| Shistosoma japonica is a kind of pathogen that leads the parasitifer to serious pathological changes and death,which induce a great of loss for human health and husbandry. Shistosoma japonica lay numerous eggs after the migration into the liver once the cercarias invade into the skin of the host,during which a lot of factors are related..The study aims at controling the prevalence and transmission of Shistosomasis.Allowing for the disadvantages such as inconvenient,low bioavailability and the fast metabolism when rumen domestic animal are takien Praziquantel orally,we have the dosage form of Praziquantel changed to find out akind of preparation that possesses curative effect and convenience.The preparation and pharmacokinetics were inspected as a focal point,which laid a foundation for the integrate control measure for shistosoma.1.The study of pharmacodynamics on Praziquantel injection.Many mice that infected by same cercarias artificially therapied with different formula.We analyzed lots of datas,and indexes on reduction of worm burden, reduction of eggs burden in livers reduction of hatching rate of eggs burden in livers, reduction of female polypide and preparation A was selected as a material for further research cohere with stability,stimulatory,difficulty of prepare.Injected dose of preparation.A at 600mg/kg.b.w,300mg/kg.b.w,100 mg/kg.b.w,50 mg/kg.b.w product significant curative effects,which was of dose dependent.600 mg/kg.b.w was optimal dose, and 50 mg/kg.b.w was not recommended dose。Preparation A was sensitive for schistosomulum and imaginal schistosome.And its reduction of worm burden was 94.23%, and reduction of eggs burden in livers was 89.2% after 30 day infected.Compared with control group,100%,100%,82.69%,94.5% absolutely in reduction of worm burden and reduction of eggs burden. Additional therapeutic test (56%,70.7%) was accordant with former results at 20th day.Trial of 3 times absolutely established that curative effect was straightforward at 20th day,and was of significant difference comparing with control group.Experiment of high concentration and slow-release agent confirmed that they were advantageous and promotive for insect disinfestation. Pathological changes of livers in infected mousse at different time-point of therpy showed that early treatment of preparation.A can grow downwards damage to host, and testrain pathogeny to spread at a certain degree.2.The study of pharmacokinetics on Praziquantel injectionWe constructed re-HPLC method which was of sensitiveness, accuracy and reproducibility。First time a mice was used for praziquantel preparation on pharmacokinetics.Preparation A and oral preparation were administrated respectively by subcutaneously and orally.Plasma that collected by venous blood in eyes was dealed to test drug in the re-HPLC method.Data Cmax,Tmax was surveyed,other parameters were obtained by software DAS 2.0Drug praziquantel was separated with plasma groundsubstance.Among 0.208μg/mL with 10.4μg/mL, blood drug level keep linear relationship with chromatographic peak area,as regression equation: C=0.000006*A+0.0149 (γ2=0.9994 n=3)。Relative standard deviation(RSD) of high,middle,low density intra-day (n=3) and day (n=3) as quality control was lower than 14%,13% separately. Absolute recovery was 60.25%,66.76%,70.72%.detectability was 50 ng/mL.Both preparation A and oral preparation were according with first-order and first elimination kinetic model. Preparation.A distributed quickly and eliminated slowly; absorb and elimination of oral preparation was swift.Half life of Preparation A, t1/2a was 2.047 h,while t1/26 was 69.315h.Clearance of oral preparation CL/F was 4.938 L/h/kg.Comparing with oral preparation,elimination half-time obviously extended.As for preparation A,it was easy to prepare and its administration was simple,so preparation A of high dose at a time will be promising toope spread in clinical operation.
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