红细胞作为吗啡载体延长吗啡镇痛时效的研究(英文)

Study of Erythrocyte as Carrier to Prolong Action Duration of Morphine

探讨用高渗法制备红细胞包蔽吗啡溶液(RBC-M)的可行性,对RBC-M制备过程中红细胞(RBC)的体积和形态的变化、RBC-M溶液内外的吗啡(M)浓度及含量的变化以及择期上腹部手术患者应用RBC-M溶液术后镇痛的时效和吗啡的血药浓度进行了研究.研究发现:(1)用高渗法制备红细胞包蔽吗啡溶液是可行的.(2)RBC-M溶液与单纯M溶液相比其术后镇痛作用显著延长;其药代动力学指标消除半衰期(T1/2)延长3倍多,曲线下面积(AUC0→∞)增加约11倍,而清除率(CL)明显减小约9倍.(3)用RBC-M溶液行术后镇痛的患者其时效明显优于单纯用吗啡的患者.

In order to study the feasibility of using intact erythrocytes (RBCs) as morphine (M) carriers to prolong its duration of action in vivo, we investigated the changes on the total volume and the shapes of RBCs during the process of preparing RBC-M solutions, the concentrations of morphine both inside and outside the RBCs, as well as the clinical analgesic effects and pharmacokinetic parameters of RBC-M solutions in patients undergoing selective upper abdominal surgeries. We found that: (1) ideal RBC-M solutions with a high encapsulating rate could be obtained by hyperosmotic method, (2) compared with plain morphine solution, the RBC-M solution had a long potent.duration as postoperative analgesia and its T1/2, AUC0→∞ were longer; CL was significantly decreased, (3) The VAS in postoperative 24 h was significantly lower in group RBC-M than that in group M.