盐酸金霉素超微粉制备及其在鸭体内的药代动力学研究

doi:10.12160/j.issn.1672-5190.2023.01.016

摘要/Abstract

摘要：

[目的] 研究盐酸金霉素超微粉在鸭体内的药代动力学特征。[方法] 采用气流粉碎技术将盐酸金霉素普通原粉制备成800目超微粉，再添加适宜辅料制成含量为20%的盐酸金霉素可溶性粉，通过影响因素试验和加速试验对制备的盐酸金霉素超微粉进行稳定性评价；将30只90日龄绍兴麻鸭随机分为A、B、C 3个试验组，每组10只，分别经口单剂量灌服60目普通原粉制备的盐酸金霉素可溶性粉、800目超微粉制备的盐酸金霉素可溶性粉、80目普通原粉制备的盐酸金霉素可溶性粉，剂量均为15 mg/（kg·BW）（以金霉素计），比较不同粒径原料制备的盐酸金霉素可溶性粉在鸭体内的药物代谢过程。[结果] 利用800目超微粉制备的盐酸金霉素可溶性粉处方、工艺稳定可行，通过稳定性试验考查，质量可靠；不同粒径原料制备的盐酸金霉素可溶性粉主要药代动力学特征如下：试验B组达峰时间（T_max）显著（P<0.05）快于A组和C组；试验B组药时曲线下面积（AUC_0-t）、达峰浓度（C_max）均显著（P<0.05）大于A组和C组；试验B组消除半衰期时间（t_1/2）显著（P<0.05）长于A组和C组，A组和C组之间无统计学差异（P>0.05）；试验B组体内存留时间（MRT）显著（P<0.05）长于A组和C组。[结论] 鸭灌服相同剂量的金霉素[15 mg/（kg·BW）]，相较于普通原粉制备的盐酸金霉素可溶性粉，盐酸金霉素超微粉在体内1.5 h即达到血药峰浓度，吸收迅速且有效血药浓度维持时间长。研究获得的药动学数据可为盐酸金霉素用于动物临床治疗提供参考。

关键词: 盐酸金霉素超微粉, 制备, 药代动力学, 鸭

Abstract:

[Objective] This study was conducted to characterize the pharmacokinetics of chlortetracycline hydrochloride ultra-fine powder in ducks. [Method] Using the raw powder of chlortetracycline hydrochloride with ordinary particle size as material, the ultra-fine powder with particle size of 800 mesh was prepared by airflow grinding technology. Subsequently, by adding a certain amount of appropriate accessories, the soluble ultra-fine powder containing 20% chlortetracycline hydrochloride was prepared. The stability of the soluble ultra-fine powder was evaluated by influencing factor test and accelerated test. A total of 30 Shaoxing ducks aged 90 days were randomly assigned to one of the following three groups: group A （n=10）, group B （n=10） or group C （n=10）, which were given a single dose of the chlortetracycline hydrochloride soluble powder [15 mg/（kg·BW）, calculated by chlortetracycline hydrochloride] prepared using raw materials with particle sizes of 60 mesh, 800 mesh (ultra-fine powder) and 80 mesh by oral gavage, respectively. The pharmacokinetics of the chlortetracycline hydrochloride soluble powder prepared with raw materials of different particle sizes in ducks were characterized and statistically compared. [Result] The prescription and technology of the soluble ultra-fine powder prepared using raw material with particle size of 800 mesh was stable and feasible, and the quality was proved to be reliable by stability test. The main pharmacokinetic characteristics of the chlortetracycline hydrochloride soluble powder prepared with raw materials of different particle sizes in ducks were as follows: the T_max in group B was significantly （P<0.05） faster than that in groups A and C; the AUC_0-t and C_max in group B were significantly （P<0.05) higher than those in groups A and C; the t_1/2 in group B was significantly （P<0.05） longer than that in groups A and C, while there was no significant （P>0.05） difference between groups A and C; the in vivo MRT in group B was significantly （P<0.05） longer than that in groups A and C. [Conclusion] When given the same dose of 15 mg/（kg·BW） of chlortetracycline hydrochloride in ducks, the soluble ultra-fine powder peaked in blood concentration at 1.5 hours post administration, indicating that it had superior absorption rate and effective blood concentration maintenance duration to the soluble powder prepared with raw materials of ordinary particle sizes. The pharmacokinetic data obtained in this study may provide references for the use of chlortetracycline hydrochloride in clinical treatment of animal diseases.

Key words: chlortetracycline hydrochloride ultra-fine powder, preparation, pharmacokinetics, ducks

中图分类号:

S859.7

郗洪生,王滨坤,张瑞强,李慧,董泽涵. 盐酸金霉素超微粉制备及其在鸭体内的药代动力学研究[J]. 畜牧与饲料科学, 2023, 44(1): 105-110.

XI Hong-sheng,WANG Bin-kun,ZHANG Rui-qiang,LI Hui,DONG Ze-han. Preparation of Chlortetracycline Hydrochloride Ultra-fine Powder and Its Pharmacokinetics in Ducks[J]. Animal Husbandry and Feed Science, 2023, 44(1): 105-110.

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