维脑路通及其各组分在7例患者的药物动力学

目的观察维脑路通及其各组分在人体内的药物动力学。方法7例患者静脉滴注维脑路通注射液600mg 后 ,用一种程序控制检测灵敏度的反相高效液相色谱法测定不同时间血清中维脑路通和各种羟乙基芦丁含量,并分别计算其药物动力学。结果维脑路通和一、二羟乙基芦丁在血清中的药物动力学为一室开放模型 ,三、四羟乙基芦丁为二室开放模型 ,各组分生物半衰期随羟乙基数目增加而缩短。结论维脑路通的动力学过程与其组分并不呈现一致性     

维脑路通及其各组分在7例患者的药物动力学

目的：观察维脑路通及其各组分在人体内的药物动力学。方法：7例患静脉滴注维脑路通注射液600mg后，用一种程序控制检测灵敏度的反相高效液相色谱法测定不同时间血清中维脑路通和各种羟乙基芦丁含量，并分别计算其药物动力学。结果：维脑路通和一、二羟乙基芦丁在血清中的药物动力学为一室开放模型，三、四羟乙基芦丁为二室开放模型，各组舂生物半衰期随羟乙基数目增加而缩短。结论：维脑路通的动力学过程及其组分并不呈现一致性。     

高效液相色谱法分离测定维脑路通

维脑路通(Venoruton)即羟乙基芦丁(HER),是治疗脑血管疾病的药物。其主要成分——(羟乙基)芦丁、二(羟乙基)、芦丁3＇,4＇,5-三(羟乙基)芦丁和3＇,4＇,5,7-四(羟乙基)芦丁等的正相和反相高效液相色谱法已     

市售曲克芦丁片质量分析

曲克芦丁(troxerutin,维脑路通,羟乙基芦丁)能降低毛细血管通透性和脆性,提高毛细血管抵抗力;抑制血小板凝集,防止血栓形成。它是由7-羟乙基芦丁、4＇,7-二羟乙基芦丁、3＇,4＇,7-三羟乙基芦丁和3＇,4＇,5,7-四羟乙基芦丁等组成的混合物。目前国内有数十家药厂生产片剂。笔者选择了市售6个省份10家药厂生产的18批次曲克芦丁片,按《山西省药品标准》1990版有关方法检验,对其性状、鉴别、崩解时限、含量进行考察。1 仪器与试药     

利用HPLC法测定维脑路通输液中三羟乙基芦丁含量的研究

维脑路通输液是由维脑路通和氯化钠组成,临床上采用静脉滴注用于治疗闭塞性脑血管病、中心性视网膜炎、动脉硬化、冠心病、血栓性静脉炎、静脉曲张、慢性静脉功能不全等。维脑路通是由一、二、三、四羟乙基芦丁组成的混合物,其显效成分主要为三羟乙基芦丁。市售常见规格为250mL和500 mL,其含量测定采用紫外法,测定结果为总黄酮,专属性较差,正相和反相高效液相色谱法已见报道,但效果不理想,我们参考文献[4]的流动相进行了筛选,得到了满意的     

维脑路通鉴定会在太原召开

维脑路通系由太原制药厂研制成功。山西省卫生局、医药局于1979年12月5～7日在太原主持召开了鉴定会。它是以槐角的主要成份芦丁经羟乙基化制成的羟乙基芦丁,经山西医学院第一附属医院等单位临床肌注或静脉滴注,治疗闭塞性脑血管病97例,痊愈35例,显效30例,好转20例,总有效率87.8%;视网膜水肿和出血25例,有效率88%。与会代表经过认真讨论认为维脑路通工艺合理、质量可靠、原料易得、疗效较好,通过了鉴定并建议组织生产,满足临床需要。     

维脑路通致尿潴留3例

维脑路通致尿潴留３例陈继祥，刘大军，陈进文（山东省单县慢性病防治院２７３７００）陈敦凤（山东省单县中心医院）维脑路通又名羟乙基芦丁，主要用于治疗缺血性心脑血管病，笔者在临床实践中遇到３例患者因静滴该药而导致尿潴留，此副作用临床上少见报道，现报告于下：...     

大剂量维脑路通过敏1例

女 ,17岁 ,学生。因皮肤瘙痒 3周 ,伴黄疸 2周于 1998年 9月 14日入院。病前否认有肝炎接触史 ,入院查体除皮肤、巩膜中重度黄疸 ,皮肤有搔抓痕迹外 ,余无特殊。经辅助检查确诊为黄疸型病毒性肝炎。遂采用大剂量维脑路通 (2g/d)静滴治疗 (江苏扬州制药厂生产 ,批号 970 82 0 ) ,约 5min后病人突感皮肤瘙痒加重 ,胸闷、咽喉不适明显 ,以及声嘶、唇绀、呼吸急促、双手抓喉、极度烦躁 ,呈频死感。立即停用维脑路通 ,经吸氧、肌注非那根、静注地塞米松后缓解 ,诊断为维脑路通过敏反应。讨论 :维脑路通又名羟乙基芦丁、曲克芦丁 ,为中草药提取有…     

不同剂量维脑路通治疗急性脑血栓病的对比

不同剂量维脑路通治疗急性脑血栓病的对比许真卫，高玉梅，任保水（河北省衡水市哈励逊国际和平医院０５３０００）维脑路通（羟乙基芦丁），对急性、缺血性脑损伤有显著保护作用，能防止血栓形成，增加血中氧含量和氧饱和度，促进新血管生成或增进侧枝血管循环，对血管内...     

维脑路通氯化钠注射液生产中的注意事项

维脑路通又称羟乙基芦丁,属国家基本药物。其制剂作为治疗心脑血管疾病的常用药物已被广泛应用于临床。因其价格低廉,疗效确切,为广大医生和患者所认可。维脑路通氯化钠注射液是维脑路通与氯化钢的灭菌水溶液,做为维脑路通制剂的新剂型（输液剂）具有使用方便、减少配药操作污染的特点,然而这种剂型临床应用并不多见,究其原因是该产品容易发生输液反应,同时澄明度问题、PH值不稳定问题也很难解决。最近一段时间,我们组织广大科技人员,在总结前期经验的基础上,通过多次实验、探索,成功地解决了影响维脑路通氯化钠注射液产品质量…     

Metabolism of the Hydroxyethylrutosides III. The Fate of Orally Administered Hydroxyethylrutosides in Laboratory Animals; Metabolism by Rat Intestinal Microflora in vitro

1. The absorption, metabolism and excretion of hydroxyethylrutosides in rat and other mammals have been studied. Following oral administration to rats of 3′,4′,7-tri-O-(β-hydroxyethyl)rutoside, 4′,7-di-O-(β-hydroxyethyl)ruto-side and 7-O-(β-hydroxyethyl)rutoside, significant levels of the administered compounds and their conjugates in bile were observed, but 3′,4′,5,7-tetra-O-(β-hydroxyethyl)rutoside was poorly absorbed. The major portion of the dose of each rutoside was excreted as the aglycone in faeces. Urinary excretion of all rutosides was low.

2. Levels of excretion of ¹⁴C in the urine of rabbits and rhesus monkeys given 3′,4′,7-tri-O-(β-hydroxy[¹⁴C₂]ethyl)rutoside and 3′,4′,5,7-tetra-O-(β-hydroxy[¹⁴C₂]ethyl)rutoside were similar (<2.5% of dose) to those observed in the rat.

3. The hydroxyethylrutosides and rutin are degraded to their aglycones by the rat intestinal microflora both in vivo and in vitro. The B rings of rutin and 7-O-(β-hydroxyethyl)rutoside give rise to the same phenolic acid metabolites. Mono-O-(β-hydroxyethyl)phloroglucinol is formed from the A ring of 7-O-(β-hydroxyethyl)rutoside. Excretion of these metabolites in urine is suppressed by concurrent administration of neomycin.

4. 3′,4′,7-Tri-O-(β-hydrcxyethyl)rutoside did not undergo cleavage to metabolites other than the aglycone after continuous administration to rats for periods of up to 5 months.     

加压制备色谱技术结合HPLC指纹图谱导向快速分离制备红花提取物中的主要黄酮类成分（英文）

以HPLC指纹图谱为导向,应用中压反相硅胶柱色谱以及半制备高压液相色谱两种方法,对红花提取物中主要化合物进行快速分离。共分离得到了12个化学成分,包括9个黄酮醇类（1–9）和3个查尔酮类（10–12）。经波谱解析并与文献数据相比对,鉴定其结构分别为：山柰酚3-氧芸香糖苷（1）,山柰酚3-氧葡萄糖苷（2）,芦丁（3）,槲皮素3-氧葡萄糖苷（4）,6-羟基山柰酚3,6,7-三氧葡萄糖苷（5）,6-羟基山柰酚3-氧葡萄糖苷（6）,6-羟基山柰酚6,7-二氧葡萄糖苷（7）,6-羟基山柰酚3-氧芸香糖苷（8）,6-羟基山柰酚3,6-二氧葡萄糖苷7-氧葡萄糖醛酸苷（9）,异红花黄色素C（10）,红花黄色素C（11）,羟基红花黄色素A（12）。结果表明,加压制备色谱结合指纹图谱导向分离是制备靶标化合物一种快速高效的技术手段。     

山莨菪碱的全合成

山莨菪碱为一新胆碱能神经阻滞药。毒性低,外周作用比中枢作用强。全合成是以呋喃为原料,合成6β-羟基托品酮,将羟基乙酰化后,再将3-位酮基催化还原为α-羟基,然后用乙酰托品酰氯酯化、水解而得。本文主要报道6β-乙酰氧基托品醇与乙酰托品酰氯的酯化反应及酯化物水解合成山莨菪碱的研究。该方法现已由工厂正式投产,药品名654-2。     

密蒙花黄酮类化合物的分离和鉴定

从密蒙花(Buddleia officinalis Maxim)的花蕾中分离得到8个黄酮类化合物,其小3个甙元:刺槐素(acacetin,1),芹菜素(apigenin,2),木犀草素(luteolin,3);5个甙:密蒙花新甙(neobudofficide,4),蒙花甙(linarin=acaciin,5),木犀草素7-O-芸香糖甙(6),木犀草素-7-O-葡萄糖甙(7),秋英甙(cosmosiin,8)。化合物4为新化合物,用化学和波谱法确定其结构为5.7-二羟基-4'-甲氧基黄酮-7-O-α-L-吡喃鼠李糖基-(1→2)-[α-L-吡喃鼠李糖基-(1→6)]-β-D-吡喃葡萄糖甙,除化合物1和5以外,其它化合物均为首次从密蒙花中得到。     

A New Isoflavone Glycoside from Dalbergia vacciniifolia (Fabaceae)

5,5'-Dihydroxy-2',4'-dimethoxy-7-[(6-O-β-d-apiofuranosyl-β-d-glucopyranosyl)-oxy]isoflavone (1) was isolated as the major constituent of Dalbergia vacciniifolia root bark ethanol extract together with the four known compounds 5,7-dihydroxy-2',4',5'-trimethoxyisoflavone (3), 5,7-dihydroxy-2',4'-dimethoxy-isoflavone (4), 5-hydroxy-2',4',7-trimethoxyisoflavone (5) and 7-hydroxy-2',4',5'-trimethoxyisoflavone (6). Identification of compounds was achieved through extensive analysis of 1D and 2D NMR and MS spectroscopy.     

Two new flavonoid glycosides from Artemisia frigida Willd

An investigation of the n-BuOH-soluble fraction from the aerial parts of Artemisia frigida has led to the isolation of two new flavonoid glycosides, named friginoside A and friginoside B. Their structures were characterized as 5,7-dihydroxy-3',4',5'-trimethoxy flavone 7-O-β-d-glucuronide (1) and 5,7-dihydroxy-3',4',5'-trimethoxyflavone 7-O-β-d-glucuronyl-(1?→?2)O-β-d-glucuronide (2) on the basis of 1D and 2D NMR spectral analysis.     

酒石酸胺盐的锑衍生物

酒石酸与对羧甲巯基苯胺、对羧甲基苯胺、对氦基苯甲酸、二甲基β-羟乙基胺、二乙基β-羟乙基胺、β-羟基乙胺、二(β-羟基乙)胺、三(β-羟基乙)胺、三甲胺、三乙胺、8-羟基喹啉等作用,再与新鲜沉淀的亚锑酸共沸,制成了相应的酒石酸胺盐的锑衍生物.对日本血吸虫病的实验治疗中,疗效均不及酒石酸锑钾.     

沙生蜡菊花降脂活性部位化学成分的分离与鉴定(Ⅱ)

目的沙生蜡菊花降脂活性部位中的化学成分研究。方法采用硅胶、ODS、制备HPLC等多种色谱方法分离纯化,依据理化性质、波谱数据分析进行结构鉴定。结果从沙生蜡菊花的降脂活性部位中分离得到11个化合物,并分别鉴定为:丁香苷(syringin,1)、二氢丁香苷(dihydrosyringin,2)、(E)-4-hydroxybenzalacetone-3-O-β-D-glucopyranoside(3)、4-烯丙基-2-甲氧基苯基1-O-β-D-呋喃芹糖(1-6)-β-D-吡喃葡萄糖苷[4-allyl-2-methoxyphenyl 1-O-β-D-apiofuranosyl-(1-6)-O-β-D-glu-copyranoside,4]、苔黑酚-β-D-吡喃葡萄糖苷(orcinol-β-D-glucopyranoside,5)、7-hydroxy-5-me-thoxyphthalide-7-O-β-D-glucopyranoside(6)、5,7-dihydroxyphthalide-7-O-β-D-glucopyranoside(7)、undulatoside A(8)、adenosine(9)、maltol-3-O-β-D-apiofuranosyl-(1-6)-β-D-glucopyranoside(10)、2,4,6-三羟基苯乙酮-2,4-二-O-β-D-吡喃葡萄糖苷(2,4,6-trihydroxylacetophenone-2,4-di-O-β-D-glu-copyranoside,11)。结论化合物1～11均为首次从蜡菊属植物中分离得到。     

The Disposition and Metabolism of 3',4',7-Tri-O-(β-hydroxyethyl) rutoside and 7-Mono-O-(β-hydroxyethyl)rutoside in the Mouse

1. Following intravenous administration of 3',4',7-tri-O-(β-hydroxy[¹⁴C₂]ethyl)rutoside or 7-mono-O-(β-hydroxy[¹⁴C₂]ethyl)rutoside to male mice, 68% of the dose of each is excreted in faeces as the corresponding hydroxyethyl-quercetin within 72?h of dosage. Mean urinary excretions of mono- and tri-hydroxyethylrutosides in 72?h were 27 and 21% respectively. Unchanged rutosides and their glucuronides were detected in urine.

2. In biliary-cannulated animals, the mean biliary excretion of both tri- and mono-hydroxyethylrutosides was 71%, in 24?h of dosage. In both cases most ¹⁴C was excreted in 3?h, as unchanged rutosides and glucuronide conjugates.

3. Fall of blood ¹⁴C concn. was rapid for both compounds. Neither compound was detected in brain but there was short-term accumulation in liver and kidney, and 2-3?h after dosage, most ¹⁴C for both compounds was associated with the gastro-intestinal contents.

4. Animals killed 72?h after dosage of either compound contained <7% of dose, mostly in the color and caecal contents.

5. Foetuses removed 3?h after dosage of either compound to the dams did not contain ¹⁴C; foetuses removed 5 min after dosage contained low levels of ¹⁴C, substantially below the maternal blood level and equiv. to <0·1% of dose in each case. No ¹⁴C was detected in amniotic fluid.     

Two new flavonoid glycosides from Artemisia frigida Willd.

An investigation of the n-BuOH-soluble fraction from the aerial parts of Artemisia frigida has led to the isolation of two new flavonoid glycosides, named friginoside A and friginoside B. Their structures were characterized as 5,7-dihydroxy-3′,4′,5′-trimethoxy flavone 7-O-β-d-glucuronide (1) and 5,7-dihydroxy-3′,4′,5′-trimethoxyflavone 7-O-β-d-glucuronyl-(1 → 2)O-β-d-glucuronide (2) on the basis of 1D and 2D NMR spectral analysis.