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采用荧光检测法,通过高效液相色谱法测定人口服或局部应用苄达明及其代谢物N -氧化物后的血浆浓度。

HPLC determination of benzydamine and its metabolite N-oxide in plasma following oral administration or topical application in man, using fluorimetric detection.

作者信息

Catanese B, Lagana A, Marino A, Picollo R, Rotatori M

出版信息

Pharmacol Res Commun. 1986 Apr;18(4):385-403. doi: 10.1016/0031-6989(86)90091-3.

DOI:10.1016/0031-6989(86)90091-3
PMID:3737653
Abstract

A method for the extraction and quantification of benzydamine and its metabolite N-oxide by liquid chromatography with fluorescence detection in plasma samples is described. This method has adequate sensitivity, specificity and is reproducible. The use of the extraction column allowed a recovery of both benzydamine and its metabolite of over 97% to be obtained. The plasma levels of benzydamine and its metabolite N-oxide were studied after oral administration as sugar-coated tablets or topical application to the vaginal mucosa as a cream to 6 healthy volunteers. After topical application, the plasma concentrations of the unchanged drug and its metabolite are lower than those obtained following oral administration. These data further stress the concept that, whenever possible, topical use should be considered the treatment of choice since, along with a more selective therapy, the incidence of systemic side effects can be considerably reduced.

摘要

描述了一种采用液相色谱-荧光检测法从血浆样本中提取并定量测定苄达明及其代谢产物N-氧化物的方法。该方法具有足够的灵敏度、特异性且可重现。使用萃取柱可使苄达明及其代谢产物的回收率均超过97%。对6名健康志愿者口服糖衣片或阴道黏膜局部涂抹乳膏形式的苄达明后,研究了其血浆水平及代谢产物N-氧化物的情况。局部涂抹后,原形药物及其代谢产物的血浆浓度低于口服给药后的浓度。这些数据进一步强调了这样一个概念,即只要有可能,应考虑将局部用药作为首选治疗方法,因为这样除了能实现更具选择性的治疗外,还可大幅降低全身副作用的发生率。

相似文献

1
HPLC determination of benzydamine and its metabolite N-oxide in plasma following oral administration or topical application in man, using fluorimetric detection.采用荧光检测法,通过高效液相色谱法测定人口服或局部应用苄达明及其代谢物N -氧化物后的血浆浓度。
Pharmacol Res Commun. 1986 Apr;18(4):385-403. doi: 10.1016/0031-6989(86)90091-3.
2
Serum levels of benzydamine following the topical use of this drug in gynecology.该药物在妇科局部使用后血清中苄达明的水平。
Clin Exp Obstet Gynecol. 1980;7(2):84-8.
3
Concentration of benzydamine in vaginal mucosa following local application: an experimental and clinical study.局部应用后苄达明在阴道黏膜中的浓度:一项实验与临床研究。
Int J Tissue React. 1987;9(2):135-45.
4
Pharmacokinetics of benzydamine after intravenous, oral, and topical doses to human subjects.苄达明在对人体受试者静脉注射、口服和局部给药后的药代动力学。
Biopharm Drug Dispos. 1991 Oct;12(7):481-92. doi: 10.1002/bdd.2510120702.
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Pharmacokinetics of benzydamine.苄达明的药代动力学。
Int J Tissue React. 1987;9(2):93-7.
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Determination of benzydamine and its N-oxide in biological fluids by high-performance liquid chromatography.高效液相色谱法测定生物流体中的苄达明及其N-氧化物
J Chromatogr. 1990 Jul 13;529(1):113-23. doi: 10.1016/s0378-4347(00)83812-8.
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Pharmacokinetics of benzydamine.苄达明的药代动力学。
Int J Tissue React. 1985;7(3):195-204.
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Human plasma metabolic profiles of benzydamine, a flavin-containing monooxygenase probe substrate, simulated with pharmacokinetic data from control and humanized-liver mice.用来自对照小鼠和人源化肝脏小鼠的药代动力学数据模拟的含黄素单加氧酶探针底物苄达明的人血浆代谢谱。
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Review of pharmacological data on benzydamine.苄达明的药理学数据综述。
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Use of topical benzydamine in gynecology.
Clin Exp Obstet Gynecol. 1981;8(3):103-10.

引用本文的文献

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Phase I Study in Healthy Women of a Novel Antimycotic Vaginal Ovule Combining Econazole and Benzydamine.一项关于结合了克霉唑和苯扎氯铵的新型抗真菌阴道栓在健康女性中的 I 期研究。
Infect Dis Obstet Gynecol. 2020 May 2;2020:7201840. doi: 10.1155/2020/7201840. eCollection 2020.
2
Benzydamine N-oxidation as an index reaction reflecting FMO activity in human liver microsomes and impact of FMO3 polymorphisms on enzyme activity.苄达明N-氧化作为反映人肝微粒体中FMO活性的指标反应以及FMO3基因多态性对酶活性的影响。
Br J Clin Pharmacol. 2000 Dec;50(6):553-61. doi: 10.1046/j.1365-2125.2000.00296.x.