硫酸钙链霉素的颗粒体外缓释性能的研究

Study on the sustained release properties of calcium sulfate streptomycin particles in vitro

目的了解载结核药链霉素的硫酸钙缓释颗粒在体外的药物缓释性能。方法实验组,将链霉素与医用硫酸钙混合制备成载药颗粒,将其置于模拟体液中,取1 d、2 d、3 d、1周、2周、4周、6周、8周、10周时缓冲液为样本,高效液相色谱法(HPLC)检测其中链霉素药物的浓度,绘制药物缓释曲线。空白组,医用硫酸钙制备成未载药颗粒。结果医用硫酸钙5 cc与链霉素1 g为最佳配比。载链霉素硫酸钙颗粒在模拟体液中浸泡,缓释颗粒3 d时累计释放量15.33%。在8周前的样本液中,药物浓度均较高;至8周时链霉素的释出浓度、仍达到的最小抑菌浓度,之后逐渐降低。未载链霉素的硫酸钙颗粒在有效检测时间内药物出峰时间处未见波峰出现。结论硫酸钙链霉素颗粒具有效缓释性能。8周内模拟体液中释出药物的浓度均可达到抑制结核分枝杆菌的浓度。

Objective To understand the drug release properties of calcium sulfate sustained-release granules carrying the tuberculosis drug streptomycin in vitro.Methods In the experimental group,streptomycin was mixed with medical calcium sulfate to prepare drug-loaded granules,which were placed in simulated body fluids.The buffer at 1 day,2 days,3 days,1 week,2,4,6,8 and 10 weeks was used as a sample.The concentration of streptomycin was detected by high performance liquid chromatography(HPLC),and the drug sustained-release curve was drawn.In the blank group,medical calcium sulfate was prepared as unloaded particles.Results The medical calcium sulfate 5 cc and streptomycin 1g were the best ratio.The streptomycin calcium sulfate particles were soaked in the simulated body fluid,and the cumulative release of the sustained-release particles was 15.33%.In the sample solution before 8 weeks,the drug concentration was higher.Release concentration of streptomycin and still reached minimum inhibitory concentration at 8 weeks,and then gradually decreased.Calcium sulfate particles without streptomycin showed no peaks at the peak time of the drug during the effective detection time.Conclusion Calcium sulfate streptomycin granules have a slow release property.The concentration of the drug released in the simulated body fluid can reach the concentration of inhibiting tuberculosis within 8 weeks.