快速且靈敏測定血漿中roxatidine濃度的高效液相層析法   全文下載

A Rapid and Sensitive HPLC Method for Determination of Roxatidine in Human Plasma

本研究利用高效液相層析儀搭配紫外光檢測器開發一快速且準確的roxatidine 於人類血漿中之分析方法。Roxatidine 為一選擇性第二型組織胺受器阻斷劑，roxatidine acetate 為roxatidine 之前驅藥，在口服後可於體內快速代謝為raxatidine。Roxatidine 及其內部標準品（ranitidine）乃經由固相萃取來純化，移動相之組成為20 mM 之磷酸二氫鉀（pH 7.0）與甲基氰（體積比為5:1）。Roxatidine 校正曲線之線性範圍由5 至1000 ng/mL，同日與異日之準確度與精密度皆在10% 以內，roxatidine 經固相萃取後之回收率為89.8%，最低可檢測濃度為5 ng/mL。此分析方法已成功地運用於人體口服多劑量roxatidine acetate 後血漿中roxatidine 濃度分析的預試驗。

A rapid and accurate assay for the determination of roxatidine, a selective H2-receptor blocker, in human plasma was developed. Analysis was performed by high-performance liquid chromatography (HPLC) with ultraviolet (UV) detector. Roxatidine acetate, a prodrug of roxatidine, is metabolized rapidly to roxatidine following oral administration. Roxatidine and the internal standard (ranitidine) were extracted from plasma by solid-phase extraction. The mobile phase of HPLC was consisted of 20 mM KH2PO4 (pH 7.0) and acetonitrile (5:1, v/v). The calibration curve for roxatidine was linear over the range of 5 to 1000 ng/mL. The precision and accuracy of within- and between-run were within 10% for roxatidine. The recovery of roxatidine was over 87% for both low and high concentrations (15 and 500 ng/mL) and the lower limit of quantitation (LLOQ) was 5 ng/mL. The method was successfully applied to a pilot pharmacokinetic study of roxatidine in healthy subjects.