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N-acyl hydrazone (NAH) is recognized as a promising framework in drug design due to its versatility, straightforward synthesis, and attractive range of biological activities, including antimicrobial, antitumoral, analgesic, and anti-inflammatory properties. In the global context of increasing resistance of pathogenic bacteria to antibiotics, NAHs represent potential solutions for developing improved treatment alternatives. Therefore, this research introduces six novel derivatives of ()-N'-benzylidene-2-(6-chloro-9-carbazol-2-yl)propanehydrazide, synthesized using a microwave-assisted method.

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Assessing Polymorphic Purity of Rifampicin in Double and Triple-Drug Fixed-Dose Combination Products.

J Pharm Sci

April 2024

Área de Análisis de Medicamentos, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario and Instituto de Química Rosario (IQUIR, CONICET-UNR), Suipacha 531, Rosario S2002LRK, Argentina.. Electronic address:

First-line tuberculostatic agents, Rifampicin (RIF), Isoniazid (ISH), Ethambutol (ETB), and Pyrazinamide (PZA) are generally administered as a fixed-dose combination (FDC) for improving patient adherence. The major quality challenge of these FDC products is their variable bioavailability, where RIF and its solid state are key factors. In this work, the analysis of the impact of the polymorphism in the performance of RIF in RIF-ISH and PZA-RIF-ISH combined products was carried out by an overall approach that included the development and validation of two methodologies combining near-infrared (NIR) spectroscopy and partial least squares (PLS) to the further evaluation of commercial products.

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Rising rates of drug abuse and pharmaceutical pollution throughout the world as a consequence of increased drug production and utilization pose a serious risk to public health and to environmental integrity. It is thus critical that reliable analytical approaches to detecting drugs and their metabolites in a range of sample matrices be developed. Recent advances in the design of nanomaterial-based electrochemical sensors and biosensors have enabled promising new approaches to pharmaceutical analysis.

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A simple signal-on strategy for fluorescent detection of tuberculostatic drug isoniazid based on Ag clusters-MnO sheets nanoplatform.

Colloids Surf B Biointerfaces

May 2021

Chongqing Research Center for Pharmaceutical Engineering, Key Laboratory of Molecular Biology for Infectious Diseases (Ministry of Education), College of Pharmacy, Chongqing Medical University, Chongqing, 400016, PR China. Electronic address:

As a first-line tuberculostatic drug, isoniazid (INH) plays effective and irreplaceable role in prevention and treatment of tuberculosis. In this work, a rapid and simple signal-on fluorescence approach is established for INH assay by employing a platform composed of silver nanoclusters (AgNCs) and MnO nanosheets. In the proposed sensing system, strong red fluorescence of poly (methacrylic acid)-stabilized AgNCs can be greatly quenched after they attach to the surfaces of MnO nanosheets.

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Despite having good efficacy in the treatment and prevention of tuberculosis, the administration of rifampicin (RIF) can cause serious side effects, resulting from the prolonged use of this substance. Thus, it is necessary to seek new systems for administering tuberculostatic drugs, to avoid unwanted adverse effects, increase their bioavailability and, consequently, improve their therapeutic efficacy. The present work describes the achievement of a pH-responsive system for RIF, using palygorskite, a fibrous clay mineral, as a nanocarrier.

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