Determination of the ophthalmic therapeutic pilocarpine and its degradation products by reversed-phase high-performance liquid chromatography.
Determination of the ophthalmic therapeutic pilocarpine and its degradation products by reversed-phase high-performance liquid chromatography.
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反相高效液相色谱法测定眼科治疗剂毛果芸香碱及其降解产物。
DOI：
10.1016/s0021-9673(00)89884-2
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发表时间：
1978
期刊：
影响因子：
--
通讯作者：
H. C. Beyerman
中科院分区：
文献类型：
--
作者：
A. Noordam;K. Waliszewski;C. Olieman;L. Maat;H. C. Beyerman
毛果芸香碱的性质包括缩瞳作用，其主要应用是在眼科中用于降低眼内压。为此，可使用0.5~ 5~ 1.5倍的硝酸毛果芸香碱或盐酸毛果芸香碱等渗缓冲溶液。然而，在水溶液中，毛果芸香碱可水解成毛果芸香酸（3）并差向异构化成异毛果芸香碱（2），异毛果芸香碱（2）又水解成异毛果芸香酸（4）3 × 4。为了测量降解的程度，已经描述了许多用于定量测定毛果芸香碱的方法，但是它们都存在不能区分四种化合物（1）-（4）的缺点。最近，基于在阳离子交换树脂上使用高效液相色谱法（HPLC），公开了几种从异毛果芸香碱中分离毛果芸香碱的方法，但毛果芸香酸和异毛果芸香酸尚未测定。本文报道用反相柱高效液相色谱法可方便、准确地分离这四种化合物。
The properties of pilocarpine include a miotic action, and its chief application is in ophthalmology for lowering the intraocular pressure. For this purpose, buffered isotonic solutions of 0.5~ 5~~ pilocarpine nitrate or hydrochloride are us&. In aqueous solution, however, pilocarpine may be hydrolysed to pilocarpic acid (3) and epimerized to isopilocarpine (2), which, in turn, is hydrolysed to isopilocarpic acid (4) 3* 4. Both hydrolysis and epimerization result in a decrease, in pharmacological activity.To measure the extent of degradation, many methods have been described for the quantitative determination of pilocarpine, but they all sufher from the disadvantage that they do not distinguish between the four compounds (l)-(4). Recently, several separations of pkcarpine from isopilocarpine, based on the use of highperformance liquid chromatography (HPLC) on a cation-exchange resin, were published ‘-‘, but pilocarpic acid and isopilocarpic acid co&l not be determined. We report here that a convenient and accurate separation of the four compounds can be achieved by HPLC on a reversed-phase coIunm.