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[原料药] 阿司匹林的发现

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药徒
发表于 2013-9-6 11:13:49 | 显示全部楼层 |阅读模式

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阿司匹林的发现

这一个月在1897年:阿司匹林,是世界上最知名的药物之一,被合成

问大多数人,如果他们认识的名字,在过去的几十年中推出,机会是最常用的药物 - 除非他们自己采取的药物 - 他们将陷入一片混乱的ZS和Xs乱蓬蓬的方式这是不可能的发音。

相比之下,一种药物在世界上的每个人都知道的 - 不只是它的简单发音的名字 - 是阿司匹林,它可以增加多样性,有效性和长寿上榜理由为什么几乎每家每户都有一箱或两药剂师是什么时,他建议大家都知道。

止痛药有长寿的确,今年庆祝其116岁生日,仍然跻身在世界上最常用的药物。

具体而言,阿司匹林的周年发生在8月10日,为它是在该日期在1897年,费利克斯·霍夫曼,在德国生活科学坚定拜耳的化学家,第一次合成的活跃成分的阿司匹林 - 乙酰水杨酸 - 是纯净的形式和稳定。

大多是由偶然
根据拜耳的霍夫曼的传记,这是“大多是由偶然化学家混合水杨酸与醋酸成功创建什么是现在公认的治疗在医学史上的突破。

解释霍夫曼的研究à常见的故事是,他,鼓励他的父亲,有关节炎,发展替代水杨酸钠治疗 - 果汁的杨柳树树皮,已被用来作为一个止痛药和治疗发烧世纪,但进行了一些不愉快的副作用,包括恶心,肠胃不适,耳鸣和肝损害。

该解决方案被看好足够引人注意拜耳的制药实验室,海因里希·席勒F霍夫曼一起测试乙酰水杨酸对动物和人类,其效果显着,足以鼓励他们申请专利的头。

然而,沃尔特Sneader提供一个替代性帐户在他的文章“发现阿司匹林:重新评估”英国医学杂志( BMJ ) ,他解释说,这样的解释不可靠的历史脚注的一部分于1934年首次出现阿尔布雷希特·施密特写的化学工程。

相反, Sneader解释说,其实是他的同事亚瑟Eichengrün的指导下,霍夫曼合成乙酰水杨酸的研究。

虽然有争议的,由拜耳, Sneader一块表明Eichengrün的想开发水杨酸钠的替代品,是目前的当数水杨酸衍生物进行了测试席勒F 。

Sneader援引Eichengrün的1949年的论文,发表在该杂志Pharmazie , Eichengrün的声称席勒F实际上否决进一步研究乙酰水杨酸,错误地认为它是对心脏有害。

尽管存在这些问题,从他的老板, Eichengrün测试乙酰水杨酸对自己,以确认其安全性,提供化合物之前同系拜耳科学家费利克斯·戈德曼,然后找来医生评估药物。

这些效果的报告是令人鼓舞的,根据Sneader ,与能够提供抗风湿药的效果,无副作用,如耳鸣的药物。

Eichengrün甚至引用牙痛病人惊呼“我的牙痛不见了! ”后,几乎立即接受治疗与乙酰水杨酸。

作为Sneader论文的一部分,他去上解释,席勒F仍然怀疑乙酰水杨酸的好处,和它只有拜耳的头的研究, ,进一步研究的化合物进行了,包括席勒F自己的复查卡尔·杜伊斯堡干预在1898年9月。

谁怀疑Sneader的纸已经注意到Eichengrün等待15年来反驳索赔约霍夫曼和他的父亲在1934年出版。

然而, Sneader的还击是Eichengrün有一个非常有效的原因 - 他是犹太人生活在纳粹德国。

这种情况下,不可能写高调反驳,虽然他写了一封信在1944年期间在特莱西恩施塔特集中营,他在其中描述了他的名字没有他发明的醋酸纤维素一起定位在慕尼黑德国博物馆,而席勒F和霍夫曼都被计入旁边的展览阿司匹林。

“这个遗漏是要归功于什么影响,只可假设, ”他若有所思地说。 “

Sneader提供他自己的猜测,在他的论文:“可以毫无疑问,他觉得,他已经写出来的历史,因为他是犹太人。 ”

在任何情况下,霍夫曼并揉合乙酰水杨酸一个纯粹的和稳定的形式, 1897年8月10日,短短两年后,拜耳生产的名义下提供玻璃瓶粉末阿司匹林药物。

从那时起,该药物已经达到难以想象的成功,使得拜耳的名字在药品世界。

那些谁促成其创作(这取决于什么样的故事,你信任)霍夫曼,谁也合成了稳定版的女主角,后来成为拜耳医药营销部门负责人之前,于1928年退休,然后在1946年死亡。

特莱西恩施塔Eichengrün发布1945年战争结束后,但于1949年在82岁临终前将只住了四个多年。
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药徒
 楼主| 发表于 2013-9-6 11:13:57 | 显示全部楼层
This month in 1897: aspirin, one of the world's best-known drugs, was synthesised

Ask most people if they recognise the names of some of the most commonly used drugs launched in the past few decades, and chances are – unless they themselves take the medicines - they'll be caught in a confusion of Zs and Xs jumbled in a way that's impossible to pronounce.

By contrast, one drug that everyone in the world is aware of – and not just for its simple to pronounce name – is aspirin, which can add diversity, efficacy and longevity to the list of reasons why almost every household has a box or two and everyone knows what the pharmacist is on about when he recommends it.

And the painkiller has longevity indeed, celebrating its 116th birthday this year and still being among the most commonly used medicines in the world.

To be specific, aspirin's anniversary occurs on August 10, for it was on that date in 1897 that Felix Hoffmann, a chemist at German life science firm Bayer, first synthesised the active ingredient of aspirin – acetylsalicylic acid – in a form that was pure and stable.

Mostly by chance
According to Bayer's biography of Hoffman, it was 'mostly by chance' that the chemist succeeded in mixing salicylic acid with acetic acid to create what is now widely recognised as a breakthrough treatment in the history of medicine.

A common story to explain Hoffman's research is that he was encouraged by his father, who had arthritis, to develop an alternative treatment to sodium salicylate – juice from the willow tree bark that had been used for centuries as a painkiller and treatment for fever, but carried several unpleasant side effects, including nausea, gastro-intestinal irritation, tinnitus and liver damage.

The solution was promising enough to catch the attention of the head of Bayer's pharmaceutical laboratory, Heinrich Dreser, who alongside Hoffman tested acetylsalicylic acid on animals and then humans, where its effect was notable enough to encourage them to apply for a patent.

However, Walter Sneader offers an alternative account in his article 'The discovery of aspirin: a reappraisal' for the British Medical Journal (BMJ), in which he explains that this explanation first appeared in 1934 as part of an unreliable footnote in a history of chemical engineering written by Albrecht Schmidt.

Instead, Sneader explains that Hoffman's research into synthesising acetylsalicylic acid was actually done under the instruction of his colleague Arthur Eichengrün.

Although disputed by Bayer, Sneader's piece suggests that Eichengrün had wanted to develop an alternative to sodium salicylate, and was present when several derivatives of salicylic acid were tested by Dreser.

Sneader cites Eichengrün's 1949 paper, published in the journal Pharmazie, in which Eichengrün claims that Dreser actually vetoed further study of acetylsalicylic acid, wrongly believing it to be harmful to the heart.

Despite these concerns from his boss, Eichengrün tested acetylsalicylic acid on himself to confirm its safety, before supplying the compound to fellow Bayer scientist Felix Goldmann, who then recruited physicians to evaluate the drug.

Reports from these effects were encouraging, according to Sneader, with the drug able to provide antirheumatic effects without side effects, such as tinnitus.

Eichengrün even quotes a patient with toothache who exclaimed “My toothache's gone!” almost immediately after receiving treatment with acetylsalicylic acid.

As part of Sneader's paper, he goes on to explain that Dreser still doubted the benefits of acetylsalicylic acid, and it was only on the intervention of Bayer's head of research, Carl Duisberg, that further research of the compound was undertaken, including Dreser's own reinvestigation in September 1898.

Those who doubt Sneader's paper have noted that Eichengrün waited 15 years to refute the claims about Hoffman and his father published in 1934.

However, Sneader's riposte is that Eichengrün had a very valid reason – he was a Jew living in Nazi Germany.

This circumstance made it impossible to write a high profile rebuttal, although he did write a letter in 1944 during a period in the Theresienstadt concentration camp, in which he described how his name was not positioned alongside his invention of acetylcellulose in the German Museum in Munich, whereas both Dreser and Hoffmann were credited beside the exhibition for aspirin.

“To what influences this omission is to be attributed, can be only assumed,” he muses.

Sneader offers his own guess in his paper: “There can be little doubt that he felt that he had been written out of history because he was a Jew.”

In any case, Hoffman did synthesise a pure and stable form of acetylsalicylic acid on August 10, 1897, and just two years later, Bayer was producing the drug under the name Aspirin as a powder supplied in glass bottles.

Since then, the drug has gone on to achieve unimaginable success, making Bayer's name in the medicines world.

Of those who contributed to its creation (depending on what story you trust) Hoffmann, who also synthesised a stable version of heroine, went on to become head of the pharmaceutical marketing department at Bayer, before retiring in 1928 then dying in 1946.

Eichengrün was released from Theresienstadt after the war ended in 1945, but would only live for four more years before dying in 1949 at the age of 82.
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