Study On The Pharmacokinetics And Bioavailability Of Forsythia And Amoxicillin Powder In PIG

The forsythia and amoxicillin powder has been developed for prevention and treatment of Streptococcus suits infections.It's made of amoxicillin and forsythia. In order to guide its clinical application,it is necessary to study its pharmacokinetic in the porcine.A sensitive and selective ultra performance liquid chromatography-tandem mass(UPLC-MS/MS)method for the determination of amoxicillin in the serum of porcine was developed. After a simple solid-phase extraction, the post-treatment samples were analyzed on a ACQUITY UPLCTM BEH C18 column interfaced with a triple quadruple tandem mass spectrometer. Positive electrospray ionization was employed as the ionization source. The mobile phase is acetonitrile-0.2%acetic acid(5:95,v/v).Multiple reaction monitoring using the precursor-product ion combifination of m/z366.3～349.2 was used to quantify amoxicillin. The linear calibration curves obtained in the concentration range of 0.06μg/mL～1μg/mL for amoxicillin. The recoveries of amoxicillin at the added concentration levels of 0.06μg/mL,0.25μg/mL,1μg/mL was (68.3±9.8)%,(72.0±6.7)%and(75.1±9.6)%, Within/day CV and inter/day CV are <10%.The method has a lower limit of quantification(LLOQ)of 0.03μg/mL for amoxicillin. The result shows that the method is consistent with the analysis of biological products and can be used to study the pharmacokinetics of amoxicillin .5 healthy pigs after oral administration of amoxicillin were used for the experiment. The date of drug concentration and time was one compartment model with 1st order absorption.The main pharmacokinetic parameters was(Cmax)were(0.96±0.29)μg/mL, Tp was(1.12±0.24)h. T1/2ka was(0.61±0.21)h, AUC were calculated to be(3.00±0.35)(μg/mL)*h. These datas show amoxicillin had good absorption,high drug concentration,widespread and quickly eliminating in swine.The method was application to study the pharmacokinetics of 5 healthy pigs after oral administration of amoxicillin compound. The date of drug concentration and time was according with one compartment model with 1st order absorption.The main pharmacokinetic parameters was(Cmax)were(0.96±0.37)μg/mL, Tp was(0.51±1.55)h. T1/2ka was(0.13±0.76)h, AUC were calculated to be ( 1.23±0.61 )(μg/mL ) *h. Pharmacokinetic parameters were statistical analysised.Single drug amoxicillin and Forsythia suspense after combined on pharmacokinetic parameters of amoxicillin had much effect. These show that Forsythia suspense don't enhance the absorption of amoxicillin, but it can accelerate the absorption of amoxicillin. Then it can maintain amoxicillin to the organization and accelerate the eliminate speed of amoxicillin in swine serum. Forsythia suspense reduced the time of roles with amoxicillin in swine.The method was application to study the pharmacokinetics of 5 healthy pigs after iv administration of amoxicillin compound.K21 were (3.301±0.78)1/h;K10 were(5.518±1.85)1/h;K21 were (15.463±2.54)1/h;AUC were (2.045±1.61)(μg/mL)*h;CLs were(7.335±1.25)mg/kg/h/(μg/mL);MRT were (2.560±3.21)h. It proves that the distribution and eliminate speed of the drug is rapid..The AUC of Amoxicillin compound by oral administration and by iv administration are (1.23±0.61)(μg/mL)*h and (2.045±1.61)(μg/mL)*h. Through the Formula, F is (60.14±2.56)%,therefore the absorption is good.