- Author:
Jia-Ming TIAN
1
Author Information
- Publication Type:Journal Article
- Keywords: Andrographolide; Hot-melt spray; LC-MS/MS; Pharmacokinetics
- From: Chinese Pharmaceutical Journal 2016;51(21):1855-1859
- CountryChina
- Language:Chinese
- Abstract: OBJECTIVE: To study the pharmacokinetics of hot-melt spray-dried andrographolide granules and compare it with andrographolide bulk drug. METHODS: A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was established for determination of the concentration of andrographolide in plasma of rats which were respectively given micronized andrographolide and hot-melt spray-dried andrographolide granules, then the pharmacokinetic parameters were calculated. RESULTS: The pharmacokinetic parameters of andrographolide after a single dose administration of micronized andrographolide and hot-melt andrographolide were as following: t1/2 were (347.33 ± 9.32) and (390.82 ± 8.78) min, tmax were (30.00 ± 5.94) and (60.00 ± 3.48) min, ρmax were (1 940.14 ± 21.21) and (1 818.22 ± 23.64) ng·mL-1, AUC0-t were (427 515.71 ± 37 350.03) and (426 406.31 ± 20 577.75) ng·min·mL-1, AUC0-inf were (545 423.14 ± 47 969.18) and (593 569.87 ± 30 247.35) ng·min·mL-1, Vz/F were (43.48 ±4.75) and (44.96 ± 3.81) kg · L-1, CL/F were (86.78 ± 3.35) and (79.74 ± 2.89) kg · L-1 · min-1, respectively. CONCLUSION: Compared with the bulk drug, the hot-melt spray-dried andrographolide granules have a longer t1/2, lower ρmax and delayed tmax in rats.