摘要
目的:研究粉防己碱(TET)缓释凝胶微丸在家犬体内的药动学特点。方法:采用自身交叉对照实验,犬分别单剂量服用TET缓释凝胶微丸和普通片,反相-高效液相色谱法测定粉防己碱血药浓度,3p97药动学软件计算相关参数。结果:TET缓释凝胶微丸和普通片的tmax分别为5.67、2.5h,Cmax分别为2.67、3.53mg.L-1,AUC0→∞分别为29.75、19.03mg.h.L-1。TET缓释凝胶微丸相对生物利用度为(106.13±14.41)%,其体内药动学特征符合单隔室一级吸收过程。体外释放度和体内吸收相关性良好(r=0.9798)。结论:TET缓释凝胶微丸与普通片比较,血药浓度平缓,释药时间显著延长,达到了预期的缓释效果。
OBJECTIVE： To study the pharmacokinetics METHODS： The dogs were assigned to receive single oral dose of tetrandrine（TET） sustained release gel pellets in dogs. of sustained release gel pellets or common tetrandrine alginate calcium tablets by crossover self- control design. Plasma concentrations of tetrandrine alginate calcium were determined by RP- HPLC and the pharmaeokinetic parameters were computed with 3P97 pharmacokinetic software. RESULTS： The t C AUC0→∞ of TET sustained- release gel pellets were 5.67 and 2.5 h, 2.67 and 3.53 mg · L ^-1,29.75 and 19.03 mg · h · L^- 1 respectively .the relative bioavailability is（106.13 ± 14.41）% .The pharmacokinetics in vivo was in line with one- compartment first order absorption process. There existed a good correlation between release in vitro and absorption in vivo（r = 0.979 8） .CONCLUSION： Compared with the common TET tablets, TET sustained release gel pellets had smooth concentration and significantly prolonged release, meeting the expected delayed release efficacy.
出处
《中国药房》
CAS
CSCD
北大核心
2009年第21期1616-1617,共2页
China Pharmacy
关键词
粉防己碱缓释凝胶微丸
药动学
体内外相关性
Tetrandrine sustained release gel pellets
Pharmacokinetics
Correlation between in vitro （release） and in vivo （absorption）
