AI Article Synopsis
Article Abstract
Introduction: Aprepitant is used for the treatment of chemotherapy induced nausea and vomiting. A liquid formulation is needed for treatment of young children. However, the commercial (powder for) suspension was not available worldwide for a prolonged period of time and, therefore, a 10 mg/mL aprepitant oral suspension was extemporarily prepared to prevent suboptimal antiemetic treatment. The current pharmacokinetic study was developed to investigate whether this extemporaneous oral suspension offers an appropriate treatment option.
Methods: From 49 pediatric patients (0.7-17.9 years) 235 plasma concentrations were collected. Patients were either treated with our extemporaneous oral suspension (n = 26; 53%), commercially available capsules (n = 18; 37%), or the intravenous prodrug formulation of aprepitant (fosaprepitant, n = 5; 10%). Pharmacokinetic analyses were performed using nonlinear mixed effects modelling.
Results: A one-compartment model adequately described the pharmacokinetics of aprepitant in children. The bioavailability of the extemporaneous oral suspension was not significantly different to that of the capsules (P = 0.26). The observed bioavailability throughout the total population was 83% (95% CI 69%-97%). The absorption of the extemporaneous oral suspension was 39.4% (95%CI 19.5-57.4%) faster than that of capsules (mean absorption time of 1.78 h (95%CI 1.32-2.35), but was comparable to that of the commercial oral suspension. The median area under the curve after (fos)aprepitant was 22.2 mg/L*h (range 8.9-50.3 mg/L*h) on day 1.
Conclusion: Our extemporaneous oral suspension is an adequate alternative for the commercially (un)available oral suspension in young children. An adequate exposure to aprepitant in children was yielded and the bioavailability of the extemporaneous suspension was comparable to capsules.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1177/10781552221089243 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
[Survey on the Size of Oral Anticancer Drugs].
Gan To Kagaku Ryoho
December 2024
Dept. of Pharmacy, Tokyo Metropolitan Bokutoh Hospital.
Oral anticancer drugs are standard treatments for many cancers and are expected to remain widely used. Owing to the super-aged nature of the Japanese society, the number of elderly patients with cancer is rapidly increasing. Poor adherence to oral medications owing to physical limitations and swallowing difficulties in elderly patients with cancer is a major problem affecting treatment.
View Article and Find Full Text PDFMass Balance Recovery, Absorption, Metabolism, and Excretion of Elinzanetant in Healthy Human Volunteers and in vitro Biotransformation.
Eur J Drug Metab Pharmacokinet
December 2024
Preclinical Development-Drug Metabolism and Pharmacokinetics, Bayer AG, Berlin, Germany.
Background: Elinzanetant is a dual neurokinin-1,3 receptor antagonist in development for the treatment of menopausal vasomotor symptoms. The objectives of these studies were to characterize the mass balance and biotransformation of elinzanetant.
Methods: In the clinical evaluation, whole blood, plasma, urine, and feces were collected from healthy fasted male volunteers (n = 6) following a single dose of 120 mg [C]-elinzanetant oral suspension for analysis of total radioactivity and metabolite profiling.
Efficacy of azithromycin combined with compounded atovaquone in treating babesiosis in giant pandas.
Parasit Vectors
December 2024
Sichuan Key Laboratory of Conservation Biology for Endangered Wildlife, Chengdu Research Base of Giant Panda Breeding, Chengdu, 610000, Sichuan, China.
Background: Babesia is a tick-borne protozoan blood parasite that can cause hemolytic anemia, thrombocytopenia, lethargy and splenomegaly in giant pandas.
Methods: We evaluated the efficacy and safety profile of a therapeutic regimen combining atovaquone and zithromycin in the context of babesiosis in giant pandas that have been naturally infected. The examined pandas underwent clinical and laboratory analyses, including hematology, biochemistry and thyroid hormone profiles.
Proteomic Analysis of Biological Fluids.
Methods Mol Biol
December 2024
Department of Environmental Toxicology, The University of California, Davis, Davis, CA, USA.
Biological fluids are proteinaceous liquids or suspensions released through different body orifices or through penetration of the skin. These fluids are the result of multiple tissues and cell types and contain extensive, highly complex, and dynamic protein populations that reflect both the transcriptional program of the originating cells and a record of the individual's health status. Body fluids are readily accessible to clinicians and researchers, and as such proteomic analyses are an important component of clinical studies, fertility studies, oral health studies, and forensic investigations.
View Article and Find Full Text PDFA Phase 1, Open-Label, Randomized, Two-Part Study in Healthy Adult Volunteers to Evaluate the Bioavailability of the Maribavir Powder for Oral Suspension, as Well as Food Effect and Impact of Rabeprazole.
Clin Pharmacol Drug Dev
December 2024
Takeda Development Center Americas, Inc., Cambridge, MA, USA.
The relative bioavailability and impact of food and the proton pump inhibitor rabeprazole on the pharmacokinetics of a maribavir powder-for-oral-suspension formulation was investigated in a Phase 1 open-label study in healthy adult volunteers. A single 200-mg maribavir dose was administered as the commercial tablet (Treatment A), powder formulation (Treatment B), or powder formulation with a high-fat/high-calorie meal (Treatment C) in Part 1, and as the powder formulation alone (Treatment D) or following administration of rabeprazole 20 mg once daily for 5 days (Treatment E) in Part 2. Maribavir maximum plasma concentration following Treatment B was 18% lower versus Treatment A, whereas the area under the concentration-time curve (AUC) from time 0 to the last quantifiable concentration or infinity were similar.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!