抗过敏药物氯雷他定的拉曼光谱研究

Study on Raman Spectroscopy of an Antiallergic Medicine Loratadine

摘要: 本文运用拉曼光谱技术测试并获得市售抗过敏药物氯雷他定的光谱，并结合理论计算归属了药物中氯雷他定原料药和辅料的拉曼位移，确定拉曼光谱可以用于准确快速测定氯雷他定原料药及市售口服制剂的主要成份。明确不同组分的特征拉曼位移并比较它们的相对强度：氯雷他定中位于1084 cm⁻¹处归属于芳环上C-Cl伸缩振动的拉曼位移，辅料中多糖或者淀粉的特征拉曼位移(位于478 cm⁻¹处)以及辅料硬脂酸镁的特征拉曼位移(位于128 cm⁻¹处)。实验采用拉曼成像技术对药品中各个组份含量分别进行初步研究，实验数据表明市售氯雷他定药品主要分为两类：有的药品(I类药品)所得的拉曼成像中，不同区域对应的光谱变化趋势类似，它们之间相对强度对比变化差异不大，说明该类药品中原料药和辅料混合比较均匀，药品中各个组份的相对含量随位置变化不明显；而有的药品(II类药品)拉曼成像中光谱之间差异较大，特别是辅料–硬脂酸镁对应的特征拉曼位移峰与氯雷他定的特征峰在不同区域中变化趋势差异明显，而且它们的相对强度差异变化大，说明辅料–硬脂酸镁在药品中的相对含量变化较大，侧面反应II类药品中主要成分氯雷他定与辅料硬脂酸镁的混合不均匀。实验结果显示，拉曼成像技术能够非常形象的表征市售口服制剂中原料药和辅料混合的均匀程度，可以初步反应口服制剂生产的工艺水平。此外，本文还结合市售不同种类氯雷他定药品在临床应用中的效果，讨论了它们和药物中成份分布的关系。

Abstract: In this paper, Raman spectroscopy was applied to investigate and obtain the spectra of loratadine, an antiallergic medicine commonly available on the market. The Raman shifts of loratadine API and excipients in the medicine were theoretically calculated and arranged as well. It was concluded that the Raman spectroscopy could be used to determine the main components of loratadine API and oral preparations quickly and accurately. The characteristic Raman shifts of different components were defined and their relative intensity was compared: the Raman shift of loratadine at 1084 cm⁻¹ was attributed to the C-Cl stretching vibration on the aromatic ring, the characteristic Raman shift of polysaccharide or starch in excipients located at 478 cm⁻¹, and the characteristic Raman shift of magnesium stearate could be found at 128 cm⁻¹. Raman imaging technology was employed to study the each component content of the medicine in experiments. The data showed that the commonly available commercial loratadine medicine could mainly be divided into two categories: the Raman imaging of some medicine (class I) showed similar change trend to the different regions of medicine, and only little difference existed in the relative intensity contrast between them. It indicated that the mixture of API and excipients was fairly uniform, and the relative content of each component in the medicine did not change significantly with the location. However, the Raman imaging of some medicine (class II) showed obvious differences; especially, the characteristic Raman shifts of excip-ients-magnesium stearate and Loratadine according to different regions of medicine displayed sig-nificantly different change trend. And their relative intensity difference varied widely, showing that the relative content of excipient-magnesium stearate in medicine changed obviously. It indicated that the API loratadine mixed with excipients magnesium stearate was not uniform in class II med-icine on the other hand. The experimental results showed that Raman imaging technology could vividly characterize the uniformity of the mixture of API and excipients in commercial oral prepa-rations, which revealed the technological level of oral preparations production. In addition, the re-lationship between different kinds of loratadine and the distribution of components in the medicine was discussed in this paper as well.