The fat nano-emulsion, which has been used as a drug carrier, especially for the poorly water soluble drug, has drawn favorable attention recently. Ubenimex is a poorly soluble drug with no parenteral treatment availa...The fat nano-emulsion, which has been used as a drug carrier, especially for the poorly water soluble drug, has drawn favorable attention recently. Ubenimex is a poorly soluble drug with no parenteral treatment available for patients. This study was aimed at the manufacture of a ubenimex loaded fat nano-emulsion for intravenous delivery by SolEmuls~ technology. The formulation and the process parameters were optimized by single-factor design and the obtained ubenimex loaded fat nano-emulsion was stable even after autoclaving. The average particle size was near 200 nm with narrow size distribution and a negative zeta potential of -44 mV. The in vitro release behavior of ubenimex from the fat nano-emulsion could be described by the double phase kinetics model and expressed by the following equation： 100 - Q = 75.27e^-0.369t ＋ 15.94e^-0.0324t, Rα = 0.9863, Rβ = 0.9878. The pharmacokinetic study showed that the pharmacokinetic curves of both the ubenimex fat nano-emulsion and the i.v. ubenimex suspension, were similar and the main parameters showed no significant difference except t1/2. In conclusion, the fat nano-emulsion with ubenimex has potential as a safe and effective parenteral delivery system for poorly water soluble anti-cancer drugs.展开更多
目的:系统评价乌苯美司联合化疗用于恶性肿瘤的疗效和安全性,为临床提供循证参考。方法:计算机检索Central、PubMed、中国期刊全文数据库、中文科技期刊数据库、万方数据库,收集乌苯美司联合化疗(试验组)对比单纯化疗(对照组)用于恶性...目的:系统评价乌苯美司联合化疗用于恶性肿瘤的疗效和安全性,为临床提供循证参考。方法:计算机检索Central、PubMed、中国期刊全文数据库、中文科技期刊数据库、万方数据库,收集乌苯美司联合化疗(试验组)对比单纯化疗(对照组)用于恶性肿瘤的随机对照试验(RCT),筛选文献、提取资料并采用Cochrane系统评价员手册5.1.0提供的偏倚风险评价标准评价纳入研究质量,采用Rev Man 5.3统计软件进行Meta分析。结果:共纳入12项RCT,包括762例患者。Meta分析结果显示,试验组患者近期有效率[RR=1.24,95%CI(1.08,1.43),P=0.002]、生存质量(KPS)评分改善率[RR=1.69,95%CI(1.46,1.95),P<0.001]显著高于对照组,胃肠道毒性发生率[RR=0.74,95%CI(0.57,0.94),P=0.02]和白细胞抑制发生率[Ⅰ°～Ⅳ°(用药≤3个月):RR=0.54,95%CI(0.37,0.79),P=0.002;Ⅲ°～Ⅳ°:RR=0.44,95%CI(0.29,0.68),P<0.001]显著低于对照组,差异均有统计学意义。结论:乌苯美司联合化疗用于恶性肿瘤,可以提高患者的近期疗效,改善生存质量,降低胃肠道毒性和骨髓毒性。展开更多
基金Shandong Province Natural Science Foundation (Grant No.ZR2009CM011)
文摘The fat nano-emulsion, which has been used as a drug carrier, especially for the poorly water soluble drug, has drawn favorable attention recently. Ubenimex is a poorly soluble drug with no parenteral treatment available for patients. This study was aimed at the manufacture of a ubenimex loaded fat nano-emulsion for intravenous delivery by SolEmuls~ technology. The formulation and the process parameters were optimized by single-factor design and the obtained ubenimex loaded fat nano-emulsion was stable even after autoclaving. The average particle size was near 200 nm with narrow size distribution and a negative zeta potential of -44 mV. The in vitro release behavior of ubenimex from the fat nano-emulsion could be described by the double phase kinetics model and expressed by the following equation： 100 - Q = 75.27e^-0.369t ＋ 15.94e^-0.0324t, Rα = 0.9863, Rβ = 0.9878. The pharmacokinetic study showed that the pharmacokinetic curves of both the ubenimex fat nano-emulsion and the i.v. ubenimex suspension, were similar and the main parameters showed no significant difference except t1/2. In conclusion, the fat nano-emulsion with ubenimex has potential as a safe and effective parenteral delivery system for poorly water soluble anti-cancer drugs.
文摘目的:系统评价乌苯美司联合化疗用于恶性肿瘤的疗效和安全性,为临床提供循证参考。方法:计算机检索Central、PubMed、中国期刊全文数据库、中文科技期刊数据库、万方数据库,收集乌苯美司联合化疗(试验组)对比单纯化疗(对照组)用于恶性肿瘤的随机对照试验(RCT),筛选文献、提取资料并采用Cochrane系统评价员手册5.1.0提供的偏倚风险评价标准评价纳入研究质量,采用Rev Man 5.3统计软件进行Meta分析。结果:共纳入12项RCT,包括762例患者。Meta分析结果显示,试验组患者近期有效率[RR=1.24,95%CI(1.08,1.43),P=0.002]、生存质量(KPS)评分改善率[RR=1.69,95%CI(1.46,1.95),P<0.001]显著高于对照组,胃肠道毒性发生率[RR=0.74,95%CI(0.57,0.94),P=0.02]和白细胞抑制发生率[Ⅰ°～Ⅳ°(用药≤3个月):RR=0.54,95%CI(0.37,0.79),P=0.002;Ⅲ°～Ⅳ°:RR=0.44,95%CI(0.29,0.68),P<0.001]显著低于对照组,差异均有统计学意义。结论:乌苯美司联合化疗用于恶性肿瘤,可以提高患者的近期疗效,改善生存质量,降低胃肠道毒性和骨髓毒性。
