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目的:制备方法简单、生物利用度高的烟酸缓释微丸。方法:采用挤出-滚圆法制备烟酸微丸,通过正交试验优化处方,比较优化制品与市售烟酸缓释胶囊(参比制剂)在不同介质(0.1 mol·L-1盐酸、水和pH6.8磷酸盐缓冲液)中的释放行为,并用Beagle犬做相对生物利用度实验。结果:两者的释放曲线相似,本品在水中的释放行为拟合为零级方程。犬体内药动学试验表明,本品与参比制剂的Cmax和tmax分别为(5.13±1.01),(5.07±1.32)mol·L-1和(4.05±0.87),(3.93±0.65)h。本品的相对生物利用度为101.95%。结论:通过挤出滚圆方法制备的烟酸缓释微丸工艺稳定,相对生物利用度高。
Objective: To prepare nicotinic acid sustained-release pellets with simple method and high bioavailability. Methods: The nicotinic acid pellets were prepared by extrusion-spheronization method. The orthogonal test was used to optimize the formulation. The optimal products were compared with nicotinic acid sustained-release capsules (reference preparation) in different media (0.1 mol·L -1 hydrochloric acid, And pH6.8 phosphate buffer) and compared their relative bioavailability with Beagle dogs. Results: The release curves of the two were similar, and the release behavior of this product in water was fitted as zero-order equation. The pharmacokinetics test in dogs showed that the Cmax and tmax of this product and reference preparation were (5.13 ± 1.01), (5.07 ± 1.32) mol·L-1 and (4.05 ± 0.87) and (3.93 ± 0.65) h, respectively. The relative bioavailability of this product is 101.95%. Conclusion: The nicotinic acid sustained-release pellets prepared by extrusion-spheronization method are stable and have relatively high bioavailability.