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Monika Wentzlaff, Volkmar Senz, Anne Seidlitz
Drug-eluting stents are often coated using single-stent coating techniques. In pharmaceutical industry, single-tablet coating is unthinkable. Instead large batches of tablets are coated in fluidized bed apparatuses or pan coaters. Therefore, it was the aim of this work to evaluate whether stents can be coated using a fluidized bed process. For this purpose stents were coated with the model fluorescent drug triamterene embedded in ammonium methacrylate copolymer. Different stent lengths as well as different coating yields were assessed and also a drug-free topcoat was evaluated...
March 13, 2019: European Journal of Pharmaceutics and Biopharmaceutics
Ahmed A Khorshed, Mohamed Khairy, Craig E Banks
Hypertension increases the risk of heart disease and stroke, is commonly known as a silent killer disease and considered as one of the key risk factor for premature death and disability over the world. Herein, we report for the first time a sensitive, costless and reproducible voltammetric method for individual determination of five antihypertensive drugs namely, propranolol (PRO), timolol (TIM), amlodipine (AML), amiloride (AMI) and triamterene (TRI) using differential pulse voltammetry at bare/unmodified screen-printed carbon electrodes (SPEs) in presence of sodium dodecyl sulfate (SDS)...
June 1, 2019: Talanta
Emily A Ridge, Sudhan Pachhain, Sayantan Roy Choudhury, Sara R Bodnar, Ray A Larsen, Vipaporn Phuntumart, Jon E Sprague
Hyperthermia induced by 3,4-methylenedioxymethamphetamine (MDMA) can be life-threatening. Here, we investigate the role of the gut microbiome and TGR5 bile acid receptors in MDMA-mediated hyperthermia. Fourteen days prior to treatment with MDMA, male Sprague-Dawley rats were provided water or water treated with antibiotics. Animals that had received antibiotics displayed a reduction in gut bacteria and an attenuated hyperthermic response to MDMA. MDMA treated animals showed increased uncoupling protein 1 (UCP1) and TGR5 expression levels in brown adipose tissue and skeletal muscle while increased expression of UCP3 was observed only in skeletal muscle...
March 13, 2019: Scientific Reports
Youming Lu, Lei Yuan, Xin Chen, Aijun Zhang, Pengqi Zhang, Dongdong Zou
Hydrocephalus is a neurological condition caused by an abnormal accumulation of cerebrospinal fluid; pharmacological intervention of the disease has been found to elicit a variety of adverse drug reactions (ADRs) in central nervous system (CNS) by unexpectedly targeting certain functional neuroproteins. Here, a systematic neuroprotein drug interactome (SNDI) is created for 11 hydrocephalus drugs/metabolites plus 20 control drugs across 518 druggable pockets on the surface of 472 CNS neuroproteins via a large-scale molecular docking approach...
February 2019: Journal of Bioinformatics and Computational Biology
Kai-Chun Cheng, Wei-Ting Chang, Feng Yu Kuo, Zhih-Cherng Chen, Yingxiao Li, Juei-Tang Cheng
Left ventricular hypertrophy is an independent risk factor in diabetic patients. TGR5 is shown to express in hearts, but its functional role in diabetes-induced cardiac hypertrophy remained unclear. The current study investigated the role of TGR5 on high glucose-induced hypertrophy of H9C2 cells. After incubation with a high level of glucose, H9C2 cells showed hypertrophic responses. Activation of TGR5 by lithocholic acid (LCA) ameliorated cell hypertrophy and enhanced SERCA2a and phosphorylated phospholamban (PLN) expression in H9C2 cells...
March 6, 2019: Scientific Reports
Marwah Aljohani, Pól MacFhionnghaile, Patrick McArdle, Andrea Erxleben
The antidiabetic drug gliclazide (GLZ) has a slow absorption rate and a low bioavailability due to its poor solubility. GLZ is often prescribed along with an antihypertensive, as many diabetic patients have coexistent hypertension. Cocrystallization and coamorphization are attractive strategies to enhance dissolution rates and to reduce the number of medications a patient has to take. In this work the formation of cocrystals and coamorphous systems of GLZ with various antihypertensive drugs was studied, namely chlorothiazide (CTZ), hydrochlorothiazide (HTZ), indapamide (IND), triamterene (TRI) and nifedipine (NIF) as well as benzamidine (BZA) as a model for the amidine pharmacophore...
February 22, 2019: International Journal of Pharmaceutics
Katharina Pruessmann, Monika Wentzlaff, Ruprecht Schilling, Anne Seidlitz
The aim of this study was to investigate if the geometry of the dissolution vessel, the dissolution medium volume and composition might contribute to the variation in drug release from drug-eluting stents (DES) in different test setups, which has been observed in previous in vitro studies. Therefore, DES containing triamterene as model substance were produced via fluidised-bed technology. Dissolution testing was carried out using different incubation setups, the reciprocating holder (USP Apparatus 7) and two flow-through methods, a method similar to the USP Apparatus 4 (FTC) and the vessel-simulating flow-through cell (vFTC) equipped with a hydrogel as a second compartment simulating the blood vessel wall...
January 2, 2019: AAPS PharmSciTech
Bo Peng, Zaiyong Zhang, Jian-Rong Wang, Meiqi Li, Qi Zhang, Xuefeng Mei
Discrimination of active pharmaceutical ingredients (APIs) existing as neutral molecules or salts is essential and complicated. However, the discrimination of pharmaceutical salts by confocal Raman micro-spectroscopy remains relatively poorly understood. In this paper, four new salts of triamterene (Tri) cocrystallized with nicotinic acid (NA), benzoic acid (BA), p-toluenesulfonic acid (TA), or isonicotinic acid (INA) were prepared and characterized comprehensively by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), polarized light microscopy (PLM), and dynamic vapor sorption (DVS)...
November 8, 2018: Analyst
Fawzia A Ibrahim, Manal M Fouad, Noha S Rashed, Mona E Fathy, Ebtesam S Mahmoud
Sensitive, simple and specific spectrophotometric and spectrofluorimetric methods were developed for the determination of triamterene in bulk powder and pharmaceutical dosage form. The spectrophotometric method (Method A) is based on the formation of an ion-pair complex with eosin Y in acetate buffered solution of pH 3.7 followed by measuring the absorbance at 545 nm. The absorbance-concentration plot is rectilinear over the range 3.0-15.0 μg/mL with a limit of detection (LOD) of 0.429 μg/mL and a limit of quantitation (LOQ) of 1...
October 25, 2018: Luminescence: the Journal of Biological and Chemical Luminescence
Violeta Carmona-Martínez, Antonio J Ruiz-Alcaraz, María Vera, Antonio Guirado, María Martínez-Esparza, Pilar García-Peñarrubia
Pteridines are aromatic compounds formed by fused pyrazine and pyrimidine rings. Many living organisms synthesize pteridines, where they act as pigments, enzymatic cofactors, or immune system activation molecules. This variety of biological functions has motivated the synthesis of a huge number of pteridine derivatives with the aim of studying their therapeutic potential. This review gathers the state-of-the-art of pteridine derivatives, describing their biological activities and molecular targets. The antitumor activity of pteridine-based compounds is one of the most studied and advanced therapeutic potentials, for which several molecular targets have been identified...
October 19, 2018: Medicinal Research Reviews
Miao Sun, Kui Li, Wei-De Zhang, Yu-Xiang Yu
In this study, a photocatalyst with a distorted skeleton and synthesized by grafting triamterene onto graphitic carbon nitride (g-C3 N4 ) frameworks was prepared. The pteridine ring of the triamterene-based nitrogen-enriched organic structure functions as a trapped electron site owing to its inductive effect. The benzene ring in triamterene plays an important role in the even dispersion of electrons by a conjugative effect. Redistribution of the intramolecular electronic potential is caused by a synergistic effect between the pteridine and benzene rings of triamterene and promotes separation and migration of the photoinduced charge carriers...
October 18, 2018: Chemistry, An Asian Journal
Neda Hosseinpour Moghadam, Sadegh Salehzadeh, Hamid Tanzadehpanah, Massoud Saidijam, Jamshid Karimi, Sadegh Khazalpour
The anticancer activity of triamterene on HCT116 and CT26 colon cancer cells lines was investigated. Furthermore, the mechanism of interaction between triamterene and calf thymus DNA (ct-DNA) and also human serum albumin (HSA) was conducted using multi-spectroscopic and molecular docking techniques. In vitro cytotoxicity of triamterene against HCT116 and CT26 cells showed promising anticancer effects with IC50 values of 31.30 and 24.45 μM, respectively. Competitive studies of the triamterene with NR (Neutral Red) and MB (Methylene Blue) as intercalator probes showed that triamterene can be replaced by these probes...
July 25, 2018: Journal of Biomolecular Structure & Dynamics
C John Sperati, Chi Zhang, Marco Delsante, Rajib Gupta, Serena Bagnasco, Ishan Barman
No abstract text is available yet for this article.
July 2018: KI Reports
Eriko Yamaguchi, Kazuhiro Yoshikawa, Izaya Nakaya, Karen Kato, Yoshikazu Miyasato, Terumasa Nakagawa, Yutaka Kakizoe, Masashi Mukoyama, Jun Soma
BACKGROUND: Liddle's syndrome is a rare monogenic form of hypertension caused by truncating or missense mutations in the C termini of the epithelial sodium channel (ENaC) β or γ subunits. Patients with this syndrome present with early onset of hypertension, hypokalemia, metabolic alkalosis, hyporeninemia and hypoaldosteronism, and a potassium-sparing diuretics (triamterene or amiloride) can drastically improves the disease condition. Although elderly patients having these characteristics were considered to have Liddle's syndrome or Liddle's-like syndrome, no previous report has indicated that Liddle's-like syndrome could be caused by nephrotic syndrome of primary glomerular disease, which is characterized by urinary excretion of > 3 g of protein/day plus edema and hypoalbuminemia, or has explained how the activity function of ENaC could be affected in the setting of high proteinuria...
May 23, 2018: BMC Nephrology
Gregg E Dinse, Christine G Parks, Helen C S Meier, Caroll A Co, Edward K L Chan, Todd A Jusko, James Yeh, Frederick W Miller
BACKGROUND: Clinical reports link specific medications with the development of antinuclear antibodies (ANA), but population-based evidence is limited. OBJECTIVE: The present study investigated associations between prescription medication use and ANA in a representative sample of the adult noninstitutionalized US population, first focusing on medications previously related to ANA and then considering all medications reported in the National Health and Nutrition Examination Survey (NHANES)...
August 2018: Journal of Autoimmunity
Felipe F Hudari, Guilherme G Bessegato, Flávio C Bedatty Fernandes, Maria V B Zanoni, Paulo R Bueno
TiO2 nanotube electrodes were self-doped by electrochemical cathodic polarization, potentially converting Ti4+ into Ti3+ , and thereby increasing both the normalized conductance and capacitance of the electrodes. One-hundred (from 19.2 ± 0.1 μF cm-2 to 1.9 ± 0.1 mF cm-2 for SD-TNT) and two-fold (from ∼6.2 to ∼14.4 mS cm-2 ) concomitant increases in capacitance and conductance, respectively, were achieved in self-doped TiO2 nanotubes; this was compared with the results for their undoped counterparts. The increases in the capacitance and conductance indicate that the Ti3+ states enhance the density of the electronic states; this is attributed to an existing relationship between the conductance and capacitance for nanoscale structures built on macroscopic electrodes...
June 19, 2018: Analytical Chemistry
Abida Rehman, Amit Delori, David S Hughes, William Jones
Pharmaceutical salt solvates (dimethyl sulfoxide, DMSO) of the drug triamterene with the coformers acetic, succinic, adipic, pimelic, azelaic and nicotinic acid and ibuprofen are prepared by liquid-assisted grinding and solvent-evaporative crystallization. The modified Δp K a rule as proposed by Cruz-Cabeza [(2012 ▸). CrystEngComm , 14 , 6362-6365] is in close agreement with the results of this study. All adducts were characterized by X-ray diffraction and thermal analytical techniques, including single-crystal X-ray diffraction, powder X-ray diffraction, differential scanning calorimetry and thermal gravimetric analysis...
May 1, 2018: IUCrJ
Martina Tetti, Silvia Monticone, Jacopo Burrello, Patrizia Matarazzo, Franco Veglio, Barbara Pasini, Xavier Jeunemaitre, Paolo Mulatero
Liddle syndrome is an inherited form of low-renin hypertension, transmitted with an autosomal dominant pattern. The molecular basis of Liddle syndrome resides in germline mutations of the SCNN1A , SCNN1B and SCNN1G genes, encoding the α, β, and γ-subunits of the epithelial Na⁺ channel (ENaC), respectively. To date, 31 different causative mutations have been reported in 72 families from four continents. The majority of the substitutions cause an increased expression of the channel at the distal nephron apical membrane, with subsequent enhanced renal sodium reabsorption...
March 11, 2018: International Journal of Molecular Sciences
Amir M Ramezani, Ghodratollah Absalan, Raheleh Ahmadi
Bilayer pseudo-stationary phase micellar liquid chromatography (MLC) was developed for simultaneous isocratic isolation of hydrochlorothiazide, as a basic-polar (hydrophilic) cardiovascular drug, as well as triamterene and losartan potassium, as acidic-nonpolar (hydrophobic) cardiovascular drugs. Utilizing a deep eutectic solvent (DES), as a novel green mobile phase additive in combination with acetonitrile (ACN) and acetic acid (ACA), drastically improved the chromatographic behavior of the drugs. Concentration of sodium dodecyl sulphate (SDS), as well as volume percentages of ACN, DES, and ACA were optimized by using a central composite design...
June 20, 2018: Analytica Chimica Acta
Felipe Fantinato Hudari, João Carlos Souza, Maria Valnice Boldrin Zanoni
Hemodialysis is the most commonly used method for the treatment of chronic kidney disease. In this procedure, some patients use diuretics to control weight gain and blood pressure. In this work, a voltammetric sensor based on a glassy carbon electrode modified with carbon nanotubes (GCE/MWCNT) is described for the simultaneous determination of the diuretics hydrochlorothiazide (HCT) and triamterene (TRT). The oxidation of the diuretics on the GCE/MWCNT surface was observed at 1.01 and 1.17V for HCT and TRT, respectively, allowing simultaneous determination, which was not possible with the unmodified glassy carbon electrode...
March 1, 2018: Talanta
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