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[摘要]
目的 以泊洛沙姆407作为载体材料制备蟾酥缓释注射液,并评价其在体内局部麻醉作用效果。方法 采用冷溶法制备蟾酥缓释注射液,以胶凝温度为指标筛选蟾酥缓释注射液最佳处方,采用豚鼠皮丘模型比较蟾酥缓释注射液和蟾酥溶液局部麻醉作用时间。结果 蟾酥缓释注射液的最佳处方是泊洛沙姆407 15.5%、乙醇10%、蟾酥提取物0.5%,胶凝温度在33 ℃,体内局部麻醉作用时间可达6~7 h,而蟾酥溶液麻醉作用时间仅为2~3 h。结论 蟾酥缓释注射液是一种长效制剂。
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[Abstract]
Objective To prepare the sustained-release injection of Venenum Bufonis using Poloxamer 407 as the carrier material and evaluate its local anesthetic activity in vivo. Methods The sustained-release injection of Venenum Bufonis was prepared through cold-dissolving and the optimal prescription was screened by determining gelation temperature. With the guinea-pig cutaneous wheal model, the local anesthetic time of the sustained-release injection was compared with the solution of Venenum Bufonis. Results The optimal prescription was composed of 15.5% Poloxamer 407, 10% alcohol, and 0.5% Venenum Bufonis extracts at the gelation temperature of 33 ℃. In vivo study, the local anesthetic effect of the sustained-release injection of Venenum Dufonis lasted for 6—7 h whereas the solution of Venenum Bufonis only lasted for 2—3 h. Conclusion The sustained-release injection of Venenum Bufonis is proved to be a prolonged action preparation.
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