Nahata Tushar, Saini Tulsi Ram
Industrial Pharmacy Research Lab, Department of Pharmacy, Shri G. S. Institute of Technology and Science, Indore, M.P., India.
Drug Dev Ind Pharm. 2008 Jul;34(7):668-75. doi: 10.1080/03639040701836545.
This work was aimed to design and optimize a long acting microsphere-based injectable formulation of aripiprazole by using D-optimal experimental design methodology. Microspheres were prepared by solvent evaporation method using PLGA and cholesterol as release rate retardant materials. The microspheres were characterized for their encapsulation efficiency, particle size, surface morphology, residual solvent content, and drug release behavior. Contour plots were plotted to study the encapsulation and release behaviour of the drug from the microspheres. Desirability technique was used for the optimization of microsphere formulation composition. By using an optimum blend of drug and cholesterol in the microsphere formulation it was possible to attain a consistent drug release for a period of 14 days. The results have confirmed that the D-optimal experimental design technique can be successfully employed for designing the long acting microsphere dosage form.
本研究旨在运用D-最优实验设计方法,设计并优化一种基于长效微球的阿立哌唑注射剂配方。采用溶剂蒸发法,以聚乳酸-羟基乙酸共聚物(PLGA)和胆固醇作为释放速率阻滞剂材料制备微球。对微球的包封率、粒径、表面形态、残留溶剂含量及药物释放行为进行了表征。绘制等高线图以研究药物从微球中的包封和释放行为。采用可取性技术优化微球制剂组成。通过在微球制剂中使用药物和胆固醇的最佳混合物,可实现14天的持续药物释放。结果证实,D-最优实验设计技术可成功用于设计长效微球剂型。