尼麦角林在健康人体中的生物等效性

目的:研究两种尼麦角林片剂在健康人体的生物等效性。方法:20名健康志愿者随机双交叉、单剂量口服受试制剂尼麦角林片和参比制剂尼麦角林片,剂量均为20mg,剂间间隔为1周。其中尼麦角林在体内的最主要的代谢产物为10α-甲氧基-9,10-二氢麦角醇(MDL),故用LC-MS内标法测定血浆中MDL浓度,应用DAS药动学程序进行有关药代动力学参数、相对生物利用度计算,并根据新药审批指导原则评价两种制剂的生物等效性。结果:表明该分析方法专属性强,方法简便。受试制剂与参比制剂的药代动力学参数,尼麦角林:tmax分别为(3.3±0.9)和(3.2±0.7)h,t1/2分别为(12.9±4.0)和(12.8±2.4)h,Cmax分别为(23±6)和(22±6)μg/L,AUC0-t分别为(291±51)和(282±44)μg.L-1.h,AUC0-∞分别为(316±50)和(299±46)μg.L-1.h。尼麦角林的相对生物利用度为(104±17)%。结论:两种尼麦角林片剂在健康人体具有生物等效性。     

维拉帕米对偏头痛的防治效果

偏头痛的防治对偏头痛有预防效果的药物包括(1)β阻滞剂,如普萘洛尔、纳多洛尔、阿替洛尔和美托洛尔;(2)抗抑郁药,如阿米替林(Amitriptyline)、去甲替林(Nortriptyline)、丙米嗪(Impramine)、地昔帕明(Desipramine)和多塞平(Doxepin);(3)麦角制剂,如麦角胺和美西麦角(Methysergide);(4)非甾体抗炎药;(5)钙拮抗剂,如维拉帕米、硝苯啶、地尔硫革、氟桂嗪和尼莫地平等。传统疗法:防治偏头痛的传统用药为β阻滞剂、麦角制剂和抗抑郁药。β阻滞剂预     

国产麦角溴烟酯缓释胶囊的相对生物利用度和生物等效…

１０名健康男性志愿者采用交叉给药方案，分别多剂量口服３０ｍｇ国产和进口麦角溴烟醌缓释胶囊，用ＨＰＬＣ法测定代谢较快者血浆中麦角溴烟酯代谢产物Ⅱ浓度，进行国产制剂睡物利用度和生物等效性评价，其生物等效性采用方差分析和单ｔ检测判定。     

二氢麦角隐亭的药理学基础与临床

<正> 二氢麦角隐亭(Dihydroergocryptine,DHEC)是一种标准的α-受体阻断药,对该药分子结构的基础研究已有十余年的历史。业已发现,它的同分异构体—二氢麦角隐亭A具有DHEC的全部特性。目前,国际上已有主要含有二氢-α-麦角隐亭(异构体A)和甲基嘌呤的制剂—Vaso     

中国野生麦角对家兔子宫的作用

麦角制剂是妇产科常用药物之一,文献曾记载江西、湖南等地有野生麦角,但迄今我国仍依赖进口,自1953年以来,本院药用植物学系的调查队曾在河北和东北各省採集了寄生在黑麦、老芒麦、披硷草、拂子茅和赖草上的麦角,化学分析证明,其中一部分麦角的生物硷含量超过中国药典的规定。本研究目的是测定这些野生麦角的生物效力。     

溴隐停的临床应用及作用机理

溴隐停又称溴麦角隐停(Bromocrip-tine,CB154),是一种半合成麦角生物碱(2-Bromo-a-ergocriptine),制剂产品为甲磺酸溴麦角环肽(Parlodel),每片含主药2.5mg,口服后吸收良好,在体内主要由肝脏代谢,从胆汁排泄。目前已开始为一些医疗单位所使用。溴隐停的主要作用是抑制Prolactin(催乳激素)的分泌。属于近年来医学上发展     

甲磺酸培高利特治疗超老年帕金森病的疗效与安全性

六十年代初,发现用左旋多巴治疗帕金森病(PD)有效,但长期用左旋多巴制剂后副反应的发生率高,连续治疗3～5年后,有20%～50%的患者出现运动波动和异动症[1].近几年国外推崇用多巴胺(DA)受体激动剂治疗PD.临床已应用的DA受体激动剂多为麦角类衍生物,如溴隐停、甲磺酸培高利特(pergolide mesylate,协良行),α-二氢麦角隐停、麦角己脲和卡麦角林(cabergoline)等;非麦角类新合成的激动剂如普拉克索(pramipexole)、罗匹尼罗(ropinirole)和泰舒达等.     

野生麦角寄生植物分布的调查

麦角是一种真菌属赤壳科(Hypocreaceae),麦角薄(Claviceps)持续性菌体。这种真菌体感染正在开花的禾草子房以后,在适宜的气候条件下,菌丝萌发,最后形成坚实、多棱、紫色的菌核(麦角)。在很早以前已做过麦角药理实验,证明对子宫有显著的收缩作用。在临床上多应用于催产,或产后流血过多止血,有着良好的效果。因而已被世界各国医师,做为一种常用的药物。目前不仅在我国国家药典中已将黑麦(Secale celops)寄生麦角列入正     

文摘

YZX2007051CA144:474944yU.S.Pat.Appl.Publ.US2006105,030麦角灵衍生物透皮制剂本发明介绍了一种透皮制剂,它由麦角灵衍生物如麦角乙脲以及一种麦角灵类物质的稳定剂组成。麦角灵制剂的氧化不稳定性通过下述成分实现:含有至少一种能捕获自由基的脂溶性抗氧化剂,如二步丁基甲酚     

国产与进口羟丙基甲基纤维素用于硝苯地平缓释片时的比较

目的比较国产与进口羟丙基甲基纤维素(HPMC)用于制备缓释片时的效果。方法以硝苯地平缓释片为模型药物,对国产和进口HPMC的理化性质、片剂制备工艺及缓释效果进行比较。结果用国产高黏度HPMC制备缓释制剂不可行,不能像进口HPMC那样形成稳定的缓释制剂。结论要将国产高黏度HPMC用于缓释制剂,还须在技术上进一步突破;要提高国产制剂水平,还须提高国产辅料的质量。     

麦角新鹼的层离及提取的研究

麦角为极常用的产科药物,其中所含生物鹼据文献中报告一般常见者有六对之多,而以水溶性之麦角新鹼效力最好,毒性最小.自Foster等发表用纸层离法鉴定麦角新鹼以后,才有了比较好的定性试验以肯定麦角新鹼的存在与否,但是这个方法至少需要十六到十八小时才能得到结果,时间上很不经济,因此有必要寻找一个比较快的方法.根据Brindle等用纸层离分离水不溶性生物鹼的结果,著者试用了含有缓的纸进行水溶性生物鹼的层离,用氯仿为推进剂,得到满意结果,不但麦角新鹼斑     

薄层层离法在研究天然化合物中的应用 Ⅱ.麦角新碱、麦角胺、麦角毒碱的定量

本文研究了应用无粘合剂氧化鋁薄层层离和光电比色相結合的方法,測定麦角中三种主要生物碱的含量。回收率試驗表明,本方法具有較高的准确性,如麦角新碱的平均回收率为97.3%,标准誤差±1.7%;麦角胺的平均回收率为96.2%,标准誤差±2.2%;麦角毒碱的平均回收率为99.3%,标准誤差±0.9%。加量試驗的結果表明,本方法可以应用于麦角中三种主要生物碱的含量測定。作者用此方法測定了披碱草、老芒麦、高滨麦三种野生麦角和二种麦角菌发酵物中各种麦角生物碱的含量。操作簡便,有机溶剂用量很少。     

Bromocriptine enhances the behavioural effects of apomorphine and dopamine after systemic or intracerebral injection in rats

The ergot alkaloid bromocriptine, given intraperitoneally produced dose-dependent, long-lasting stereotyped behaviour in rats which was partly antagonised by the injection of trifluoperazine into the caudate nucleus. The stereotyped behaviour produced by apomorphine (s.c.) in both na?ve and catecholamine-depleted rats was significantly enhanced by prior treatment with bromocriptine (i.p.). The bilateral application of bromocriptine (2.5-40 micrograms/side in either 0.5% tartaric acid or 50% propylene glycol aqueous vehicles) to the nucleus accumbens (NAC) of rats had no effect on locomotion over a 12 hr period after injection. In contrast, another ergot alkaloid, ergometrine, dissolved in the propylene glycol vehicle, and dopamine (DA) dissolved in either of the vehicles or in saline, produced marked stimulation of locomotion. As well as being inactive after direct application to the nucleus accumbens, bromocriptine (10-160 micrograms/side) did not induce stereotyped behaviour after bilateral injection into the caudate nucleus. However, the local application of bromocriptine (10 micrograms/side) to the nucleus accumbens, while itself inactive, significantly enhanced the locomotor stimulant effect of DA (5 micrograms/side) applied to the same nucleus. The data suggest that bromocriptine is able to enhance the effects of agonists such as DA and apomorphine at DA receptors, even under conditions where bromocriptine itself is inactive.     

几种制剂中生物碱的离子交换分离测定法

制剂中生物碱的含量測定,各国药典經典方法均采用有机溶剂提取,分离杂貭后再测定含量。近几年来,采用离子交换法分离制剂中生物碱的方法已有不少报导。由于离子交換剂能够比較簡单的定量交換生物碱,并可以用一定溶剂洗脫,这样可以避免一般較复杂费时的提取手續,因而采用离子交换法分离生物碱具有一定的优点。Kamp等报告了用IMAC-22強酸树脂,从顛茄、番木鱉等数种生药及其制剂中分离生物碱,对于用交換柱操作方法、洗脫条件等都进行一定工作。Brochmann-Hanssen連續报导了快速分离测     

有机砷锑药物中砷锑之含量测定

有机砷锑化合物中砷锑的测定在药品鉴定及有机化合物的分析研究上均有很大的价值。文献上的方法很多,目前各国药典较常用的有以下类型:(一)Lehmann氏类型;(二)Ewins氏类型;(三)Robertson氏类型;(四)Schulek及Villecz氏类型。这几类型中:(一)手续繁复且不能用于某些抗氧化力强之化合物;(二)(三)费时颇长,且操作中产生大量有害气体;(四)手续及时间虽较前三种简短,但操作稍有不慎,易得不一致结果。     

血液及尿中微量锑的比色测定

血液中微量锑的测定,目前仍广泛应用罗丹明 B 法.用此法测定微量锑时,为了免除铁离子的干扰作用,可利用醋酸戊酯在酸性溶液中将 HSbCl_6萃出,但必须控制溶液的酸度,当溶液酸度太高时,铁也同时被萃出.若利用结晶紫作为测定血液中微量锑的试剂,不但灵敏度大于罗丹明 B,空白试验着色浅,并且铁离子的干扰作用极其微小,因此在用醋酸戊酯提取 HSbCl_6时不必严格控制溶液的酸度.     

Packed column supercritical fluid chromatography of sodium stearyl fumarate aqueous suspension

A method for the determination of sodium stearyl fumarate aqueous suspension is described. This straightforward method is based on homogenisation of the sample, dilution of a known aliquot with methanol to a suitable clear solution and mixing with an internal standard; (S)-naproxen. Separation and quantification is performed by packed column supercritical fluid chromatography on a commercial tartaric acid network polymeric column (tertbutylbenzoyl) with UV-detection at 214 nm. The precision of the presented method upon repeated analysis of a 20 mg/ml suspension is 0.5% (n = 8), and the yield is near 100%. Less than 5 min is required for the chromatographic separation with a resolution of about 3 to the internal standard. With some modification of the chromatographic conditions water samples can also be analysed.     

锑的比色测定法(二)用结晶紫及孔雀绿试剂之比色法

罗丹明 B,已被广泛地采用为 Sb 的微量分析及比色分析之用.苏联文献报告甲基紫可用做锑的定性分析试剂.日本文献方面也有用甲基紫做锑定量分析的记载.由于罗丹明 B(Ⅰ)、甲基紫(Ⅱ)、结晶紫(Ⅲ)及孔雀绿(Ⅳ)四者具有相似的化     

Evaluation of Ethanol and Aqueous extracts of Cinnamomum verum Leaf Galls for Potential Antioxidant and Analgesic activity

In the present study, ethanol and aqueous extracts of leaf galls of Cinnamomum verum were prepared to evaluate the antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay and superoxide radical scavenging assay with ascorbic acid as a standard, and analgesic activity by tail immersion test and acetic acid-induced writhing test methods using diclofenac sodium as the reference drug. Swiss albino mice maintained under standard laboratory conditions were used for analgesic tests. In the 2,2-diphenyl-1-picrylhydrazyl assay it was found that the aqueous and the ethanol extract possessed almost equal capacity to inhibit free radicals (IC₅₀=13.3 and 13.53 µg/ml) but found less than ascorbic acid (IC₅₀=9.96 µg/ml). And in superoxide assay the ethanol extract was found to be more potent in scavenging super oxide radicals when compared to ascorbic acid and the aqueous extract (IC₅₀=237.1 and 197.8 µg/ml) with the IC₅₀=119.7 µg/ml. For analgesic activity, ethanol extract showed the maximum time required for response against thermal stimuli (6.75±0.47 s) and maximum % of writhing inhibition (44.57%) when compared to aqueous extract (5.25±0.48 s and 32.61%), whereas diclofenac showed response in 7.25±0.25 s 67.39% inhibition in tail immersion and writhing tests, respectively. These results demonstrate that the ethanol extracts of leaf galls possessed high antioxidant and analgesic activity.     

Phase behavior of beta hydroxy-acids with laureth 4

The colloidal structures of beta carboxylic acid topical vesicle formulations were determined and the changes during evaporation after applications were estimated from phase diagrams. The results showed significant difference during evaporation between salicylic acid on one hand and three water soluble acids; malic, tartaric, and citric acid, on the other. The water soluble acids showed an increase in the acid concentration in the aqueous solution to levels that must be considered harmful, while salicylic acid showed no increase in concentration in the individual phases even after 99% evaporation of water.