The effect of reduced gastric acid secretion on the gastrointestinal disposition of a ritonavir amorphous solid dispersion in fasted healthy volunteers: an in vivo – in vitro investigation.

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This paper summarizes efforts to (i) better understand the behavior of amorphous solid dispersions (ASDs) under real-life dosing conditions and (ii) evaluate the capability of in vitro methodologies to capture […]

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Converting a batch based high-shear granulation process to a continuous dry granulation process; a demonstration with ketoprofen tablets.

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When one wishes to convert a batch based manufacturing process of an existing tablet product to a continuous process, there are several available strategies which can be adopted. Theoretically, the […]

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6-hydroxydopamine lesion and levodopa treatment modify the effect of buspirone in the substantia nigra pars reticulata.

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Abnormal involuntary movements known as L-3,4-dihydroxyphenylalanine (L-DOPA)-induced dyskinesia (LID) are considered a major complication of the pharmacological treatment in Parkinson’s disease (PD). Serotonin (5-HT)-based drugs such as buspirone, a 5-HT1A […]

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Prediction of drug exposure in critically ill encephalopathic neonates treated with therapeutic hypothermia based on a pooled population pharmacokinetic analysis of seven drugs and five metabolites.

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Drug dosing in encephalopathic neonates treated with therapeutic hypothermia is challenging; exposure is dependent on body size and maturation but can also be influenced by factors related to disease and […]

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How to Transition from Single Gene Pharmacogenetic Testing to Preemptive Panel-Based Testing: A Tutorial.

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There have been significant advancements in precision medicine and approaches to medication selection based on pharmacogenetic results. With the availability of direct-to-consumer genetic testing and growing awareness of genetic inter-individual […]

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Intestinal P-gp and Putative Hepatic OATP1B Induction: ITC Perspective on Drug Development Implications.

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There is an increasing interest in transporter induction (i.e., decreased systemic drug exposure due to increased efflux-limited absorption or transporter-mediated clearance) as a mechanism of drug-drug interactions (DDIs), although evidence […]

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Interpretation of Cytochrome P-450 Inhibition and Induction Effects from Clinical Data: Current Standards and Recommendations for Implementation.

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Agents that modify cytochrome P-450 (CYP) enzyme activity are characterized as strong, moderate, or weak inhibitors or inducers based on the magnitude of their impact on substrate exposure in clinical […]

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Genetic association of co-trimoxazole-induced severe cutaneous adverse reactions is phenotype-specific: HLA class I genotypes and haplotypes.

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Co-trimoxazole (CTX) causes various forms of severe cutaneous adverse reactions (SCARs). This case-control study was conducted to investigate the involvement between genetic variants of human leukocyte antigen (HLA) and CYP2C9 […]

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Population pharmacokinetic/pharmacodynamic modelling of nifekalant in healthy Chinese volunteers.

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Nifekalant is a class III antiarrhythmic drug, and its major adverse effect is prolongation of the QT interval. This study analysed data generated from a pharmacokinetic (PK) study to develop […]

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Rac1: A Potential Radiosensitization Target of Human Nasopharyngeal Carcinoma CNE2 Cells.

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Radiotherapy has a high cure rate for early nasopharyngeal carcinoma(NPC). However, the radiation resistance of poorly differentiated NPC cells impacts the effectiveness of treatment of early-stage NPC patients. Here, we […]

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Safety and Effectiveness of Sedation With Adjunctive Ketamine Versus Nonketamine Sedation in the Medical Intensive Care Unit.

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Ketamine, an N-methyl-d-aspartate receptor antagonist with sedative and analgesic properties, is becoming more popular as an adjunctive sedative in the critically ill patients.We conducted a single center, retrospective cohort study […]

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Improved surface adhesion and wound healing effect of madecassoside liposomes modified by temperature-responsive PEG-PCL-PEG copolymers.

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Madecassoside (MA) exhibits excellent therapeutic effects in wound healing and scar management. However, its high hydrophilic nature and low permeability through skin tissue limits its topical application. Liposomes are widely […]

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REGULATION OF GENE EXPRESSION BY MF63, A SELECTIVE INHIBITOR OF INDUCIBLE PROSTAGLANDIN E SYNTHASE-1 (mPGES-1) IN HUMAN OSTEOARTHRITIC CHONDROCYTES.

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mPGES-1 catalyzes the production of prostaglandin E2 (PGE2 ), the most abundant prostanoid related to inflammation and pain in arthritis. mPGES-1 is suggested to be a safer and more selective […]

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Pyridine and quinoline molecules as crucial protagonists in the never-stopping discovery of new agents against tuberculosis.

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Tuberculosis (TB) disease remains to be an alarming infection worldwide with nearly 1.6 million deaths per year ranking above HIV/AIDS. Although Mycobacterium tuberculosis (Mtb), which causes TB, was identified more […]

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Mucoadhesive emulgel systems containing curcumin for oral squamous cell carcinoma treatment: from pre-formulation to cytotoxicity in tissue-engineering oral mucosa.

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Current oral squamous cell carcinoma chemotherapies demonstrate off-target toxicity, which could be reduced by local delivery. Curcumin acts via many cellular targets to give anti-cancer properties; however the bioavailability is […]

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Enhancing the oral bioavailability of simvastatin with silica-lipid hybrid particles: The effect of supersaturation and silica geometry.

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Silica-lipid hybrid (SLH) microparticles are a solidified lipid-based drug delivery system under investigation for their aptitude to enhance the oral bioavailability of poorly water-soluble drugs. The cholesterol-lowering agent, simvastatin (SIM), […]

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From real-world patient data to individualized treatment effects using machine learning: Current and future methods to address underlying challenges.

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Clinical decision making needs to be supported by evidence that treatments are beneficial to individual patients. While randomized control trials are the gold standard for testing and introducing new drugs, […]

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Physiologically based pharmacokinetic model outputs depend on dissolution data and their input: case examples glibenclamide and dipyridamole.

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A plethora of dissolution tests exists for oral dosage forms, with variations in selection of the dissolution medium, the hydrodynamics and the dissolution equipment. This work aimed at determining the […]

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Effect of Selective IK,ACh Inhibition by XAF-1407 in an Equine Model of Tachypacing-induced Persistent Atrial Fibrillation (AF).

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Inhibition of the G-protein gated acetylcholine-activated inward rectifier potassium (K+ ) current, IK,ACh , may be an effective atrial selective treatment strategy for atrial fibrillation. Therefore, the anti-arrhythmic and electrophysiological […]

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A physiologically based pharmacokinetic – pharmacodynamic modelling approach to predict incidence of neutropenia as a result of drug-drug interactions of paclitaxel in cancer patients.

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Paclitaxel is the backbone of standard chemotherapeutic regimens used in a number of malignancies and is frequently given with concomitant medications. Newly developed oncolytic agents, including tyrosine kinase inhibitors are […]

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