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氟比洛芬酯在子宫肌瘤的靶向分布及对前列腺素E2的影响
黄文莺1,陈莉2,王长连1*,龚世菊1,陈雄刚2
0
(1. 福建医科大学附属第一医院药学部, 福州 350005;
2. 福建医科大学附属第一医院麻醉科, 福州 350005
*通信作者)
摘要:
目的 探讨氟比洛芬酯(FA)在子宫肌瘤的靶向分布及对前列腺素E2(PGE2)的影响。 方法 选择ASAⅠ~Ⅱ级择期子宫肌瘤切除术女性患者40例,随机分为空白对照组及3个不同剂量FA给药组,每组10例。4组病例分别于手术切皮前15 min静脉注射生理盐水或0.5、1.0、1.5 mg/kg FA。手术切取肿瘤组织及正常组织并记录取材时间。采用HPLC法检测两种组织中FA活性代谢物氟比洛芬(FP)浓度,采用ELISA法检测两种组织中PGE2浓度。 结果 空白对照组两种组织均未能检测到FP。0.5、1.0、1.5 mg/kg FA给药组肿瘤组织中FP浓度随FA给药剂量的增加呈现增高趋势,组间比较差异有统计学意义(P <0.05);而正常组织中FP浓度在3组间两两比较差异均无统计学意义。3个FA给药组肿瘤组织中FP浓度均高于正常组织,差异有统计学意义(P <0.01)。随着FA给药剂量的增加,肿瘤组织中PGE2浓度呈现下降趋势,1.0、1.5 mg/kg FA给药组同空白对照组比较差异有统计学意义(P <0.01),但0.5 mg/kg FA给药组同空白对照组比较差异无统计学意义。4组病例肿瘤组织中PGE2浓度均高于正常组织,差异有统计学意义(P <0.01)。4组病例正常组织中PGE2浓度两两比较差异均无统计学意义。 结论 氟比洛芬酯在子宫肌瘤中具有一定的靶向分布并可降低子宫肌瘤中PGE2水平。
关键词:  氟比洛芬酯  氟比洛芬  子宫肌瘤  前列腺素E2
DOI:10.3724/SP.J.1008.2015.00914
投稿时间:2015-04-09修订日期:2015-07-03
基金项目:福建省科学技术厅重大项目(2008Y035).
Targeted distribution of flurbiprofen axetil in hysteromyoma and its influence on prostaglandin E2
HUANG Wen-ying1,CHEN Li2,WANG Chang-lian1*,GONG Shi-ju1,CHEN Xiong-gang2
(1. Department of Pharmacy, The First Affiliated Hospital of Fujian Medical University, Fuzhou 350005, Fujian, China;
2. Department of Anesthesiology, The First Affiliated Hospital of Fujian Medical University, Fuzhou 350005, Fujian, China
*Corresponding author)
Abstract:
Objective To explore the targeted distribution of flurbiprofen axetil (FA) in hysteromyoma and its influence on prostaglandin E2 (PGE2). Methods A total of 40 female patients undergoing myomectomy (ASAⅠ-Ⅱ) were enrolled in the present study. The patients were randomly divided into blank control group and FA groups of three different doses. The four groups were injected with normal saline, 0.5, 1, or 1.5 mg/kg of FA 15 min before the operation. Tumor tissues and normal tissues were collected by surgical operation and the sampling time was recorded. The concentration of flurbiprofen (FP), which was the active metabolite of FA, was detected in the tumor tissues and normal tissues by HPLC. The concentrations of PGE2 were detected by ELISA in the two samples. Results FP was not detected in the tumor tissues or normal tissues of the blank group. With the increase of FA dose in the three groups, the concentration of FP had an increasing tendency in the tumor tissues, with significant differences found among the three groups (P <0.05), but not in the normal tissues (P >0.05).The concentrations of FP in the tumor tissues were significantly higher than those in the normal tissue in the three FA groups (P <0.01).With the increase of FA dose, the concentration of PGE2 had a tendency to decrease in the tumor tissues; and there were significant differences between blank group and 1, 1.5 mg/kg FA groups (P <0.01), not between blank group and 0.5 mg/kg FA group. The concentrations of PGE2 in the tumor tissues were significantly higher than those in the normal tissues in the four groups (P <0.01), and there were no significant differences in pairwise comparisons in the normal tissues among the four groups (P >0.05). Conclusion FA has a certain targeted distribution in hysteromyoma and can reduce the level of PGE2.
Key words:  flurbiprofen axetil  flurbiprofen  hysteromyoma  prostaglandin E2