The Pilot Study Of Roxithromycin Injection

Roxithromycin (RXM) is a semisynthetic macrolides antibiotic with a broad and essentially bateriostatic action against many Gram-positive and some Gram-negative bacteria,as well as some anaerobes.Roxithromycin has been widely used clinically to treat a variety of tissues and organs infection,especially as the first picked medicine to therapy pediatric respiratory tract infection. Late years, go with the new found of Pharmacological Action and the new use in non-infection about macrolide antibiotics, enlarge continually clinical uses of roxithromycin. In order to adapt to the demand of clinical uses,and offer multi-choice to medical staff and patients,inclusion compound of roxithromycin can be prepared by reaction with hydroxypropyl-β-cyclodextrin, roxithromycin injection prepared from the inclusion compound may fill up the vacancy that roxithromycin was not injection preparation.The thesis carried out investigate to roxithromycin injection.Through these studies of thermal stability , in vitro antibacterial activities, pharmacokinetics and relative bioavailability in goats,probing of dosage regimen to go by pharmacokinetics /pharmacodynamics(PK/PD) parameters and postantibiotic effect(PAE) in that roxithromycin injection was treat the infection caused by Staphylococcus in goats.Information available suggests that roxithromycin injection is a new dosage form possessing develop prospect extremely.Above all, roxithromycin injection suitable for clinical apply was selected by assessing the thermal stability of roxithromycin injection I and roxithromycin injection II ,which were respectively wraped by hydroxypropyl- β -cyclodextrin and γ -cyclodextrin. The inclusion compounds were prepared by trituration method. A reversed-phase HPLC method was developed for the determination of contents in RXM injection I and RXM injection II at different temperture and time.Initial equal-speed method was adopted to predict the period of validity.Results,expiry date of roxithromycin injection I is t_0.9^25℃=1.8a ,and t_0.9^25℃=0.87a for roxithromycin injection II .It showed roxithromycin injection I wraped by hydroxypropyl- β -cyclodextrin could be stored for 1 .8 year at room temperature .It is suitable for clinical circumstances demand.Secondly,to study bacteriostatic activity of the roxithromycin injection in vitro. As was demanded by the practicing principles of clinical new medicines, liquid doubling dilution method was used to detect the MIC of roxithromycin injection on tested strain: four Gram-positive bacteria and five Gram-negative bacteria. Results ,the MIC of roxithromycin injection to swine erysipelas, swine streptococcus, Listeria monocytogenes, staphylococcus aureus, swine pasteurella, avian pasteurella, swine coleocele, avian coleocele, avian salmonella were 0.098, 0.025, 0.098, 0.195,...