红花抗帕金森病有效成分滴丸的制备和表征

doi:10.5246/jcps.2019.01.004

中国药学(英文版) ›› 2019, Vol. 28 ›› Issue (1): 27-39.DOI: 10.5246/jcps.2019.01.004

红花抗帕金森病有效成分滴丸的制备和表征

程士轩¹, 马迎聪¹, 刘瑜洁¹, 庞宁¹, 李骥¹, 沙勐², 任汝通³, Nuramatjan Ablat³, 曹静⁴, 孙懿³, 蒲小平³, 叶敏⁴, 齐宪荣^1*

1. 北京大学医学部药学院药剂学系, 北京, 100191
2. 北京大学医学部药学院化学生物学系, 北京, 100191
3. 北京大学医学部药学院分子与细胞药理学系, 北京 100191
4. 北京大学医学部药学院天然药物学系, 北京 100191

收稿日期:2018-05-17 修回日期:2018-10-08 出版日期:2019-01-27 发布日期:2018-11-14
通讯作者: Tel.: +86-010-82801584, E-mail: qixr@bjmu.edu.cn
基金资助:
Science and Technology Major Projects: Significant New-Drugs Creation (Grant No. 2012ZX09103201-042).

Preparation and characterization of drop pills of effective part from safflower for anti-Parkinson’s disease

Shixuan Cheng¹, Yingcong Ma¹, Yujie Liu¹, Ning Pang¹, Ji Li¹, Meng Sha², Rutong Ren³, Nuramatjan Ablat³, Jing Cao⁴, Yi Sun³, Xiaoping Pu³, Min Ye⁴, Xianrong Qi^1*

1. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
2. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
3. Department of Molecular and Cellular Pharmacology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
4. Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China

Received:2018-05-17 Revised:2018-10-08 Online:2019-01-27 Published:2018-11-14
Contact: Tel.: +86-010-82801584, E-mail: qixr@bjmu.edu.cn
Supported by:
Science and Technology Major Projects: Significant New-Drugs Creation (Grant No. 2012ZX09103201-042).

摘要/Abstract

摘要：

帕金森病(PD)是中枢神经系统常见的退行性疾病,其病理特征主要是黑质和多巴胺神经元的变性。研究表明,红花黄酮提取物(SAFE)具有神经保护作用。本研究采用SAFE和基质PEG6000通过加热熔融法制备抗帕金森病红花黄酮提取物滴丸(SAFE-DPs)。用粉末X射线衍射(PXRD),差示扫描量热法(DSC),傅立叶变换红外光谱(FT-IR),扫描电子显微镜(SEM)和溶出度测试评价药丸的性能。分析结果表明,在没有任何化学反应的情况下, 基质PEG6000中的SAFE分散体具有无定形状态。在制造过程和储存期间, SAFE-DP都表现出可接受的化学和物理稳定性。在三种溶解介质(pH 1.0, pH 6.8和pH 7.5)中的溶解测试表明SAFE-DP具有优异的溶解性质。山奈酚-3-O-芸香糖苷(K3R)在Caco-2单层上的转运和在原位肠灌注的吸收揭示SAFE的主要成分具有良好的转运和吸收能力。因此,滴丸在胃肠道中具有好的释放和吸收,预计体内有较好的药理学和药效学结果。

关键词: 红花黄酮提取物, 帕金森病, 固体分散体, 滴丸, 山奈酚-3-O-芸香糖苷, 性质

Abstract:

Parkinson's disease (PD) is a common degenerative disease of the central nervous system, and the pathologic features are mainly degeneration of substantianigra and dopamine neurons. Studies have shown that safflower flavonoid extract (SAFE) exhibits the neuroprotective effect. In this study, the safflower flavonoid extract drop pills (SAFE-DPs) for anti-PD were prepared by the heating and melting method using SAFE and matrix PEG6000. The performances of the pills were evaluated with powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM) and dissolution testing. The analysis results demonstrated an amorphous state for SAFE dispersion in the matrix PEG6000 without any chemical reaction. The SAFE-DPs demonstrated acceptable chemical and physical stability irrespective of the manufacturing process and the storage period. Dissolution testing in three dissolution media (pH 1.0, pH 6.8 and pH 7.5) indicated that SAFE-DPs had excellent dissolution property. The transport of Kaempferol-3-rutinoside (K3R) on the Caco-2 monolayer and the absorption of K3R in situ intestinal perfusion revealed that the principal component of SAFE had a good transport and absorption capacity. Therefore, the drop pills had better release and absorption in the gastrointestinal tract, corresponding with the pharmacological and pharmacodynamic results for PD in vivo.

Key words: Safflower flavonoid extract, Parkinson’s disease, Solid dispersion, Drop pills, Kaempferol-3-O-rutinoside, Characterizations

中图分类号:

R943

Supporting:

程士轩, 马迎聪, 刘瑜洁, 庞宁, 李骥, 沙勐, 任汝通, Nuramatjan Ablat, 曹静, 孙懿, 蒲小平, 叶敏, 齐宪荣. 红花抗帕金森病有效成分滴丸的制备和表征[J]. 中国药学(英文版), 2019, 28(1): 27-39.

Shixuan Cheng, Yingcong Ma, Yujie Liu, Ning Pang, Ji Li, Meng Sha, Rutong Ren, Nuramatjan Ablat, Jing Cao, Yi Sun, Xiaoping Pu, Min Ye, Xianrong Qi. Preparation and characterization of drop pills of effective part from safflower for anti-Parkinson’s disease[J]. Journal of Chinese Pharmaceutical Sciences, 2019, 28(1): 27-39.

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红花抗帕金森病有效成分滴丸的制备和表征

Preparation and characterization of drop pills of effective part from safflower for anti-Parkinson’s disease

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