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Ram Manohar Basnet, Daniela Zizioli, Michela Guarienti, Dario Finazzi, Maurizio Memo
BACKGROUND: Zebrafish embryos are emerging as a model for pharmacological and toxicological studies. We used zebrafish embryos to study the general toxicity and cardiovascular effects of eight methylxanthines: aminophylline, caffeine, diprophylline, doxofylline, etophylline, 3-isobutyl-1-methylxanthine (IBMX), pentoxifylline and theophylline. METHODS: Microinjections of the eight methylxanthines were performed in 1-2 cell stage zebrafish embryos and the general toxicity and cardiovascular effects were analyzed at different time points...
November 15, 2017: BMC Pharmacology & Toxicology
Yanira Riffo-Vasquez, Radhakrishnan Venkatasamy, Clive P Page
Glucocorticosteroids are widely used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). However, there are growing concerns about the side effect profile of this class of drug, particularly an increased risk of pneumonia. Over the last two decades there have been many attempts to find drugs to allow a reduction of glucocorticosteroids, including xanthines such as theophylline. Use of xanthines has been shown to lead to a reduction in the requirement for glucocorticosteroids, although xanthines also have a narrow therapeutic window limiting their wider use...
October 12, 2017: Pulmonary Pharmacology & Therapeutics
P Sasi Rekha, S Gunasekaran
Photostability studies of drugs and drug products are an integral part of the product development process in the pharmaceutical industry. These studies are carried out to ensure quality, efficacy and safety of the formulated products during manufacture, storage and use. In this investigation, a novel spectroscopic approach has been adopted by employing the FTIR-ATR and UV/Visible techniques to detect the photochemical reactions of the drug Doxofylline, chemically designated as 7-(1, 3 dioxolane-2-yl methyl) theophylline, in its raw (pure) form...
September 11, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Brijeshkumar S Patel, Michael J Kugel, Gina Baehring, Alaina J Ammit
The xanthine doxofylline has been examined in clinical trials and shown to have efficacy and greater tolerability than theophylline in asthma and chronic obstructive pulmonary disease. The 'novofylline' doxofylline has demonstrated bronchodilatory and anti-inflammatory actions in in vivo and ex vivo experimental models of respiratory disease. However, there are limited studies in vitro. We address this herein and examine whether doxofylline has anti-inflammatory impact on primary cultures of airway smooth muscle (ASM) cells...
August 2017: Pulmonary Pharmacology & Therapeutics
Peixi Zhu, Jingxian Lu, Liya Hong, Weike Su, Ann Van Schepdael, Erwin Adams
During quality control of doxofylline, a novel impurity was detected, which was above the identification threshold defined by ICH. First, a liquid chromatographic method compatible with mass spectrometric (MS) detection was developed. Based on tandem multistage MS and high resolution MS data, the unknown impurity was found to consist of two theophylline groups connected by a methylene group. The structure was further confirmed by 1D and 2D nuclear magnetic resonance (NMR) experiments after semi-preparative isolation...
June 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
Ch Krishnam Raju, Avadhesh K Pandey, Gururaj S, Kaushik Ghosh, Arunima Pola, Sanath Kumar Goud P, Mrunal A Jaywant, Sameer G Navalgund
Forced degradation of Doxofylline (DFL) in different stress (base and peroxide) conditions gave rise to two potential unknown impurities. These unknown degradation products DFL DEG-I and DFL DEG-II were evaluated using a new-reverse-phase high performance liquid chromatography (HPLC), where it was eluted at 0.44 and 1.09 relative retention times to DFL peak. DFL DEG-I and DFL DEG-II were isolated using preparative HPLC from degradation mixtures. The structure of DFL DEG-I and DFL DEG-II were elucidated using high resolution MS, multi-dimensional NMR and FTIR spectroscopic techniques, and characterized...
June 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
Jinrong Wang, Zhaobo Cui, Shuhong Liu, Xiuling Gao, Pan Gao, Yi Shi, Shufen Guo, Peipei Li
Noninvasive positive-pressure ventilation (NPPV) might be superior to conventional mechanical ventilation (CMV) in patients with acute exacerbations of chronic obstructive pulmonary disease (AECOPDs). Inefficient clearance of respiratory secretions provokes NPPV failure in patients with hypercapnic encephalopathy (HE). This study compared CMV and NPPV combined with a noninvasive strategy for clearing secretions in HE and AECOPD patients.The present study is a prospective cohort study of AECOPD and HE patients enrolled between October 2013 and August 2015 in a critical care unit of a major university teaching hospital in China...
March 2017: Medicine (Baltimore)
D Spina, C P Page
Theophylline is an orally acting xanthine that has been used since 1937 for the treatment of respiratory diseases including asthma and chronic obstructive pulmonary disease (COPD). However, in most treatment guidelines, xanthines have now been consigned to third-line therapy because of their narrow therapeutic window and propensity for drug-drug interactions. However, lower than conventional doses of theophylline considered to be bronchodilator are now known to have anti-inflammatory actions of relevance to the treatment of respiratory disease...
2017: Handbook of Experimental Pharmacology
Yajun Zhang, Kaizhu Zeng, Jing Wang, Haiyang Gao, Yefei Nan, Xiaohui Zheng
As a xanthine derivative, doxofylline is believed to be dominant for fighting against asthma in practice. Unlike other xanthines, the antiasthmatic effects of doxofylline lack any definite proof of target and mediating mechanism according to previous reports. In this work, the interaction between doxofylline and β2 -AR was investigated by high performance affinity chromatography using frontal analysis and nonlinear model. The methodology involved the immobilization of β2 -AR on the silica gel by a random linking method, the determination of the binding parameters by frontal analysis and nonlinear chromatography and the exploration of the binding mechanism by site-directed molecular docking...
October 2016: Journal of Molecular Recognition: JMR
K K Aswini, A M Vinu Mohan, V M Biju
Theophylline is an inexpensive drug employed in asthma and chronic obstructive pulmonary disorder medications and is toxic at higher concentration. The development of a molecularly imprinted polymer based theophylline electrochemical sensor on glassy carbon electrode by the electropolymerization of 4-amino-5-hydroxy-2,7-naphthalenedisulfonic acid is being discussed in this work. The MIP modification enhances the theophylline recognition ability and the electron transfer kinetics of the bare electrode. The parameters, controlling the performance of the imprinted polymer based sensor, like number of electropolymerization cycles, composition of the pre-polymerization mixture, pH and immersion time were investigated and optimized...
August 1, 2016: Materials Science & Engineering. C, Materials for Biological Applications
Sami Manzoor Margay, Samina Farhat, Sharanjit Kaur, Hilal Ahmad Teli
BACKGROUND: Asthma is a non communicable chronic disease prevalent all over the world. Two commonly used methylxanthines, theophylline and doxofylline were compared in the study in stable asthmatic patients at recommended doses by various spirometric lung function tests with forced expiratory volume at second one (FEVI) between 50 to 80% of predicted FEVI. MATERIALS AND METHODS: A total of 100 patients were divided in two groups. Group I was administered 300 mg theophylline twice a day and Group II was administered doxofylline 400 mg twice a day orally for six weeks...
April 2015: Journal of Clinical and Diagnostic Research: JCDR
Dushyant Lal, Sachin Manocha, Arunabha Ray, V K Vijayan, Raj Kumar
BACKGROUND: Bronchial asthma and chronic obstructive pulmonary disease (COPD) are the major obstructive disorders that may contribute to the severity in individual patients. The present study was designed to compare the efficacy and safety of theophylline and doxofylline in patients with bronchial asthma and COPD. METHODS: A total of 60 patients, 30 each with bronchial asthma and COPD, were enrolled for the study. Each group of 30 patients received standard treatment for asthma and COPD...
September 2015: Journal of Basic and Clinical Physiology and Pharmacology
Yu Zhao, Nan Ji, Lihui Yin, Jun Wang
Drug safety has become a very important subject, and more countries have joined in the fight against counterfeit drugs. This study demonstrated a non-invasive Raman spectroscopy method that could be utilized for screening liquid injectable drugs for spurious/falsely-labeled/falsified/counterfeit medical products (SFFCs). Two problems were solved to remove the blocks in identification and quantitation: one problem was the weak API signal extraction from the non-invasive Raman spectra and the other was the problem of Raman absolute measurement...
August 2015: AAPS PharmSciTech
Muhasaparur Ganesan Rajanandh, Arcot D Nageswari, Kaliappan Ilango
PURPOSE: Data comparing various second-line treatments for asthma with subjective and objective assessment are lacking. This study aimed to compare the efficacy and safety of montelukast, doxofylline, and tiotropium with a low-dose budesonide in patients with mild to moderate persistent asthma. METHODS: Patients, all of whom were concurrently using inhaled budesonide (400 µg), were treated for 6 months with formoterol (12 µg), montelukast (10 mg), doxofylline (400 mg), or tiotropium (18 µg)...
February 1, 2015: Clinical Therapeutics
Muhasaparur Ganesan Rajanandh, Arcot Deenadayalu Nageswari, Kaliappan Ilango
Many patients with persistent asthma cannot achieve the treatment goal for asthma with a single controller medication. The aim of the present study was to assess lung function and rescue medication use in asthma patients receiving four different categories of drugs in combination with an inhaled corticosteroid. Patients recruited to the study were randomized into four groups to receive budesonide with either formoterol, doxofylline, montelukast or tiotropium for a period of 3 months. Lung function (i.e. forced expiratory volume in 1 s (FEV1 )) and rescue medication use were determined at baseline and on Day 15, 30, 45, 60 and 90 of treatment...
July 2014: Clinical and Experimental Pharmacology & Physiology
Muhasaparur G Rajanandh, Arcot D Nageswari, Kaliappan Ilango
BACKGROUND: There is no comparative study among asthma patients receiving first-line versus various second-line treatment regimens for mild to moderate persistent asthma. OBJECTIVE: We assessed the pulmonary function in asthma patients receiving montelukast, doxofylline, and tiotropium with budesonide in a pilot group. METHODS: Patients were recruited as per the study criteria and randomly allocated to 4 groups to receive budesonide (400 µg) with formoterol (12 µg), doxofylline (400 mg), montelukast (10 mg), or tiotropium (18 µg) for a period of 3 months...
April 1, 2014: Clinical Therapeutics
Gananadhamu Samanthula, Krishnaveni Yadiki, Shantikumar Saladi, Sreekanth Gutala, K V Surendranath
An isocratic, stability-indicating, reversed-phase high-performance liquid chromatography (RP-HPLC) method was developed for the quantitative determination of doxofylline and terbutaline sulphate, used for the treatment of respiratory problems. The chromatographic separation was achieved on a Zorbax-SB Phenyl 250 × 4.6mm × 5 μm column with the mobile phase consisting of a mixture of 25 mM ammonium acetate (pH 5.0) : acetonitrile (85:15 %v/v) at a flow rate of 1.0 ml/min. The eluate was monitored at 274 nm using a PDA detector...
October 2013: Scientia Pharmaceutica
Yanira Riffo-Vasquez, Francis Man, Clive P Page
RATIONAL: Doxofylline is a xanthine drug that has been used as a treatment for respiratory diseases for more than 30 years. In addition to doxofylline being a bronchodilator, some studies have indicated that doxofylline also has anti-inflammatory properties, although little is known about the effect of this drug on lung inflammation. OBJECTIVES: We have investigated the actions of doxofylline against the effects of Escherichia coli LPS in the lungs of BALB/c mice...
April 2014: Pulmonary Pharmacology & Therapeutics
Priti S Patil, Purnima D Hamrapurkar, Mitesh D Phale, Masti I Desai, Sandeep B Pawar
The purpose of this work was to study the stability behavior of doxofylline under different stress conditions and to develop a sensitive stability-indicating HPLC assay method. The stress conditions applied included heat, moisture, acid-base hydrolysis, oxidation, and UV light. The drug was particularly labile under oxidative and thermal stress conditions, with 58.40 and 53.90% degradation, respectively. Good resolution of drug from degradation products formed under stress conditions was achieved on a C18 column using 10 mM KH2PO4 buffer solution (pH 6) methanol (40 + 60, v/v) as the mobile phase (pH 7...
July 2013: Journal of AOAC International
R Revathi, T Ethiraj, P Thenmozhi, V S Saravanan, V Ganesan
AIM: Some literatures revealed that the high performance liquid chromatography (HPLC) method for single component or multicomponent analysis of montelukast sodium with other drugs. However, these methods deals with time consuming, so it is necessary to develop a cost-effective and less time consuming method for the estimation of doxofylline and montelukast sodium in combined pharmaceutical formulation. MATERIALS AND METHODS: The separation was performed on an inertsil C8 (5 μm, 4...
October 2011: Pharmaceutical Methods
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