He Shuai, Zhang Zhongyi, Xu Feng, Zhang Shouyao, Lei Zhengjie
Department of Pharmacy, Zhujiang Hospital, Southern Medical University, Guangzhou 510282, China.
Chem Pharm Bull (Tokyo). 2010 Feb;58(2):154-9. doi: 10.1248/cpb.58.154.
A rapid expansion of supercritical solution (RESS) technology was presented for the micronization of Chinese medicinal material. Magnolia bark extract (MBE) obtained by supercritical carbon dioxide (scCO(2)) extraction technology was chosen as the experimental material. RESS process produced 4.7 microm size MBE microparticles (size distribution, 0.2-24.1 microm), which was significantly smaller than the 55.3 microm size particles (size distribution, 8.3-102.4 microm) obtained from conventional mechanical milling. Dissolution rate study showed that drug dissolution was significantly enhanced by the RESS progress. At 90 min, the amount dissolved of mechanical milling MBE was 6.37 mg x l(-1), which was significantly lower than that of micronized MBE (14.77 mg x l(-1)), according to the results of ANOVA (p<0.01). The effect of extraction temperature (30, 40, 50 degrees Celsius), extraction pressure (200, 250, 300 bar) and nozzle size (50, 100, 200 microm) on the size distribution of microparticles was investigated. The characteristics of microparticles were also studied by differential scanning calorimetry (DSC), infrared spectroscopy (IR), scanning electron microscopy (SEM), and image analysis. This study demonstrates that RESS is applicable for preparing microparticles of MBE at low operating temperature; the process is simple without residual solvent.
介绍了一种用于中药材微粉化的超临界溶液快速膨胀(RESS)技术。选用通过超临界二氧化碳(scCO₂)萃取技术获得的厚朴树皮提取物(MBE)作为实验材料。RESS工艺制备出了粒径为4.7微米的MBE微粒(粒径分布为0.2 - 24.1微米),这明显小于通过传统机械研磨得到的粒径为55.3微米的微粒(粒径分布为8.3 - 102.4微米)。溶出度研究表明,RESS工艺显著提高了药物的溶出度。根据方差分析结果(p < 0.01),在90分钟时,机械研磨的MBE溶出量为6.37毫克/升,明显低于微粉化MBE的溶出量(14.77毫克/升)。研究了萃取温度(30、40、50摄氏度)、萃取压力(200、250、300巴)和喷嘴尺寸(50、100、200微米)对微粒粒径分布的影响。还通过差示扫描量热法(DSC)、红外光谱法(IR)、扫描电子显微镜(SEM)和图像分析对微粒特性进行了研究。本研究表明,RESS适用于在低温下制备MBE微粒;该工艺简单且无残留溶剂。