独一味有效部位的筛选及其制剂研究
摘要
独一味Lamioplomis rotata(Benth.)Kudo是唇形科独一味属植物,生长于海拔4000m左右的高山草甸、河滩等处,主产于西藏、青海、云南、四川、甘肃等省区,具有止血、镇痛消肿、活血化瘀、抗菌消炎、增强免疫力等功效。
国内外学者研究表明,独一味主要含有黄酮、环烯醚萜苷、苯乙醇苷等成分,但反映独一味临床功效与药理作用的有效成分尚不明确。我们从四川石渠县采集独一味药材,将其醇提取物分为石油醚、乙酸乙酯、正丁醇、水4个部位,分别采用小鼠醋酸扭体法和断尾止血法对各部位进行了初步药效学试验,结果表明,独一味的正丁醇部位能显著减少小鼠扭体反应次数以及缩短出血时间。对正丁醇提取部分大孔树脂水洗部分、30%、90%乙醇洗脱部位,继续采用小鼠醋酸扭体法和断尾止血法筛选,其中30%乙醇洗脱部位对小鼠具有明显的镇痛、止血作用。
在有效部位的研究基础上,制备得到了以有效部位为主的独一味中间体。为了提高独一味制剂的生物利用度,减少服用量,我们以中间体为原料制备了独一味滴丸,并且建立了质量标准控制体系。
Lamioplomis rotata (Benth) Kudo, a plant of lamioplomis genus (labiatae family),widely grows in alpine meadow and flood land at altitude 4000m. It distributes in Tibet, Mongolia and Naxi people to promote blood circulation, remove blood stasis, subdue swelling and alleviate pain.
That main compounds in Lamiophlomis rotata (Benth) Kudo were reported as flabonoids, iridoids and phenethanol glycoside, but the active components reflecting clinical effectiveness were still unkown. 70% ethanol extraction of the herb, collected in Shiqu county of Sichuan province, was partitioned into four fractions as petroleum spirit, acetic ether, n-butanol and water portion. Guide with initial pharmacological activities test on mice streching model and broken tail model, n-butanol fraction was showed to have obvious analgesic action on reducing the times of mice writing reaction caused by acetic acid and reducing the times of bloodsheding. The portion of water, 30% and 90% ethanolic elution obtained after purification with macroporous resin from n-butanol fraction. 30% of them was found to show strong stanching blood and analgesia activity.
Effective in the study were based on the preparation to be effective parts of the mainly Duyiwei intermediates. To improve the preparation Duyiwei bioavailability, and reduce use of volume, We intermediates for the preparation of study materials Duyiwei pills, and to establish the quality standards.
国内外学者研究表明,独一味主要含有黄酮、环烯醚萜苷、苯乙醇苷等成分,但反映独一味临床功效与药理作用的有效成分尚不明确。我们从四川石渠县采集独一味药材,将其醇提取物分为石油醚、乙酸乙酯、正丁醇、水4个部位,分别采用小鼠醋酸扭体法和断尾止血法对各部位进行了初步药效学试验,结果表明,独一味的正丁醇部位能显著减少小鼠扭体反应次数以及缩短出血时间。对正丁醇提取部分大孔树脂水洗部分、30%、90%乙醇洗脱部位,继续采用小鼠醋酸扭体法和断尾止血法筛选,其中30%乙醇洗脱部位对小鼠具有明显的镇痛、止血作用。
在有效部位的研究基础上,制备得到了以有效部位为主的独一味中间体。为了提高独一味制剂的生物利用度,减少服用量,我们以中间体为原料制备了独一味滴丸,并且建立了质量标准控制体系。
Lamioplomis rotata (Benth) Kudo, a plant of lamioplomis genus (labiatae family),widely grows in alpine meadow and flood land at altitude 4000m. It distributes in Tibet, Mongolia and Naxi people to promote blood circulation, remove blood stasis, subdue swelling and alleviate pain.
That main compounds in Lamiophlomis rotata (Benth) Kudo were reported as flabonoids, iridoids and phenethanol glycoside, but the active components reflecting clinical effectiveness were still unkown. 70% ethanol extraction of the herb, collected in Shiqu county of Sichuan province, was partitioned into four fractions as petroleum spirit, acetic ether, n-butanol and water portion. Guide with initial pharmacological activities test on mice streching model and broken tail model, n-butanol fraction was showed to have obvious analgesic action on reducing the times of mice writing reaction caused by acetic acid and reducing the times of bloodsheding. The portion of water, 30% and 90% ethanolic elution obtained after purification with macroporous resin from n-butanol fraction. 30% of them was found to show strong stanching blood and analgesia activity.
Effective in the study were based on the preparation to be effective parts of the mainly Duyiwei intermediates. To improve the preparation Duyiwei bioavailability, and reduce use of volume, We intermediates for the preparation of study materials Duyiwei pills, and to establish the quality standards.
引文
1、马世林,王振华,毛继祖译注.月王药疹[M].甘肃民族出版社,兰州,1993
2、宇妥·元丹贡布等著,马世林等译注.四部医典[M].上海科学技术出版社,上海,1987
3、帝玛尔·丹增彭措著,马世林等译注.晶珠本草[M].上海科学技术出版社,上海,1986
4、梁重栋.藏药独一味的基础与临床研究[J].兰州医学院学报,1987,40(2):472-491
5、易进海,钟炽昌,罗泽渊,等.糙苏属和独一味属植物的化学成分及其分类学意义[J].中草药,1992,23(7):382-384
6、张承忠,李冲,石建功,等.藏药独一味中的环烯醚萜[J].中草药,1992,23(10):509-511
7、易进海,钟炽昌,罗泽渊,等.藏药独一味根化学成分的研究[J].药学学报,1990,26(1):37-41
8、易进海,钟炽昌,罗泽渊,等.独一味C的结构[J].药学学报,1992,27(3):204-206
9、易进海,黄小平,陈燕,等.藏药独一味根环烯醚萜甙的研究[J].药学学报,1997,32(5):357-360
10、易进海,颜贤忠,罗泽渊,等.藏药独一味根化学成分的研究[J].药学学报,1995.30(3):206-210
11.Jin-Hai Yi,Guo-Lin Zhang,Bo-Gang Li,et al.phentlpropanoid glycosides from Lamiophlomis rotata[J].Phytochemistry,1999,51:825-828
12、国家中医药管理局《中华本草》编委会.中华本草(第七卷)[M].上海科学技术出版社,上海,1999:6074-6075
13、贾孝荣,忘镜.藏药独一味止血机理探讨[J].甘肃中医学院学报,1994,11 (2):4-6
14、程国权,席时芳,王雁,等.独一味皂苷及其醇提取物对小鼠移植性肿瘤的抑制作用和对荷瘤小鼠免疫器官重量的影响[J].甘肃医药,1985,4(3):3-5
15、贾孝荣,忘镜.藏药独一味对粒系祖细胞影响的实验研究[J].兰州医学院学报,1995,21(3):138-140
16、王肖蓉.应用藏药独一味片止痛化瘀临床观察[J].中国民族民间医药杂志,2000,46(5):275-276
17、叶光华.独一味片治疗骨外科疾病356例镇痛疗效总结[J].白云医药信息,1995,4(2):10-12
18、郑晓霞,代大平.独一味胶囊在骨折治疗中的临床观察[J].现代中医药,2002,(5):86
19、秦万龙.独一味胶囊治疗癌性疼痛128例[J].中国中医药信息杂志,2001,8(10):65-66
20、李洪亮,郝民安,王宝太,等.藏药独一味对癌痛的镇痛作用[J].河北医药,2002,24(2):14-15
21、覃刚,任正心,殷泽登,等.独一味胶囊治疗鼻出血疗效观察[J].中国中西医结合耳鼻咽喉科杂志,1999,7(增刊):321
22、覃刚,任正心,殷泽登,等.藏药独一味用于手术后疗效观察[J].中国民间医药杂志,2000,6(3):14-15
23、张国英.藏药独一味治疗各种疼痛142例疗效分析[J].青海医药杂志,2000,30(10):8
24、曹崇媛,谭毅勇.独一味片对镇痛疗效的开放观察[J].四川省卫生干部管理学院学报,2000,19(2):105-106
25、孙福忠,乔培诰.独一味止血镇痛作用观察[J].时珍国医国药,2001,12(1):79
26、李凌,钟晓东,何爱群.独一味胶囊对外眼术后出血镇痛疗效观察[J].中华医学丛刊,2003,3(1):79
27、闫美章,胡德芬,邓蜀华.独一味胶囊治疗药物流产后阴道出血60例[J].中 国药业,2001,10(6):35
28、李冬枝.独一味治疗鼻出血的临床观察[J].河南职工医学院学报,2002,14(4):341
29、李新民,张春红.独一味胶囊保留灌肠治疗溃疡性结肠炎的临床观察[J].长治医学院学报,2002,16(3):196-197
30、漆明,赵丽萍,叶丽霞.独一味胶囊治疗复发性阿弗他溃疡46例疗效观察[J].新中医,2002,34(3):30-31
31、金海英.独一味片剂治疗附件肿瘤30例[J].实用中医药杂志,2001,17(5):35
2、宇妥·元丹贡布等著,马世林等译注.四部医典[M].上海科学技术出版社,上海,1987
3、帝玛尔·丹增彭措著,马世林等译注.晶珠本草[M].上海科学技术出版社,上海,1986
4、梁重栋.藏药独一味的基础与临床研究[J].兰州医学院学报,1987,40(2):472-491
5、易进海,钟炽昌,罗泽渊,等.糙苏属和独一味属植物的化学成分及其分类学意义[J].中草药,1992,23(7):382-384
6、张承忠,李冲,石建功,等.藏药独一味中的环烯醚萜[J].中草药,1992,23(10):509-511
7、易进海,钟炽昌,罗泽渊,等.藏药独一味根化学成分的研究[J].药学学报,1990,26(1):37-41
8、易进海,钟炽昌,罗泽渊,等.独一味C的结构[J].药学学报,1992,27(3):204-206
9、易进海,黄小平,陈燕,等.藏药独一味根环烯醚萜甙的研究[J].药学学报,1997,32(5):357-360
10、易进海,颜贤忠,罗泽渊,等.藏药独一味根化学成分的研究[J].药学学报,1995.30(3):206-210
11.Jin-Hai Yi,Guo-Lin Zhang,Bo-Gang Li,et al.phentlpropanoid glycosides from Lamiophlomis rotata[J].Phytochemistry,1999,51:825-828
12、国家中医药管理局《中华本草》编委会.中华本草(第七卷)[M].上海科学技术出版社,上海,1999:6074-6075
13、贾孝荣,忘镜.藏药独一味止血机理探讨[J].甘肃中医学院学报,1994,11 (2):4-6
14、程国权,席时芳,王雁,等.独一味皂苷及其醇提取物对小鼠移植性肿瘤的抑制作用和对荷瘤小鼠免疫器官重量的影响[J].甘肃医药,1985,4(3):3-5
15、贾孝荣,忘镜.藏药独一味对粒系祖细胞影响的实验研究[J].兰州医学院学报,1995,21(3):138-140
16、王肖蓉.应用藏药独一味片止痛化瘀临床观察[J].中国民族民间医药杂志,2000,46(5):275-276
17、叶光华.独一味片治疗骨外科疾病356例镇痛疗效总结[J].白云医药信息,1995,4(2):10-12
18、郑晓霞,代大平.独一味胶囊在骨折治疗中的临床观察[J].现代中医药,2002,(5):86
19、秦万龙.独一味胶囊治疗癌性疼痛128例[J].中国中医药信息杂志,2001,8(10):65-66
20、李洪亮,郝民安,王宝太,等.藏药独一味对癌痛的镇痛作用[J].河北医药,2002,24(2):14-15
21、覃刚,任正心,殷泽登,等.独一味胶囊治疗鼻出血疗效观察[J].中国中西医结合耳鼻咽喉科杂志,1999,7(增刊):321
22、覃刚,任正心,殷泽登,等.藏药独一味用于手术后疗效观察[J].中国民间医药杂志,2000,6(3):14-15
23、张国英.藏药独一味治疗各种疼痛142例疗效分析[J].青海医药杂志,2000,30(10):8
24、曹崇媛,谭毅勇.独一味片对镇痛疗效的开放观察[J].四川省卫生干部管理学院学报,2000,19(2):105-106
25、孙福忠,乔培诰.独一味止血镇痛作用观察[J].时珍国医国药,2001,12(1):79
26、李凌,钟晓东,何爱群.独一味胶囊对外眼术后出血镇痛疗效观察[J].中华医学丛刊,2003,3(1):79
27、闫美章,胡德芬,邓蜀华.独一味胶囊治疗药物流产后阴道出血60例[J].中 国药业,2001,10(6):35
28、李冬枝.独一味治疗鼻出血的临床观察[J].河南职工医学院学报,2002,14(4):341
29、李新民,张春红.独一味胶囊保留灌肠治疗溃疡性结肠炎的临床观察[J].长治医学院学报,2002,16(3):196-197
30、漆明,赵丽萍,叶丽霞.独一味胶囊治疗复发性阿弗他溃疡46例疗效观察[J].新中医,2002,34(3):30-31
31、金海英.独一味片剂治疗附件肿瘤30例[J].实用中医药杂志,2001,17(5):35