Studies On The Sustained-Release Tablets And Pellets Capsules For Levofloxacin Aspartate

Levofloxacin aspartate(LEF-ASP) was the water dissolvably salt of the levofloxacin(LEF). The salts of levofloxacin had better dissolvable character and stability.It was also reported that the salts making by aspartic acid and alkaline antibiotic possed great antibacterial action,low toxicity and adverse reaction. In this article, the preparation of sustained-release tablets and pellets capsules were included with the purpose of getting steady blood drug level and better therapeutic efficacy while decreasing the administration times. Pharmacokinetics of levofloxacin aspartate sustained-release pellets capsules in dogs were also included in this article.The methods of HPLC and UV were established.High performance liquid chromatographic method was conducted to assay the content of drug in tablets, Ultraviolet (UV) spectrophotometry method was conducted to assay the release of drug in vitro.The Papp and solubility of levofloxacin aspartate were investigated.The results showed that the drug had higher value of Papp in pH6.8 PBS while the solubility was comparatively high. Stability studies was also investigated.The methods of HPLC which assay the biology samples in rats and mouse were established.The methods were simple and sensitive.The mean plasma concentrations were determined after i.v. LEF-ASP and LEF to rats.The results showed that LEF-ASP fited two-compartments model and LEF fited single-compartment model. Pharmacokinetic parameters Ke, T_1/2(Ke), CL(s), MRT and K of LEF-ASP and LEF had no significance disparity;but AUC had a significance disparity. It was supposed that the main reason was that the molecular, dissolvability and conveying rate of LEF-ASP could have been changed after salification. Pharmacokinetic parameters V(c) of LEF-ASP and LEF were both high,which showed distribution of two drugs widely in vivo. The tissues concentrations were determined after i.v. LEF-ASP and LEF to mouse. The results showed that two drugs could distribute to all tissues rapidly and LEF-ASP possed higer drug concentration for a long time. All segments of the rats' intestine had absorption and no significant difference in absorption rage between each segments by the method of intestinal...