固体分散技术与包合技术对吡罗昔康溶出度的影响

Improvement in Dissolution Properties of piroxicam by Complexation with β-Cyclodextrin and PVP

目的考察固体分散技术及包合技术对吡罗昔康溶出度的影响。方法以聚乙烯吡咯烷酮(PVP)为载体制备固体分散体;以β-环糊精(β-CD)包合技术制备包合物。以差示扫描量热法(DSC)鉴定吡罗昔康在体系中的存在形态;以水为溶出介质,紫外分光光度法测定不同制备工艺下成品的体外溶出度。结果差热分析图谱表明,吡罗昔康β-CD包合物以及吡罗昔康-PVP(1:6,1:8)的固体分散体中药物以非晶型存在,而吡罗昔康-PVP(1:2,1:4)的固体分散体中,药物与载体形成低共熔物,药物以微晶形式存在于载体中;体外溶出结果表明环糊精包合物和载药比为1:6,1:8的固体分散体的溶出速率与相应物理混合物及原料药间差异有极显著性(P<0.01)。结论制成固体分散体和β-环糊精包合物均能显著提高吡罗昔康的溶出速率。

Objective To study the dissolution of Piroxicam by complexation with β-cyclodextrin and PVP. Methods The sample was prepared by PVP solid dispersion or β-CD complexation and characterized by differential scanning calorimetry. Dissolution of finished products produced with different technology was determined by UV spectrophotometry. Results The result of differential scanning calorimetry indicated that in β-CD complexation and piroxicam-PVP （ 1 ： 6,1 ： 8 ） solid dispersion piroxicam existed as an amorphous form and in piroxicam-PVP （ 1 ： 2,1 ： 4） solid dispersion , Piroxicam was finely crystalline. The dissolution rate of β-CD complexation and solid dispersion with the drug-carrier ratio 1 ： 6 and 1 ： 8 was markedly increased in comparison with that of the physical mixture and piroxicam substance （ P 〈 0.01 ）. Conclusion Both solid dispersion and β-CD complexation can significantly increase the dissolution rate of piroxicam.