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目的:建立犬血浆中喷昔洛韦的高效液相色谱测定方法,并研究喷昔洛韦缓释微球在犬体内的药动学和生物利用度。方法:12只犬随机分为两组,每组6只,分别口服给予喷昔洛韦缓释微球和普通片剂375mg后,采用高效液相色谱法检测血药浓度。结果:喷昔洛韦缓释微球和普通片剂的达峰时间(Tmax)分别为(4.70±0.82)h和(1.83±0.27)h,达峰浓度(Cmax)分别为(2.62±1.14)μg.mL-1和(4.50±0.763)μg.mL-1,半衰期(T1/2)分别为(20.256±0.436)h和(6.865±0.607)h,曲线下面积(AUC0-8)为(25.34±6.33)μg.h.mL-1和(26.77±4.95)μg.h.mL-1。结论:喷昔洛韦缓释微球具有明显的缓释特性。
OBJECTIVE: To establish a HPLC method for the determination of penciclovir in canine plasma and to study the pharmacokinetics and bioavailability of penciclovir sustained-release microspheres in dogs. Methods: Twelve dogs were randomly divided into two groups with 6 mice in each group. The dogs were given oral administration of 375 mg penciclovir sustained-release microspheres and ordinary tablets, respectively, and the plasma concentrations were determined by HPLC. Results: The peak time (Tmax) of penciclovir sustained-release microspheres and common tablets were (4.70 ± 0.82) h and (1.83 ± 0.27) h respectively, and the peak concentrations (Cmax) were (2.62 ± 1.14) The half-life (T1 / 2) were (20.256 ± 0.436) h and (6.865 ± 0.607) h, respectively, and the area under the curve (AUC0-8) was (25.34 ± 0.763) μg.mL- ± 6.33) μg.h.mL-1 and (26.77 ± 4.95) μg.h.mL-1. Conclusion: The sustained release microspheres of penciclovir have obvious sustained release characteristics.