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目的研究川芎嗪自乳化缓释固体分散体(TMP-SESD)及普通缓释固体分散体(TMP-SD)在兔体内的药动学特征。方法 6只新西兰兔随机分为2组,采用自身交叉对照实验,单剂量口服TMP-SESD和TMP-SD后,采用高效液相色谱法测定血浆中TMP的浓度,DAS2.1数据处理软件计算药动学参数。结果 TMP-SESD和TMP-SD给药后,药动学参数如下:tmax分别为4 h和6 h;Cmax分别为(3.217±0.4581)mg.L-1和(6.105±0.298)mg.L-1;AUC0-∞分别为(63.877±3.786)mg.L-1.h和(39.067±2.971)mg.L-1.h;与TMP-SD比较,TMP-SESD的相对生物利用度为(163.5±9.58)%。结论家兔体内川芎嗪的药动学规律均符合一级吸收二室模型,与普通缓释固体分散体相比,自乳化缓释固体分散体Cmax和AUC0-∞均较高,说明自乳化缓释固体分散体能显著提高药物的生物利用度。
Objective To study the pharmacokinetics of ligustrazine self-emulsifying sustained-release solid dispersion (TMP-SESD) and conventional sustained-release solid dispersion (TMP-SD) in rabbits. Methods Six New Zealand white rabbits were randomly divided into two groups. TMP-SESD and TMP-SD were orally administered in a single oral dose. TMP concentrations in plasma were determined by high performance liquid chromatography (HPLC). DAS2.1 data processing software Dynamic parameters. Results After administration of TMP-SESD and TMP-SD, the pharmacokinetic parameters were as follows: tmax was 4 h and 6 h respectively; Cmax was (3.217 ± 0.4581) mg.L-1 and (6.105 ± 0.298) mg.L- 1 and AUC0-∞ were (63.877 ± 3.786) mg.L-1.h and (39.067 ± 2.971) mg.L-1.h, respectively. The relative bioavailability of TMP-SESD was ± 9.58)%. Conclusion The pharmacokinetics of tetramethylpyrazine in rabbits accords with the first-order absorption two-compartment model. Compared with the ordinary sustained-release solid dispersion, the Cmax and AUC0-∞ of the self-emulsifying sustained-release solid dispersion are higher, indicating that self- Release solid dispersion can significantly improve the bioavailability of drugs.