Preparation and controlled release of colon-targeted carboxymethylchitosan microspheres containing levofloxacin; an in vivo study
- Author:
Yang LI
1
Author Information
1. Department of General Surgery
- Publication Type:Journal Article
- From:
Academic Journal of Second Military Medical University
2006;27(5):517-520
- CountryChina
- Language:Chinese
-
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 °C. 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 λem 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.
