SYNTHESIS OF CARBAZOLE DERIVATIVE PLX01107 AND ITS PHARMACOKINETICS FOR VARIOUS ADMINISTRATION ROUTES IN CD-1 MICE

Eremina N. V.; Kazei V. I.; Purmal A. A.; Durnev A. D.

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SYNTHESIS OF CARBAZOLE DERIVATIVE PLX01107 AND ITS PHARMACOKINETICS FOR VARIOUS ADMINISTRATION ROUTES IN CD-1 MICE

机译：咔唑衍生物PLX01107的合成及其在CD-1小鼠中的各种施用途径的药代动力学

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The substituted carbazole drug PLX01107 is being developed for the treatment of invasive pulmonary aspergillosis. A synthetic method for PLX01107 drug substance was developed in order to produce the required amount of drug substance of a quality suitable to support preclinical trials. An analytical method using HPLC-MS/MS was employed to determine the drug concentration in whole blood and internal organs. Preclinical trials of the new drug found that PLX01107 possessed linear pharmacokinetics in the i.v. dose range 5 - 20 mg/kg in CD-1 mice. Pharmacokinetic modeling determined the optimum i.v. dose regime for attaining the maximum effective concentration as a loading dose of 5 mg/kg with a maintenance dose of 5 mg/kg every 12 h. Analysis of the PLX01107 content in various organs found that lungs of test animals had the maximum concentrations after both i.v. and oral administration. This gave the developed drug a considerable advantage with respect to targeted delivery of the active ingredient.

机译：正在开发取代的咔唑药物PLX01107以治疗侵入性肺曲线症。开发了一种用于PLX01107药物的合成方法，以生产适合支持临床前试验的质量所需量的药物物质。使用使用HPLC-MS / MS的分析方法来确定全血和内器官中的药物浓度。新药的临床前试验发现PLX01107在I.V中具有线性药代动力学。剂量范围为5-20mg / kg CD-1小鼠。药代动力学建模确定了最佳I.v.剂量制度，用于获得5mg / kg的负载剂量的最大有效浓度，每12小时5mg / kg的维持剂量为5mg / kg。分析各种器官中PLX01107含量发现，检测动物的肺在I.v中具有最大浓度。和口头行政管理。这使得开发的药物相当于靶向递送的活性成分的优势。

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来源
《Pharmaceutical Chemistry Journal》 |2017年第2期|共7页
作者
Eremina N. V.; Kazei V. I.; Purmal A. A.; Durnev A. D.;
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作者单位

Russian Acad Med Sci Zakusov State Inst Pharmacol Moscow 125315 Russia;

Panacela Labs LLC Moscow 101000 Russia;

Cleveland Biolabs Inc Buffalo NY USA;

Russian Acad Med Sci Zakusov State Inst Pharmacol Moscow 125315 Russia;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
PLX01107; carbazole derivatives; synthesis; pharmacokinetics; biodistribution;

机译：PLX01107;咔唑衍生物;合成;药代动力学;生物分布;

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1. SYNTHESIS OF CARBAZOLE DERIVATIVE PLX01107 AND ITS PHARMACOKINETICS FOR VARIOUS ADMINISTRATION ROUTES IN CD-1 MICE [J] . Eremina N. V., Kazei V. I., Purmal A. A., Pharmaceutical Chemistry Journal . 2017,第2期

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SYNTHESIS OF CARBAZOLE DERIVATIVE PLX01107 AND ITS PHARMACOKINETICS FOR VARIOUS ADMINISTRATION ROUTES IN CD-1 MICE

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