论文部分内容阅读
目的:制备塞来昔布纳米混悬剂(CXB-NSs),并考察大鼠灌胃给药后体内药动学特征。方法:采用反溶剂沉淀-高压均质法制备CXB-NSs,并考察其粒度分布,多聚分散系数和Zeta电位。将12只Wistar大鼠随机分为CXB-NSs组和CXB混悬液组,灌胃给药剂量均为100 mg·kg~(-1),采用高效液相色谱法测定大鼠血浆中的CXB浓度,用3P97软件计算相应的药动学参数。结果:CXB-NSs平均粒径为(442.5±61.9)nm,多聚分散系数为0.312±0.057,Zeta电位为(-31.6±3.9)m V。CXBNSs和CXB混悬液在大鼠体内的AUC_(0-t)分别为(5.13±0.77)和(13.51±3.18)mg·L~(-1)·h;t_(1/2)分别为(12.31±1.91)和(12.73±1.83)h;T_(max)分别为(2.48±0.37)和(1.41±0.27)h;C_(max)分别为(0.94±0.31)和(2.38±0.25)mg·L~(-1)。结论:CXB-NSs能显著提高药物在大鼠体内的生物利用度。
OBJECTIVE: To prepare celecoxib nanosuspension (CXB-NSs) and study the pharmacokinetics in rats after gavage. Methods: Anti-solvent precipitation-high pressure homogenization method was used to prepare CXB-NSs. The particle size distribution, dispersion coefficient and zeta potential were also investigated. Twelve Wistar rats were randomly divided into CXB-NSs group and CXB suspension group. The intragastric administration dose was 100 mg · kg -1, and the plasma levels of CXB Concentration, using 3P97 software to calculate the corresponding pharmacokinetic parameters. Results: The average particle size of CXB-NSs was (442.5 ± 61.9) nm, the polydispersity was 0.312 ± 0.057 and the Zeta potential was (-31.6 ± 3.9) mV. The AUC_ (0-t) of CXBNSs and CXB suspension in rats were (5.13 ± 0.77) and (13.51 ± 3.18) mg · L -1 · h, respectively; t 1/2 was 12.31 ± 1.91 and 12.73 ± 1.83 h, respectively; T max was (2.48 ± 0.37) and (1.41 ± 0.27) h, respectively; C max was 0.94 ± 0.31 and 2.38 ± 0.25 mg · L ~ (-1). Conclusion: CXB-NSs can significantly improve the bioavailability of drugs in rats.