Pharmacokinetics of bullatine A in Aconitum brachypodum total alkaloids gel in transdermal delivery.
- Author:
Yu-Mei WU
1
;
Xiao-Lan CHEN
1
;
Wen LIU
1
;
Fang-Fang YANG
1
;
Hong-Yan TANG
1
;
Ya-Jie DAI
1
Author Information
- Publication Type:Journal Article
- Keywords: Aconiti Lateralis Radix Preparatal; Aconitum brachypodum total alkaloids; microemulsion gel; ordinary gel; pharmacokinetic; toxicity reduction
- From: China Journal of Chinese Materia Medica 2016;41(8):1530-1534
- CountryChina
- Language:Chinese
- Abstract: In this study, the changes of bullatine A in plasma and skin of mice with time in microemulsion gel and ordinary gel of Aconitum brachypodum total alkaloids were compared through UPLC-MS/MS, and their pharmacokinetic parameters were also compared and analyzed, to investigate the feasibility of microemulsion agent in the transdermal drug delivery. UPLC-MS/MS method for simultaneous determination of bullatine A in plasma and skin had high sensitivity and was in line with the pharmacokinetic study requirements for transdermal drug delivery. The main pharmacokinetic parameters for microemulsion gel in the plasma were as follows: Cmax=(37.62±14.31) μg•L⁻¹, Tmax=(3.40±1.34) h, AUC0-∞=(1 027.7±260) μg•L⁻¹•h⁻¹, MRT=(34.80±12.31) h, MRTlast=(10.68±0.57) h, t1/2=(23.11±9.20) h; main pharmacokinetic parameters for ordinary gel in the blood: Cmax=(52.23±15.90) μg•L⁻¹, Tmax=(4.00±0.00) h, AUC0-∞=(728.60±280.80) μg•L⁻¹•h⁻¹, MRT=(20.69±3.98) h, MRTlast=(9.34±0.42) h, t1/2=(14.69±3.15) h. The results showed that the microemulsion gel had more stable transdermal absorption, longer duration of action and higher bioavailability than ordinary gel, indicating that the microemulsion gel had a good and stable transdermal effect. There was no significant difference in bioavailability of bullatine A in skin between microemulsion gel and ordinary gel.
