In this study, a natural gum mastic was evaluated as a microencapsulating and matrixforming material for sustained drug release. Mastic was characterized for its physicochemical properties. Microparticles were prepare...In this study, a natural gum mastic was evaluated as a microencapsulating and matrixforming material for sustained drug release. Mastic was characterized for its physicochemical properties. Microparticles were prepared by oil-in-oil solvent evaporation method. Matrix tablets were prepared by wet and melt granulation techniques. Diclofenac sodium(DFS) and diltiazem hydrochloride(DLTZ) were used as model drugs. Mastic produced discrete and spherical microspheres with DLTZ and microcapsules with DFS. Particle size and drug loading of microparticles was in the range of 22–62 μm and 50–87%, respectively. Increase in mastic:drug ratio increased microparticle size, improved drug loading and decreased the drug release rate. Microparticles with gum: drug ratio of 2:1 could sustain DLTZ release up to 12 h and released 57% DFS in 12 h. Mastic produced tablets with acceptable pharmacotechnical properties. A 30% w/w of mastic in tablet could sustain DLTZ release for 5 h from wet granulation,and DFS release for 8 h and 11 h from wet and melt granulation, respectively. Results revealed that a natural gum mastic can be used successfully to formulate matrix tablets and microparticles for sustained drug release.展开更多
本文基于“质量源于设计”(Quality by Design, QbD)理念设计并优化了氨来呫诺(Amlexanox, AML)亲水凝胶骨架缓释片(简称为“AML缓释片”)的处方工艺。在风险评估的基础上结合单因素考察结果和鱼骨分析法确定潜在关键工艺参数(Critical ...本文基于“质量源于设计”(Quality by Design, QbD)理念设计并优化了氨来呫诺(Amlexanox, AML)亲水凝胶骨架缓释片(简称为“AML缓释片”)的处方工艺。在风险评估的基础上结合单因素考察结果和鱼骨分析法确定潜在关键工艺参数(Critical process parameters, CPPs),采用Plackett-Burman设计对CPPs进行筛选,然后用Box-Behnken设计对CPPs进行优化,建立统计模型,对优化后的工艺进行验证并考察其体外释放行为。结果表明骨架材料用量、黏合剂用量和片剂硬度对片剂释放行为有显著影响,当三者分别为50%~55%、62.5%~100%(占干物料的量)、124~142N时制备的氨来呫诺亲水凝胶骨架缓释片能达到释放目标,即2、6、12、18、24 h的累积释放率分别为8%~10%、25%~30%、50%~55%、75%~80%、95%以上。基于QbD理念设计的氨来呫诺亲水凝胶骨架缓释片处方工艺稳定可行,符合制剂设计的释放要求,具有良好的商业前景。展开更多
文摘In this study, a natural gum mastic was evaluated as a microencapsulating and matrixforming material for sustained drug release. Mastic was characterized for its physicochemical properties. Microparticles were prepared by oil-in-oil solvent evaporation method. Matrix tablets were prepared by wet and melt granulation techniques. Diclofenac sodium(DFS) and diltiazem hydrochloride(DLTZ) were used as model drugs. Mastic produced discrete and spherical microspheres with DLTZ and microcapsules with DFS. Particle size and drug loading of microparticles was in the range of 22–62 μm and 50–87%, respectively. Increase in mastic:drug ratio increased microparticle size, improved drug loading and decreased the drug release rate. Microparticles with gum: drug ratio of 2:1 could sustain DLTZ release up to 12 h and released 57% DFS in 12 h. Mastic produced tablets with acceptable pharmacotechnical properties. A 30% w/w of mastic in tablet could sustain DLTZ release for 5 h from wet granulation,and DFS release for 8 h and 11 h from wet and melt granulation, respectively. Results revealed that a natural gum mastic can be used successfully to formulate matrix tablets and microparticles for sustained drug release.
文摘本文基于“质量源于设计”(Quality by Design, QbD)理念设计并优化了氨来呫诺(Amlexanox, AML)亲水凝胶骨架缓释片(简称为“AML缓释片”)的处方工艺。在风险评估的基础上结合单因素考察结果和鱼骨分析法确定潜在关键工艺参数(Critical process parameters, CPPs),采用Plackett-Burman设计对CPPs进行筛选,然后用Box-Behnken设计对CPPs进行优化,建立统计模型,对优化后的工艺进行验证并考察其体外释放行为。结果表明骨架材料用量、黏合剂用量和片剂硬度对片剂释放行为有显著影响,当三者分别为50%~55%、62.5%~100%(占干物料的量)、124~142N时制备的氨来呫诺亲水凝胶骨架缓释片能达到释放目标,即2、6、12、18、24 h的累积释放率分别为8%~10%、25%~30%、50%~55%、75%~80%、95%以上。基于QbD理念设计的氨来呫诺亲水凝胶骨架缓释片处方工艺稳定可行,符合制剂设计的释放要求,具有良好的商业前景。
