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目的研究尼扎替丁注射液的药动学。方法选择20名中国健康成年志愿者,男女各半,单次静滴尼扎替丁注射液100和200mg及100mg多次给药。血及尿中药物浓度分别用LC-MS/MS和高效液相色谱测定。利用血药浓度,以DAS软件计算药动学参数;利用尿药浓度计算尿药累积排泄率。结果受试者静滴尼扎替丁注射液100,200mg及100mg多次给药后,主要药动学参数分别是ρmax(1623.58±429.34),(3722.78±571.70)和(2155.47±652.39)μg·L-1,AUC0-8(2183.81±545.60),(4776.04±828.05)和(2741.56±827.81)μg·h·L-1,AUC0-∞(2222.35±553.84)(,4854.36±837.43)和(2793.17±828.18)μg·h·L-1,t1/2(1.50±0.23),(1.48±0.16)和(1.62±0.29)h。100mg单次和100mg多次给药组经t检验,差异无统计学意义;100和200mg组除ρmax和AUC与剂量成正比外,其余主要药动学参数组间差异无显著性。静滴尼扎替丁注射液100,200及100mg多次给药后,0~12h内尿药累积排泄率分别为(50.63±8.55)%,(58.30±16.22)%和(54.85±14.58)%,经t检验差异无统计学意义。结论本品每8h给药1次,每次静滴100mg,共给3次,连续给药3d,可达稳态浓度,多次给药后其药动学行为无异常改变。该制剂平均有50%以上的原型药物从肾脏排出,表明该药主要以原型从肾脏排泄。
Objective To study the pharmacokinetics of nizatidine injection. Methods Twenty Chinese healthy adult volunteers were selected and divided into two groups: male and female, single intravenous infusion of nizatidine 100 and 200 mg and 100 mg. Blood and urine drug concentrations were measured by LC-MS / MS and high performance liquid chromatography. Pharmacokinetic parameters were calculated using DAS software based on plasma concentration. Urinary drug excretion rate was calculated using urine concentration. Results The main pharmacokinetic parameters of nizatidine injection 100, 200mg and 100mg intravenously were ρmax (1623.58 ± 429.34), (3722.78 ± 571.70) and (2155.47 ± 652.39) μg · L -1, AUC0-8 (2183.81 ± 545.60), (4776.04 ± 828.05) and (2741.56 ± 827.81) μg · h · L -1, AUC0-∞ (2222.35 ± 553.84) (4854.36 ± 837.43) and (2793.17 ± 828.18 ) μg · h · L-1, t1 / 2 (1.50 ± 0.23), (1.48 ± 0.16) and (1.62 ± 0.29) h, respectively. 100mg single and 100mg multiple administration groups by t test, the difference was not statistically significant; 100 and 200mg group except pmax and AUC and the dose is proportional to the rest of the main pharmacokinetic parameters were no significant difference between groups. After intravenous infusion of nizatidine 100, 200 and 100 mg, the accumulative excretion rate of urinary drug within 0-12 h were (50.63 ± 8.55)%, (58.30 ± 16.22)% and (54.85 ± 14.58)%, respectively t test difference was not statistically significant. Conclusion This product is administered once every 8 hours and 100 mg intravenously every time for 3 consecutive days. The drug is stable for 3 days, and its pharmacokinetic behavior is unchanged after multiple administrations. On average, over 50% of the prototype drug is excreted from the kidneys, indicating that the drug is excreted primarily from the kidneys as a prototype.