The In Vivo Evaluation on Total Components from Extract of Aconitum Based on a New Analytic Method of Area under Absorbance-Wavelength Curve

Miaomiao Yang,Xiaodong Li,Huasong Wu

doi:10.1155/2019/6385165

Abstract

Objective. To study oral pharmacokinetics of Aconitum extract in randomized Sprague-Dawley (SD) rats and observe the profile change in vivo between plasma concentration and time with an aim to disclose relevant delivery rule for total components from Aconitum extract and finally to evaluate the research of Aconitum sustained-release preparation. Methods. Randomized rats were administered orally with the single and multiple dose of Aconitum extract based on the clinical use of Aconitum injection. Blood samples were collected at predetermined interval time from an eye of rats. The concentration of total components in those samples was determined by a new analytic method of area under absorbance-wavelength curve, the data were analyzed by Drug and Statistics software, and then the pharmacokinetic parameters and compartment model were acquired and compared, respectively. Results. The pharmacokinetic parameters of single and multiple doses were similar, and both of them showed characteristics of the one-compartment model. Cav, DF, and AUCss were (2.075 ± 0.282) µg/ml, (2.405 ± 0.175), and (24.901 ± 0.422) µg/ml/h, respectively. However, the concentrations of total components in the fifth and sixth day were 0.32 and 0.44 µg/ml, which were lower than the value of Cav. Conclusion. The method of AUAWC is feasible for the pharmacokinetics study in vivo analysis on total components of Aconitum with good sensitivity, specificity, and repeatability. The results demonstrated that both absorption and elimination of total components from Aconitum extract in rats were rapid and pharmacokinetic behavior was consistent at the level of single and multiple doses, which confirms that Aconitum injection is available to transform the oral sustained-release preparation. This will bring a good instruction to the research of sustained-release preparation of traditional Chinese medicine (TCM), which still lacks of an evaluation method available for total components in vivo analysis.

Highlights

Aconitum is a famous traditional Chinese medicine that had been used extensively for centuries to treat pain resulted from arthritis and cancer and to strengthen the function of the heart [1,2,3,4]. e main bioactive components of Aconitum are Aconitum alkaloids with a narrow therapeutic index, and the activity is closely related to the structure which differs from the number, type, and position of the substituents [5]
Aconitum injection composed of raw Chuanwu and Caowu, a kind of traditional Chinese medicine injection, is used for treatment of serious pain in the terminal gastric and liver cancer and has significant analgesic effect without addiction
Medium, high QC concentrations for aconitine were prepared for recovery, as shown in Table 1. e recoveries of aconitine were satisfactory and reproducible. e mean absolute recovery of aconitine was from 80.45 to 99.52% at three QC levels. e mean relative recovery was from 100.64 to 107.34% for aconitine at three QC levels

Summary

Introduction

Aconitum is a famous traditional Chinese medicine that had been used extensively for centuries to treat pain resulted from arthritis and cancer and to strengthen the function of the heart [1,2,3,4]. e main bioactive components of Aconitum are Aconitum alkaloids with a narrow therapeutic index, and the activity is closely related to the structure which differs from the number, type, and position of the substituents [5]. Aconitum injection composed of raw Chuanwu and Caowu, a kind of traditional Chinese medicine injection, is used for treatment of serious pain in the terminal gastric and liver cancer and has significant analgesic effect without addiction [6,7,8,9]. It has such promising therapeutic effects, its potential neurotoxicity and cardiotoxicity are frequently observed in clinics [10,11,12,13].

Methods

Results

Conclusion