羧基化碳纳米管-醋氯芬酸的离体肠吸收特性变化研究

Intestinal Absorption of Carboxylated Carbon Nanotubes-Aceclofenac in vitro

目的:研究羧基化多壁碳纳米管负载醋氯芬酸(AC)的制备工艺,以及负载物(AC-MWCNTs-COOH)的肠吸收特性。方法:采用冷冻球磨法制备负载物,采用FIR、紫外光谱进行表征;采用离体外翻肠囊模型研究AC及负载物在不同肠段的吸收特性,采用HPLC法测定样品浓度,计算吸收速率常数(Ka)。结果:AC原料与负载物均随着药液中AC浓度上升,Ka呈线性增加;负载物的Ka均低于AC原料。AC原料在各个肠段的Ka差异均无统计学意义(P>0.05),而负载物在十二指肠的Ka大于空肠、回肠、结肠,后三者差异无统计学意义(P>0.05);负载物浓度为0.54 mg·ml-1时,各肠段的Ka依次为0.740 6、0.129 2、0.181 3、0.241 1μg·h-1·cm-2。结论:负载物具有缓释效果,在小肠内的Ka与原料相比发生改变;在小肠中均为被动扩散吸收。

Objective：To study the preparation process and in vitro intestine absorption of aceclofenac （AC）-loaded carboxylated multi-walled carbon nanotubes （AC-MWCNTs-COOH）.Methods：Frozen ball milling method was used to prepare AC-loaded carboxylated multi-walled carbon nanotubes,and then FIR and UV spectroscopy were applied in the characterization.The isolated everted intestine model was used to study the absorption in different regions of rat intestine（duodenum,jejunum,ileum and colon）.The samples were collected at different times and determined by HPLC.Results：The intestine absorption rate constant （Ka） was increased with the AC concentration.The Ka of AC-MWCNTs-COOH was lower than that of AC solution.The Ka of AC had no significant difference among various intestine regions （P 〉 0.05）,while the Ka of AC-MWCNTs-COOH showed the difference.The Ka of duodenum was greater than that of jejunum,ileum and colon while there was no significant difference among the latter three （P 〉 0.05）,and the Ka was 0.740 6,0.129 2,0.1813 and 0.2411 μg · h-1 · cm-2 correspondingly with the AC concentration of 0.54 mg · mL-1.Conclusion：The absorption of AC and AC-MWCNTs-COOH shows passive diffusion process with different Ka.