吲达帕胺冻干口腔崩解片在Beagle犬体内药物动力学研究

Pharmacokinetics of Indapamide Lyophilized Oral Disintegrating Tablets in Beagle Dogs

目的:研究自制吲达帕胺冻干口腔崩解片和市售吲达帕胺片在Beagle犬体内的药物动力学行为及其相对生物利用度。方法:6只Beagle犬,随机分为两组,分别单剂量口服自制吲达帕胺冻干口腔崩解片和市售吲达帕胺普通片,剂量均为5.0mg。1周后交叉给药。采用HPLC法测定给药后不同时间的血药浓度。结果:供试制剂自制吲达帕胺冻干口腔崩解片和参比制剂吲达帕胺普通片的主要药动学参数:达峰时间tmax分别为(1.59±0.04)h和(2.71±0.32)h,达峰时药物浓度ρmax分别为(6.10±0.32)和(5.89±0.44)μg·mL-1,t1/2分别为(15.04±0.48)h和(14.65±0.73)h,AUC0-∞分别为(89.66±8.34)和(67.58±2.56)μg·h·mL-1。结论:统计学分析结果表明自制吲达帕胺冻干口腔崩解片的生物利用度要高于市售吲达帕胺普通片。

Objective： To study the relative bioavailability and pharmacokinetic of Indapamide lyophilized oral disintegrating tablets and indapamide tablets in beagle dogs. Methods：The Indapamide lyophilized oral disintegrating tablets（test）or Indapamide tablets（reference）were orally administered to 6 beagle dogs at a dosage of 5.0mg. The crossover dosing was taken in one week after the first single dose. The Indapamide concentrations in the blood samples were determined by HPLC. Results：The main pharmacokinetic parameters of the test and reference tablets were as follows：tmax（1. 59±0. 04） and （2.71±0.32）h,ρmax（6.10±0. 32） and （5.89 ±0.44）μg · mL^-1 ,t1/2 （15. 04±0. 48） and （14. 65±0.73）h,AUC0-∞ （89.66±8. 34） and （67.58±2.56）μg · h ·mL^-1. Conclusion：The results showed that the Indapamide lyopbilized oral disintegrating tablets increased relative bioavailability.