Gautier H, Daculsi G, Merle C
Centre de recherche sur les matériaux d'intérêt biologique, Equipe INSERM 99-03, Faculté de chirurgie dentaire, Nantes, France.
Biomaterials. 2001 Sep;22(18):2481-7. doi: 10.1016/s0142-9612(00)00436-1.
Dynamic compaction has rarely been used to produce drug-delivery devices in granule form. This report considered four processes associating vancomycin and compared dynamic compaction with wet granulation, a classical method. In the wet granulation study, vancomycin was associated with biphasic calcium-phosphate (BCP) granules either by adsorption or incorporation with a new granulation. In the dynamic compaction study, BCP powder was compacted at 1.1, 1.5 and 1.9 MPa. The compacts obtained were crushed and sieved (200-500 microm), and the vancomycin solution was adsorbed on the resulting granules. After crushing and sieving, the compaction of BCP and vancomycin powders produced vancomycin-loaded granules. In each study, 4.76% of vancomycin was associated with BCP. Granules were characterized in terms of porosity, vancomycin release and vancomycin biological activity. Physicochemical studies of BCP and vancomycin showed their structural integrity after dynamic compaction, which prolonged vancomycin release time from 1 to 6 days. However, a microbiological assay indicated that vancomycin had been altered since only 27.7% was found to be active.
动态压制很少用于生产颗粒形式的药物递送装置。本报告考虑了四种将万古霉素结合的工艺，并将动态压制与经典方法湿法制粒进行了比较。在湿法制粒研究中，万古霉素通过吸附或与新制粒结合的方式与双相磷酸钙（BCP）颗粒相结合。在动态压制研究中，BCP粉末在1.1、1.5和1.9兆帕的压力下进行压制。将得到的压块粉碎并筛分（200 - 500微米），然后将万古霉素溶液吸附在所得颗粒上。经过粉碎和筛分后，BCP和万古霉素粉末的压制产生了载有万古霉素的颗粒。在每项研究中，4.76%的万古霉素与BCP相结合。对颗粒的孔隙率、万古霉素释放和万古霉素生物活性进行了表征。对BCP和万古霉素的物理化学研究表明，动态压制后它们的结构保持完整，这使得万古霉素的释放时间从1天延长至6天。然而，一项微生物检测表明万古霉素发生了变化，因为发现只有27.7%具有活性。
