聚酸酐-全反式维甲酸长效缓释剂制备及体内外释药  

Study on the preparation of a long-acting release agent of poly anhydrides-all trans retinoic acid and its release in vitro and in vivo

作　　者：孙蓓[1] 于美丽[2] 

机构地区：[1]天津医科大学附属肿瘤医院肿瘤防治重点实验室,天津300060 [2]天津市第三中心医院肝胆疾病重点实验室,天津300170

出　　处：《中国医院药学杂志》2013年第17期1395-1398,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:以可生物降解高分子材料聚酸酐(Polyanhydrides,PAD)作载体,包埋全反式维甲酸(ATRA),研制长效缓释微球ATRA-PAD肿瘤治疗剂。方法:建立高效液相色谱法(HPLC)测定体系,以检测缓释治疗剂中ATRA含量,探讨体内外ATRA经时缓释变化规律。采用乳剂-扩散溶剂挥发法制备维甲酸长效缓释微球ATRA-PAD肿瘤治疗剂,用激光散射粒度测定仪进行粒径检测,HPLC检测微球载药量、包封率及体内外释药量。结果:所制治疗剂微球光滑圆整,大小均一,平均粒径:(154.42±26.76)μm,载药率:(16.52±1.45)%,包封率:(87.84±4.79)%;体外释放试验证明该微球治疗剂可持续释放ATRA约50 d,将其采用肌内注射法注入到大耳白兔体内,可稳定缓释ATRA近约45 d。结论:ATRA-PAD治疗剂体内外释药释药平稳,并且具有明显的长效缓释作用。OBJECTIVE To develop a long-acting release micro-spheres ATRA-PAD tumor therapeutic agent; the biode gradable polymer materials poly-anhydride （Poly-anhydrides, PAD） were used as carrier, embedding of all-trans retinoic acid （ATRA）. METHODS A high-performance liquid chromatography （HPLC） assay system was created to detect the content of sustained release therapeutic agent ATRA and to explore the changes of rule of in vitro and in vivo ATRA sustained-release. Retinoid ATRA-PAD cancer therapeutic agent long-acting release micro-spheres were prepared by emulsion-diffusion solvent e vaporation, laser light scattering particle size analyzer was used to detect particle size, HPLC was used to detect micro-sphere drug loading, encapsulation efficiency and in vitro and in vivo drug release amount. RESULTS The therapeutic agent micro- spheres were smooth and rounded, uniform size, average particle size.. （154. 42±26. 76） m, drug loading rate： （16. 52±1.45）%, encapsulation efficiency： （87. 84±4. 79）% ; in vitro release experiments proved that the micro-sphere sustained re- lease therapeutic agent released ATA lasting about 50 days, intramuscular injection to rabbits in vizx） could stably release AT- RA approximately 45 days. CONCLUSION ATRA-PAD therapeutic agents in vitro and in vivo drug release is smooth, and has a significant long-term sustained release.

关 键 词：全反式维甲酸 聚酸酐 长效 缓释 微球 

分 类 号：R944[医药卫生—药剂学]