Isolation, Characterization, and Toxicity Study of Stress Degradation Products of Pranlukast Hydrate.

Pranlukast hydrate (PRN), a cysteinyl leukotriene receptor antagonist (CysLT), is used to treat bronchial asthma. The objective of this study is to perform the isolation, characterization, and toxicity analysis of stress degradation products of PRN. In high-performance liquid chromatography (HPLC), the separation was achieved using a Phenomenex Gemini C18 (250 × 4.

Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.

Herein, we describe the discovery and optimization of a novel series that inhibits bacterial DNA gyrase and topoisomerase IV binding to, and stabilization of, DNA cleavage complexes. Optimization of this series led to the identification of compound , which has potent activity against Gram-positive bacteria, a favorable safety profile, and excellent pharmacokinetic properties. Compound was found to be efficacious against fluoroquinolone-sensitive infection in a mouse thigh model at lower doses than moxifloxacin.

Development and Validation of a Stability Indicating LC-MS/MS Method for the Determination of Clenbuterol HCl.

Clenbuterol hydrochloride (CLT), β adrenergic agonist is used as a bronchodilator in the therapeutic treatment of asthma. It is important to know the stability behaviour of the drug in different degradation conditions as per ICH Q1A (R2) guidelines for safety and efficacy purpose. The main objective of the study is to develop and validate stability indicating LC-MS/MS method for the determination of Clenbuterol HCl.

Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.

Since their discovery over 5 decades ago, quinolone antibiotics have found enormous success as broad spectrum agents that exert their activity through dual inhibition of bacterial DNA gyrase and topoisomerase IV. Increasing rates of resistance, driven largely by target-based mutations in the GyrA/ParC quinolone resistance determining region, have eroded the utility and threaten the future use of this vital class of antibiotics. Herein we describe the discovery and optimization of a series of 4-(aminomethyl)quinolin-2(1)-ones, exemplified by , that inhibit bacterial DNA gyrase and topoisomerase IV and display potent activity against ciprofloxacin-resistant Gram-negative pathogens.

Impurity Profile of Bronchodilators used in Asthma: A Critical Review.

Background: Asthma is defined as a heterogeneous disease usually characterized by chronic airway inflammation (GINA 2016) affecting almost 334 million people worldwide (Global asthma report 2014). Treatment of asthma with a long-acting bronchodilator is important because it reduces the symptoms that occur at night or in the early morning and it is very effective to use as a long term control medication for asthma by preventing asthmatic symptoms. The main objective of this review is to describe the impurity profile and force degradation studies for three major classes of bronchodilators namely β2-adrenoceptor agonists, muscarinic receptor antagonists and xanthine.

Treatment outcome of patients having extensively drug-resistant tuberculosis in Gujarat, India.

Background: To investigate the factors affecting treatment outcome of extensively drug resistant tuberculosis (XDR-TB) in Gujarat, India.

Methods: A prospective, observational study was conducted on patients with XDR TB from January 2012 to October 2016. Details of demography, clinical symptoms, sputum/culture and radiological examination, drug treatment, adverse drug reactions (ADRs) and treatment outcome were recorded in pretested case record form (CRF).

Critical Analysis of Cardiovascular and Central Nervous System Fixed Dose Combinations Available in Indian Market.

Introduction: Fixed Dose Combinations (FDCs) are being increasingly used to improve compliance and achieve greater benefits of the two or more active ingredients given together than the corresponding individual drug components given separately.

Aim: To analyse the rationality of Cardiovascular (CV) and Central Nervous System (CNS) FDCs available in Indian market.

Materials And Methods: CVS and CNS FDCs, enlisted in Indian Drug Review, 2014, were analysed by a pretested validated eight point criteria tool.