Torrado-Durán J J, Torrado S, Cadórniga R, Augsburger L L
School of Pharmacy, University of Maryland at Baltimore 21201, USA.
J Pharm Pharmacol. 1995 Feb;47(2):115-9. doi: 10.1111/j.2042-7158.1995.tb05761.x.
The tableting characteristics of micro-aggregated egg albumin particles containing paracetamol were evaluated and compared with non-micro-encapsulated paracetamol and coagulated egg albumin particles. Mean yield pressure values of micro-aggregated egg albumin particles containing paracetamol and coagulated egg albumin particles were 30.5 and 49.3 MPa, respectively, which were lower than the mean yield pressure obtained for paracetamol (97.5 MPa). Paracetamol tablets obtained with micro-aggregated egg albumin particles did not show the capping characteristic of conventional paracetamol tablets. Crushing strength of paracetamol tablets obtained with egg micro-aggegated particles was similar to that obtained using paracetamol granulated with povidone and gelatin as binders at 3 and 6% (w/w) concentrations. Drug release from the paracetamol tablets depends on the choice of excipients. Crospovidone showed good protective characteristics for the tableting of micro-aggregated particles. Crushing strength of paracetamol tablets formed from egg albumin-coated particles could be increased using crospovidone or microcrystalline cellulose as fillers and was decreased by the use of magnesium stearate. Nevertheless, magnesium stearate was useful to decrease the ejection force.
对含有扑热息痛的微团聚蛋清蛋白颗粒的压片特性进行了评估，并与未微囊化的扑热息痛及凝固蛋清蛋白颗粒进行了比较。含有扑热息痛的微团聚蛋清蛋白颗粒和凝固蛋清蛋白颗粒的平均屈服压力值分别为30.5 MPa和49.3 MPa，均低于扑热息痛的平均屈服压力（97.5 MPa）。用微团聚蛋清蛋白颗粒制得的扑热息痛片剂未表现出传统扑热息痛片剂的裂片特性。用微团聚蛋清蛋白颗粒制得的扑热息痛片剂的抗压强度，与使用浓度为3%和6%（w/w）的聚维酮和明胶作为粘合剂制粒的扑热息痛片剂的抗压强度相似。扑热息痛片剂的药物释放取决于辅料的选择。交联聚维酮对微团聚颗粒的压片显示出良好的保护特性。使用交联聚维酮或微晶纤维素作为填充剂可提高由蛋清蛋白包衣颗粒制成的扑热息痛片剂的抗压强度，而使用硬脂酸镁则会降低抗压强度。不过，硬脂酸镁有助于降低顶出力。
