腰痛宁胶囊中马钱子粉的制备方式对其质量和体外溶出性质的影响
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摘要
为了研究粒径及制备方式对腰痛宁胶囊中马钱子粉中有效成分(也是有毒成分)马钱子碱、士的宁的含量及体外释放的影响,本文制备了不同粒径的马钱子粉样品集1,低比例乳香、没药与制马钱子混合粉碎的样品集2,高比例乳香、没药与制马钱子混合粉碎的样品集3以及乳香粉、没药粉与制马钱子混合粉碎的样品4。建立了马钱子碱、士的宁的高效液相色谱(HPLC)含量测试方法,测定马钱子粉中马钱子碱、士的宁含量并对各组样品的微观形貌进行了扫描电镜(SEM)分析。以人工胃液为溶出介质,采用桨法对以上各组样品进行马钱子碱、士的宁的体外溶出度测试。
     结果表明不同粒径下马钱子粉样品微观形态组成比例存在差异且其马钱子碱、士的宁含量不尽相同,马钱子碱(或士的宁)在部分样品中的含量存在显著性差异。将马钱子粉粒径控制在100-200目之间时,马钱子碱、士的宁含量变化很小。样品集2~3及样品4的SEM分析结果显示乳香、没药均可附着在马钱子粉表面且随着乳香、没药比例的增加附着更加充分;样品集3中样品1:1与样品4药材配比相同但制备方式不同,者的微观形貌无明显差异。溶出度测试结果表明,样品集1、2中各样品中马钱子碱与士的宁在80min后停止释放,样品集3与样品4中马钱子碱与士的宁在240min后不再释放,说明高比例乳香(粉)、没药(粉)与制马钱子混合粉碎可使马钱子粉中马钱子碱、士的宁的释放时间延迟160min。
In order to study the effect of particle size and preparation way on the content and release rate in vitro of brucine and strychnine, which are active (also toxic) components of semen strychni powder in Yaotongning capsule, a series of samples of semen strychni powder were made as follows:semen strychni powder with different particle sizes (sample set 1), semen strychni powder prepared by crushing mixture of processed semen strychni and low proportion of frankincense and myrrh (sample set 2), semen strychni powder prepared by crushing mixture of processed semen strychni and high ratio of frankincense and myrrh (sample set 3) and sample 4 which was made by crushing mixture of processed semen strychni and powder of frankincense and myrrh. High performance liquid chromatography (HPLC) methods for determining brucine and strychnine were established. The microstructures of all samples were examined by scanning electronic microscope (SEM). The oar method was used to test the dissolution in vitro of burcine and strychnine of all samples in artificial gastric juice.
     It is shown that the morphology compositions and contents of brucine and strychnine in semen strychni powder samples of sample set 1 with different particle sizes are different. And there are significant difference between contents of brucine and strychnine in some samples of sample set 1. When particle size of semen strychni powder is controlled in the region of 100-200 mesh, the contents of brucine and strychnine vary little. SEM images demonstrate that frankincense and myrrh adhered to the surface of semen strychni powder in sample set 2~3 and sample 4. The adhesion is stronger with increasing the quantity addition of frankincense and myrrh. Sample 1:1 in sample set 3 has the same proportion of frankincense, myrrh and processed semen strychni with sample 4, but the crushing way of the two samples are different. There is no significant difference between their SEM images. The dissolving experiment in vitro show that brucine and strychnine stopped releasing after 80min in sample set 1~2. For sample set 3 and sample 4, the release time of brucine and strychnine is 240min. The result indicates that crushing mixture of processed semen strychni and high ratio of frankincense and myrrh can delay the release time of brucine and strychnine 160min.
引文
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