布地奈德结肠定位片的大鼠结肠靶向性评价

Evaluation on the Colon-Targeting Characteristics of Budesonide Colonic Localization Tablet in Rat

目的比较大鼠口服不同布地奈德制剂后药物在胃肠道各段中的组织浓度,评价布地奈德结肠定位片的结肠定位效果。方法大鼠分别饲服布地奈德定位片、布地奈德普通片和布地奈德混悬液后,定时取样,采用HPLC测定药物在大鼠胃、小肠、大肠等各组织中的浓度分布。结果大鼠口服定位片后,大肠组织中的药物浓度于6 h时达到峰值,cmax=(7.17±2.32)μg·g-1,明显高于混悬液组(1.37±0.82)μg·g-1和普通片组(0.47±0.18)μg·g-1;考察同一时间不同口服制剂对布地奈德在大鼠胃肠道组织分布的影响,发现口服定位片后,除大肠组织外,在胃部和小肠部等其他组织均无药物分布。结论布地奈德结肠定位片具有显著的结肠靶向性。

OBJECTIVE To evaluate the colon-targeting effects of budesonide colonic localization tablet by comparing the budesonide concentration in gastrointestinal tissue after oral administration of different budesonide preparations. METHODS The different tissue fluids were sampled and the HPLC method was used to determine the budesonide concentration in stomach, small intestine, large intestine tissue after budesonide localization tablet, budesonide tablet and budesonide suspension were administrated in rats, respectively. RESULTS With oral administration of budesonide localization tablets, the peak concentration of budesonide [ Cmax = （7. 17± 2. 32）μg·g^-1] in large intestine tissue was reached at the 6 h and it was significantly higher than that of suspension group （1.37 ±0. 82 ） μg·g^-1 and common tablet group （0.47 ±0. 18 ）μg·g^-1 By investigating the effects of different oral preparations on the gastrointestinal tissue distribution of budesonide in rats at the same time, budesonide was found only in the large intestine tissue, but no drug was distributed in the stomach and the small intestine tissue with oral administration of budesonide localization tablet. CONCLUSION The budesonide colonic localization tablet has conspicuous colon-targeting property.