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本文按 BP(1980)所载生物测定法对志愿者单剂量口服诺氟沙星(Ⅰ)片剂400mg后的唾药及尿药浓度进行了测定,并研究了志愿者同服下列金属药物后对(Ⅰ)药动学的影响:枸橼酸钾(K~+)3g,碳酸氢钠(Na~+)0.5g,硫酸亚铁(Fe~(2+))0.2g,三硅酸镁(Mg~(2+))0.5g,氢氧化铝(Al~(3+))0.5g 和碳酸钙(Ca~(2+))0.5g,结果如下。唾液数据用二室模型拟合得到动力学参数分别为:T_(max)2.40～2.60h,C_(max)1.40～1.51mg/L,AUC_(0～9)6.95～7.01mg·h/L,T_(1/2β)3.61～3.80h,T_(1/2x)0.64～0.75。志愿者同服 Fe~(2+)、Mg~(2+)或 K~+后可使(Ⅰ)的 C_(max)和 AUC_(0～9)分别降低至3%,33%～20%和50%～60%;Na~+,Al~(3+)对(Ⅰ)的药动学无明显影响;同服 Ca~(2+)对(Ⅰ)的 C_(max)无明显影响,但可使 AUC 降低47%。
In this paper, according to BP (1980) contained in the bioassay of volunteers single oral dose of norfloxacin (I) tablets 400mg after saliva and urine concentration was measured and the volunteers with the service after the following metal drugs (I) Pharmacokinetics: potassium citrate (K ~ +) 3g, sodium bicarbonate (Na ~) 0.5g, ferrous sulfate (Fe ~ (2 +)) 0.2g, magnesium trisilicate (Mg2 +) 0.5g, aluminum hydroxide (Al3 +) 0.5g and calcium carbonate (Ca2 +) 0.5g, the results are as follows. The kinetic parameters of salivary data fitted by two-compartment model were as follows: T max 2.40-2.60 h, C max 1.40-1.51 mg / L, AUC 0-9 9 6.95-7.01 mg · h / L, T ½ 1/2 β 3.61 ~ 3.80h, T 1 / 2x 0.64 ~ 0.75. After the volunteers fed with Fe 2+, Mg 2+ or K +, the C max and AUC 0-9 of (Ⅰ) were decreased to 3%, 33% to 20% And 50% ~ 60% respectively. Na ~ + and Al ~ (3+) had no significant effect on the pharmacokinetics of (Ⅰ), while Ca ~ (2+) However, AUC can be reduced by 47%.