纳米制剂中7-表多西他赛的体内外抗肿瘤作用研究
摘要
目的:研究7-表多西他赛体内外抗肿瘤活性。方法:建立动物荷瘤模型,以多西他赛为阳性对照,考察7-表多西他赛抗肿瘤活性;通过体外细胞实验,考察7-表多西他赛的毒性。结果:7-表多西他赛在动物实验中,对肿瘤有一定抑制作用,但其抑制作用弱于多西他赛;在体外细胞实验中,7-表多西他赛毒性与多西他赛相当。结论:7-表多西他赛作为多西他赛的主要杂质,毒性与多西他赛相当,抗肿瘤活性弱于多西他赛,为确保多西他赛抗肿瘤活性,应对7-表多西他赛进行含量控制。
Objective:Evaluate the anti-tumor activity of 7-epi docetaxel. Methods:Establish aninmal tumor model,research the toxicity and anti-tumor activity of 7-epi docetaxel both in vitro and vivo. Results:The toxicity of 7-epi docetaxel is similar with docetaxel and anti-tumor effect of 7-epi docetaxel is weaker than docetaxel. Conclusion:To ensure the anti-tumor effect of docetaxel,the control of 7-epi docetaxel is necessary.
Objective:Evaluate the anti-tumor activity of 7-epi docetaxel. Methods:Establish aninmal tumor model,research the toxicity and anti-tumor activity of 7-epi docetaxel both in vitro and vivo. Results:The toxicity of 7-epi docetaxel is similar with docetaxel and anti-tumor effect of 7-epi docetaxel is weaker than docetaxel. Conclusion:To ensure the anti-tumor effect of docetaxel,the control of 7-epi docetaxel is necessary.
引文
[1]Bissery MC,Nohynek G,et al.Docetaxel(Taxotere):a review of preclinical and clinical experience.Part I:Preclinical experience.Anti-cancer Drugs,1995,6(3):339-355,363-368.
[2]Lavelle F,et al.Preclinical Evaluation of Docetaxel(Taxotere).Seminars in Oncology,1995,22(2):3-16.
[3]Fujimoto-Ouchi K,Y.Tanaka,and T.Tominaga,Schedule dependency of antitumor activity in combination therapy with capecitabine/5'-deoxy-5-fluorouridine and docetaxel in breast cancer models.Clinical Cancer Research,2001,7(4):1079-1086.
[4]Musumeci T,et al.PLA/PLGA nanoparticles for sustained release of docetaxel.Int J Pharm,2006,325(1-2):172-179.
[5]Xu Z,et al.The performance of docetaxel-loaded solid lipid nanoparticles targeted to hepatocellular carcinoma.Biomaterials,2009,30(2):226-232.
[6]饶雅琨,王猛,丁黎,等.LC-MS/MS法鉴定注射用多西他赛中的有关物质[J].药学学报,2012(6):779-784.
[7]Kumar D,et al.Isolation and characterization of degradation impurities in docetaxel drug substance and its formulation.J Pharm Biomed Anal,2007,43(4):1228-1235.
[8]Artiges A,[The European directorate for the quality of medicines].Ann Pharm Fr,2001.59(1):63-68.
[9]张关敏,刘红,张艳华.抗肿瘤药的肝肾毒性及其防治[J].中国药房,2010(14):1327-1330.
[2]Lavelle F,et al.Preclinical Evaluation of Docetaxel(Taxotere).Seminars in Oncology,1995,22(2):3-16.
[3]Fujimoto-Ouchi K,Y.Tanaka,and T.Tominaga,Schedule dependency of antitumor activity in combination therapy with capecitabine/5'-deoxy-5-fluorouridine and docetaxel in breast cancer models.Clinical Cancer Research,2001,7(4):1079-1086.
[4]Musumeci T,et al.PLA/PLGA nanoparticles for sustained release of docetaxel.Int J Pharm,2006,325(1-2):172-179.
[5]Xu Z,et al.The performance of docetaxel-loaded solid lipid nanoparticles targeted to hepatocellular carcinoma.Biomaterials,2009,30(2):226-232.
[6]饶雅琨,王猛,丁黎,等.LC-MS/MS法鉴定注射用多西他赛中的有关物质[J].药学学报,2012(6):779-784.
[7]Kumar D,et al.Isolation and characterization of degradation impurities in docetaxel drug substance and its formulation.J Pharm Biomed Anal,2007,43(4):1228-1235.
[8]Artiges A,[The European directorate for the quality of medicines].Ann Pharm Fr,2001.59(1):63-68.
[9]张关敏,刘红,张艳华.抗肿瘤药的肝肾毒性及其防治[J].中国药房,2010(14):1327-1330.