微粉化和固体分散体技术对吡罗昔康在Beagle犬体内口服生物利用度的影响  

Effects of Micronization and Solid Dispersion Technologies on Oral Bioavailability of Piroxicam in Beagle Dogs

作　　者：李模勇[1] 杨澄[2] 彭强[3] 

机构地区：[1]四川省自贡市第四人民医院药剂科,四川自贡643000 [2]四川省肿瘤医院(四川省第二人民医院),四川成都610041 [3]四川大学华西口腔医院口腔疾病研究国家重点实验室,四川成都610041

出　　处：《中国医药工业杂志》2015年第1期32-35,共4页Chinese Journal of Pharmaceuticals

摘　　要：为增加吡罗昔康(1)的溶出速度,采用气流粉碎法对1原药进行微粉化处理,或采用溶剂法以共聚维酮S630为载体制备固体分散体。将所得的微粉化药物和固体分散体分别制成片剂,并以市售1片为参比制剂,采用Beagle犬为模型进行药动学研究。结果表明,微粉化处理对1在Beagle犬体内的药动学行为无显著影响,但制备固体分散体能有效提高1的口服生物利用度。与参比制剂相比,采用微粉化1制备的片剂口服相对生物利用度为103.6%;当固体分散体片剂中1与共聚维酮S630质量比为1:3和1:5时,口服相对生物利用度为128.9%和138.9%。To improve the dissolution of piroxicam（1）, the micronized 1 and the solid dispersion of 1 with Plasdone $630 as carrier were prepared. Then the tablets based on micronized drug or solid dispersion were prepared and their pharmacokinetics in Beagle dogs were evaluated with commercial 1 tablets as reference preparation. The results showed that micronization had little effect on the improvement of pharmacokinetic behavior of 1, while forming solid dispersion could significantly enhance its oral bioavailability. Compared with the reference tablets, the relative oral bioavailability of tablets based on micronized I was 103.6%, while the relative bioavailabilities of the tablets based on solid dispersion of 1-Plasdone $630 in the ratio of 1 ： 3 and 1 ： 5 were 128.9 % and 138.9 %, respectively.

关 键 词：吡罗昔康 微粉化 固体分散体 生物利用度 

分 类 号：R944.9[医药卫生—药剂学]