高效氟苯尼考粉剂研究

Research of Efficient Florfenicol powder

为解决氟苯尼考本身溶出较慢和吸收缓慢等问题导致的疗效不稳定现象,制备高效氟苯尼考粉剂。采用无定形技术和药物吸收促进技术制备高效氟苯尼考粉剂。结果:90 min在体大鼠药物肠吸收率达40%,较原药提高1倍,与国外同类产品(38%)相比无显著性差异(P>0.05);体外5 min累计溶出达85%,为原药的17倍;优化后药物小鼠灌胃给药,Tmax为0.6h、Cmax为54.03μg/mL,与国外同类产品Tmax为0.91 h、Cmax为49.86μg/mL相比,均有显著性提高(P<0.05);其生物利用度是国外同类产品的99.08%((P>0.05)、是氟苯尼考溶液的124.4%(P<0.05)。表明无定形技术和药物吸收促进技术结合制备的高效氟苯尼考粉剂,能显著提高氟苯尼考的溶出速度和吸收效率。

To prepare efficient florfenicol powder to solve the phenomenon of its efficacy instability which is caused by its slower dissolution and absorption.Methods：Using amorphous technology and drug absorption enhancer technology to get efficient florfenicol powder.Results：The efficient florfenicol powder has a drug absorption rate of 40% at 90 min in rat intestinal,which is twice that of the original drug.The absorption rate of the similar foreign products is 38%.which showed no significant difference（P〉 0.05）.It also had an accumulated dissolution rate of 85% at 5min in vitro,which was 17 times that of the original drug; Compared with the similar foreign products whose Tmax is 0.91 h and Cmax is 49.86 μg/mL,mice gavaged with the optimized powder（Tmax is 0.6h and Cmax is54.03μg/mL）shoued a significant increase（P 〉0.05）;Compared to the similar foreign products its bioavailability was 99.08%（P 0.05）Compared to the similar foreign products and 124.4% was compared to florfenicol solution（P 〈0.05）.Conclusion：Amorphous technology combin-ed with drug absorption enhancer technology can significantly increase the dissolution rate and absorption efficiency of efficient florfenicol powder.