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Effect of Food on Pharmacokinetics of an Inhaled Drug: A Case Study with a VLA‐4 Antagonist, HMR1031
TLDR
It is suggested that food unexpectedly decreases the systemic exposure of inhaled HMR1031 by ∼30%, probably due to increased liver blood flow and increased biliary excretion.
In vitro and in vivo metabolism of a novel chymase inhibitor, SUN13834, and the predictability of human metabolism using mice with humanized liver
TLDR
In vitro and in vivo metabolic profiles of SUN13834 were compared between severe combined immunodeficiency mice, chimeric mice with humanized liver and humans, and it was concluded that Chimeric mice are useful for predicting SUN138 34 metabolism in humans during early stages of drug development.
Mass Balance Study of [14C]M100240, a Dual Angiotensin-Converting Enzyme/Neutral Endopeptidase Inhibitor, in Healthy Male Subjects
TLDR
The apparent terminal elimination half-life of MDL 100,173 was longer than that of 14C-radioactivity, attributable to assay sensitivity and the saturable binding phenomenon commonly associated with angiotensin-converting enzyme inhibitors.
Development of a Dry Powder Inhaler, the Ultrahaler®, Containing Triamcinolone Acetonide Using In Vitro-In Vivo Relationships
TLDR
In vitro and in vivo data were in agreement and good control over the target-dose delivery and dose proportionality could be achieved in the early stages of the development of the Ultrahaler®.
A Pharmacokinetic Study to Evaluate the Absolute Bioavailability of Triamcinolone Acetonide following Inhalation Administration
TLDR
Delineation of the airway contribution of triamcinolone acetonide absorption showed that 10.4% of an inhaled dose is absorbed as triaminolone Acetonide from the lungs, higher than the mean (± SD) absolute bioavailability value.
A Study Comparing the Clinical Pharmacokinetics, Pharmacodynamics, and Tolerability of Triamcinolone Acetonide HFA‐134a Metered‐Dose Inhaler and Budesonide Dry‐Powder Inhaler following Inhalation
TLDR
The study drugs were well tolerated, with adverse events characterized as mild to moderate in severity, and chronic dosing did result in a statistically significant 20% reduction in basal 24‐hour serum cortisol AUC for both compounds.
Pharmacokinetics, Pharmacodynamics, and Safety of a Lipid-Lowering Adenosine A1 Agonist, RPR749, in Healthy Subjects
TLDR
RPR7 49 has the ability to reduce circulating levels of FFA that can be related to plasma RPR749 concentrations and thus possesses pharmacological properties that may be beneficial in treating coronary artery diseases and hyperlipidemia.
Pharmacoscintigraphic Comparison of HMR 1031, a VLA-4 Antagonist, in Healthy Volunteers Following Delivery Via a Nebulizer and a Dry Powder Inhaler
TLDR
The lung deposition of HMR 1031 after administration by Ultrahaler was approximately 37% higher compared with the lung deposition from the nebulizer, in agreement with the relative difference in the plasma AUC values achieved after administration of the two formulations.
Pharmacokinetics, Safety, and Tolerability of Single Intravenous Infusions of an Adenosine Agonist, AMP 579, in Healthy Male Volunteers
TLDR
The pharmacokinetics of an adenosine agonist, AMP 579, following intravenous administration were evaluated to allow the design of dosage regimens that would maximize plasma AMp 579 concentrations and minimize the incidence of adverse events.
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