布洛芬和酮洛芬二元共晶的物理化学研究，以增强经皮药物传递。

Physicochemical studies of binary eutectic of ibuprofen and ketoprofen for enhanced transdermal drug delivery.

机构信息

Department of Pharmaceutical Sciences, Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, USA.

出版信息

Drug Dev Ind Pharm. 2010 Oct;36(10):1168-76. doi: 10.3109/03639041003695071.

DOI:10.3109/03639041003695071

PMID:20367290

Abstract

METHODS

The thermodynamic, eutectic, and crystalline properties of ibuprofen and ketoprofen binary mixtures were investigated using differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRPD).

RESULTS

The DSC studies showed that melting point (61 degrees C), enthalpy (11.3 kJ/mol), and entropy of fusion (33.7 J/K/mol) of the binary eutectic were significantly lower than those of the individual anti-inflammatory drugs (NSAIDs). Due to the melting-point depression and enhanced skin lipid solubility, the steady-state flux of ibuprofen and ketoprofen from preparations of the binary eutectic increased as compared to pure NSAIDs using shed snakeskin as a model membrane. The NSAID membrane flux values were calculated by flux ratio equations based on drug thermodynamic data, and compared to experimental values obtained from permeation studies.

CONCLUSION

The proposed flux ratio equations correctly predicted flux increase.

摘要

方法

使用差示扫描量热法（DSC）和 X 射线粉末衍射法（XRPD）研究了布洛芬和酮洛芬二元混合物的热力学、共晶和结晶性质。

结果

DSC 研究表明，二元共晶的熔点（61°C）、焓（11.3 kJ/mol）和熔化熵（33.7 J/K/mol）明显低于单独的抗炎药物（非甾体抗炎药）。由于熔点降低和皮肤脂溶性增强，与使用蛇蜕作为模型膜的纯 NSAIDs 相比，二元共晶制剂中布洛芬和酮洛芬的稳态通量增加。根据药物热力学数据，通过通量比方程计算 NSAID 膜通量值，并与渗透研究中获得的实验值进行比较。