摘要
目的 研究盐酸利多卡因缓释胶丸 (简称缓释胶丸 )的动物药代动力学。方法 用高效液相色谱分别测定缓释胶丸的释药动力学、血药浓度及组织分布浓度。结果 家兔皮下植入缓释胶丸 40mg·kg-1·丸 -1·只 -1后第 3 60min ,仍有近 1/ 3残留率。缓释胶丸 2 0、40和 80mg·kg-13组的Ta1/2 分别比对照组 (盐酸利多卡因水溶液 10mg·kg-1皮下浸润注射 )明显延长 ;Te1/2 与对照组接近 ;随着剂量增大 ,缓释比提高 ,Tr1/2 明显延长。缓释胶丸 3组的Tmax比对照组明显延长 ,40mg·kg-1组的Cmax比对照组还低 ,80mg·kg-1组的Cmax接近或达到人的中毒浓度。大鼠皮下植入缓释胶丸 40mg·kg-1后 ,局部皮肤组织的药物浓度明显升高 ,肝脏中较低 ,肾脏中较高。结论 皮下植入缓释胶丸能使局部组织内利多卡因保持长时间、高浓度 。
AIM To investigate animal pharmacokinetics of lidocaine hydrochloride slow released gelatin pill (slow released gelatin pill). METHOD The release drug kinetics, blood concentration and tissue distributing concentration of slow released gelatin pill were separately determined with the high performance liquid chromatography. RESULT At the 360 min after implanting slow released gelatin pill, 40 mg·kg -1 , below the rabbit skin, the remaining rate of drug still were near 1/3. T a 1/2 of the groups 20, 40 and 80 mg·kg -1 slow released gelatin pill were longer than the control group (water solution of lidocaine hydrochloride 10 mg·kg -1 infiltrating injection below the skin). T e 1/2 of theirs approach to the control group. Along with increasing dosage, their slow released ratios were elevated and their T r 1/2 were strikingly prolonged. T max of theirs were strikingly increased than the control group. C max of slow released gelatin pill of group 40 mg·kg -1 was lower than the control group and that of group 80 mg·kg -1 approached or achieved hominine toxic concentration. After implanting slow released gelatin pill, 40 mg·kg -1 , below rat skin, drug concentration was strikingly increased in local skin tissue, lower in lever and higher in kidneys. CONCLUSION The implanting slow released gelatin pill below skin can keep longer time and higher concentration within local tissue, and obtain satisfied incision analgesic effect of local anesthesia after operation.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2002年第6期700-703,共4页
Chinese Pharmacological Bulletin
关键词
缓释胶丸
利多卡因
血药浓度
药代动力学
镇痛
lidocaine hydrochloride, slow released, pharmacokinetics, analgesia
