羧基化碳纳米管负载羟基喜树碱的制备、表征及肠吸收特性考察  

Investigation of Preparation,Characterization and in vitro Intestinal Absorption Characteristics for Carboxylated Carbon Nanotubes Load Hydroxycamptothecin

作　　者：邓亚利[1] 林芳花[2] 何秀华[1] 周莉玲[3] 

机构地区：[1]华南农业大学制药工程系,广州510642 [2]惠州学院生命科学系,广东惠州516007 [3]广州中医药大学,广州510405

出　　处：《中国实验方剂学杂志》2013年第4期5-9,共5页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(30672669)

摘　　要：目的:研究羧基化多壁碳纳米管负载羟基喜树碱(HCPT)的制备工艺及负载物(HCPT-MWCNTs-COOH)的肠吸收特性。方法:比较球磨法、超声法与振荡法的吸附量差异,选择最优负载法;负载物采用FIR,紫外光谱进行表征,通过HPLC测定其含量;采用离体外翻肠囊模型研究负载物在不同肠段的吸收特性,HPLC测定样品质量浓度,计算吸收速率常数(Ka)。结果:冷冻球磨法负载量最高(12.5 mg.g-1);紫外、红外图谱变化表明碳纳米管负载了HCPT;肠吸收试验表明随HCPT质量浓度上升,肠吸收速率常数呈线性增加;高质量浓度在十二指肠、空肠、回肠、结肠的Ka分别为150.9,92.7,148.9,183.0 ng.cm-2.h-1,在各个肠段的Ka均无显著性差异。结论:负载物中HCPT溶解性增加并保护了内酯环,提高了肠透过速率;在小肠中为被动扩散吸收。Objective： To study on preparation process of carboxylated multi-walled carbon nanotubes load hydroxycamptothecin （HCPT） and intestine absorption characteristics of HCPT-MWCNTs-COOH. Method： Optimum load method for HCPT-MWCNTs-COOH was selected by comparing adsorption capacity of oscillation method, milling method and ultrasonic method; FIR and UV spectroscopy were used to characterize, the content of it was determined by HPLC ; Isolated everted intestine model was used to investigate absorption characteristics in different regions of rat intestine （duodenum, jejunum, ileum, colon ）, the concentration of samples were determined by HPLC, and calculated absorption rate constant （Ka）. Result： Ball milling method with frozen had the highest load （12.5 mg ~ g-l） for preparing HCPT-MWCNTs-COOH; FIR and UV spectroscopy changes showed carbon nanotubes had loaded HCPT. Intestine absorption test showed that Ka increased linearly along with increasing of HCPT concentration; Ka had no significant difference between different regions of intestines, Ka of the high concentration in duodenum, jejunum, ileum, colon were 150.9, 92.7, 148.9, 183.0 ng cm-2 h-1, respectively. Conclusion： Solubility of HCPT and intestine transmission rate in the load were increased and lactone ring was protected; The load in small intestine was passive diffusion absorption.

关 键 词：羧基化碳纳米管 羟基喜树碱 离体外翻肠囊模型 肠吸收 

分 类 号：R283.6[医药卫生—中药学]