高效液相色谱法测定吲哚美辛控释胶囊的血药浓度和生物利用度

Determination of Plasma Drug Concentration and Bioavailability of Indomethacin Controlled Release Capsule by High Performance Liquid Chromatography

采用ＯＤＳ柱，甲醇－稀磷酸溶液（７６２４）为流动相，２６０ｎｍ为检测波长，建立了测定血浆中吲哚美辛浓度的高效液相色谱法，并测定了吲哚美辛控释胶囊炎痛康的血药浓度。结果表明，血浆中吲哚美辛浓度在０．１２５～５．０ｍｇ／Ｌ范围内线性关系良好（ｒ＝０．９９９６），检测限６２．５μｇ／Ｌ（Ｓ／Ｎ＝３１），平均回收率为１００．４％，日内和日间ＲＳＤ均小于５％。１１位受试者单剂量口服炎痛康后的相对生物利用度为１０２．３８％。

A simple, rapid, sensitive and accurate reversedphase high performance liquid chromatographic (RPHPLC) method for the determination of indomethacin in plasma is established. To 1mL of plasma were added 200μL of amobarbitone solution (internal standard; 1g/L), 100μL of phosphate buffer solution (pH 70), 100150mg of sodium chloride and 2.5mL of ethyl acetate. The mixture was vortexmixed for 10 min and centrifuged at 3 000 r/min for 5min. The organic layer was evaporated to dryness at 50℃ on waterbath and the residue was dissolved in methanol(100μL). A 20μL portion of the resulting solution was analysed by HPLC on a column (25cm×4.6mm) of μBondapak C 18 (10μm) with 76% methanol in 0.035mol/L phosphoric acid (pH 5.5) aqsolution as mobile phase (1mL/min) and UV detection at 260nm. The column temperature was 30℃ Within the range of 0.12550mg/L of indomethacin there was a good linearity (r=0.999 6). The mean recovery of indomethacin was 100.4%. The detectable limit was 62.5μg/L(S/N=3∶1) The within day and daytoday RSD were less than 5% at three drug levels. This method has been used to determine plasma drug concentration and bioavailability of indomethacin controlled release capsule for healthy volunteers 〖KH*2D]