元胡止痛分散片药学研究
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摘要
元胡止痛分散片系由《中国药典》之元胡止痛片改剂而来。元胡止痛片由元胡、白芷两味药组成，临床对胃痛、胁痛、头痛及月经痛等症疗效确切，但元胡止痛片崩解、溶出迟缓，起效慢，不能满足病人希望迅速止痛的要求。为了适应临床需要，使药物崩解、溶出快，止痛迅速，将其改剂成速释剂型分散片，同时全面系统地研究改进制备工艺、质量控制方法，使其成为速效且质量稳定、可控的现代剂型。
首先根据处方药物所含成分的理化性质及处方的功能主治，以镇痛作用为评价指标，确定了合理的提取工艺路线；然后以筛选出的有效部位所含的指标成分延胡索乙素、欧前胡素为评价指标，筛选优化提取、浓缩工艺条件，采用喷雾干燥技术制成浸膏粉，同时对此半成品进行了质量控制，以确保成品质量稳定；着重研究了该分散片制备难点成型工艺，以分散片所要求的特殊崩解时限为指标，结合半成品性质研究筛选了崩解剂、填充剂的种类、配比、加入方法等，并考察了成品的体外溶出行为；进行了全面的质量标准研究，改进了薄层鉴别方法，建立了稳定的延胡索乙素的HPLC含量测定方法，对其崩解时限、溶出度进行了控制。
本实验研究所制备出的元胡止痛分散片崩解时间在3分钟以内，延胡索乙素10分钟内可溶出70％以上、20分钟后溶出趋于完全，同时，通过对制备工艺的改进，药材、半成品、成品的质量控制，保证了成品的质量，初步稳定性试验及药理实验结果表明，成品性质稳定、药效确切、质量可控。元胡止痛分散片无论在制备工艺、剂型、质量标准还是成品质量等方面较元胡止痛片均有所提高，符合四类新药改剂的要求。
Yuanhu zhitong dispersible tablet comes from yuanhu zhitong tablet by modifying the form. Consisting of Rhizoma Corydalis and Radix Angelicae Dahuricae, Yuanhu zhitong tablet has being effective in curing many pains causing by Qi stagnation and Blood stasis, such as headache, pain in the hypochondrium and stomach, pain happening in menstruation and so on.In order to alleviate pain of patients quickly, its form is now changed into dispersible tablet which disintegrates very quickly and drug in it will dissolve faster .The study has been done on pre-clinical pharmacy including determining preparation route on the basis of pharmacological experiments associated with the function of prescription, selecting the extration and concentration technology according to the contents of tetrahydropalmatine and imperatorin .controlling the quality of extract powders dried by spraying drier ,completing the form of dispersible table which is a difficult procedure by selecting the disintegrants and diluents ,and assessing the
quality of product especially establishing the metrod of determining tetrahydropalmatine by HPLC and test its dissolution and disintegrating time.
As a result, Yuanhu zhitong dispersible tablet can disintegrate within 3 mimute and tetrahydropalmatine can dissolve 70% in ten minute as well as wholly dissolve after 20 minute.Besides, the quality of the product is well controlled by contyolling the qualities of the crude hurbs and semi-product.The preliminary stability and pharmacological experiments show that the product has stable and controllable quality as well as definite effect, on alleviating pain.
首先根据处方药物所含成分的理化性质及处方的功能主治，以镇痛作用为评价指标，确定了合理的提取工艺路线；然后以筛选出的有效部位所含的指标成分延胡索乙素、欧前胡素为评价指标，筛选优化提取、浓缩工艺条件，采用喷雾干燥技术制成浸膏粉，同时对此半成品进行了质量控制，以确保成品质量稳定；着重研究了该分散片制备难点成型工艺，以分散片所要求的特殊崩解时限为指标，结合半成品性质研究筛选了崩解剂、填充剂的种类、配比、加入方法等，并考察了成品的体外溶出行为；进行了全面的质量标准研究，改进了薄层鉴别方法，建立了稳定的延胡索乙素的HPLC含量测定方法，对其崩解时限、溶出度进行了控制。
本实验研究所制备出的元胡止痛分散片崩解时间在3分钟以内，延胡索乙素10分钟内可溶出70％以上、20分钟后溶出趋于完全，同时，通过对制备工艺的改进，药材、半成品、成品的质量控制，保证了成品的质量，初步稳定性试验及药理实验结果表明，成品性质稳定、药效确切、质量可控。元胡止痛分散片无论在制备工艺、剂型、质量标准还是成品质量等方面较元胡止痛片均有所提高，符合四类新药改剂的要求。
Yuanhu zhitong dispersible tablet comes from yuanhu zhitong tablet by modifying the form. Consisting of Rhizoma Corydalis and Radix Angelicae Dahuricae, Yuanhu zhitong tablet has being effective in curing many pains causing by Qi stagnation and Blood stasis, such as headache, pain in the hypochondrium and stomach, pain happening in menstruation and so on.In order to alleviate pain of patients quickly, its form is now changed into dispersible tablet which disintegrates very quickly and drug in it will dissolve faster .The study has been done on pre-clinical pharmacy including determining preparation route on the basis of pharmacological experiments associated with the function of prescription, selecting the extration and concentration technology according to the contents of tetrahydropalmatine and imperatorin .controlling the quality of extract powders dried by spraying drier ,completing the form of dispersible table which is a difficult procedure by selecting the disintegrants and diluents ,and assessing the
quality of product especially establishing the metrod of determining tetrahydropalmatine by HPLC and test its dissolution and disintegrating time.
As a result, Yuanhu zhitong dispersible tablet can disintegrate within 3 mimute and tetrahydropalmatine can dissolve 70% in ten minute as well as wholly dissolve after 20 minute.Besides, the quality of the product is well controlled by contyolling the qualities of the crude hurbs and semi-product.The preliminary stability and pharmacological experiments show that the product has stable and controllable quality as well as definite effect, on alleviating pain.
引文
[1] 陈鹰等，中国药师，2001；4(1)：62
[2] 王卓，韩丽梅，张晓青，等．沈阳药科大学学报，1996；13(4)：235
[3] 南京药学院《中草药学》编写组．中草药学(中册)，南京：江苏人民出版社，1976：340
[4] 傅小勇，等．中成药，1986：17(12)：5
[5] 傅小勇，等．药学学报，1986；21(7)：527
[6] 马贻兴，等．中西医结合杂志，1985；5(12)：758
[7] 肖崇厚主编．中药化学，上海；上海科学技术出版社，1987
[8] 任仁安主编．中药鉴定学，上海：上海科学技术出版社，1983：131
[9] 姚川，等．中药材，1990；13(12)：34
[10] 李宏宇等，中国中药杂志，1991；6(11)：16
[11] 魏玉平等，中草药，2001：32(4)：318
[12] 中药药理与临床，1992；(8)
[13] 李国栋等，解放军药学学报，1999：15(6)
[2] 王卓，韩丽梅，张晓青，等．沈阳药科大学学报，1996；13(4)：235
[3] 南京药学院《中草药学》编写组．中草药学(中册)，南京：江苏人民出版社，1976：340
[4] 傅小勇，等．中成药，1986：17(12)：5
[5] 傅小勇，等．药学学报，1986；21(7)：527
[6] 马贻兴，等．中西医结合杂志，1985；5(12)：758
[7] 肖崇厚主编．中药化学，上海；上海科学技术出版社，1987
[8] 任仁安主编．中药鉴定学，上海：上海科学技术出版社，1983：131
[9] 姚川，等．中药材，1990；13(12)：34
[10] 李宏宇等，中国中药杂志，1991；6(11)：16
[11] 魏玉平等，中草药，2001：32(4)：318
[12] 中药药理与临床，1992；(8)
[13] 李国栋等，解放军药学学报，1999：15(6)
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