崔景斌, 奚念朱, 蒋新国. 安乃近代谢物4-甲氨基安替比林的HPLC测定及其鼻腔滴剂在人体的相对生物利用度J. 药学学报, 1997, 32(1): 65-68.
引用本文: 崔景斌, 奚念朱, 蒋新国. 安乃近代谢物4-甲氨基安替比林的HPLC测定及其鼻腔滴剂在人体的相对生物利用度J. 药学学报, 1997, 32(1): 65-68.
JB Cui, NZ Xi , XG Jiang, . STUDIES ON HPLC METHOD FOR DETERMINATION OF 4-METHYLAMINOANTIPYRINE AND RELATIVE BIOAVAILABILITIES OF ANALGIN NASAL DROPS IN HUMAN VOLUNTEERSJ. Acta Pharmaceutica Sinica, 1997, 32(1): 65-68.
Citation: JB Cui, NZ Xi , XG Jiang, . STUDIES ON HPLC METHOD FOR DETERMINATION OF 4-METHYLAMINOANTIPYRINE AND RELATIVE BIOAVAILABILITIES OF ANALGIN NASAL DROPS IN HUMAN VOLUNTEERSJ. Acta Pharmaceutica Sinica, 1997, 32(1): 65-68.

安乃近代谢物4-甲氨基安替比林的HPLC测定及其鼻腔滴剂在人体的相对生物利用度

STUDIES ON HPLC METHOD FOR DETERMINATION OF 4-METHYLAMINOANTIPYRINE AND RELATIVE BIOAVAILABILITIES OF ANALGIN NASAL DROPS IN HUMAN VOLUNTEERS

  • 摘要: 安乃近进入血液后,迅速、完全地被代谢为4-甲氨基安替比林(MAA),血浆中检测不出安乃近原型药,故血浆MAA水平可反映安乃近的吸收情况。本文建立了MAA的HPLC测定法,并用于安乃近鼻腔滴剂人体内药代动力学和肌内注射剂及口服片剂的相对生物利用度研究。结果表明鼻腔滴剂较口服片剂吸收快,较肌内注射剂生物利用度高。

     

    Abstract: A new HPLC method for the determination of a metabolite of analgin, MAA (4 methylaminoantipyrine), in plasm and its application to determine the bioavailabilities of analgin nasal drops in human volunteers is reported in this paper. A Waters Model 481 instrument was used throughout the experiment. IAA (isopropylaminoantipyrine) was shown to be the most suitable internal standard at absorption wavelength of 254 nm. A mixture of phosphate buffer (pH 5.5) and methanol (68∶32) was used as the mobile phase with a flow rate of 2 ml·min-1, and YWG-C18 H37 as stationary phase. Calibration curve was linear (γ=0.9998) in the concentration range of 0.1~5 μg·ml-1. The within day and day to day precision (RSD) of this method were 2.35% and 2.61%, respectively, with average recoveries of 99.3%~103.9%. No interference was found in the body fluid. The plasma samples of healthy volunteers were treated with acid and extracted with ether. The system of mobile phase and the process of blood sample treatment were simpler than those reported in literature. So, the method is suitable for the study of pharmacokinetics and clinical determination of blood level of analgin. The studies on bioavailabilities of analgin nasal drops were carried out in 8 men relative to intramuscular injection and 6 men relative to oral tablets, respectively, at the dose of 250 mg analgin in different preparations administered by cross over method. The main pharmacokinetic parameters were shown in Table 3. The results indicate that analgin nasal drops exhibited a higher bioavailability (relative to injection) and faster absorption (relative to tablet). So, analgin is suitable to be developed as a nasal preparation.

     

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