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目的:建立兔血浆中壬苯醇醚-9(NP-9)的反相高效液相色谱(RP-HPLC)方法,研究NP-9栓剂在健康雌性新西兰兔体内的药代动力学。方法:6只健康雌性新西兰兔(体质量2.0～2.2kg)单剂量(64mg/只)阴道给药NP-9栓剂;取血浆经预处理后采用DiamonsilTM ODS柱(200mm×4.6mm,5μm),以甲醇-水(95:5)作为流动相,流速1.0ml/min,荧光检测的激发波长226nm,发射波长300nm,柱温30℃,测定NP-9经时血药浓度,计算药代动力学参数。结果:NP-9在0.05～5.00μg/ml范围内线性关系良好,日内、日间精密度均小于10%,低、中、高3种浓度(0.10、0.50、2.00μg/ml)的方法回收率分别为(101.67±8.12)%、(100.84±5.42)%、(100.29±3.81)%。主要药代动力学参数为:t1/2(3.75±0.87)h,tmax(3.2±0.4)h,Cmax(2.75±0.32)μg/ml,AUC0～12(12.72±2.14)μg.h.ml-1,AUC0～∞(15.05±2.84)μg.h.ml-1,平均滞留时间(6.85±1.13)h。结论:本方法简便、灵敏、专属性好,可用于NP-9栓剂在健康雌性新西兰兔体内的药代动力学研究。
Objective: To establish a reverse-phase high performance liquid chromatography (RP-HPLC) method for the non-phenyl alcohol ether-9 (NP-9) in rabbits plasma to study the pharmacokinetics of NP-9 suppositories in healthy female New Zealand rabbits. Methods: Six healthy female New Zealand rabbits (body weight 2.0-2.2kg) were given vaginal administration of NP-9 suppository at a single dose (64mg / body). The plasma was pretreated with DiamonsilTM ODS column (200mm × 4.6mm, 5μm) The pharmacokinetics were calculated using methanol-water (95: 5) as the mobile phase at a flow rate of 1.0 ml / min, fluorescence excitation at 226 nm, emission at 300 nm and column temperature at 30 ° C parameter. Results: The linearity of NP-9 in the range of 0.05 ~ 5.00μg / ml was good, the intra-day and inter-day precision were less than 10%, and the concentrations of NP- The rates were (101.67 ± 8.12)%, (100.84 ± 5.42)% and (100.29 ± 3.81)%, respectively. The main pharmacokinetic parameters were t1 / 2 (3.75 ± 0.87) h, tmax (3.2 ± 0.4) h, Cmax (2.75 ± 0.32) μg / ml and AUC0-12 (12.72 ± 2.14) μg.h.ml- 1, AUC0 ~ ∞ (15.05 ± 2.84) μg.h.ml-1, mean retention time (6.85 ± 1.13) h. Conclusion: The method is simple, sensitive and specific and can be used to study the pharmacokinetics of NP-9 suppository in healthy female New Zealand rabbits.