Preparation Of Ciprofloxacin Sustained Release Particles

Object: Prepararing of Ciprofloxacin sustained release formulation with mordenpharmacy technique, offering a safety,high efficiency and convenient new dosageform for health care of Animals.Content and Methods: Making ciprofloxacin material, to prepare Ethyl Cellulosenanoparticles by the way of evaporation from liquor and Gelatin microspheres in W/O microemulsion. Research the prescription and acertain the main influencing factors;characterized in terms of morphology,size,encapsulation efficiency,etc.comparingsingle microparticles and complex microparticles in vitro drug release,then screensizing the best mixing ratio among EC nanoparticles,GL microspheres andciprofloxacin; Progression of bacteriostasis experiment in vitro and acute toxicity test,evaluating antibacterial activity in vitro and security in vivo; researched preliminarythe Ciprofloxacin sustained release medication's security and pharmacokinetics inrabbits.Results: The EC nanoparticles prepared with the optimized method had a mean diameterof 680nm,a drug content of 18.2ï¼…, and an enveloping rate of 84.5ï¼…. 90ï¼…of the drug wasreleased in 15d;The gelatine microspheres prepared with the optimized method had amean diameter of 4.Sum,the drug loading and enveloping rate were 19.2ï¼…and 89ï¼…, abave80ï¼…of the drug was released in 3d; the best complex sustaind release formulation wascomposed of EC nanoparticles, GL microspheres and ciprofloxacin, their rate was 2:4:1;after 100 hours, about 90ï¼…of the drug was released from the complex sustained releaseformulation; at the later period of the staphylococcal bacteria bacteriostasis experiment invitro, EC nanoparticles showed the controlled release antibacterial activity;themicroparticles' toxicity was very low, and the biggest dosage was 9500mg/kg in the acutetoxicity test for mouses; The T_1/2(Ke) of the sustained release medication was 23.9h inrabbits, it is sixfold as much as ciprofloxacin; the biocompatibility was 119.4ï¼…andtwofold as much as ciprofloxacin.Conclusion: The Ciprofloxacin complex sustained release medication showedsignificant sustained release effect, it was safety and innocuity for animals at the doserange. We hope exploit it as a new sustained release formulation.