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采用喷雾干燥法制备了异烟肼PLA缓释微球(IN-PLA-MS).首先采用球磨法制备IN微粉颗粒,平均粒径为0.161μm,然后将IN微粉超声分散于溶有PLA的二氯甲烷溶液中(S/O),将制备的混悬液进行喷雾干燥.制备得到的微球形态圆整光滑,无粘连,分散性好,平均粒径为5.62μm,粒径均一;体外释放试验中,IN-PLA-MS23天累积释放70%,且无明显突释;大鼠(Rattus norvegicus)体内考察中,采用液相色谱-质谱/质谱(LC-MS/MS)测定肺部药物浓度,微球在大鼠体内持续释药4周.该制备方法操作简单过程容易控制,采用包裹IN微粉颗粒的方法,未引入水分,一方面避免了因水分挥发在微球内部留下的空隙,另一方面抑制了药物在微球表面的迁移,有效地减少突释,达到较好的缓释效果.
Isoniazid PLA sustained-release microspheres (IN-PLA-MS) were prepared by spray drying method.Firstly, IN microparticles were prepared by ball milling with an average particle size of 0.161μm, then the IN microparticles were dispersed ultrasonically (S / O), the prepared suspension was spray-dried.The prepared microspheres were round and smooth with no blocking and good dispersibility, with an average particle size of 5.62 μm and uniform particle size. The in vitro release In the experiment, IN-PLA-MS was released 70% cumulatively for 23 days without significant burst release. In the in vivo study of Rattus norvegicus, the concentration of pulmonary drug was determined by liquid chromatography-mass spectrometry / mass spectrometry (LC-MS / MS) , Microspheres sustained release in rats for 4 weeks.The preparation method is easy to control the process of simple operation, the method of wrapping IN microparticles particles, without the introduction of moisture, on the one hand to avoid the voids in the microspheres left behind due to water evaporation, On the other hand, it inhibits drug migration on the surface of microspheres and effectively reduces burst release to achieve better sustained-release effect.