Pharmacokinetics and bioequivalence of evodiamine novel nano emulsion in rats
10.16781/j.0258-879x.2016.10.1256
- Author:
Ting-Ting LEI
1
Author Information
1. Medicine Engineering Research Center in University, Chongqing Medical University
- Publication Type:Journal Article
- Keywords:
Biological availability;
Evodiamine;
Half-life;
Intestinal absorption;
Nano emulsion;
Pharmacokinetics
- From:
Academic Journal of Second Military Medical University
2016;37(10):1256-1260
- CountryChina
- Language:Chinese
-
Abstract:
Objective To establish an HPLC approach for determining the plasma drug concentration of evodiamine (EVO) in evodiamine novel nano emulsion (ENNE) in rats, and to investigate the pharmacokinetics and bioequivalence of ENNE in rats. Methods Twelve SD rats were evenly randomized into two groups andwere administered intragastrically with ENNE (containing EVO 100mg/kg) or EVO (100mg/kg). The plasma drug concentrations of EVO were measured at 5min,min, 15 min, 30 min, 45 min, 1 h, 2 h, 5 h, 8 h, 12 h, 24 h, 48 h and 72 h after administration of ENNE or EVO by HPLC. The chromatographic conditions were as following: the mobile phase was methanol and 0.1% of formic acid-water solution (66: 34, V/V), the flow rate was 1 mL/min, the injection volume was 100 μL, and the detection wavelength was 225 nm. The concentration-time curve was drawn by excel software, and the main pharmacokinetic parameters and bioequivalence were calculated by DAS 2. 1. 1 software. Results The established method was fast, accurate, and had good linear correlation. The AUCo-∞ of ENNE and EVO were (8 248. 88 ± 69. 92) μg • h • L-1 and (884. 82 ± 83. 52) μg • h • L-1, and the t1/2 of ENNE and EVO were (1. 70 ± 0. 60) h and (1. 05 ± 0. 45) h, respectively. The AUCo-∞ of ENNE was 9 times that of EVO, and the t1/2 of ENNE was 1. 62 times that of EVO. ENNE and EVO were not bioequivalent. Conclusion Bioavailability and absorption of ENNE are higher than EVO, and ENNE and EVO are not bioequivalent.
