塞来昔布固体脂质纳米粒的制备及其在大鼠体内的药动学

发布时间：2018-10-18 06:54

【摘要】：目的:制备塞来昔布固体脂质纳米粒,并考察大鼠灌胃给药后体内的药动学特征。方法:采用热熔乳化超声-低温固化法制备塞来昔布固体脂质纳米粒,并对制得的纳米粒进行表征。将12只Wistar大鼠随机分为为塞来昔布原料药组和塞来昔布固体脂质纳米粒组,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塞来昔布的浓度,采用3P97程序计算塞来昔布药动学参数。结果:塞来昔布固体脂质纳米粒平均粒径为(183.6±44.5)nm,Pd I为(0.217±0.052),Zeta电位为(-30.4±5.2)m V。塞来昔布原料药和塞来昔布固体脂质纳米粒在大鼠体内的AUC(0-t)分别为(4.47±0.72)和(11.64±2.01)mg·L-1·h;t1/2分别为(13.45±1.89)和(10.12±1.24)h;tmax分别为(2.33±0.21)和(1.31±0.14)h;Cmax分别为(0.86±0.12)和(2.14±0.46)mg·L-1。结论:塞来昔布固体脂质纳米粒能够明显改善大鼠体内塞来昔布的药动学行为,与塞来昔布原料药相比具有明显的缓释效果,同时提高了药物的生物利用度。
[Abstract]:Aim: to prepare celecoxib solid lipid nanoparticles and investigate the pharmacokinetics of celecoxib in rats. Methods: celecoxib solid lipid nanoparticles were prepared by hot melt emulsification and low temperature curing method. Twelve Wistar rats were randomly divided into two groups: celecoxib group and celecoxib solid lipid nanoparticles group. The dosage of celecoxib was 100 mg kg-1,. The concentration of celecoxib in rat plasma was determined by HPLC. The pharmacokinetic parameters of celecoxib were calculated by 3P97 program. Results: the average particle size of celecoxib solid lipid nanoparticles was (183.6 卤44.5) nm,Pd I = (0.217 卤0.052), Zeta potential was (-30.4 卤5.2) m V.). The AUC (0-t) of celecoxib crude drug and celecoxib solid lipid nanoparticles in rats were (4.47 卤0.72) and (11.64 卤2.01) mg L-1 ht1 / 2, respectively (13.45 卤1.89) and (10.12 卤1.24) htmax were (2.33 卤0.21) and (1.31 卤0.14) mg L-1, respectively. Conclusion: celecoxib solid lipid nanoparticles can significantly improve the pharmacokinetic behavior of celecoxib in rats.
【作者单位】：唐山职业技术学院;唐山市协和医院药剂科;
【分类号】：R96

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