HPLC-MS Method for Determination of Nisodipine Concentration in Human Plasma and Its Pharmacokinetic Studies

To establish a HPLC-MS method for determining the concentrations of nisodipine in human plasma and to evaluate the pharmacokinetics of sustained-and immediate-release preparations.Method:A C18 column was used to separate nisodipine in plasma with a mobile phase of a mixture of methanol-water-acetic acid(75:25:0.1) at a flow rate of 1.0 mL·min-1.Atmosperic pressure electronic spray ionisation(AP-ESI)and ion mass spectral(m/z)of 411 were selected to quantify nisodipine,and 441 for nimodipine(internal standard).Results:The linear range of the standard curve of nisodipine was 0.250 ng·mL-1,and the determination limit was 0.15 ng·mL-1.The extraction recovery was more than 72.6%,intra-day and inter-day RSD were less than 9.8%.After a single dose of 10 mg,the main pharmacokinetics of nisodipine sustained-release tablets,sustained-release capsules and tablets were as follows,t1/2(h)6.08±1.48,7.06±1.80,3.70±0.25Tmax(h)5.41±0.72,5.83±0.44,2.02±0.23Cmax(ng·mL-1)3.43±0.55,3.71±0.24,9.18±3.78AUC0t(ng·h·mL-1)31.11±5.00,33.63±7.16,32.72±5.09,F(%)95.53±11.66,102.20±9.32.After multiple doses,Cmax(ng·mL-1)5.20±0.27,3.91±0.22,5.30±1.04;Cmin(ng·mL-1)0.72±0.10,0.77±0.07,0.53±0.07,DF(%)175.00±16.34,177.10±18.43,247.92±57.71;Cavng·mL-11.78±0.181.78±0.181.93±0.33;AUCss0tng·h·mL-145.71±3.5042.82±4.3923.23±3.98respectively.Conclusions:The method is sensitive,fast and accurate.It is suitable for therapeutic drug monitoring and human pharmacokinetic studies of nisodipine.

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