Identification, characterization, and in silico ADMET prediction of nirmatrelvir and its degradation products using HPLC-PDA and LC-QTOF-MS/MS.

Rationale: Nirmatrelvir is a protease inhibitor that is essential for virus replication. Nirmatrelvir is indicated for the management of mild to severe cases of COVID-19 in individuals who are 12 years of age or older. Forced degradation studies of nirmatrelvir were carried out on the drug substance in solid and solution forms, subjecting it to various stress conditions according to International Conference on Harmonisation (ICH) Q1A(R2) and Q1B guidelines.

Development of a Stability Indicating UPLC Method for the Determination of Tirbanibulin in Bulk and Its Pharmaceutical Dosage Form.

Objectives: The primary goal of this study was to create and validate a simple, precise, sensitive, and accurate ultra-performance liquid chromatography (UPLC) method for estimating tirbanibulin in pure and dosage form.

Materials And Methods: A UPLC technique was developed using a Waters Acquity UPLC Phenyl (100 x 2.1 mm, 1.

Liquid Chromatography Tandem Mass Spectrometric Method for Quantification of Margetuximab in Rat Plasma and Application to a Pharmacokinetic Study.

Margetuximab was approved for the treatment of advanced HER2+ breast cancer. A feasible analytical technique that can measure this drug was obligatory. In light of this, a novel and thoroughly validated liquid chromatographic (LC)-tandem mass spectrometric (MS/MS) approach was developed for the quantification of margetuximab in rat plasma.

Identification, characterisation and in silico ADMET prediction of ozenoxacin and its degradation products using high-performance liquid chromatography-photodiode array and liquid chromatography-quadrupole time-of-flight-tandem mass spectrometry.

Rationale: Ozenoxacin (OXC) is an antibiotic used topically to treat impetigo. This study aimed to evaluate the degradation products (DP) of OXC drug substance under different stress conditions, including hydrolysis, oxidation, thermal and photolysis, in accordance with the International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use (ICH) guidelines Q1A(R2) and Q1B. The analytical technique was validated in compliance with ICH Q2(R1) requirements.

Development and validation of a simple microwave-assisted digestion sample preparation technique for the estimation of aluminium and magnesium in a few pharmaceutical dosage forms by an inductively coupled-mass spectrometer (ICP-MS).

A simple, sensitive, reliable, validated, inductively coupled plasma mass spectrometric method for the determination of aluminium and magnesium using a simple common microwave-assisted digestion sample preparation technique for a few commonly used formulations was developed and validated according to International Conference on Harmonization Q3D and the United States Pharmacopeia general chapter <232> and <233>. The following pharmaceutical dosage forms were considered for estimation of aluminium and magnesium: Alumina, magnesia simethicone oral suspension, Alumina, magnesia simethicone chewable tablets, alumina and magnesia oral suspension, alumina and magnesium carbonate oral suspension. The methodology included optimizing a common microwave assisted digestion method, selecting the isotopes, choosing the measurement technique, and designating internal standards.

Determination of arsenic, cadmium, mercury, lead and nickel as elemental impurities in atorvastatin calcium by inductively coupled mass spectrometer.

Atorvastatin calcium is employed as front-line treatment for cardiovascular diseases. According to the international conference on harmonization (ICH) guideline ICH Q3D, elemental impurities can come into drug products from various sources. These elemental impurities do not have any therapeutic benefit to the end-user.

Novel 1-(4-substituted benzylidene)-4-(1-(substituted methyl)-2,3-dioxoindolin-5-yl)semicarbazide derivatives for use against Mycobacterium tuberculosis H37Rv (ATCC 27294) and MDR-TB strain.

A series of eighteen new 1-(4-substituted benzylidene)-4-(1-(substituted methyl)-2,3-dioxoindolin-5-yl)semicarbazide derivatives were designed, synthesized and characterized by spectral and elemental analyses. The derivatives were screened in vitro for antimicrobial activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) and MDR-TB strains. The activity was expressed as the minimum inhibitory concentration in μg/mL.

Anticonvulsant activity of novel 1-(substituted benzylidene)-4-(1-(morpholino/piperidino methyl)-2,3-dioxoindolin-5-yl) semicarbazide derivatives in mice and rats acute seizure models.

A series of novel 1-(substituted benzylidene)-4-(1-(morpholino/piperidino methyl)-2,3-dioxoindolin-5-yl) semicarbazides 6a-6t was designed and synthesized on the basis of semicarbazide-based pharmacophoric model to meet the structural requirements necessary for anticonvulsant activity. The compounds were subjected to in vivo antiepileptic evaluation using maximal electroshock test and subcutaneous pentylenetetrazole seizure test methods. The neurotoxicity was determined by rotorod test.

Design, synthesis and antiepileptic properties of novel 1-(substituted benzylidene)-3-(1-(morpholino/piperidino methyl)-2,3-dioxoindolin-5-yl)urea derivatives.

Twenty new 1-(substituted benzylidene)-3-(1-(morpholino/piperidino methyl)-2,3-dioxoindolin-5-yl) urea derivatives were designed and synthesized. Antiepileptic screening was performed using MES and scPTZ seizures tests. The neurotoxicity was determined by rotorod test.

Neuroprotective effect of Manasamitra vatakam against aluminium induced cognitive impairment and oxidative damage in the cortex and hippocampus of rat brain.

Manasamitra vatakam (MMV) has long been used as a traditional medicine in India for the treatment of psychosomatic diseases, anxiety neurosis, and stress. The present study was designed to examine the neuroprotective effect of MMV against aluminum (Al)-induced memory impairment and oxidative damage in rats. Neurotoxicity was induced by the administration of Al [100 mg/kg body weight (b.

Evaluation of phytoconstituents and anti-nephrotoxic and antioxidant activities of Monochoria vaginalis.

Monochoria vaginalis is an herbaceous medicinal plant used to treat, liver problems India. Acetaminophen is a commonly used analgesic and antipyretic agent which, at high doses, causes liver and kidney necrosis in man and animals. The aim of the present study is to evaluate phytoconstituents and investigate the nephroprotective & antioxidant activities of the ethanol extract of Monochoria vaginalis on acetaminophen induced toxicity in rats.

Synthesis, characterization, and analgesic activity of novel schiff base of isatin derivatives.

In the present study, a series of novel Schiff bases of isatin [5a-5l] were synthesized by condensation of imesatin with different aromatic aldehydes. The imesatins were synthesized by the reaction of isatin with p-phenylenediamine. The chemical structures of the synthesized compounds were confirmed by means of Infrared (IR), Mass spectroscopy, and Elemental analysis.

Cytisus scoparius link--a natural antioxidant.

Background: Recent investigations have shown that the antioxidant properties of plants could be correlated with oxidative stress defense and different human diseases. In this respect flavonoids and other polyphenolic compounds have gained the greatest attention. The plant Cytisus scoparius contains the main constituent of flavone and flavonals.

Anti-diarrhoeal potential of Asparagus racemosus wild root extracts in laboratory animals.

Purpose: Asparagus racemosus Wild root has been used traditionally in Ayurveda for the treatment of diarrhoea and dysentery. However, the claims of Ayurveda need to be validated by a suitable experimental model. Therefore, the present study was undertaken to evaluate the effect of ethanol and aqueous extracts of Asparagus racemosus for its antidiarrhoeal potential against several experimental models of diarrhoea in Albino Wistar rats.