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

发布时间：2018-12-10 18:59

【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%。
[Abstract]:In order to increase the dissolution rate of Piroxicam (1), the solid dispersions were prepared by the method of airflow pulverization, or the preparation of solid dispersion by solvent copolymerization of Vitamin S630 as the carrier. The micropowdered drugs and solid dispersions were prepared into tablets respectively. The pharmacokinetics of the tablets was studied by using Beagle canine model. The results showed that micropowder treatment had no significant effect on the pharmacokinetic behavior of 1 in Beagle dogs, but the oral bioavailability of 1 was significantly increased by the preparation of solid dispersion. Compared with the reference preparation, the relative bioavailability of the tablets prepared by micropowder 1 was 103.6; The relative bioavailability was 128.9% and 138.9% at 1:3 and 1:5 when the mass ratio of 1 to VT630 was 1:3 and 1:5 in solid dispersible tablets.
【作者单位】：四川省自贡市第四人民医院药剂科;四川省肿瘤医院(四川省第二人民医院);四川大学华西口腔医院口腔疾病研究国家重点实验室;
【分类号】：R965

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