本文選題：藥用高分子輔料 + 細胞毒性��； 參考：《海峽藥學(xué)》2016年03期

【摘要】：目的通過細胞與動物實驗,比較聚乙二醇1000維生素E琥珀酸酯(TPGS1000)、普朗尼克(F127)、單甲氧基聚乙二醇外消旋聚乳酸兩嵌段共聚物(m PEG-PLA)及其三嵌段共聚物(PLA-PEG-PLA)、外消旋聚乳酸乙醇酸三嵌段共聚物(PLGA-PEG-PLGA)5種常用藥用高分子輔料的體內(nèi)外毒性,為選擇安全有效的藥用輔料提供實驗依據(jù)。方法采用CCK-8法檢測以上5種常用高分子藥用輔料對人臍靜脈內(nèi)皮細胞HUVEC和人肝癌細胞Bel-7402的毒性;采用動物毒性試驗方法初步觀察5種輔料對小鼠的毒性反應(yīng)。結(jié)果 TPGS在5種輔料中對細胞的毒性作用較強,其余4種輔料在1mg·m L~(-1)幾無毒性表現(xiàn),僅在5mg·m L~(-1)劑量下才表現(xiàn)出低毒。體內(nèi)毒性實驗中,TPGS的LD50約為500mg·kg~(-1),其他輔料在各劑量組小鼠均未出現(xiàn)明顯毒性現(xiàn)象或死亡。結(jié)論體內(nèi)外毒性試驗結(jié)果提示:藥用高分子輔料具有一定的毒性作用,將TPGS用作藥用高分子輔料時,需特別考慮其用量,以確保新劑型的安全性;其他4種輔料在相同劑量下未表現(xiàn)出明顯毒性,是比較安全的藥用輔料。
[Abstract]:Objective through cell and animal experiments, Five kinds of polyethyleneglycol 1000 vitamin E succinic acid triblock copolymers (PLGA-PEG-PLAX, PLGA-PEG-PLGAA), Poly (ethylene glycol) triblock copolymers (PLGA-PEG-PLGAA), poly (ethylene glycol) (PEG-PEG-PLA), poly (glycolic acid) triblock copolymers (PLGA-PEG-PLGAA) were compared. In vivo and in vitro toxicity of polymer excipients for drug use, To provide experimental basis for the selection of safe and effective pharmaceutical excipients. Methods CCK-8 method was used to detect the toxicity of the above five kinds of macromolecule medical excipients to human umbilical vein endothelial cells (HUVEC) and human hepatoma cells (Bel-7402), and the animal toxicity test method was used to observe the toxicity of the five kinds of excipients to mice. Results the cytotoxicity of TPGS was stronger in the five kinds of excipients. The other four excipients showed little toxicity in 1mg mLL ~ (-1), but low toxicity only in the dosage of 5mg m L ~ (-1). In vivo toxicity test, the LD50 of LD50 was about 500mg KG-1, other excipients did not appear obvious toxic phenomenon or death in each dose group of mice. Conclusion the results of in vivo and in vitro toxicity tests suggest that medicinal polymer excipients have certain toxic effects, and the dosage of TPGS should be taken into account in order to ensure the safety of the new dosage form. The other four kinds of excipients showed no obvious toxicity at the same dose, and were relatively safe for medicinal excipients.
【作者單位】： 福建中醫(yī)藥大學(xué)藥學(xué)院;福建衛(wèi)生職業(yè)技術(shù)學(xué)院藥學(xué)系;
【基金】：國家衛(wèi)計委科研項目(WKJ-FJ-06) 福建省中醫(yī)藥科研課題(wzzy201307) 福建衛(wèi)生職業(yè)技術(shù)學(xué)院科研啟動資助項目(2013-1-1)
【分類號】：R96

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