| 摘要: |
| 目的:制备左氧氟沙星羧甲基壳聚糖(LVFX/CMC)微球并检测其在大鼠体内结肠靶向释药的性能.方法:色谱柱:KromasilRKR100-5C18(250 mm×4.6 mm),流动相:乙腈-0.1％三氟醋酸溶液(2080),柱温:50℃,激发波长:295 nm,发射波长:495 nm,流速:1.0 ml/min .SD大鼠60只,随机分为2组,分别以LVFX/CMC微球(含40 mg左氧氟沙星)及等量左氧氟沙星溶剂灌胃,以高效液相色谱法对LVFX/CMC微球和左氧氟沙星(LVFX)灌胃后大鼠胃、小肠、盲肠、结肠及血液中药物浓度进行定量检测.结果:灌胃后LVFX/CMC微球组5 h盲肠、结肠药量分别达(3.394±0.197)和(1.873 ±0.216) mg,远高于LVFX组的(0.489±0.123)和(0.078±0.002) mg (P<0.01).在9 h时LVFX/CMC微球组盲肠和结肠药量仍分别达到(1.580±0.234)和(0.713±0.073) mg,明显高于LVFX组的(0.105±0.023)和(0.054±0.016) mg (P<0.01).LVFX/CMC微球组血药浓度于5 h后达到最高,而LVFX组1 h后即达最高血药浓度峰.微球组盲肠和结肠内容物的药量在7、9 h时段均明显大于胃和小肠内的药量.结论:左氧氟沙星羧甲基壳聚糖微球在体内实验中的释放符合结肠靶向释药的特点. |
| 关键词: 左氧氟沙星羧甲基壳聚糖、微球体、结肠 |
| DOI：10.3724/SP.J.1008.2006.00517 |
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| 基金项目:全军医药科研基金指令性课题（01L056）. |
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| Preparation and controlled release of colon-targeted carboxymethylchitosan microspheres containing levofloxacin:an in vivo study |
| 李扬,王强,钱方,沈宏亮,LI Yang,WANG Qiang,QIAN Fang,SHEN Hong-liang |
| () |
| Abstract: |
| Objective：To prepare levofloxacin-carboxymethyl-chitosan （LVFX/CMC） microspheres and to study their colon-targeted release in rats. Methods： KromasilRKR100-5C18（250 mm× 4.6 mm）was used as the analytical column and the temperature was maintained at 50℃. The mobile phase consisted of a mixture of acetonitrile： 0. 1 % trifluoroacetic acid （20 ： 80） pumped at a flow rate of 1.0 ml/min, with λex 295 nm and hem 495 nm. Sixty healthy male SD rats were randomized into 2 groups： to receive gastric lavage with normal LVFX （40 mg,control group） and LVFX/CMC microspheres （40 mg,treatment group）. HPLC was used to detect the concentrations of LVFX in the stomach,intestine,cecum,colon and blood in rats in both groups. Results： LVFX was detectable 3 h after LVFX/CMC microsphere lavage. Five hours after lavage,the levels of LVFX in cecum and colon were respectively （3. 394±0. 197） mg and （1. 873±0. 216） mg in treatment group,and （0. 489±0. 123） mg and （0. 078±0. 002） mg in control group （P〈0. 01） . Nine hours after lavage,the levels of LVFX in cecum and colon were （1. 580±0. 234） mg and （0. 713±0. 073） mg in treatment group,and （0. 105±0. 023） mg and （0. 054±0. 016） mg in control group（P〈0.01） ,respectively. Serum level of LVFX peaked at 5 h in treatment group and at 1 h in control group. The concentrations of LVFX were obviously higher in cecum and colon than those in stomach and intestine. Conclusion： The prepared LVFX/CMC microspheres have the property of colon-targeted release in rats. |
| Key words: levofloxacin-carboxymethyl-chitosan microshperes colon |
