Amelioration Of Methazine Injection And Its Pharmacokinetics In Rabbits

Methylquine is a commonly used quinoxaline drug.The main dosage form is injection.The traditional cosolvent is salicylic acid and its salts.However,the study found that salicylic acid is a cosolvent in 5%of mequindox injections.The high salt content will affect its detection.At the same time,because salicylic acid and its salts have physiological and pharmacological effects,when its content is too high,there is a certain safety risk.Therefore,we improve the prescription of mequindox injection and filter out an analysis of the stability and muscle irritation of salicylic acid and its salts,and its pharmacokinetics in rabbits.1.Detection of equinox injection:Acetonitrile injection was performed on a C18column with a mobile phase of methanol-0.01mol/L phosphoric acid in water?pH=7?at 45:55 at a flow rate of 1.0 mL/min,and acetyl was detected at 25°C and 254 nm.Methylpurine,the results show that the high degree of separation,good peak shape,short peak time,a good linear relationship in the concentration range of 40⁶0?g/mL,its methodological inspection results show that high precision RSD<2%,recovery rate is greater than 95%,It can meet the detection of the content of mequindox injection.2.Through the screening of the solvent of mequindazine injection,according to different solvent proportions,the concentration of acetomethlyene,organic reagent,stability,finally a prescription was confirmed:the content of methoquinone was 5%the benzyl alcohol content was 10%,N-methylpyrrolidone 20%,sodium bisulfite0.2%,and pH 5.3.The photoperiod test,high temperature test and accelerated test were performed on the prepared mequindox injection.The results showed that the content was reduced after 4500±500Lx light exposure for 15 days,and the light was prevented from being stored and transported.The high temperature test and the accelerated test equinox injection were both it can exist stably,all indexes meet the requirements,and it can be used for intramuscular injection through hemolysis test.The irrigative test shows that it has low irrelativeness and meets the general requirements for injection.4.The mesylate injection of salicylic acid was used as the control group.The mequindox injection was prepared as the experimental group to study the pharmacokinetics of methaququine in rabbits.The results showed that it met the one-compartment open model and its t_1/2 is 1.379±0.017 and 1.519±0.265h,V_d/F were0.762±0.098 and 0.729±0.069 L/kg,respectively.AUC?0-t?were 25.469±2.937 and28.945±3.487mg/L×h,T_max is 0.542±0.012 and 0.583±0.129h,C_max is 11.879±1.322and 11.736±0.838mg/L,respectively,which indicated that methaququine was widely distributed in rabbits,with rapid absorption and rapid metabolism.The results of the paired sample T test showed improvement.The post-injection pharmacokinetic parameters can be achieved until the improvement,and the prescription can be used for actual production.