頁籤選單縮合
題名 | Plasma and Red Blood Cell Disposition Kinetics of Delavirdine in Rats |
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作者 | 鄭靜玲; | 書刊名 | 中華藥學雜誌 |
卷期 | 53:5 2001.10[民90.10] |
頁次 | 頁269-279 |
分類號 | 414.33 |
關鍵詞 | Delavirdine; Disposition; RBC plasma partitioning; Non-nucleoside reverse transcriptase inhibitor; HIV-1; AIDS; |
語文 | 英文(English) |
英文摘要 | Delavirdine mesylate is a non-nucleoside reverse transcriptase inhibitor of HIV-1 used in AIDS therapy. The objectives of this study were to investigate the plasma and red blood cell (RBC) disposition kinetics of delavirdine in rats and to explore the RBC/plasma partitioning characteristics of delavirdine. Rats were given a relatively low bolus dose of delavirdine mesylate (0.45 mg/kg) via the jugular vein and blood samples were collected. The concentrations of delavirdine in plasma and RBCs were analyzed by HPLC. The plasma concentration-time profile for delavirdine showed typical monoexponential disposition features with an elimination half-life (t1/2) of 36.7 min. The steady-state volume of distribution (Vss), and clearance (Cl) were 1.22 L/kg and 23.6 mL/min/kg, respectively. The RBC concentration-time curve declined in parallel with that for plasma, albeit at a much lower magnitude. The mean value of the partition coefficient between RBC and plasma (Kep) for delavirdine was 0.25, and showed no trends over time or concentration-dependency. The results indicated that delavirdine is rapidly and widely distributed into RBCs and extravascular tissues. Although delavirdine binds strongly to plasma proteins and partitions into RBC, it is highly extracted and exhibits one-compartmental disposition characteristics in plasma and RBC. |
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