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利用拉曼光谱进行片剂水分表面分析:片剂表面标志物。

Using Raman spectroscopy in tablet moisture surface analysis: tablet surface markers.

机构信息

Department of Pharmaceutical Sciences, School of Pharmacy-Boston, Massachusetts College of Pharmacy and Health Sciences, 179 Longwood Avenue, Boston, MA 02115, USA.

出版信息

J Pharm Biomed Anal. 2010 Dec 1;53(4):852-9. doi: 10.1016/j.jpba.2010.06.009. Epub 2010 Jun 19.

Abstract

A method was developed to monitor the hydration of a tablet surface using chemical functional groups able to bind atmospheric water through H-bonding. In this study, generic oral dissolving loratadine tablets were used. These tablets have relatively high mannitol and lactose concentrations. Both mannitol and lactose have C-OH alcohol functional groups, several of which are potentially available for H-bonding with atmospheric water. The Raman intensity of the alcohol functional groups decreases upon hydration. This observation can be used to indirectly monitor water adsorbed to tablet surfaces at the alcohol sites. The hydration assay is based on the change in the Raman peak intensity of the alcohol C-OH stretching at 875.5 cm(-1). Consequently the decrease in the Raman intensity of this vibration can be used to monitor water adsorption. The Raman measurement of tablet surface water was compared to the direct moisture measurement method using a microbalance. The Raman spectroscopy is used to monitor the water that is specifically bound to the C-OH alcohol functional groups available for hydration. The microbalance was used to monitor the tablets' weight change during water adsorption and desorption. The distribution of the ratio of the Raman intensity of C-OH peak at 875.5 cm(-1) divided by the intensity of loratadine's C-Cl peak at 712.6 cm(-1) was experimentally determined to be a Gaussian distribution with a mean of 3.22+/-0.277. Raman analysis indicates that there is both tightly and loosely bound water at the tablet surface. This can be a useful technique with regard to inspecting and controlling the tablet drying process.

摘要

开发了一种使用能够通过氢键结合大气水的化学官能团监测片剂表面水合作用的方法。在本研究中,使用了通用的口服溶解氯雷他定片。这些片剂具有相对较高的甘露醇和乳糖浓度。甘露醇和乳糖都具有 C-OH 醇官能团,其中几个官能团可能与大气水形成氢键。醇官能团的拉曼强度在水合作用时降低。这种观察结果可用于间接监测在醇位吸附到片剂表面的水。水合作用测定基于醇 C-OH 伸缩在 875.5 cm(-1)处的拉曼峰强度的变化。因此,这种振动的拉曼强度的降低可用于监测水的吸附。将片剂表面水的拉曼测量与使用微天平的直接水分测量方法进行了比较。拉曼光谱用于监测可用于水合作用的特定结合到 C-OH 醇官能团的水。微天平用于监测水吸附和解吸过程中片剂重量的变化。在 875.5 cm(-1)处的 C-OH 峰的拉曼强度与 712.6 cm(-1)处的氯雷他定的 C-Cl 峰的强度之比的分布通过实验确定为具有平均值 3.22+/-0.277 的高斯分布。拉曼分析表明片剂表面存在紧束缚和松束缚水。这对于检查和控制片剂干燥过程可能是一种有用的技术。

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