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[摘要]
目的 采用液相-质谱联用(LC-MS/MS)分析硫磺熏蒸(硫熏)对浙贝母中贝母素甲、贝母素乙在大鼠体内药动学的影响。方法 SD大鼠分别ig给予硫熏、鲜切浙贝母提取物(生药剂量15 g/kg),采用LC-MS/MS技术检测贝母素甲和贝母素乙的血药浓度,并用3P97软件计算药动学参数。结果 硫熏浙贝母中贝母素甲和贝母素乙的主要药动学参数:达峰浓度(Cmax)分别为(66.40±4.65)、(146.72±10.88)ng/mL,药时曲线下面积(AUC0~t)分别为(181.79±7.85)、(457.38±58.81)ng∙h/mL;鲜切浙贝母中贝母素甲和贝母素乙的主要药动学参数:Cmax分别为(186.37±18.80)、(227.65±7.01)ng/mL,AUC0~t分别为(197.70±18.69)、(566.16±41.55)ng∙h/mL。硫熏浙贝母组大鼠体内贝母素甲、贝母素乙的Cmax、AUC0~t明显低于鲜切浙贝母组。结论 硫熏降低浙贝母中贝母素甲、贝母素乙的血药浓度,影响浙贝母中主要生物碱贝母甲素和贝母乙素的药动学行为。
[Key word]
[Abstract]
Objective To study the influence of sulfur-fumigation on pharmacokinetic of peimine and peiminine of Fritillaria thunbergii in rat plasma by LC-MS/MS. Methods After random grouping, 18 SD rats were given the solution of fresh-cut and sulfur-fumigated F. thunbergii by ig administration. The blood drug concentration of peimine and peiminine in rat plasma was determined by HPLC-MS/MS, and the pharmacokinetic parameters were calculated with 3P97 software. Results The pharmacokinetic parameters of peimine and peiminine of sulfur-fumigated F. thunbergii in rat plasma were (66.40 ± 4.65), (146.72 ± 10.88) ng/mL for Cmax, and (181.79 ± 7.85), (457.38 ± 58.81) ng∙h/mL for AUC, respectively. Those of fresh-cut sample in rat plasma were (186.37 ± 18.8), (227.65 ± 7.01) ng/mL for Cmax, and (197.70 ± 18.69), (566.16 ± 41.55) ng∙h/mL for AUC, respectively. The pharmacokinetic parameters of perimine and peiminine of sulfur-fumigated sample in rat plasma were less than those of fresh-cut sample. Conclusion The results showed that sulfur-fumigation decreased the bioavailability of peimine and peiminine. This study could provide a basis for further clarifying the influence of sulfur-fumigation on efficacy material base of F. thunbergii.
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[基金项目]
国家中药标准化项目(ZYBZH-Y-ZY-45);国家中医药行业专项(201507002);浙江省公益性技术应用研究计划(2015C33152);浙江省中医药科学研究基金计划(2012ZB032,2013ZA027);浙江中医药大学重中之重一级学科——中药学学科开放基金