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目的研究穿心莲内酯热熔喷雾细粉的药物动力学,并比较与穿心莲内酯原料药动学差异。方法采用建立的LC-MS/MS分别测定穿心莲内酯热熔喷雾细粉和穿心莲内酯原料给药大鼠血浆中的穿心莲内酯浓度,分别计算药物动力学参数。结果穿心莲内酯原料药与热熔喷雾产物的t1/2分别为(347.33±9.32)和(390.82±8.78)min,tmax分别为(30.00±5.94)和(60.00±3.48)min,ρmax分别为(1 940.14±21.21)和(1 818.22±23.64)ng·m L-1,AUC0-t分别为(427 515.71±37 350.03)和(426 406.31±20 577.75)ng·min·m L-1,AUC0-inf分别为(545 423.14±47 969.18)和(593 569.87±30 247.35)ng·min·m L-1,Vz/F分别为(43.48±4.75)和(44.96±3.81)kg·L-1,CL/F分别为(86.78±3.35)和(79.74±2.89)kg·L-1·min-1。结论穿心莲内酯热熔喷雾细粉与穿心莲内酯原药相比,使药物半衰期延长,达峰时间推迟,最大血药浓度降低,但曲线下面积,表观分布容积与清除率均无显著性差异。
Objective To study the pharmacokinetics of andrographolide hot-melt spray powder and compare the kinetic differences with andrographolide raw materials. Methods The LC-MS / MS was used to determine the concentrations of andrographolide in plasma of andrographolide powder and andrographolide respectively. Pharmacokinetic parameters were calculated. Results The t1 / 2 of andrographolide APIs and hot melt spray products were (347.33 ± 9.32) and (390.82 ± 8.78) min, respectively. The tmax values were (30.00 ± 5.94) and (60.00 ± 3.48) min, The mean AUC0-t was (427 515.71 ± 37 350.03) and (426 406.31 ± 20 577.75) ng · min · m L-1, and the AUC0- (545 423.14 ± 47 969.18) and (593 569.87 ± 30 247.35) ng · min · m L-1, respectively, with Vz / F of (43.48 ± 4.75) and (44.96 ± 3.81) / F were (86.78 ± 3.35) and (79.74 ± 2.89) kg · L-1 · min-1, respectively. Conclusion Andrographolide hot-melt spray powder prolongs the half-life of drug, delays the peak time and decreases the maximum plasma concentration compared with the original drug of andrographolide, but the area under the curve, the volume of apparent distribution and the clearance rate are not significant difference.