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研究生:郭人華
研究生(外文):Jen-Hua Kuo
論文名稱:N-Acetyl-leucyl-leucyl-norleucinal對Etoposide在老鼠口服吸收的影響
論文名稱(外文):N-Acetyl-leucyl-leucyl-norleucinal on the Absorption of Etoposide in Rats
指導教授:蘇聖芳蘇聖芳引用關係
指導教授(外文):Sheng-Fang Su
學位類別:碩士
校院名稱:國立成功大學
系所名稱:臨床藥學研究所
學門:醫藥衛生學門
學類:藥學學類
論文種類:學術論文
論文出版年:2002
畢業學年度:90
語文別:中文
論文頁數:86
中文關鍵詞:多重抗藥性
外文關鍵詞:EtoposideALLNP-glycoproteinMDRHPLCAbsorption
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多重抗藥性(Multidrug resistance;MDR)是指癌細胞對許多功能上、結構上不盡相同的藥物產生交叉抗藥性。而原因之一是癌細胞上Pgp過度表現所造成。Etoposide為一抗腫瘤藥物,口服身體可用率變異大,亦為Pgp受質。已有實驗證實,在老鼠everted gut sacs實驗模式下ALLN可明顯增加etoposide在老鼠小腸中的吸收。本研究建立一HPLC分析法,以測定ALLN之血中濃度,來進一步探討ALLN對於etoposide在老鼠體內吸收及排除的影響。同時,探討ALLN在老鼠體內的動態。
ALLN血液檢品以dichloromethane萃取後再與2,4-dinitrophenyl- hydrazine進行衍生反應。檢量線濃度範圍由0.2-10 μg/ml呈線性關係(r>0.999),此萃取方法之回收率達65∼80﹪,最低定量極限(LOQ)為0.2 μg/ml。當靜脈IV bolus投予5 mg ALLN後,其血中濃度經時變化為biphasic。其藥動參數如下:t1/2約為30 min、AUC0∼∞為162.55 ±25.25 min*μg/ml、CLT為32.60 ±3.96 ml/min、Vss為931.93 ±125 ml。
實驗結果顯示,同時給予500 μΜ ALLN,etoposide在腸中的清除率明顯下降35%,etoposide的血中濃度也增加1.4倍。然而,ALLN對etoposide在腸道中的吸收並無明顯影響。此證明ALLN及etoposide在老鼠體內有交互作用的現象,除了Pgp的作用外,也與其它的運送子有關。
Overexpression of P-glycoprotein(Pgp)is one of causes of multidrug resistance (MDR) in chemotherapy. Etoposide, an anti-neoplastic agent with variable oral bioavailability, and a substrate of Pgp. Previous study has proved that the absorption of etoposide was significantly increased in the presence of N-acetyl-leucyl-leucyl-norleucinal (ALLN) in the rat everted gut sacs. Therefore, the effect of ALLN on the absorption and exsorption of etoposide in vivo were assessed in the current study. In addition, the HPLC analytical method was established to determined the ALLN plasma concentration and further to investigate the pharmacokinetics of ALLN in rats.
ALLN plasma samples were extracted with dichloromethane and were derivatized with 2,4-dinitrophenylhydrazine. The analytical method was specific and linear the range of 0.2-10 μg/ml (r>0.999). No endogenous substances were found to interfere. The recovery of ALLN was in the range of 65-80%. The detection limit was 0.2 μg/ml. After intravenous administration of 5 mg ALLN, the kinetic of concentration-time profile was biphasic. The pharmacokinetic parameters of ALLN:t1/2 =30 min, AUC0∼∞=162.55 ±25.25 min*μg/ml, CLT=32.60 ±3.96 ml/min, Vss=931.93 ±125 ml.
The result from the in vivo exsorption study showed that the etoposide intestinal clearance was significantly decreased by 35% and the serum etoposide concentration also increased by 1.5 times in the presence of 500 μM ALLN. However, no significant difference was observed in the intestinal absorption of etoposide by the addition of 500 μM ALLN in the in vivo absorption study. The result of the current study suggests that drug interaction betweent ALLN and etoposide occurs in rats. Transporters other than Pgp might be involved in the drug interaction.
中文摘要 I
Abstract II
誌謝 III
目錄 IV
圖目錄 VI
表目錄 VIIII
縮寫表 IX
第一章 緒論 1
第一節 多重抗藥性(Multidrug resistance;MDR) 1
第二節 P-glycoprotein(Pgp) 4
第三節 Etoposide 7
第四節 MDR調控劑(modulator) 9
第五節 N-acetyl-leucyl-leucyl-norleucinal(ALLN) 12
第二章 研究目的 20
第三章 實驗材料、儀器及方法 21
第一節 材料 21
第二節 儀器 23
第三節 實驗方法 26
第四章 實驗結果 42
第一節 ALLN分析方法之確效 42
第二節 ALLN於老鼠體內之藥物動力學 43
第三節 In vivo etoposide的排出 43
第四節 In vivo etoposide的吸收 44
第五章 討論 58
參考文獻 62
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