通关舒缓释胶囊的药学研究
|
摘要
通关舒缓释胶囊为治疗类风湿关节炎的现代中药复方制剂，由百合科植物土金刚和防已科植物野芙蓉二味药组成，本文按照中药新药的有关要求，进行了以下主要研究：
应用单因素筛选和正交实验的方法进行了有效部位的提取研究，以单因素试验方法对大孔吸附树脂精制土金刚总皂苷和离子交换树脂精制野芙蓉总生物碱的工艺进行了研究，制得了工艺可行，质量稳定、可控的中间体—土金刚总皂苷和野芙蓉总生物碱。
在制剂成型过程中，以中间体为原料，采用淀粉内外同加的方法，以泛制法制备了通关舒微丸，并以Surelease包衣制备了通关舒缓释微丸，对微丸性质进行了研究。
按照《中华人民共和国药典》2000版二部(附录Ⅺ ⅩD)缓释、控释制剂指导原则和一部(附录ⅠLD)胶囊剂项下要求，对通关舒缓释胶囊的外观性状、鉴别、有关胶囊剂的常规检查进行了研究；以总皂苷为指标，建立了体外累积释放度检查方法，确定了药物在不同时间的释放限度，以不同的数学模型进行拟合，解释了释药机理；研究了高效液相色谱法测定了胶囊中M皂苷元和生物碱N的含量的方法，制订了其在制剂中的含量限度。
通过本文的研究，将药物制成缓释胶囊剂，有望为临床提供一个长效而副作用小、服用及携带方便的治疗类风湿关节炎的中药复方制剂。同时也对复方中药缓释制剂的工艺特点进行了有益的探索，为中药复方缓释制剂的研制积累了一定的经验和数据。
Tongguanshu sustained release capsule is a modern Chinese herbal drug for the therapy of Rheumatoid Arthritis.It consists of two kinds of Chinese herbs, one comes from Liliaceae, the other is a plant of Menispermaceae. According to correlative regulations of patent traditional Chinese medicine, the primary researches were done as follows.
To research the extraction process of effective parts, single factor and orthogonal experiments were used. By single factor experiment, the purifying process of Tujingan total saponins extraction was researched by means of Macroporous resin; and Yefurong total alkaloids extraction was puried by Ion exchange resin. By these experiments, the practicable process was choosed.The qualities of intermediate of Tujingantang total saponins extraction and Yefurong total alkaloids extraction were stable and controllable.
As the material of preparation, the intermediates were mixed with starch both inside and ouside. The pellets were prepared by means of layering in coating pan. Then the pellets were coated by Surelease. The characters of coated pellets were also studied.
According to correlative regulations of "pharmacopoeia of the People's Republic of China" 2000's edition, the character, identifying methods, and general checks of Bitong sustained release capsule were studied; Selecting total saponins as technological marker, the method of determining the cumulate release rate was established, and the release percentage of different time was ascertained; The releasing characteristic parameter was explored by different mathematical model to explain the mechanism of drugs release. The methods of determining the content of M saponin and N alkaloid by HPLC were studied, and the limits of content were also established.
Through the research of the thesis, we made the herbs into sustained
release capsules. It's hopeful that we can offer a preparation made of compound modern Chinese herbs for clinic, which can sustainedly release and have few side effects. It is convenient for taking and earring. At the same time, through the research of process characters of compound Chinese herbs preparation, some beneficial experience and data for preparing preparation of compound Chinese herbs was accumulated.
应用单因素筛选和正交实验的方法进行了有效部位的提取研究，以单因素试验方法对大孔吸附树脂精制土金刚总皂苷和离子交换树脂精制野芙蓉总生物碱的工艺进行了研究，制得了工艺可行，质量稳定、可控的中间体—土金刚总皂苷和野芙蓉总生物碱。
在制剂成型过程中，以中间体为原料，采用淀粉内外同加的方法，以泛制法制备了通关舒微丸，并以Surelease包衣制备了通关舒缓释微丸，对微丸性质进行了研究。
按照《中华人民共和国药典》2000版二部(附录Ⅺ ⅩD)缓释、控释制剂指导原则和一部(附录ⅠLD)胶囊剂项下要求，对通关舒缓释胶囊的外观性状、鉴别、有关胶囊剂的常规检查进行了研究；以总皂苷为指标，建立了体外累积释放度检查方法，确定了药物在不同时间的释放限度，以不同的数学模型进行拟合，解释了释药机理；研究了高效液相色谱法测定了胶囊中M皂苷元和生物碱N的含量的方法，制订了其在制剂中的含量限度。
通过本文的研究，将药物制成缓释胶囊剂，有望为临床提供一个长效而副作用小、服用及携带方便的治疗类风湿关节炎的中药复方制剂。同时也对复方中药缓释制剂的工艺特点进行了有益的探索，为中药复方缓释制剂的研制积累了一定的经验和数据。
Tongguanshu sustained release capsule is a modern Chinese herbal drug for the therapy of Rheumatoid Arthritis.It consists of two kinds of Chinese herbs, one comes from Liliaceae, the other is a plant of Menispermaceae. According to correlative regulations of patent traditional Chinese medicine, the primary researches were done as follows.
To research the extraction process of effective parts, single factor and orthogonal experiments were used. By single factor experiment, the purifying process of Tujingan total saponins extraction was researched by means of Macroporous resin; and Yefurong total alkaloids extraction was puried by Ion exchange resin. By these experiments, the practicable process was choosed.The qualities of intermediate of Tujingantang total saponins extraction and Yefurong total alkaloids extraction were stable and controllable.
As the material of preparation, the intermediates were mixed with starch both inside and ouside. The pellets were prepared by means of layering in coating pan. Then the pellets were coated by Surelease. The characters of coated pellets were also studied.
According to correlative regulations of "pharmacopoeia of the People's Republic of China" 2000's edition, the character, identifying methods, and general checks of Bitong sustained release capsule were studied; Selecting total saponins as technological marker, the method of determining the cumulate release rate was established, and the release percentage of different time was ascertained; The releasing characteristic parameter was explored by different mathematical model to explain the mechanism of drugs release. The methods of determining the content of M saponin and N alkaloid by HPLC were studied, and the limits of content were also established.
Through the research of the thesis, we made the herbs into sustained
release capsules. It's hopeful that we can offer a preparation made of compound modern Chinese herbs for clinic, which can sustainedly release and have few side effects. It is convenient for taking and earring. At the same time, through the research of process characters of compound Chinese herbs preparation, some beneficial experience and data for preparing preparation of compound Chinese herbs was accumulated.
引文
[1] 吴启富．类风湿性关节炎血瘀证分析研究[J]．中国中西医结合风湿病志．1996，5(1)：19
[2] 曾宪明．无机盐对大孔吸附树脂吸附人参总皂苷的影响．中国医药工业杂志．1992，23(8)：339
[3] 于少云，王洪光，尔艳．微丸的进展．中国新药杂志．1999，8(12)：802，汪芸，姜洪芳，汪国华．微九的成型性研究进展．江西中医学院学报．2002，14(1)：59
[4] 汪芸，姜洪芳，汪国华．微丸成型性研究进展．江西中医学院学报．2002，14(1)：59
[5] 张均寿，刘国杰．乙基纤维素水性包衣技术的研究．药学进展．1999，23(2)：71
[6] 牟晓红，金京花，庄殿友．羟丙甲基纤维素酞酸酯假乳胶的制备及应用于消炎痛肠溶包衣片的质量评价．沈阳药科大学学报．1997，13(2)：157
[7] 张立超，胡晋红．聚合物水分散体包衣技术的进展．药学实践杂志．1999，17(3)：144
[8] 丁劲松，闫军．胶乳／假胶乳水性包衣技术在药剂学中的应用．华西药学杂志．2003，18(5)：349
[9] Ritger R. L. peppas, NA. Asimple equation for description of solute release Ⅰ Fickian and non-Fickian release from non-swellable devices in the form of slabs, spheres, cylinders or dixcs. J control Release, 1987, 5 (1): 23-26
[2] 曾宪明．无机盐对大孔吸附树脂吸附人参总皂苷的影响．中国医药工业杂志．1992，23(8)：339
[3] 于少云，王洪光，尔艳．微丸的进展．中国新药杂志．1999，8(12)：802，汪芸，姜洪芳，汪国华．微九的成型性研究进展．江西中医学院学报．2002，14(1)：59
[4] 汪芸，姜洪芳，汪国华．微丸成型性研究进展．江西中医学院学报．2002，14(1)：59
[5] 张均寿，刘国杰．乙基纤维素水性包衣技术的研究．药学进展．1999，23(2)：71
[6] 牟晓红，金京花，庄殿友．羟丙甲基纤维素酞酸酯假乳胶的制备及应用于消炎痛肠溶包衣片的质量评价．沈阳药科大学学报．1997，13(2)：157
[7] 张立超，胡晋红．聚合物水分散体包衣技术的进展．药学实践杂志．1999，17(3)：144
[8] 丁劲松，闫军．胶乳／假胶乳水性包衣技术在药剂学中的应用．华西药学杂志．2003，18(5)：349
[9] Ritger R. L. peppas, NA. Asimple equation for description of solute release Ⅰ Fickian and non-Fickian release from non-swellable devices in the form of slabs, spheres, cylinders or dixcs. J control Release, 1987, 5 (1): 23-26
© 2004-2018 中国地质图书馆版权所有 京ICP备05064691号 京公网安备11010802017129号 地址：北京市海淀区学院路29号 邮编：100083 电话：办公室：(+86 10)66554848；文献借阅、咨询服务、科技查新：66554700 |