厄贝沙坦胃滞留渗透泵片的制备及其在犬体内的药动学研究

厄贝沙坦胃滞留渗透泵片的制备及其在犬体内的药动学研

究

方瑜;潘振华;曹德英

【期刊名称】《中国药房》 【年(卷),期】2013(024)001

【摘要】OBJECTIVE: To prepare Irbesartan intragastric floating osmotic pump tablets (IFOPT), and to study the pharmacokinetics of irbesartan in dogs. METHODS: Irbesartan IFOPT was prepared by wet granulation coating method. A single oral dose of 150 mg Irbesantan tablets and Irbesartan IFOPT were given to 6 dogs in a randomized crossover design. The concentrations of irbe-santan in plasma were determined by HPLC-fluorescence before medication and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36, 48 and 72 h after medication. The pharmacokinetic parameters were calculated with DAS statistics software to evaluate sustained-release

effect.

RESULTS:

The

main

pharmacokinetic

parameters of Irbesartan tablet and Irbesartan IFOPT 150 mg were as follows: tmax: (1.21 ±0.76) h and (5.43±3.79) h; Cmax: (2.93×l04± 0.71×l04) ug/L and(1.87×104± 0.45×l04) ug/L; t1/2: (14.2± 4.9) h and (17.5±4.7)

h;

AUC0-72h(6.57×l05±

1.19×l05)

μg·h/L

and

(6.07×l05±8.61×l04) μg·h/L. The relative bioavailability of IFOPT was (92.1 ± 18.5)%. There were significant differences in tmax and Cmax. CONCLUSION: Irbesantan IFOPT have good sustained-release effect in