A Novel Quantitative Method for the Simultaneous Assay of Rifampicin (RIF), Isoniazid (INH), Ethambutol (EMB), and Pyrazinamide (PYP) in 4-FDC Tablets

Hagga, Mohamed; Sultana, Shaheen

doi:10.13005/ojc/320629

Cited by 6 publications

(3 citation statements)

References 18 publications

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“…In addition to the pharmacotechnical challenges for the preparation of formulations containing this association, it is necessary to develop new analytical methods for the simultaneous determination of drugs. Several published studies used different analytical techniques for the determination of antituberculosis drugs alone and in combination, including High Performance Liquid Chromatography (HPLC) with UV detector (8,9), High Performance Thin Layer Chromatography (HPTLC) (10), Ultra-high Performance Liquid Chromatography (UHPLC) with UV detector (11,12), Fourier Transform Infrared (FTIR) spectroscopy in combination with multivariate calibration of partial least square (13) and UV spectrophotometry (14). Due to the absence of an analytical method for the simultaneous determination of PYZ and RIF by derivative spectrophotometric method and considering the importance of analytical methods for the simultaneous determination of drugs, this study aims to develop and validate a simple and rapid derivative spectrophotometric method for the determination of PYZ and RIF in cubosome formulation.…”

Section: Introductionmentioning

confidence: 99%

Development of derivative spectrophotometric method for simultaneous determination of pyrazinamide and rifampicin in cubosome formulation

et al. 2021

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The ultraviolet spectrophotometry analysis for quantitative assay of drugs is a method accurate, sensitive, selective and reproductive with the advantage of being a simple and less expensive method. In this study, a derivative ultraviolet spectrophotometric method was developed for simultaneous determination of pyrazinamide (PYZ) and rifampicin (RIF). The spectrophotometric method was evaluated according to validation guidelines for specificity, linearity, limits of detection and quantification, precision, accuracy and robustness. The first-derivative spectra were obtained and by the zerocrossing point, the wavelength 247 nm and 365 nm were selected for PYZ and RIF quantification, respectively. No interference from cubosome excipients was detected in the proposed method. The results demonstrated linearity in a range of 4.0 – 12.0 µg/mL with an adequate correlation coefficient for both drugs. The intra and inter-day precision results (RSD < 5%) indicated the reproducibility of the method. The accuracy data showed satisfactory results (RSD < 5%) from recovery test. In addition, the robustness results showed that the PYZ and RIF content were unaffected by the solvent alteration of methanol to methanol:water (99:1, v/v). The derivative ultraviolet spectrophotometric method proved to be an excellent strategy for simultaneous determination of PYZ and RIF.

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Section: Introductionmentioning

confidence: 99%

Development of derivative spectrophotometric method for simultaneous determination of pyrazinamide and rifampicin in cubosome formulation

et al. 2021

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“…In the latter one , INH, PYZ and EMB are determined together and RIF separately. Methods employing separation techniques capable of simultaneously determine the four drugs in FDC tablets, such as CE, HPLC, UHPLC and TLC are found in literature . Furthermore, quantitative methods employing UV‐Vis, Raman, FTIR and near infrared spectroscopies with a chemometric approach were also developed .…”

Section: Introductionmentioning

confidence: 99%

Sub‐minute determination of rifampicin and isoniazid in fixed dose combination tablets by capillary zone electrophoresis with ultraviolet absorption detection

Duarte

Amorim

Chellini

et al. 2018

J of Separation Science

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A validated sub minute capillary zone electrophoresis method with direct ultraviolet absorption detection for simultaneous determination of isoniazid and rifampicin in fixed‐dose combination tablets was developed. Background electrolyte was defined based on the analytes effective mobility curve and it was composed by 20 mmol/L of sodium carbonate/sodium bicarbonate at pH 10.2. A careful validation procedure considering the main figures of merit was performed. Regression models were satisfactory for isoniazid and rifampicin, showing no lack of fit within 95% significance interval. Interday and intraday precision were evaluated in standard and sample and slight relative standard deviations were achieved for concentration, area, and migration time. Recovery values for accuracy in two levels were 99.97 and 90.08% for isoniazid and 95.45 and 95.12% for rifampicin. The limits of detection for isoniazid and rifampicin were 0.22 and 0.34 mg/L, respectively, and the limits of quantification were 0.74 and 1.13 mg/L, respectively. Method selectivity was verified by injecting diluent, background electrolyte, a standard mixture, and a sample, confirming no interferent peaks. The method proved to be simple, environmentally friendly, sensitive, and was successfully applied for simultaneous quantification of isoniazid and rifampicin in fixed‐dose combination tablets.

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“…However, patient adherence can be significantly low leading to treatment failure and risk of the bacteria developing resistance. [52][53][54] Rifampicin is from the rifamycin group of antibiotics and inhibits bacterial DNAdependent RNA polymerase, prohibiting a cell's ability to synthesise new proteins, leading to cell death. Isoniazid targets the synthesis of mycolic acid, disrupting the formation of the cell wall.…”

Section: Preventative Treatmentmentioning

confidence: 99%

Towards a New Class of Anti-Tuberculosis Drugs: Design and Synthesis of AnPRT TS Analogues

Mason¹

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Tuberculosis (TB) is an infectious disease caused by the bacterium Mycobacteria tuberculosis (Mtb). In 2021 over 10 million people were diagnosed with TB. It is the number two cause of death behind COVID-19, being attributed to 1.6 million deaths in 2021. Although TB is curable the current multidrug treatment regimens are lengthy, which leads to low adherence and unfavourable treatment outcomes. This has given rise to antibiotic resistance, with 170,000 cases confirmed to be resistant to at least one of the first-line drugs in 2021. The COVID-19 pandemic has also had a significant impact on the global TB burden. This highlights the need for a new class of anti-tuberculosis drugs to tackle this current health crisis. Tryptophan (Trp) is an amino acid that is important for the survival and virulence of Mtb. The Mtb Trp biosynthetic pathway is absent in mammals, therefore the inhibition of this pathway represents a great opportunity for the development of novel tuberculosis drugs. Our group is experienced in transition state analysis (TSA) techniques, which is a sophisticated and rational technique to design potent enzyme inhibitors. This is exemplified by Mundesine®, a drug used for the treatment of peripheral T-cell lymphoma in Japan. In pursuit of a new class of anti-tuberculosis drug candidates, a series of potential TS analogues of anthranilate phosphoribosyl transferase (AnPRT), an enzyme involved in Trp biosynthesis pathway, were designed and synthesised. For the synthesis of the first generation of compounds we used 5-O-tert-butyldimethylsilyl-1,N-dehydro-1,4-dideoxy-1,4-imino-2,3-O-isopropylidene-N-oxide-D-ribitol as a common intermediate. Seven targets were successfully isolated and the synthetic route leading to these targets has been optimised. These iminoribitol derivatives were then tested against the intended target AnPRT, using an enzyme-coupled assay. Unfortunately, the enzymatic assay revealed that the compounds tested displayed minimal inhibitory activity. Co-crystallisation with the enzyme and subsequent x-ray crystallography confirmed that this series of compounds did not bind in the active site of the enzyme. In order to facilitate entry into the active site, a more flexible second and third generation of acyclic phosphate and acyclic phosphonate derivatives were designed. The synthesis of the second generation of targets proved to be challenging and required several alterations to the initial proposed synthetic route. This resulted in the preparation of a single compound. The third generation required less optimisation. Although there were difficulties with the final purification, five compounds were successfully isolated. Evaluating the inhibitory activity of these compounds will assist in drawing structure activity relationships between our compounds and the enzyme, which can be used for the refinement of future generations of inhibitors.

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A Novel Quantitative Method for the Simultaneous Assay of Rifampicin (RIF), Isoniazid (INH), Ethambutol (EMB), and Pyrazinamide (PYP) in 4-FDC Tablets

Cited by 6 publications

References 18 publications

Development of derivative spectrophotometric method for simultaneous determination of pyrazinamide and rifampicin in cubosome formulation

Development of derivative spectrophotometric method for simultaneous determination of pyrazinamide and rifampicin in cubosome formulation

Sub‐minute determination of rifampicin and isoniazid in fixed dose combination tablets by capillary zone electrophoresis with ultraviolet absorption detection

Towards a New Class of Anti-Tuberculosis Drugs: Design and Synthesis of AnPRT TS Analogues

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