Evaluation of Dosage form Characteristics of Fuzi Lizhongwan Based on Dissolution Behavior

Mao-yuan JIANG; Xia LIN; Sha-sha YANG; Sheng-jia ZHAO; Xin-yi WEI; You HUANG; Zhen ZHANG; Chao-mei FU

doi:10.13422/j.cnki.syfjx.20191650

您当前的位置：

首页 >

文章列表页 >

Evaluation of Dosage form Characteristics of Fuzi Lizhongwan Based on Dissolution Behavior

Classic Prescriptions | 更新时间：2021-02-09

- Evaluation of Dosage form Characteristics of Fuzi Lizhongwan Based on Dissolution Behavior
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 25, Issue 24, Pages: 15-22(2019)
- 作者机构：
  
  成都中医药大学　药学院，中药材标准化教育部重点实验室，四川省中药资源系统研究与开发利用重点实验室——省部共建国家重点实验室培育基地，成都　 611137
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.20191650
  CLC： R22; O657; R28; C37; R94
- Published：20 December 2019，
  
  Published Online：07 May 2019，
  
  Received：18 January 2019，
- 稿件说明：
扫描看全文
Mao-yuan JIANG, Xia LIN, Sha-sha YANG, et al. Evaluation of Dosage form Characteristics of Fuzi Lizhongwan Based on Dissolution Behavior. [J]. Chinese Journal of Experimental Traditional Medical Formulae 25(24):15-22(2019)
DOI：

Mao-yuan JIANG, Xia LIN, Sha-sha YANG, et al. Evaluation of Dosage form Characteristics of Fuzi Lizhongwan Based on Dissolution Behavior. [J]. Chinese Journal of Experimental Traditional Medical Formulae 25(24):15-22(2019) DOI： 10.13422/j.cnki.syfjx.20191650.

摘要

目的：

基于前期对附子理中丸中甘草成分溶出度的研究结果，通过同时测定君药附子中的3种指标成分苯甲酰新乌头碱、苯甲酰乌头碱、苯甲酰次乌头碱的溶出度，进一步对附子理中丸的溶出行为进行研究，为该丸剂的质量控制提供依据，同时为该丸剂的体内释药行为研究奠定基础。

方法：

建立同时测定附子理中丸中苯甲酰新乌头碱、苯甲酰乌头碱、苯甲酰次乌头碱含量的HPLC-QQQ-MS；测定5个厂家共15批附子理中丸在不同时间点3种指标成分的溶出量，计算累积溶出度，绘制溶出曲线；采用

相似因子法，比较同一厂家不同批次样品中3个指标成分溶出曲线的相似性和同一厂家样品中不同指标成分间溶出曲线的相似性；对溶出数据进行模型拟合以归属附子理中丸的溶出模型。

结果：

以pH 1.2的盐酸溶液作为溶出介质时，3种生物碱溶出效果最为理想。附子理中丸中3种单酯型乌头碱的溶出基本同步，且溶出行为可持续到24 h。厂家1，3，4，5的各自3批样品之间溶出行为相似，表明绝大多数厂家样品溶出行为的相似度较好。厂家2中批次1样品与批次2，3样品的溶出行为存在一定的差异性，提示厂家2不同批次样品的质量可能存在一定差异性。不同厂家样品中有效成分的溶出数据拟合结果一致，且均以Weibull模型为最佳。

结论：

5个厂家15批样品中指标成分均在24 h内持续溶出，表明样品具有“丸者缓也”的缓慢溶释特征。同一厂家样品的溶出曲线相似情况总体较好，表明大多数厂家的批次间制剂质量具有稳定性。不同厂家样品间的苯甲酰新乌头碱、苯甲酰乌头碱、苯甲酰次乌头碱溶出曲线相似度具有一定的差异性，可能由于不同厂家的药材或制剂生产工艺参数不一致造成的。

Abstract

Objective:

Based on the previous studies

to investigate the dissolution behavior of Fuzi Lizhongwan by simultaneously determining the dissolution of benzoylmesaconine

benzoylaconine and benzoylhypaconine in Aconiti Lateralis Radix Praeparata.

Method:

The simultaneous determination of benzoylmesaconine

benzoylaconine and benzoylhypaconine in Fuzi Lizhongwan was established by HPLC-QQQ-MS. The dissolution amounts of three compositions in 15 batches of Fuzi Lizhongwan from 5 manufacturers at different time points

the cumulative dissolution was calculated and the dissolution curve was drawn. The

similarity factor method was adopted to evaluate similarity of dissolution curves of index components in different batches of samples from the same manufacturer

and to evaluate similarity of dissolution curves of samples from different manufacturers based on the same index component. The dissolution model of Fuzi Lizhongwan was concluded by fitting with the dissolution data.

Result:

When hydrochloric acid solution with pH of 1.2 was used as the dissolution medium

the three alkaloids had the best dissolution effect. The dissolution behavior of three monoester alkaloids in Fuzi Lizhongwan was basically synchronous and the dissolution lasted for 24 h. Three batches of samples from the same manufacturer (manufacturer 1

4 and 5) appeared to be similar on dissolution behavior

indicating that the dissolution behavior of the majority of samples from different manufacturers was similar. The dissolution behavior of batch 1 sample was different from batch 2 and 3 samples in manufacturer 2

suggesting that the quality of different batches of samples in manufacturer 2 might be different. The fitting results of dissolution data of index components in samples from different manufacturers were consistent

and the Weibull model was the best.

Conclusion:

Index components in fifteen batches of samples from 5 manufacturers are continuously dissolved within 24 h

indicating that the samples have the characteristics of slow dissolution. The dissolution curves of samples from the same manufacturer are similar to each other

indicating that the quality of different batches of products from most manufacturers is stable. The dissolution behavior of benzoylmesaconine

benzoylaconine and benzoylhypaconine in samples form different manufacturers has some differences

which may be caused by the source of medicinal materials and preparation technology parameters.

关键词

附子理中丸溶出行为苯甲酰新乌头碱苯甲酰乌头碱苯甲酰次乌头碱剂型特征Weibull模型

Keywords

Fuzi Lizhongwandissolution behaviorbenzoylmesaconinebenzoylaconinebenzoylhypaconinecharacteristics of dosage formsWeibull model

references

甘嘉荷，王淳，宋志前，等．炼蜜用量对附子理中丸中9种生物碱类成分药代动力学的影响[J]．中国实验方剂学杂志，2018，24(3)：90-96．

国家药典委员会．中华人民共和国药典．一部[M]．北京：中国医药科技出版社，2015：1013-1014．

陈荣昌，孙桂波，张强，等．附子毒性研究进展[J]．中国中药杂志，2013，38(8)：1126-1129．

韩屾，吕雷，王汉蓉，等．3种乌头类中药在大鼠体内外的神经毒性[J]．华西药学杂志，2007，22(3)：286-288．

Sheikh-Zade Y R, Cherednik I L, Galenko-Yaroshevskii P A. Peculiarities of cardiotropic effect of aconitine [J].Bull Exp Biol Med, 2000, 129(4): 365-366.

雷怀成，宋道江，易建华，等．大鼠乌头碱中毒心肌细胞凋亡的研究[J]．中国工业医学杂志，2004，17(6)：373-374．

SUN B, LI L, WU S, et al. Metabolomic analysis of biofluids from rats treated with Aconitum alkaloids using nuclear magnetic resonance and gas chromatography/time-of-flight mass spectrometry [J].Anal Biochem, 2009, 395(2): 125-133.

温瑞卿，李东辉，赵昕，等．基于化学分析的毒性中药附子炮制方法的合理性研究[J]．药学学报，2013，48(2)：286-290．

周远鹏．从双酯型生物碱的水解来看附子的解毒(二)[J]．中药药理与临床，2014，30(3)：154-157．

蒲含林，姜华，陈蓉蓉．金银花和干姜对小鼠的毒性研究[J]．实用药物与临床，2011，14(4)：277-278．

赵安莎，孙于兰，张立实．白术提取液安全性评价[J]．中国公共卫生，2006，22(1)：43-45．

江茂源，张臻，石金凤，等．基于甘草中2种成分同时测定的附子理中丸溶出行为研究[J]．中国中药杂志，2018，43(5)：952-958．

肖娅，常金花，薛禾菲，等．栀子金花丸中3种成分溶出度的比较[J]．中成药，2017，39(10)：2076-2080．

郑晓霞，徐剑，田洪星，等．妇科再造丸的体外溶出度测定[J]．中国药房，2018，29(18)：2497-2500．

玄敏，程雪梅，王峥涛，等．不同厂家龙胆泻肝丸中龙胆苦苷、栀子苷、黄芩苷的溶出度测定和比较[J]．中成药，2016，38(4)：790-795．

张臻，高天慧，傅超美，等．中药丸剂剂型理论与应用现状关键问题分析[J]．中国中药杂志，2017，42(12)：2408-2412．

何艳梅，林虓，王雪，等．基于UPLC测定桂枝茯苓胶囊中8种活性成分的溶出度[J]．中国实验方剂学杂志，2018，24(1)：14-19．

张定堃，韩雪，李瑞煜，等．UPLC-Q-TOF-MS分析不同产地泥附子化学成分的差异[J]．中国中药杂志，2016，41(3)：463-469．

李燕，赵梦杰，袁岸，等．给药剂量对附子总生物碱在大鼠体内药代动力学特征的影响[J]．中国实验方剂学杂志，2016，22(22)：82-85．

孙兰，周海燕，赵润怀，等．HPLC法同时测定附子中6种单酯和双酯型生物碱[J]．中草药，2009，40(1)：131-134．

国家食品药品监督管理总局．普通口服固体制剂溶出度试验技术指导原则[Z]．2015-02-05．

姚俊娜，杜茂波，易红，等．复方蒿甲醚本芴醇片溶出度的一致性评价[J]．中国实验方剂学杂志，2018，24(15)：43-50．

刘珈羽，郭换，肖佳雯，等．不同粒径白及粉的粉体学性质及体外溶出度比较[J]．中国实验方剂学杂志，2018，24(3)：25-29．

闫冉，李智慧，石森林，等．不同厂家桂枝茯苓丸在不同溶出介质中的多条溶出曲线比较[J]．中华中医药杂志，2016，31(3)：1044-1048．

国家食品药品监督管理总局．普通口服固体制剂溶出曲线测定与比较指导原则[Z]．2016-03-18．

吴克红，唐力英，王祝举，等．附子的化学和生物活性研究进展[J]．中国实验方剂学杂志，2014，20(2)：212-220．

陈荣昌，孙桂波，张强，等．附子炮制减毒的研究进展[J]．中国实验方剂学杂志，2014，20(15)：237-241．

周林，任玉珍，李飞，等．不同炮制方法对附子生物碱类成分的影响[J]．安徽中医学院学报，2012，31(5)：71-74．

林彦君，游宇，季宁平，等．HPLC-Q-TOF/MS指纹技术对比分析附子配伍炙甘草前后化学组分变化[J]．中草药，2014，45(11)：1556-1560．

章津铭，傅超美，何宇新，等．附子-甘草配伍前后汤液中沉积物的化学组分对比研究[J]．中草药，2013，44(2)：165-169．

王亭，徐暾海．附子甘草配伍研究进展[J]．中草药，2009，40(8)：1332-1334．

随志刚，陈明玉，刘志强，等．附子煎煮与配伍应用中乌头类生物碱含量的变化及意义[J]．吉林大学学报：医学版，2009，35(2)：226-229．

Views

下载量

CSCD

Alert me when the article has been cited

提交

Tools

Publicity Resources

Mechanism of Fuzi Lizhongwan Improving Injury in Cisplatin-induced CIPN Mice by Regulating MAPK Signaling Pathway

Comparison of Total Daily Doses of 16 Active Components in Three Dosage Forms of Fuzi Lizhongwan

Effect of Refined Honey Amount on Pharmacokinetics of 9 Different Alkaloids in Fuzi Lizhongwan

Dissolution Behavior and Influencing Factors Analysis of Alkaloids in Xianglian Pills

Related Author

Feng-yun YAO

Rui LIU

Yong-xin LI

Lin WANG

Yan-kun CUI

Yan-mei HUANG

Zheng-yun ZUO

Chun WANG

Related Institution

Formula-pattern Research Center of Jiangxi University of Chinese Medicine

College of Traditional Chinese Medicine， Jiangxi University of Chinese Medicine

Institute of Basic Theory of Chinese Medicine, China Academy of Chinese Medical Sciences

Postal code：100700
Tel：010-84076882 Email：syfjx_2010@188.com
Technical support is provided by Beijing Founder electronics co., LTD 京ICP备11006657号-10 京公网安备11010802024621
It is recommended to read the content of this site in Chrome&IE9+. Please switch to extreme mode in browser 360.
Cookies We use cookies to help provide and enhance our service and tailor content. By continuing, you agree to the use of cookies.

⁰