Lee Chin Chiat, Ong Charlene Li Ching, Heng Paul Wan Sia, Chan Lai Wah, Wong Tin Wui
ISP Asia Pacific Pte Ltd, Singapore Science Park, Republic of Singapore.
Drug Dev Ind Pharm. 2008 Feb;34(2):206-14. doi: 10.1080/03639040701542291.
The effectiveness of an interactive mixture as a rapid drug delivery system is compared with that of a solid dispersion. The influences of drug load, particle size, and crystallinity of these test systems are investigated. The interactive mixtures and solid dispersions were prepared from polyethylene glycol (PEG) 3350 and hydrophobic nifedipine drug by means of physical mixing and melting methods, respectively. The formed products were subjected to drug particle size and crystallinity analyses, and dissolution tests. In comparison with the interactive mixtures, the solid dispersions with low drug load were more effective as a rapid drug delivery system, as the size of a given batch of drug particles was markedly reduced by the molten PEG 3350. The rate and extent of drug dissolution were mainly promoted by decreasing effective drug particle size. However, these were lower in the solid dispersions than in the interactive mixtures when a high load of fine drug particles was used as the starting material. This was attributed to drug coarsening during the preparation of the solid dispersion. Unlike solid dispersions, the interactive mixtures could accommodate a high load of fine drug particles without compromising its capacity to enhance the rate and extent of drug dissolution. The interactive mixture is appropriate for use to deliver a fine hydrophobic drug in a formulation requiring a high drug load.
将交互式混合物作为快速给药系统的有效性与固体分散体进行了比较。研究了这些测试系统的载药量、粒径和结晶度的影响。交互式混合物和固体分散体分别通过物理混合和熔融法由聚乙二醇(PEG)3350和疏水性硝苯地平药物制备而成。对形成的产物进行药物粒径和结晶度分析以及溶出度测试。与交互式混合物相比,低载药量的固体分散体作为快速给药系统更有效,因为给定批次的药物颗粒尺寸被熔融的PEG 3350显著减小。药物溶出的速率和程度主要通过减小有效药物粒径来促进。然而,当使用高负载的细药物颗粒作为起始原料时,固体分散体中的这些参数低于交互式混合物。这归因于固体分散体制备过程中药物的粗化。与固体分散体不同,交互式混合物可以容纳高负载的细药物颗粒,而不会损害其提高药物溶出速率和程度的能力。交互式混合物适用于在需要高载药量的制剂中递送细疏水性药物。