摘要
目的研究硫酸吗啡栓在中、晚期癌痛患者体内多次给药后的药动学特性。方法16名符合入选条件的中、晚期癌痛患者按入组顺序随机分组,每组8人接受一个剂量(10或20mg)的多次给药试验,每隔8h给药1次,连续给药13次。采用高效液相色谱-串联质谱(HPLC-MS/MS)测定血药浓度。结果多次给予硫酸吗啡栓10mg后,主要药动学参数分别为:ρmax为(19.28±6.77)μg·L-1;tmax为(0.91±0.50)h,AUCss为(70.79±16.34)μg·h·L-1,ρav为(8.85±2.04)μg·L-1,DF为(145.4±48.31)%;多次给予硫酸吗啡栓20mg后,主要药动学参数分别为:ρmax为(36.76±15.02)μg·L-1;tmax为(1.56±1.09)h;AUCss为(189.81±111.44)μg·h·L-1,ρav为(23.73±13.93)μg·L-1,DF为(108.64±51.40)%。试验过程中,各项检查未见异常,未见不良反应发生。结论该药在试验剂量下具有良好的安全性;对各组药动学参数进行方差分析,各组药动学参数间未显示性别差异。
OBJECTIVE To evaluate the pharmacokinetics of multiple doses of morphine sulfate suppository in cancer patients with moderate and severe pain. METHODS Sixteen cancer patients received multiple doses of 10 or 20 mg morphine sulfate suppository in a randomized open study. The serum concentrations were detected by HPLC-MS/MS. RESULTS The main pharmacokinetic parameters of 10 mg morphine sulfate suppository were as follows： ,Omax （19.28±6.77） μg·L^-1; tmax（0.91±0.50）h, AUCss（70.79±1 6.34）μg·h·L^-1, Pav（8.85±2.04）μg·L^-1, DF（145.4±48.31）%. The main pharmacokinetic parameters of 20 mg morphine sulfate suppository were as follows： ρmax（36.76±15.02）μg ·L^-1, tmax（1.56±1.09）h, AUCss（189.81±111.44） μg·h·L^-1, ρav（23.73±13.93）μg·L^-1, DF（108.64±51.40）%. All the results of lab test before and after drug administration were normal. CONCLUSIONS he preparation is safe at the dose of 10 and 20 mg. The ANOVA analysis of the pharmacokinetic parameters show no differences between male and female volunteers.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2009年第14期1101-1104,共4页
Chinese Pharmaceutical Journal
