Newa Madhuri, Bhandari Krishna Hari, Li Dong Xun, Kim Jong Oh, Yoo Dong Sung, Kim Jung-Ae, Yoo Bong-Kyu, Woo Jong-Soo, Choi Han-Gon, Yong Chul-Soon
College of Pharmacy, Yeungnam University, Gyongsan, 712-749, South Korea.
Biol Pharm Bull. 2008 May;31(5):939-45. doi: 10.1248/bpb.31.939.
To improve its dissolution, ibuprofen solid dispersions (SDs) were prepared in a relatively easy and simple manner, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR), and evaluated for solubility, in-vitro drug release and oral bioavailability of ibuprofen in rats. Loss of individual surface properties during melting and resolidification 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 drug-polymer interactions. FT-IR spectra showed the presence of drug crystalline in SDs. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in AUC and Cmax, and a significant decrease in Tmax over pure ibuprofen. Preliminary results from this study suggested that the preparation of fast dissolving ibuprofen SDs by low temperature melting method using polyethylene glycol 4000 (PEG 4000) as a meltable hydrophilic polymer carrier could be a promising approach to improve solubility, dissolution and absorption rate of ibuprofen.
为提高布洛芬的溶出度,采用相对简便的方法制备了布洛芬固体分散体(SDs),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(FT-IR)对其进行表征,并对布洛芬在大鼠体内的溶解度、体外药物释放和口服生物利用度进行了评估。SEM显微照片显示,在熔融和再固化过程中,个体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了药物与聚合物相互作用的可能性。FT-IR光谱显示固体分散体中存在药物晶体。与纯布洛芬相比,布洛芬在大鼠肠道中从固体分散体中的更快释放导致AUC和Cmax显著增加,Tmax显著降低。本研究的初步结果表明,以聚乙二醇4000(PEG 4000)作为可熔融亲水性聚合物载体,通过低温熔融法制备快速溶解的布洛芬固体分散体,可能是提高布洛芬溶解度、溶出度和吸收速率的一种有前景的方法。