Vanhoorne V, Peeters E, Van Snick B, Remon J P, Vervaet C
Eur J Pharm Biopharm. 2014 Nov;88(3):939-44. doi: 10.1016/j.ejpb.2014.10.018.
A continuous crystal coating method was developed to improve both flowability and tabletability of powders. The method includes the introduction of solid, dry particles into an atomized spray during spray drying in order to coat and agglomerate individual particles. Paracetamol was used as a model drug as it exhibits poor flowability and high capping tendency upon compaction. The particle size enlargement and flowability were evaluated by the mean median particle size and flow index of the resulting powders. The crystal coating coprocessing method was successful for the production of powders containing 75% paracetamol with excellent tableting properties. However, the extent of agglomeration achieved during coprocessing was limited. Tablets compressed on a rotary tablet press in manual mode showed excellent compression properties without capping tendency. A formulation with 75% paracetamol, 5% PVP and 20% amorphous lactose yielded a tensile strength of 1.9 MPa at a compression pressure of 288 MPa. The friability of tablets compressed at 188 MPa was only 0.6%. The excellent tabletability of this formulation was attributed to the coating of paracetamol crystals with amorphous lactose and PVP through coprocessing and the presence of brittle and plastic components in the formulation. The coprocessing method was also successfully applied for the production of directly compressible lactose showing improved tensile strength and friability in comparison to a spray dried direct compression lactose grade.
为了改善粉末的流动性和可压性,开发了一种连续结晶包衣方法。该方法包括在喷雾干燥过程中将固体干燥颗粒引入雾化喷雾中,以便对单个颗粒进行包衣和团聚。对乙酰氨基酚作为模型药物,因为它在压实过程中表现出较差的流动性和较高的裂片倾向。通过所得粉末的平均中值粒径和流动指数来评估粒径增大和流动性。结晶包衣共处理方法成功地生产出了含75%对乙酰氨基酚且具有优异压片性能的粉末。然而,共处理过程中实现的团聚程度有限。在手动模式下在旋转压片机上压制的片剂显示出优异的压缩性能且无裂片倾向。含有75%对乙酰氨基酚、5%聚乙烯吡咯烷酮(PVP)和20%无定形乳糖的配方在288MPa的压缩压力下产生的抗张强度为1.9MPa。在188MPa下压制的片剂的脆碎度仅为0.6%。该配方优异的可压性归因于通过共处理用无定形乳糖和PVP对乙酰氨基酚晶体进行包衣以及配方中存在脆性和塑性成分。与喷雾干燥直接压片乳糖等级相比,共处理方法还成功地应用于生产具有改善的抗张强度和脆碎度的直接压片乳糖。