Melting Process of the Peritectic Mixture of Lidocaine and Ibuprofen Interpreted by Site Percolation Theory Model

Melting Process of the Peritectic Mixture of Lidocaine and Ibuprofen Interpreted by Site Percolation Theory Model
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DOI:
10.1016/j.xphs.2017.04.010
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发表时间:
2017-10-01
影响因子:
3.8
通讯作者:
Goto, Satoru
Goto, Satoru
中科院分区:
医学3区
文献类型:
--
作者:
Kataoka, Hikaru;Sakaki, Yoshinori;Goto, Satoru

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共晶混合物常用于药物的设计和递送。在本研究中,我们使用差示扫描量热法、拉曼光谱法和显微镜检查了利多卡因(LDC)和布洛芬(IBP)的包晶混合物。所获得的相图显示,随着混合物被加热,首先LDC在293 K时熔化,然后IBP在310 K时溶解在液化的LDC中,最后所有剩余的晶体都熔化。在H - 1 NMR光谱中,由于这些部分之间的分子间相互作用,IBP中的羧基以及LDC中的酰胺或胺基的信号在IBP/LDC混合物中向低磁场方向移动。使用傅里叶变换红外光谱法,确定了在LDC过量、等摩尔和IBP过量的混合物中熔化过程的动力学“反应”级数分别为+1/2、- 1/2和0。在IBP摩尔分数为1/3和2/3时,液相线与310 K处较高熔点线之间的2个接触点是根据位点渗流理论来解释的。(C)2017美国药剂师协会(R)。由爱思唯尔公司出版。保留所有权利。
Eutectic mixtures are often used in the design and delivery of drugs. In this study, we examined the peritectic mixture of lidocaine (LDC) and ibuprofen (IBP) using differential scanning calorimetry, Raman spectroscopy, and microscopy. The obtained phase diagram showed that as the mixture was heated, first LDC melted at 293 K, then IBP dissolved in the liquefied LDC at 310 K, and finally all remaining crystals melted. In the H-1 NMR spectra, the signals of the carboxyl group in IBP and amide or amine group in LDC shifted to the low magnetic field in the IBP/LDC mixtures, because of the intermolecular interaction between these moieties. Using FTIR spectroscopy, the kinetic "reaction" order of the melting process in the mixtures with excess LDC, equimolar, and excess IBP was determined to be +1/2, -1/2, and 0, respectively. The 2 contacts between the liquidus line and the higher melting line at 310 K at IBP molar fractions of 1/3 and of 2/3 were explained on the basis of the site percolation theory. (C) 2017 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.