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更新于：2025-05-07

Croconazole Hydrochloride

盐酸氯康唑

更新于：2025-05-07

概要

基本信息

药物类型

小分子化药

别名

Croconazole hydrochloride (JP17)、Pilzcin

靶点

CYP2C9

作用方式

抑制剂

作用机制

CYP2C9抑制剂(细胞色素P450家族成员2C9抑制剂)

治疗领域

感染皮肤和肌肉骨骼疾病

在研适应症-

非在研适应症

念珠菌病真菌病花斑癣

原研机构-

在研机构-

非在研机构-

权益机构-

最高研发阶段撤市

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C18H16Cl2N2O

InChIKeyLWJUIYYIILPRRI-UHFFFAOYSA-N

CAS号77174-66-4

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关联

100 项与盐酸氯康唑相关的临床结果

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100 项与盐酸氯康唑相关的转化医学

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100 项与盐酸氯康唑相关的专利（医药）

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项与盐酸氯康唑相关的文献（医药）

2021-02-02·Analytical Chemistry1区 · 化学

Fabric-Phase Sorptive Membrane Array As a Noninvasive In Vivo Sampling Device For Human Exposure To Different Compounds

1区 · 化学

Article

作者: Ulusoy, Songul ; Santavenere, Francesco ; Rossi, Sandra ; Ulusoy, Halil I. ; Bassotti, Elisa ; Tartaglia, Angela ; Locatelli, Marcello ; Furton, Kenneth G. ; Savini, Fabio ; Merone, Giuseppe M. ; Rosato, Enrica ; Kabir, Abuzar ; D’Ovidio, Cristian

This study introduces an innovative device for the noninvasive sampling and chromatographic analysis of different compounds present in exhaled breath aerosol (EBA). The new sampling device, especially in light of the recent COVID-19 pandemic that forced many countries to impose mandatory facemasks, allows an easy monitoring of the subject's exposure to different compounds they may come in contact with, actively or passively. The project combines the advantages of a fabric-phase sorptive membrane (FPSM) as an in vivo sampling device with a validated LC-MS/MS screening procedure able to monitor more than 739 chemicals with an overall analysis time of 18 min. The project involves the noninvasive in vivo sampling of the EBA using an FPSM array inserted inside an FFP2 mask. The study involved 15 healthy volunteers, and no restrictions were imposed during or prior to the sampling process regarding the consumption of drinks, food, or drugs. The FPSM array-LC-MS/MS approach allowed us to effectively exploit the advantages of the two complementary procedures (the convenient sampling by an FPSM array and the rapid analysis by LC-MS/MS), obtaining a powerful and green tool to carry out rapid screening analyses for human exposure to different compounds. The flexible fabric substrate, the sponge-like porous architecture of the high-efficiency sol-gel sorbent coating, the availability of a large cache of sorbent coatings, including polar, nonpolar, mixed mode, and zwitterionic phases, the easy installation into the facemask, and the possibility of sampling without interrupting regular activities provide FPSMs unparalleled advantages over other sampling techniques, and their applications are expected to expand to many other clinical or toxicological studies.

2020-10-01·AAPS PharmSciTech3区 · 医学

A Novel Nanoemulsion Intermediate Gel as a Promising Approach for Delivery of Itraconazole: Design, In Vitro and Ex Vivo Appraisal

3区 · 医学

Article

作者: Mansour, Heba F ; Hussein, Amal K ; Botros, Sara R

The aim the study was to design, formulate, and evaluate self-nanoemulsifying drug delivery systems (SNEDDS) of itraconazole for improving the topical antifungal properties of the drug by adopting the nanoemulsion intermediate gel of the optimized system. Solubility study was conducted to select the most appropriate oils and surfactants for formulation. Different possible systems were created. Ternary phase diagrams were constructed to select the most promising system for further study. The nanoemulsion intermediate gel of the selected system was evaluated for stability, dilution effect, viscosity, pH, antifungal activity, droplet size, PDI, and zeta potential. In vitro release of the drug from the selected intermediate gel was investigated, and the kinetic model of drug release was determined. Ex vivo permeation of itraconazole was studied, and the amount of drug accumulated in the skin was calculated. Solubility and phase diagrams revealed that the system consisting of 60% cotton seed oil and 40% span 80 provided the nanoemulsion intermediate gel with the highest drug concentration. The selected system had a droplet size of about 236 nm and zeta potential of - 59.8. The viscosity of the corresponding intermediate gel was 1583.47 cp. The system exhibited high stability at 4°C and 25°C for 12 months and improved antifungal activity. In vitro release study showed complete release of itraconazole within 4 h, while the ex vivo permeation study revealed accumulation of the majority of the drug within the skin layers (72.5%).

2014-03-01·Parasitology3区 · 医学

In vitro and in vivoactivity of the chloroaryl-substituted imidazole viniconazole againstTrypanosoma cruzi

3区 · 医学

Article

作者: Hammer, Erica Ripoll ; Lionel, Jessica ; Batista, Marcos Meuser ; Brun, Reto ; Batista, Denise da Gama Jaen ; Soeiro, Maria de Nazaré Correia ; Silva, Cristiane França da

SUMMARYChagas disease (CD) is caused by the intracellular protozoan parasiteTrypanosoma cruziand affects more than 10 million people in poor areas of Latin America. There is an urgent need for alternative drugs with better safety, broader efficacy, lower costs and shorter time of administration. Thus the biological activity of viniconazole, a chloroaryl-substituted imidazole was investigated usingin vitroandin vivoscreening models ofT. cruziinfection. Ultrastructural findings demonstrated that the most frequent cellular damage was associated with plasma membrane (blebs and shedding events), Golgi (swelling aspects) and the appearance of large numbers of vacuoles suggesting an autophagic process. Our data demonstrated that although this compound is effective against bloodstream and intracellular forms (16 and 24 μm, respectively)in vitro, it does not presentin vivoefficacy. Due to the urgent need for novel agents againstT. cruzi, the screening of natural and synthetic products must be further supported with the aim of finding more selective and affordable drugs for CD.

100 项与盐酸氯康唑相关的药物交易

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