褪黑激素明胶微球的鼻腔给药  

STUDIES ON MELATONIN GELATIN MICROSPHERES FOR INTRANASAL ADMINISTRATION

作　　者：陈建明[1] 毛世瑞[1] 毕殿洲[1] 

机构地区：[1]沈阳药科大学药剂教研室,辽宁沈阳110015

出　　处：《药学学报》2000年第10期786-789,共4页Acta Pharmaceutica Sinica

摘　　要：目的　制备经鼻粘膜给药的褪黑激素明胶微球 ,以提高其生物利用度。方法　用乳化交联技术制备褪黑激素明胶微球 ,用放射性核素99mTc标记 ,用γ射线闪烁显像技术考察微球在鼻粘膜滞留时间 ,用HPLC法测定药物的体内吸收。结果　褪黑激素明胶微球粒径在 30～ 70 μm ,平均粒径为 5 0 2 μm ,褪黑激素含量为 13 48%。与滴鼻液相比 ,明胶微球在鼻粘膜滞留时间明显延长。褪黑激素明胶微球的绝对生物利用度为 87 47%。结论　鼻粘膜给药明胶微球 ,能避免肝脏首过作用 ,延长药物在鼻粘膜滞留时间 ,提高药物吸收 。AIM To increase the bioavailability of melatonin (MT), MT gelatin microspheres (MT-GMS) for intranasal administration were prepared. METHODS MT-GMS were prepared using emulsifying-cross linking technique. Orthogonal tests were used to optimize the preparation conditions. The residence time of technetium-99m ( 99m Tc ) labeled gelatin microspheres (GMS) in the nasal cavity of rabbits as compared to gelatin solution, was investigated using gamma scintigraphy. Furthermore the bioavailability in rabbits was examined for evaluating MT-GMS. RESULTS The mean diameter of MT-GMS was 50 2 μm, the particle size focused on 30～70 μm. The drug content was 13 48%. The release profile in vitro showed sustained effect. The residence time of GMS in the nasal cavity of rabbits was longer than that of gelatin solution. After intranasal administration in rabbits, the bioavailability of MT-GMS was 87 47% as compared to vein injection, while the bioavailability of MT solution was 69 72%. CONCLUSION MT-GMS prepared could meet the needs of intranasal administration, and could increase the bioavailability of MT.

关 键 词：褪黑激素 明胶微球 鼻粘膜给药 生物利用度 

分 类 号：R977.1[医药卫生—药品]