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使用衰减全反射傅里叶变换红外光谱(ATR-FTIR)和多元光谱分析研究模型制剂和市售布洛芬制剂在Carbosil及人体皮肤中的渗透情况。

Investigation of the permeation of model formulations and a commercial ibuprofen formulation in Carbosil and human skin using ATR-FTIR and multivariate spectral analysis.

作者信息

Russeau Wanessa, Mitchell John, Tetteh John, Lane Majella E, Hadgraft Jonathan

机构信息

Medway Sciences, University of Greenwich, School of Science, Central Avenue, Chatham Maritime, UK.

出版信息

Int J Pharm. 2009 Jun 5;374(1-2):17-25. doi: 10.1016/j.ijpharm.2009.02.018. Epub 2009 Mar 9.

Abstract

The purpose of the present study was to use attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR) and target factor analysis (TFA) to investigate the permeation of model drugs and formulation components through Carbosil membrane and human skin. Diffusion studies of saturated solutions in 50:50 water/ethanol of methyl paraben (MP), ibuprofen (IBU) and caffeine (CF) were performed on Carbosil membrane. The spectroscopic data were analysed by target factor analysis, and evolution profiles of the signal for each component (i.e. the drug, water, ethanol and membrane) over time were obtained. Results showed that the data were successfully deconvoluted as correlations between factors from the data and reference spectra of the components, were above 0.8 in all cases. Good reproducibility over three runs for the evolution profiles was obtained. From the evolution profiles it was observed that water diffused better through the Carbosil membrane than ethanol, confirming the hydrophilic properties of the Carbosil membrane used. IBU diffused slower compared with MP and CF. The evolution profile of CF was very similar to that of water, probably because of the high solubility of CF in water, indicating that both compounds are diffusing concurrently. The second part of the work involved a study of the evolution profiles of the components of a commercial topical gel containing 5% (w/w) of ibuprofen as it permeated through human skin. Although the system was much more complex, data were still successfully deconvoluted and the different components of the formulation identified except for benzyl alcohol which might be attributed to the low concentrations of benzyl alcohol used in topical formulations.

摘要

本研究的目的是使用衰减全反射傅里叶变换红外光谱法(ATR-FTIR)和目标因子分析(TFA)来研究模型药物和制剂成分透过Carbosil膜及人体皮肤的渗透情况。对尼泊金甲酯(MP)、布洛芬(IBU)和咖啡因(CF)在50:50水/乙醇中的饱和溶液在Carbosil膜上进行了扩散研究。通过目标因子分析对光谱数据进行分析,得到了各成分(即药物、水、乙醇和膜)信号随时间的变化曲线。结果表明,数据成功解卷积,各成分数据与参考光谱之间的相关性在所有情况下均高于0.8。对变化曲线进行三次测量得到了良好的重现性。从变化曲线可以观察到,水透过Carbosil膜的扩散比乙醇更好,这证实了所用Carbosil膜的亲水性。与MP和CF相比,IBU的扩散较慢。CF的变化曲线与水的非常相似,可能是因为CF在水中的高溶解度,这表明两种化合物同时扩散。工作的第二部分涉及研究一种含有5%(w/w)布洛芬的市售外用凝胶在透过人体皮肤时各成分的变化曲线。尽管该体系更为复杂,但数据仍成功解卷积,并识别出了制剂的不同成分,除了苯甲醇,这可能归因于外用制剂中使用的苯甲醇浓度较低。

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