摘要
目的：研究硫酸吗啡控释片（ＣＲＭＳ）和即刻释放片（ＩＲＭＳ）在中国癌痛患者中多次给药后的稳态血药浓度，其波动性及与临床疗效的相关性。方法：１７例癌症病人，随机ｐｏＣＲＭＳ或ＩＲＭＳ７ｄ，用ＧＣＭＳ测定服药第５，６，７天吗啡血药浓度的峰谷水平。同时观察记录临床镇痛效果，计算各日各时点的疼痛缓解率和中度以上疼痛缓解率。结果：癌症病人连续给药４ｄ后，血药浓度达稳态，ＣＲＭＳ和ＩＲＭＳ的峰浓度分别为（２７．４３±０．３３）ｎｇ·ｍｌ－１，（２２．６８±０．１６）ｎｇ·ｍｌ－１；谷浓度分别为（１９．４５±１．４４）ｎｇ·ｍｌ－１，（１８．１４±０．４９）ｎｇ·ｍｌ－１，波动系数分别为（３４．４３±２２．１２）％，（２３．８２±７．２９）％。临床镇痛效果观察表明，第５天各时点中度以上疼痛缓解率ＣＲＭＳ与ＩＲＭＳ均为１００％。结论：ＣＲＭＳ和ＩＲＭＳ的血药浓度在第４天已达稳态，并出现良好的临床镇痛效应，两种制剂的波动系数无显著性差异。
OBJECTVE: To study the steady state plasma concentration of two formulations of morphine sulphate in Chinese cancer patients after multiple doses and their relations with clinical analgesic effect. METHODS: 17 cancer patients were randomly given 30 mg controlled release morphine sulphate (CRMS) every 12 h or 10 mg immediate release morphine sulphate (IRMS) every 4 h for 7 days. The concentration of morphine in plasma was measured by GC MS. At the same time, clinical analgesic effect was observed. RESULTS: Steady state plasma concentration was achieved after morphine was continuously given for 4 days. c max , c min , the fluctuation index (FI) of CRMS and IRMS were (27.43± 0.33 )ng·ml -1 and (22.68±0.16)ng·ml -1 ; (19.45±1.44)ng·ml -1 and (18.14±0.49)ng·ml -1 ; (34.43± 22.12 )% and (23.82±7.29)%, respectively. The effective analgesic rate (sum of rates of grade 2～4 pain relief) of both CRMS and IRMS on the 5th day medication was 100%. CONCLUSIONS: There was no significant difference in FI of CRMS and IRMS. The satisfied analgesic effect was observed at the steady state concentration of morphine in cancer patients with moderate or severe pain.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1997年第6期356-359,共4页
Chinese Pharmaceutical Journal
关键词
硫酸吗啡
控释片
镇痛
GC-MS
癌性疼痛
controlled release morphine sulphate tablet, analgesic effect, GC MS
