西替伪麻缓释片中盐酸伪麻黄碱的动物药代动力学研究

Pharmacokinetics of cetirizine/pseudoephedrine sustained release tablets in Beagle dogs

目的：采用高效液相色谱法测定Beagle犬体内盐酸伪麻黄碱血药浓度,并对其药动学参数、相对生物利用度及体内外的相关性作初步研究。方法：Beagle犬6只,单次口服西替伪麻缓释片2片．用HPLC法,采用Diamonsil^(TM)C_(18)色谱柱(5μm,250×4．6mm),0．05mol/L的磷酸二氢钠溶液-甲醇(75：25),以磷酸调节pH3．0为流动相,盐酸苯丙醇胺为内标,检测波长213nm,测定血浆中的药物浓度。结果：盐酸伪麻黄碱的相对生物利用度为(95．9±2．3)%,单次口服西替伪麻缓释片药动学参数分别为MRT=8．21h,T_(peak)=4h,C_(max)=2008．7ng/mL。结论：经统计数据分析自制片与对照片药动学过程相似,生物利用度等效,并且自制片体内外累积释放有着良好的相关性。

Objective： To study the pharmacokinetics of cetirizine/pseudoephedrine sustained release tablets in Beagle dogs. Methods ：Pseudoephedrine concentrations in serum were assayed by HPLC with DiamonsilTM C18 （250 × 4. 6 mm, 5μm ） column, 0.05mol/L sodium dihydrogen phosphate-mathanol （75 ： 25 ）, pH adjusted to 3.0 with phosphoric acid as mobile phase, and detection wavelength of 213nm. The pharmacokinetic parameters were researched after single admininstration of cetirizine/pseudoephedrine sustained release tablets in 6 Beagle dogs. Results：The pharmacokinetic parameters cetirizine/pseudoephedrine sustained release tablets were followed ： MRT = 8.21 h, Tpeak = 4h, Cmax = 200 8.7ng/mL. The relative hioavailahilty of cetirizine/pseudoephedrine sustained release tablets was （ 95.9 ±2. 3 ） %. Condusion： The pharmacokinetic profile of cetirizine/pseudoephedrine sustained release tablets was similar to the reference tablets. The self-made one was bioequivalent to Zycted-D 12h tablets, and its released profile in vivo/in vitro was correlation.