水飞蓟素自微乳化药物传递系统制剂在泰国健康志愿者中的生物利用度和药代动力学研究。
The Bioavailability and Pharmacokinetics of Silymarin SMEDDS Formulation Study in Healthy Thai Volunteers.
作者信息
Sornsuvit Chuleegone, Hongwiset Darunee, Yotsawimonwat Songwut, Toonkum Manatchaya, Thongsawat Satawat, Taesotikul Wandee
机构信息
Pharmacy Service Center, Pharmacy Faculty, Chiang Mai University, Chiang Mai 50200, Thailand.
Department of Pharmaceutical Care, Chiang Mai University, Chiang Mai 50200, Thailand.
出版信息
Evid Based Complement Alternat Med. 2018 Jul 19;2018:1507834. doi: 10.1155/2018/1507834. eCollection 2018.
The present study aimed to determine the pharmacokinetic parameters and bioavailability of silymarin 140 mg SMEDDS formulation. An open-label, single-dose pharmacokinetic study was conducted. Twelve healthy volunteers were included in the study. After the volunteers had fasted overnight for 10 h, a single-dose generic silymarin 140 mg SMEDDS soft capsule was administered. Then 10 ml blood samples were taken at 0.0, 0.25, 0.50, 0.75, 1.0, 1.33, 1.67, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, 10.0, and 12.0 h. The plasma silybin concentrations were analyzed using validated LC-MS/MS. The pharmacokinetic parameters were analyzed and calculated. The pharmacokinetic parameters were calculated after silymarin had been administered as a single capsule. The mean (range) C was 812.43 (259.47-1505.47) ng/ml at 0.80 (0.25-1.67) h (t). The mean (range) AUC and AUC were 658.80 (268.29-1045.01) ng.h/ml and 676.98 (274.10-1050.96) ng.h/ml, respectively. The mean k and t were 0.5386 h and 1.91 h, respectively. The silymarin SMEDDS formulation soft capsule showed rapid absorption and high oral bioavailability.
本研究旨在测定水飞蓟素140毫克自微乳化药物传递系统（SMEDDS）制剂的药代动力学参数和生物利用度。进行了一项开放标签、单剂量药代动力学研究。12名健康志愿者纳入该研究。志愿者过夜禁食10小时后，给予单剂量140毫克水飞蓟素通用型SMEDDS软胶囊。然后在0.0、0.25、0.50、0.75、1.0、1.33、1.67、2.0、2.5、3.0、4.0、6.0、8.0、10.0和12.0小时采集10毫升血样。使用经过验证的液相色谱-串联质谱法（LC-MS/MS）分析血浆水飞蓟宾浓度。分析并计算药代动力学参数。水飞蓟素作为单粒胶囊给药后计算药代动力学参数。在0.80（0.25 - 1.67）小时（tmax）时，平均（范围）Cmax为812.43（259.47 - 1505.47）纳克/毫升。平均（范围）AUC0 - t和AUC0 - ∞分别为658.80（268.29 - 1045.01）纳克·小时/毫升和676.98（274.10 - 1050.96）纳克·小时/毫升。平均k和t1/2分别为0.5386小时和1.91小时。水飞蓟素SMEDDS制剂软胶囊显示出快速吸收和高口服生物利用度。
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