黑胡椒和白胡椒(Piper nigrum L.)中大量活性药物成分胡椒碱的分离

Z. Khan, F. Moni, S. Sharmin, M. A. Al-Mansur, A. Gafur, O. Rahman, F. Afroz
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引用次数: 20

摘要

在制药领域,大多数活性药物成分(API)都是从天然产物中获得的。胡椒碱是一种天然存在的生物碱,具有广泛的药理活性,是主要的生物活性植物化学物质。它是从最有价值的民族药用香料胡椒中提取的,即黑胡椒和白胡椒,它们是亚洲藤蔓胡椒的果实。由于这种药用化合物的广泛传统用途,本文揭示了一种简单有效的分离散装胡椒碱的方法。本研究的新颖之处在于为利用这种天然方法大规模商业化生产原料药提供了一种思路。胡椒碱以纯晶体形式分离出来,并通过熔点、x射线衍射(XRD)研究和光谱数据(包括二维核磁共振(2D-NMR)光谱)进行了表征。采用薄层色谱(TLC)和高效液相色谱(HPLC)等色谱技术测定所得胡椒碱的纯度。黑胡椒胡椒碱的产率在2.5% ~ 3.0%之间,白胡椒胡椒碱的产率在4.0% ~ 4.5%之间,黑胡椒胡椒碱的纯度为98.5%,白胡椒胡椒碱的纯度为98.2%。从产率和纯度来看,这种有效的分离方法可以成功地用于工业大规模生产。根据结果,可以认为分离得到的胡椒碱作为天然产物,也可以像其他昂贵的化学合成胡椒碱一样,在不同的药物配方中作为原料药使用。
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Isolation of Bulk Amount of Piperine as Active Pharmaceutical Ingredient (API) from Black Pepper and White Pepper (Piper nigrum L.)
In the pharmaceutical world the majority of the active pharmaceutical ingredients (API) have been obtained from the natural products. Piperine is such naturally occurring alkaloid which can be considered as major bioactive phytochemical having broad spectrum of pharmacological activities. It is obtained from the most valuable ethnomedicinal spices peppercorns i.e. black pepper and white pepper, which are the fruits of the Asian vine Piper nigrum L. Because of the widespread traditional uses of this medicinal compound, present article reveals a simple and effective isolation method of bulk piperine. The novelty of this investigation is to provide an idea for utilizing such natural method of large scale commercial piperine production as API drug in spite of chemical synthesis. Piperine was isolated in a pure crystal form and characterized by its melting point, X-Ray diffraction (XRD) studies and spectral data, including two-dimensional nuclear magnetic resonance (2D-NMR) spectroscopy. Chromatographic techniques like Thin Layer Chromatography (TLC) and High Performance Liquid Chromatography (HPLC) were applied to determine the purity of the yielded piperine. It was found that piperine yield from black pepper was within 2.5% - 3.0% and from white pepper within 4.0% - 4.5% and the purity of the yielded piperine was found to be up to 98.5% for black pepper and 98.2% for white pepper. Considering this yield value and purity it is indicated that, such effective isolation method can be successfully utilized for industrial large-scale production commercially. According to the result, it can be claimed that, as a natural product the isolated piperine can also be utilized as API drug like other expensive chemically synthesized piperine in different drug formulation.
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