~3H-甲硝唑控释药膜体内外释放测定  

The release of the^3 Hmetronidazole controlled release strip in vivo and vitro

作　　者：李德懿[1,2] 叶秀琴 俞兵 张文生 

机构地区：[1]第二医科大学口腔医学研究所 [2]上海中华制药厂

出　　处：《中国药学杂志》1998年第2期101-103,共3页Chinese Pharmaceutical Journal

摘　　要：目的：测定甲硝唑控释药膜在体内外不同时相点甲硝唑释放量。方法：３Ｈ标记甲硝唑（放射性比强度５．４４×１０４Ｂｑ·ｍｍｏｌ－１，放化纯度≥９５％）按原工艺做成控释药膜［每块重（１９．０±０．１）ｍｇ，含甲硝唑（５．５９±０．０３）ｍｇ］，置于豚鼠牙周部位及放１００μｌ生理盐水的微量板小孔中测定释放量。结果：实验表明该控释药膜能有效地降低过高峰，推迟过早峰，能在预定４８ｈ内在龈沟液持续释放相对恒定的有效浓度（２００μｇ·ｍｌ－１）。结论：３Ｈ标记甲硝唑能不断释放β射线，通过放射性探测仪器可随时追踪药物在体内的数量与位置，这在药动学和药物示踪研究中值得推广应用。OBJECTIVE: To measure the release profile of metronidazole from controlled release strip in different time phases in vivo and vitro. METHOD: Tritium labelled metronidazole (specific activity=5.44×104 Bq·mmol-1, purification ≥95%) was prepared for metronidazole controlled release strip [weight (19.0±0.1)mg, containing metronidazole (5.59±0.03)mg] according to original art. The release was measured by inserting into the periodontal site of guinea pig and 100 μl normal saline in microplate. RESULTS: The results turned out that it can decrease the superhigh peak and delay the previous peak. It can constantly release effective level about 200 μg·ml-1 metronidazole in gingival crevicular fluid within 48 h. CONCLUSION: 3 H labelled metronidazole could release β redial which could be traced the amount and location of the drug in vivo from time to time. This is a good method for development and application in pharmacokinetics and drug tracer.

关 键 词：氢3 甲硝唑 同位素 控释药膜 

分 类 号：R978.61[医药卫生—药品] R944.9[医药卫生—药学]