Newa Madhuri, Bhandari Krishna Hari, Li Dong Xun, Kwon Tae-Hyub, Kim Jung Ae, Yoo Bong Kyu, Woo Jong Soo, Lyoo Won Seok, Yong Chul Soon, Choi Han Gon
College of Pharmacy, Yeungnam University, Gyongsan 712-749, South Korea.
Int J Pharm. 2007 Oct 1;343(1-2):228-37. doi: 10.1016/j.ijpharm.2007.05.031. Epub 2007 May 21.
Ibuprofen-Poloxamer 188 (P 188) binary solid dispersions (SD) with different drug loadings were prepared, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR), and evaluated for solubility, in vitro release, and oral bioavailability of ibuprofen in rats. Loss of their individual surface properties during melting and solidification as revealed by SEM micrographs indicated the formation of effective SDs. Absence or shifting towards the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of its interactions with P 188. However, no such interactions in the solid state were confirmed by FTIR spectra which showed the presence of drug crystalline in SDs. Immediate and complete release of ibuprofen from SDs might be because of the reduction in the drug crystalline due to eutectic formation, and their dosing to fasted rats resulted in a significant increase in the area under curve (AUC) of the plasma concentration versus time curve and the maximum plasma concentration (Cmax), and a significant decrease in the time to reach Cmax (Tmax) over ibuprofen and physical mixtures.
制备了不同载药量的布洛芬 - 泊洛沙姆188（P188）二元固体分散体（SD），通过扫描电子显微镜（SEM）、差示扫描量热法（DSC）和傅里叶变换红外光谱（FTIR）对其进行表征，并评估了布洛芬在大鼠体内的溶解度、体外释放度和口服生物利用度。SEM显微照片显示，它们在熔化和固化过程中各自表面性质的丧失表明形成了有效的固体分散体。DSC研究中，固体分散体和物理混合物中药物峰的缺失或向较低熔点温度的移动表明其与P188相互作用的可能性。然而，FTIR光谱未证实固态中有此类相互作用，该光谱显示固体分散体中存在药物晶体。布洛芬从固体分散体中立即完全释放可能是由于共晶形成导致药物晶体减少，给禁食大鼠给药后，与布洛芬和物理混合物相比，血浆浓度 - 时间曲线的曲线下面积（AUC）和最大血浆浓度（Cmax）显著增加，达到Cmax的时间（Tmax）显著缩短。
