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About 166,163 results

Comparative Pharmacology of the 3 Marketed Dual Orexin Antagonists-Daridorexant, Lembor...
https://doi.org/10.1097/PRA.0000000000000690
Journal of Psychiatric Practice; Preskorn SH

Jan 18th, 2023 - This column is the second in a 2-part series presenting the comparative pharmacology of the 3 Food and Drug Administration-approved dual orexin receptor antagonists, daridorexant, lemborexant, and suvorexant. Both of the columns in this series emphasize the pharmacokinetics of these drugs as they are relevant to their use as sleep medications. Although other classes of sleep medications are not...

Population Pharmacokinetic and Pharmacokinetic/Pharmacodynamic Target Attainment Analys...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9835671
The Pediatric Infectious Disease Journal; Carrothers TJ, Lagraauw HM et. al.

Jan 14th, 2023 - Dalbavancin, approved for the treatment of pediatric and adult patients with acute bacterial skin and skin structure infections, has a terminal half-life of >14 days allowing administration as a single-dose regimen. We developed a population pharmacokinetic (PK) model using 1124 dalbavancin concentrations from 211 pediatric patients, with allometric scaling of clearance and volume parameter exp...

In Vivo Evaluation of Almotriptan malate Formulation through Intranasal Route for the T...
https://doi.org/10.1208/s12249-022-02496-2
AAPS PharmSciTech; Gupta S, Perla A et. al.

Jan 11th, 2023 - Migraine headaches are usually intolerable, and a quick-relief treatment remains an unmet medical need. Almotriptan malate is a serotonin (5-HT1B/1D) receptor agonist approved for the treatment of acute migraine in adults. It is currently available in an oral tablet dosage form and has a Tmax of 1-3 h, and therefore, there is a medical need to develop a non-invasive rapidly acting formulation. ...

Safety and Tolerability of Tecarfarin (ATI-5923) in Healthy Chinese Volunteers: Multipl...
https://doi.org/10.1007/s40256-022-00562-5
American Journal of Cardiovascular Drugs : Drugs, Devices... Zhou Q, Wang Z et. al.

Jan 10th, 2023 - Tecarfarin (ATI-5923), a structural analog of warfarin, was designed to provide more uniform and stable anticoagulation. We aimed to evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic profile of tecarfarin when administered in multiple ascending doses (MADs) to healthy Chinese volunteers. Forty healthy Chinese volunteers were enrolled into four sequential cohorts (10, 20, 30...

Evaluation of Empirical Dosing Regimens for Meropenem in Intensive Care Unit Patients U...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9872596
Antimicrobial Agents and Chemotherapy; An G, Creech CB et. al.

Jan 10th, 2023 - In the present study, population pharmacokinetic (PK) analysis was performed based on meropenem data from a prospective study conducted in 114 critically ill patients with a wide range of renal functions and various disease conditions. The final model was a one-compartment model with linear elimination, with creatinine clearance and continuous renal replacement therapy affecting clearance, and ...

Population Pharmacokinetics and Dosage Optimization of Vancomycin in Pediatric Patients...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9879599
Antimicrobial Agents and Chemotherapy; Lv M, Yang P et. al.

Jan 10th, 2023 - Vancomycin is recommended for the treatment of skin and soft tissue infections (SSTI) and bone and joint infections (BJI). However, a detailed investigation of the pharmacokinetic profile and optimal dosing regimens of vancomycin in pediatric patients with SSTI and BJI is lacking. We successfully developed a new PopPK model of vancomycin in this population by using scavenged blood samples with ...

Processability and Oral Bioavailability Improvement of Itraconazole by Particle Enginee...
https://doi.org/10.1208/s12249-022-02486-4
AAPS PharmSciTech; Kapalatiya H, Patel D et. al.

Dec 29th, 2022 - The current study aimed to improve the processability and oral bioavailability of itraconazole (ITZ) via spherical agglomeration. ITZ-spherical agglomerates (ITZ-SA) and ITZ-poloxamer 407-spherical agglomerates (ITZ-PLX-SA) were optimized using Box-Behnken design. Here, the drug release was affected by polymer concentration and stirring speed, whereas particle size was altered by stirring speed...

Preparation and Optimization of Liposome Containing Thermosensitive In Situ Nasal Hydro...
https://doi.org/10.1089/adt.2022.088
Assay and Drug Development Technologies; Mathure D, Sutar AD et. al.

Dec 29th, 2022 - Drug absorption is improved by the intranasal route's wide surface area and avoidance of first-pass metabolism. For the treatment of central nervous system diseases such as migraine, intranasal administration delivers the medication to the brain. The study's purpose was to develop an in situ nasal hydrogel that contained liposomes that were loaded with sumatriptan succinate (SS). A thin-film hy...

Effect of Rifampicin on the Pharmacokinetics of Evogliptin in Healthy Volunteers.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9789683
Drug Design, Development and Therapy; Shin Y, Choi C et. al.

Dec 28th, 2022 - Evogliptin (DA-1229) is a novel, potent, and selective dipeptidyl peptidase 4 (DPP-4) inhibitor for treating type 2 diabetes mellitus. This study investigates the effect of rifampicin on evogliptin pharmacokinetics. An open-label, crossover, one-sequence study was conducted on 12 healthy subjects. Reference baseline pharmacokinetic samples were collected on day 1 after the subjects were adminis...

Physiologically based modelling of dermal absorption and kinetics of consumer-relevant ...
https://doi.org/10.1016/j.taap.2022.116357
Toxicology and Applied Pharmacology; Wiśniowska B, Linke S et. al.

Dec 27th, 2022 - Bisphenol A (BPA) is one of the best studied industrial chemicals in terms of exposure, toxicity, and toxicokinetics. This renders it an ideal candidate to exploit the recent advancements in physiologically based pharmacokinetic (PBPK) modelling to support risk assessment of BPA specifically, and of other consumer-relevant hazardous chemicals in general. Using the exposure from thermal paper as...

Pharmacokinetics and tissue distribution of deferoxamine-based nanochelator in rats.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9869290
Nanomedicine (London, England); Jones G, Zeng L et. al.

Dec 23rd, 2022 - Aim: To characterize the pharmacokinetics of deferoxamine-conjugated nanoparticles (DFO-NPs), a novel nanochelator for removing excess iron. Materials & methods: The pharmacokinetics of DFO-NPs were evaluated in Sprague-Dawley rats at three doses (3.3, 10 and 30 μmol/kg) after intravenous and subcutaneous administration. Results: DFO-NPs exhibited a biphasic concentration-time profile after int...

Clinical Impact of Melphalan Pharmacokinetics on Transplantation Outcomes in Children U...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9772935
Cell Transplantation; Maemura R, Wakamatsu M et. al.

Dec 21st, 2022 - Melphalan is widely used for hematopoietic stem cell transplantation (HSCT) conditioning. However, the relationship between its pharmacokinetic (PK) and transplantation outcomes in children has not been thoroughly investigated. We prospectively analyzed the relationship between melphalan area under the curve (AUC) and transplantation outcome and examined the development of a predictive model fo...

Encapsulation Dynamics of Neuromuscular Blocking Drugs by Sugammadex.
https://doi.org/10.1097/ALN.0000000000004442
Anesthesiology Irani AH, Voss L et. al.

Dec 14th, 2022 - The clinical actions of sugammadex have been well studied, but the detailed molecular mechanism of the drug encapsulation process has not been systematically documented. The hypothesis was that sugammadex would attract rocuronium and vecuronium via interaction with the sugammadex side-chain "tentacles," as previously suggested. Computational molecular dynamics simulations were done to investiga...

Brain pharmacokinetics of mono- and bispecific amyloid-β antibodies in wild-type and Al...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9743601
Fluids and Barriers of the CNS; Julku U, Xiong M et. al.

Dec 13th, 2022 - Treatment with amyloid-β (Aβ) targeting antibodies is a promising approach to remove Aβ brain pathology in Alzheimer's disease (AD) and possibly even slow down or stop progression of the disease. One of the main challenges of brain immunotherapy is the restricted delivery of antibodies to the brain. However, bispecific antibodies that utilize the transferrin receptor (TfR) as a shuttle for tran...

Pharmacokinetics and Safety of Follitropin Delta in Gonadotropin Down-Regulated Healthy...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9834375
Clinical Drug Investigation; Shao F, Jiang Y et. al.

Dec 9th, 2022 - Follitropin delta, a novel recombinant follicle-stimulating hormone (rFSH) preparation derived from a human cell line, has different pharmacokinetic and pharmacodynamic properties compared with existing rFSH preparations expressed by Chinese hamster ovary cells (CHO). The objective of this study was to assess the pharmacokinetic characteristics, dose proportionality, and safety of follitropin d...

Pharmacokinetic, Safety, and Tolerability Evaluations of Gepotidacin (GSK2140944) in He...
https://doi.org/10.1002/cpdd.1192
Clinical Pharmacology in Drug Development; Barth A, Hossain M et. al.

Dec 6th, 2022 - Gepotidacin is a novel, bactericidal, first-in-class triazaacenaphthylene antibiotic in late-phase development for uncomplicated urinary tract infection and uncomplicated urogenital gonorrhea. Two clinical studies were conducted to assess the pharmacokinetics (PK) and interethnic comparisons of oral gepotidacin (free-base and to-be-marketed mesylate formulations) administered as single doses ra...

Exposure and virologic outcomes of dolutegravir combined with ritonavir boosted darunav...
https://doi.org/10.1016/j.ijantimicag.2022.106697
International Journal of Antimicrobial Agents; Prins HAB, Zino L et. al.

Dec 6th, 2022 - To the authors' knowledge, there is currently no literature or guidance recommendation regarding whether the dose of dolutegravir (DTG) should be increased when co-administered with darunavir/ritonavir (DRV/r) in patients with acute human immunodeficiency virus infection (AHI). This study assessed the pharmacokinetics (PK) of twice-daily (BID) DTG and once-daily (QD) DRV/r, and compared this wi...

Modulating the pharmacokinetic profile of Actinium-225-labeled macropa-derived radiocon...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9691366
Theranostics Reissig F, Zarschler K et. al.

Nov 29th, 2022 - Rationale: Small 225Ac-labeled prostate-specific membrane antigen (PSMA)-targeted radioconjugates have been described for targeted alpha therapy of metastatic castration-resistant prostate cancer. Transient binding to serum albumin as a highly abundant, inherent transport protein represents a commonly applied strategy to modulate the tissue distribution profile of such low-molecular-weight radi...

Pharmacokinetic characteristics of emodin in polygoni Multiflori Radix Praeparata.
https://doi.org/10.1016/j.jep.2022.115945
Journal of Ethnopharmacology; Wang D, Duan J et. al.

Nov 27th, 2022 - Polygoni Multiflori Radix Praeparata (Zhiheshouwu) has been a Wudang Taoist medicine for tonifying the liver and kidney, resolving turbidity and reducing lipid. Emodin is one of the active anthraquinones in Zhiheshouwu. Our previous studies showed that emodin (EM) and the other anthraquinones in Zhiheshouwu extract (HSWE) exerted similar inhibitory effects on liver cancer cells in vitro. Howeve...

Clinical outcomes of low-dose pharmacokinetic-guided extended half-life versus low-dose...
https://doi.org/10.1111/hae.14700
Haemophilia : the Official Journal of the World Federatio... Rakmanotham A, Moonla C et. al.

Nov 22nd, 2022 - Despite receiving standard half-life (SHL) factor VIII (FVIII) concentrates prophylaxis, some severe haemophilia A (HA) patients still encounter spontaneous breakthrough bleeding. Individualized pharmacokinetic (PK)-guided dosing of extended half-life (EHL) FVIII concentrates may reduce their bleeding events. To compare clinical outcomes before and after switching low-dose prophylaxis using wei...