in rats. β-Cyclodextrin inclusion delays CA release in vitro, decreases Cmax in vivo in rats and significantly increases AUC0-∞. All animal experiments were approved by the Animal Ethics Committee of Jiangsu Province Hospital of Integrated Traditional Chinese and Western Medicine (Ethics Approval Number: AEWC-20220815-230). Our findings revealed that porous silica adsorption significantly enhanced both the in vitro release and the in vivo uptake rate of trans-cinnamaldehyde. Conversely, β-cyclodextrin inclusion of CA led to a noticeable retardation in its in vitro release and a moderate decrease in the in vivo uptake rate.

     

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