格拉司琼鼻喷雾剂在比格犬体内的相对生物利用度研究

Study on pharmacokinetics and bioavailability of granisetron nasal spray in beagles

目的:对格拉司琼鼻喷雾剂在比格犬体内的药代动力学进行研究,评价其相对生物利用度。方法:比格犬采用随机、自身交叉给药,分别口服片剂、鼻腔给喷雾剂,用HPLC荧光方法测定格拉司琼血浆浓度。结果:比格犬分别单剂量口服片剂、鼻腔给喷雾剂2 mg后的主要药代动力学参数tmax分别为1.50±0.41和0.31±0.13 h,Cmax分别为6.45±1.15和11.93±1.33 ng.ml-1,AUC0-12分别为25.14±3.75和27.76±3.46 ng.h.ml-1,AUC0-∞分别为28.46±4.17和31.46±3.43 ng.h.ml-1,鼻喷雾剂对片剂的相对生物利用度为(111.9±18.9)%。结论:格拉司琼鼻喷雾剂比片剂吸收快,生物利用度较高。

AIM： To study the bioavailability of granisetron nasal spray in beagles. METHODS： A single 2 mg dose of granisetron tablet or nasal spray was given to beagles in a randomized crossover design. The drug plasma concentrations were determined by HPLC fluorescence method using bisoprolol fumarate as internal standard. RESULTS： The phannacokinetic parameters of granisetron tablet and nasal spray were as follow： tmax were 1.50 ±0.41 and 0.31±0.13 h, Cmax were 6.45±1.15 and 11.93 ± 1.33 ng. ml^-1, AUC0-12 were 25.14±3.75 and 27.76±3.46 ng.h.ml^-1 , AUCo-∞ were 28.46 ± 4.17 and 31.46 ± 3.43 ng. h. ml^-1, respectively. The mean relative bioavailability of nasal spray vs tablet was （ 111.88 ± 18.94） %. CONCLUSION： Gmnisetron nasal spray is readily absorbed and owns better bioavailability than the tablet.