烟酸缓释微丸的制备

Preparation of nicotinic acid sustained release pellets

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 high bioavailability of nicotinic acid sustained-release micro pills. METHODS The opti mized product reached similar release curve as the current market-selling nicotinic acid sustained release capsules （reference preparation） in different medium （0. 1 mol·L^-1 hydrochloric acid, water and pH 6. 8 phosphate buffer）. RESULTS The re- lease behavior in water of this optimized product was in line with the zero-order equation. Pharmacokinetics in Beagle dogs test showed that the Cmax and tmax of this product and the reference preparation were （5. 13 ± 1.01）, （5.07 ± 1.32） mg·L^-1 and （4. 05 ± 0. 87）, （3.93 ± 0. 65） h respectively, and the relative bioavailability of this product was 101.95%. CONCLUSION Through extruding rolling method preparation technology, the nicotinic acid sustained release micro pill is stable, relatively high bioavailability.