Hussein Khaled, Türk Michael, Wahl Martin A
1 Pharmazeutische Technologie, Eberhard-Karls-Universität Tübingen, Auf der Morgenstelle 8, D-72076 Tübingen, Germany.
Pharm Res. 2007 Mar;24(3):585-92. doi: 10.1007/s11095-006-9177-0.
The preparation of drug/cyclodextrin complexes is a suitable method to improve the dissolution of poor soluble drugs. The efficacy of the Controlled Particle Deposition (CPD) as a new developed method to prepare these complexes in a single stage process using supercritical carbon dioxide is therefore compared with other conventional methods.
Ibuprofen/beta-cyclodextrin complexes were prepared with different techniques and characterized using FTIR-ATR spectroscopy, powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). In addition, the influences of the processing technique on the drug content (HPLC) and the dissolution behavior were studied.
Employing the CPD-process resulted in a drug content of 2.8+/-0.22 wt.% in the carrier. The material obtained by CPD showed an improved dissolution rate of ibuprofen at pH 5 compared with the pure drug and its physical mixture with beta-cyclodextrin. In addition CPD material displays the highest dissolution (93.5+/- 2.89% after 75 min) compared to material obtained by co-precipitation (61.3 +/-0.52%) or freeze-drying (90.6 +/-2.54%).
This study presents the CPD-technique as a well suitable method to prepare a drug/beta-cyclodextrin complex with improved drug dissolution compared to the pure drug and materials obtained by other methods.
制备药物/环糊精复合物是提高难溶性药物溶出度的一种合适方法。因此,将一种新开发的使用超临界二氧化碳在单步过程中制备这些复合物的控制颗粒沉积(CPD)方法的效果与其他传统方法进行了比较。
采用不同技术制备布洛芬/β-环糊精复合物,并通过傅里叶变换红外光谱-衰减全反射(FTIR-ATR)、粉末X射线衍射(PXRD)、差示扫描量热法(DSC)和扫描电子显微镜(SEM)进行表征。此外,还研究了加工技术对药物含量(高效液相色谱法)和溶出行为的影响。
采用CPD工艺在载体中得到的药物含量为2.8±0.22 wt.%。与纯药物及其与β-环糊精的物理混合物相比,CPD法制备的材料在pH 5时布洛芬的溶出速率有所提高。此外,与共沉淀法(61.3±0.52%)或冷冻干燥法(90.6±2.54%)得到的材料相比,CPD材料的溶出度最高(75分钟后为93.5±2.89%)。
本研究表明,与纯药物及其他方法得到的材料相比,CPD技术是一种制备具有改善药物溶出度的药物/β-环糊精复合物的合适方法。