Development and validation of a chromatographic method for the estimation of rifampicin in bulk and pharmaceutical formulations

Venkataramana, N V; Desai, Nivedita R; Sreenivasa, S.; Chaluvaraju, K. C.; Kumar, D B Aruna

doi:10.5958/0974-360x.2016.00444.3

Cited by 3 publications

(1 citation statement)

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“…H451Y and S456L mutants have increased their binding energy respectively to -7.3 kcal/ mol and -8.2 kcal/mol compared to native protein (Table 1). Both of these variants have been confirmed to be resistant to rifampicin [39][40][41] . In another study also found the difference of binding energies observed in the docking study, evidently that RMP is less effective in the treatment of patients with S425L variant 20 .…”

Section: Resultsmentioning

confidence: 93%

Molecular Docking Analysis of the T450A Mutation of the Gene rpoB Mycobacterium leprae from Leprosy Patients in Papua, West Papua and North Maluku, Indonesia

Maladan¹,

Krismawati²,

Wahyuni³

et al. 2021

RJPT

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Leprosy persists to be a health problem in Indonesia, especially in the provinces of North Maluku, West Papua and Papua. Early diagnosis and complete treatment with multidrug therapy (MDT) remain the key strategy for reducing the disease burden. One of the major components of MDT is rifampicin which in certain cases in several countries, M. leprae resistance to this drug issue has been reported albeit only a few. This research aimed to detect and analyze polymorphism in M. leprae rpoB gene that was isolated from leprosy patients in three provinces: North Maluku Province, West Papua Province and Papua Province, Indonesia. The identification of mutations in the M. leprae rpoB gene was carried out by aligning the results of DNA sequencing with the reference strain. The 3D structure of rpoB was derived using the Swiss Model. The T450A, S456L, and H451Y variants of RNA Polymerase B subunits were constructed using FoldX based on the wild-type structure. The structures were repaired, and protein stability was evaluated using foldX under the Yasara viewer. The QC of the rpoB M. leprae homology models was conducted with Ramachandran Plot modeling using PROCHECK. The difference in binding affinity between native protein and T450A, S456L, and H45I variants were analyzed using molecular docking. rpoB gene of M. leprae contains a mutation found in nucleotide of 1348 bp. The mutation triggered the conversion of the amino acid Threonine to Alanine in the amino acid to 450 rpoB subunit B. The structure of 3D RNA Polymerase Subunit B was constructed using rpoB Mycobacterium tuberculosis with PDB code 5UH5 as template. According to Ramachandran Plot, the percentage of residues in the most favored regions are 91.9%, and there was no significant number of residues in the disallowed regions. The results of molecular docking showed that the T450A variant had the same binding affinity with the native protein which was -8.9 kcal. Binding affinity on the S456L and H451Y variants increased by -7.3 kcal and -8.2 kcal, respectively. According to Molecular Docking analysis, T450A variant did not affect the energy binding between RNA polymerase and rifampicin.

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Section: Resultsmentioning

confidence: 93%

Molecular Docking Analysis of the T450A Mutation of the Gene rpoB Mycobacterium leprae from Leprosy Patients in Papua, West Papua and North Maluku, Indonesia

Maladan¹,

Krismawati²,

Wahyuni³

et al. 2021

RJPT

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Development and validation of a stability indicating UPLC method for determination of Darolutamide in its tablet formulation

Venkatesh

Kulandaivelu

Rao

et al. 2022

RJPT

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Darolutamide is an orally active, second generation non-steroidal anti-androgen. The objective of this study was to develop a simple and fast stability indicating method for the determination of Darolutamide in bulk and tablets. Darolutamide was eluted on a Zorbax SB-C18 column (100X2.1mmX1.8µ) with a mobile phase of 8mM ammonium acetate, pH: 5.4: acetonitrile (66:34 v / v) in isocratic mode at a flow rate of 0.4 ml / min. The analyte was quantified using a 272 nm PDA detector. The chromatograms of darolutamide obtained with this method showed a well resolved retention time at 0.83 min of its excipients and degradation products. The area of the peak with respect to the concentration calibration curves, which were linear from 70 to 210 µg / ml, had a regression coefficient (r2) greater than 0.999. The detection limit (LOD) and the limit of quantification (LOQ) were found at 1.80 and 6.01 µg/mL respectively. Accuracy and precision have been determined and perfectly matched to the ICH standards. The study showed that the proposed UPLC method was simple, fast, robust and reproducible, which can be used for the evaluation of the purity and stability of the drug without interference from excipients or decomposition products of active pharmaceutical ingredients.

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Development and Validation of Quality by Design based RP-HPLC Method for determination of Tenofovir Alafenamide Fumarate from Bulk drug and Pharmaceutical dosage form and its application to Forced Degradation Studies

Wankhade¹,

Hamrapurkar²

2022

RJPT

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The present research work entails the development and validation of a simple, robust and sensitive stability indicating reverse phase high performance liquid chromatographic method using Quality by Design methodology for estimation of Tenofovir alafenamide fumarate in bulk drug and its marketed dosage form. Chromatographic separation was performed in isocratic mode using Inertsil C18 column, mobile phase composed of Acetonitrile: ammonium formate buffer pH 5(40: 60) at a flow rate of 1mL/min with Photo Diode Array (PDA) detection at 261nm. A Box-Behnken statistical design with 3 factors and 3 levels was selected for the optimization study. Interaction effects of Critical Quality Parameters (Buffer pH, Organic Phase-% acetonitrile, flow rate) were evaluated for critical quality attributes (Retention time, NTP and symmetry factor). The optimized method was validated according to the current International Conference Harmonization (ICH) Q2 R1 guidelines. The method was found to be linear, covering the range from 1.5 μg/mL – 4.5 μg/mL with correlation coefficient r2 of 0.9996 and precision was found to be less than 2%. Limit of Detection and Limit of Quantification was found to be 1µg/mL and 1.2µg/mL respectively. Accuracy was between 99% and 102%. Forced degradation study was conducted under degradation conditions like light, oxidation, dry heat, acidic, basic, hydrolysis in order to establish the intrinsic stability of molecule. The method was successfully applied for the determination of the drug in commercial dosage form. This holistic stability indicating chromatographic method focused on QbD approach ensured reproducibility and was found to be useful for routine analysis of Tenofovir alafenamide fumarate.

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Development and validation of a chromatographic method for the estimation of rifampicin in bulk and pharmaceutical formulations

Cited by 3 publications

References 0 publications

Molecular Docking Analysis of the T450A Mutation of the Gene rpoB Mycobacterium leprae from Leprosy Patients in Papua, West Papua and North Maluku, Indonesia

Molecular Docking Analysis of the T450A Mutation of the Gene rpoB Mycobacterium leprae from Leprosy Patients in Papua, West Papua and North Maluku, Indonesia

Development and validation of a stability indicating UPLC method for determination of Darolutamide in its tablet formulation

Development and Validation of Quality by Design based RP-HPLC Method for determination of Tenofovir Alafenamide Fumarate from Bulk drug and Pharmaceutical dosage form and its application to Forced Degradation Studies

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