摘要
目的建立超高效液相色谱-质谱联用技术(UPLC-MS)测定大鼠血浆中甘油三油酸酯含量的方法,研究薏苡仁油纳米粒给药系统大鼠体内药物动力学和口服生物利用度。方法将随机分组的大鼠分别灌胃给药薏苡仁油原料、普通口服制剂康莱特软胶囊(市售薏苡仁油普通软胶囊)以及薏苡仁油纳米粒,分别于0.083、0.167、0.25、0.5、0.75、1、2、4、6、8、12、24、36、48、72、96、120 h取血,采用超高效液相色谱-质谱联用技术法测定大鼠血浆样品中甘油三油酸酯的浓度,计算药动学参数。结果比较薏苡仁油原料、普通口服制剂康莱特软胶囊、薏苡仁油纳米粒的药动学参数,大鼠血浆甘油三油酸酯的ρmax分别为(5.43±0.45)、(7.54±0.44)和(7.30±1.13)mg·L^(-1),薏苡仁油纳米粒与薏苡仁油原料相比,甘油三油酸酯的ρmax存在显著性差异(P<0.05),薏苡仁油纳米粒与普通薏苡仁油软胶囊相比,甘油三油酸酯的ρmax无显著性差异(P>0.05);大鼠血浆甘油三油酸酯的AUC0-∞分别为(68.71±5.12)、(46.61±3.86)、(178.91±6.26)mg·h·L^(-1),薏苡仁油纳米粒的AUC0-∞明显高于薏苡仁油原料药及薏苡仁油普通口服制剂;以薏苡仁油原料为参比,薏苡仁油纳米粒中甘油三油酸酯的相对生物利用度为260.38%;以薏苡仁油普通口服制剂为参比,薏苡仁油纳米粒中甘油三油酸酯的相对生物利用度为383.84%。结论薏苡仁油制成薏苡仁纳米粒给药系统能提高其口服生物利用度并改善其药剂学性质。
OBJECTIVE To delevop a UPLC-MS method for determining the content of olein in rat plasma, and investigate the pharmacokinetics and bioavailability of nanopartieles of eoix seed oil in rats. METHODS The rats were divided into three groups ran- domly. They were administered orally suspension of the raw material of the coix seed oil, Kang lai te soft capsules and nanoparticles of coix seed oil, respectively. Blood samples were collected at 0. 083, 0. 167, 0. 25, 0. 5, 0. 75, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 h and the concentrations of olein in rat plasma were determined by UPLC-MS. The pharmacokinetic parameters were cal- culated by 3P97 pharmacokinetic program. RESULTS The pharmacokinetic parameters of olein in the the raw material of eoix seed oil, KLT soft capsules and nanoparticles of coix seed oil in rat plasma were as follows ： pmax were （ 5.43± 0. 45 ） , （7.54 ±0. 44 ） and （7. 30 ±1.13） mg · L-1 , respectively, with significant difference between the nanoparticles and raw material （P 〈0. 05）, while no significant difference between nanoparticles and common oral prepatation （P 〉 0.05 ）; AUC0-∞ were （68.71±5.12）, （46. 61±3.86）, and （178.91± 6. 26） mg· h· L-1 , respectively, which was the highest for the nanoparticles. The relative bioavailability of olein in the nanoparticles of coix seed oil was 260. 38% to the raw material and 383.84% to the common oral prepatation. CONCLU- SION The nanoparticles system can increase the bioavailability of coix seed oil and improve its biophmnaceutical property.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2016年第1期40-45,共6页
Chinese Pharmaceutical Journal
基金
福建省科技计划重点项目(2014Y0062)
福建省科技计划项目(2010Y2004)
