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Showing 1 to 18 of 18 for “"Acetaminophen (APAP)"”.
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Identification of Novel CYP2E1 Inhibitor to Investigate Cellular and Exosomal CYP2E1-Mediated Toxicity
… prevent xenobiotics such as alcohol- (ALC/ETH), acetaminophen- (APAP) induced toxicity and disease (e.g. HIV-1) pathogenesis. DAS imparts its beneficial effect by inhibiting CYP2E1-mediated metabolism of xenobiotics, especially at high concentration. However, DAS also causes toxicity at …
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Effects of API particle size on the dissolution rate in molten polymer excipient matrices during hot melt extrusion, conducted in a co-rotating twin-screw extruder
… with three different screw configurations. Acetaminophen (APAP) and amphiphilic polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PVCap-PVAc-PEG) (Soluplus) are chosen as the model API and water- soluble polymer excipient, respectively. APAP is milled using a fluid …
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Towards Fluorinated Substrate Analogs and N-Acylated 2-Aminopyrimidine Inhibitors of Lipoxygenases
… inflammatory drugs (NSAIDs) such as aspirin, acetaminophen (ApAP) and ibuprofen. However, there are still fundamental questions surrounding the LOX family of enzymes, which has limited the development of isoform specific inhibitors. The structural basis and regio- and stereoselectivity of the …
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Effects of acetaminophen on estrogen-responsive alkaline phosphatase in Ishikawa endometrial cancer cells
This study examines the effect of acetaminophen (APAP) on the estrogen-responsive gene alkaline phosphatase in Ishikawa endometrial cancer cells. Basal levels of alkaline phosphatase activity were significantly inhibited in cells treated with 0.03, 0.1, 0.3 and 1mM APAP compared to control. …
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The Effect of acetaminophen on isoniazid metabolism
Acetaminophen (APAP, paracetamol, N-acetyl-p-aminophenol), an analgesic and antipyretic drug, causes liver necrosis in overdose. Isoniazid (INH, isonicotinyl hydrazide), an antituberculous drug, also causes liver damage in some patients at therapeutic doses. The two medications are likely to be …
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Identification of Novel Regulatory Genes in Acetaminophen Induced Hepatocyte Toxicity by a Genome-Wide CRISPR/Cas9 Screen
Acetaminophen (APAP) is a commonly used analgesic responsible for over 56,000 overdose-related emergency room visits annually. A long asymptomatic period and limited treatment options result in a high rate of liver failure, generally resulting in either organ transplant or mortality. The underlying …
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Development and Characterization of Sustained-Release Formulations via Novel Hot Melt Extrusion Techniques
… (2) to prepare floating mini tablets of acetaminophen (APAP) with the hydrophobic carriers Eudragit® RL PO and Eudragit® RS PO by HME/P-CO2 and to evaluate the buoyancy efficiency through <em>in-vitro</em> methods. Moreover, scanning electron microscopy (SEM) was utilized to visually …
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Citrobacter rodentium induced liver changes in C57BL/6 mice : animal model of acute inflammatory stress and injury
… specific cytokine/chemokine profiles. Using Acetaminophen (APAP), a widely used analgesic and well-characterized hepatotoxin, we evaluated liver responses in isolation and in the context of host inflammation to gain insight into the role of live bacterial infection in altering liver …
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LATE PROTECTIVE EFFECTS OF NETRIN-1 AND ADENOSINE A2B RECEPTOR ACTIVATION IN THE MURINE ACETAMINOPHEN HEPATOTOXICITY MODEL
Acetaminophen (APAP) overdose causes severe hepatotoxicity and the current antidote N-acetylcysteine (NAC), has a narrow early therapeutic window. Since most patients present late to the clinic, novel late acting therapeutic options are needed. The neuronal guidance cue netrin-1 has been shown to …
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Application of raman spectroscopy in pharmaceuticals
… chapter, polymorphs of another model API, acetaminophen (APAP), were studied by Raman spectroscopy with supporting information obtained from x-ray diffraction, SEM images and intrinsic dissolution profiles. An important result was the stabilization and characterization of the metastable …
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Electrostatic powder deposition as a dry powder process to prepare orodispersible films
… physical mixtures and composite particles of acetaminophen (APAP) and PEO. Films prepared using a physical mixture exhibited significantly higher drug content variability. The active films exhibited favorable mechanical properties due to the plasticizing effect of APAP on PEO. Additionally, …
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Tabletability Flip of Drugs upon Formulation
… of TFP in dry granulated formulations using acetaminophen (APAP) and ibuprofen (IBU) as model APIs, which exhibit TFP in non-granulated blends. For the more porous granules (19% porosity), extensive fragmentation of granules during compaction preserved TFP observed in the pre-blends. In …
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Hot-melt mixing of partially miscible active pharmaceutical ingredient-polymer mixtures
… dissertation, solid dispersions of a model drug acetaminophen (APAP) and a pharmaceutical grade polymer poly(ethylene oxide) (PEO) were prepared by using hot- melt mixing (HMM), a process closely related to HME. APAP's solubility in PEO at HME processing temperature was measured utilizing a novel …
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ROLE OF DNA DAMAGE RESPONSE IN LIVER REGENERATION AFTER APAP OVERDOSE INDUCED ALF
Acetaminophen (APAP) overdose is a leading cause of acute liver failure (ALF) with limited treatment options. The mechanisms of APAP-induced liver injury include formation of a reactive metabolite N-acetyl-p-quinoneimine (NAPQI) and it’s covalent binding to protein, oxidative stress, mitochondrial …
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Hepatic stellate cell heterogeneity and function during the hepatic regenerative response
INTRODUCTION: Acetaminophen (APAP) poisoning is the commonest cause of acute liver failure (ALF) in the Western world1 and results in centrilobular hepatic necrosis. In non-severe cases the liver regenerates to normal microarchitecture and function. However, in severe APAP-induced ALF, …
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High-throughput approaches to sourcing of human hepatocytes for cell-based therapies
… of acute liver failure induced by overdose of acetaminophen (APAP), PH1 and FHl acted as hepatoprotectants that increased liver size, and in the case of FHi, rescued zebrafish survival. At sub-lethal concentrations (5mM APAP), the respective therapeutic windows of FHl and PHI both exceed that …
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Investigation of experimental cell lines and non-invasive online sensor technologies in a 3D bioreactor system for extracorporeal liver support therapy
… sessions, the effect of the hepatotoxic drug acetaminophen (APAP) was evaluated. The response of the cells to toxic drug exposure was successfully monitored by sensor-based measurements, confirming the results from B-13/H cultures. Based on the results a procedure for culture prediction and …
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In vivo Examination of Peripheral Drivers of Alzheimer’s Disease
<p>Alzheimer’s disease (AD) is the leading cause of dementia worldwide, and predominantly affects elderly populations. This disease is well known for its effects on the brain, but a wealth of clinical reports show that dementia can also modify, or be modified by, various peripheral and systemic …