赵甘霖, 王鸿辰. 布洛芬包衣缓释颗粒释药动力学及体内外相关性研究J. 药学学报, 1995, 30(4): 291-297.
引用本文: 赵甘霖, 王鸿辰. 布洛芬包衣缓释颗粒释药动力学及体内外相关性研究J. 药学学报, 1995, 30(4): 291-297.
CL Zhao, HC Wang. DRUG RELEASE KINETICS OF IBUPROFEN COATED GRANULES AND THEIR IN VITRO-IN VIVO CORRELATIONJ. Acta Pharmaceutica Sinica, 1995, 30(4): 291-297.
Citation: CL Zhao, HC Wang. DRUG RELEASE KINETICS OF IBUPROFEN COATED GRANULES AND THEIR IN VITRO-IN VIVO CORRELATIONJ. Acta Pharmaceutica Sinica, 1995, 30(4): 291-297.

布洛芬包衣缓释颗粒释药动力学及体内外相关性研究

DRUG RELEASE KINETICS OF IBUPROFEN COATED GRANULES AND THEIR IN VITRO-IN VIVO CORRELATION

  • 摘要: 在研制出布洛芬速释处方的基础上,用乙基纤维素为材料对颗粒进行包衣,考察其体外释药动力学,并观察了颗粒大小、包衣厚度、pH值和压力诸因素对释药速率的影响。结果表明,包衣量较少时,释药过程更符合Higuchi方程;包衣量较大时,更符合零级动力学。在相同包衣量条件下,释药速率随颗粒的增大而减慢;当颗粒大小相同时,则随着包衣量增大释药速率减慢;释药速率随pH值的降低而显著减慢;包衣颗粒压片后,释药速率增大。经7名健康志愿受试者实验表明,体内外相关性显著。

     

    Abstract: A sustained release of ibuprofen granules coated with ethyl cellulose has beenstudied both in vitro and in vivo with a selected formulation。The drug release process follows Higuchiequation when coating extent is low,and zero-order kinetics when coating extent is high.The primaryfactors that influence drug release include granule size ,coating extent ,pH of dissolution medium andpressure,The release rate decreases when either granule size or coating extent increases or pH valuedecreases.The release rate increases greatly when the coated granules are compressed directly intotablets in that the coating film is destroyed.The results from oral administration of coated granules byseven healthy volunteers show that the in vitro and in vivo correlation of drug release from coatedgranules is highly significant.

     

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