scholarly journals Pharmacokinetic modelling of the plasma concentration-time profile of the vitamin retinyl palmitate following intramuscular administration

1990 ◽  
Vol 11 (8) ◽  
pp. 689-700 ◽  
Author(s):  
D. Hartmann ◽  
D. Gysel ◽  
U. C. Dubach ◽  
I. Forgo
Keyword(s):  
Plasma Concentration ◽  
Retinyl Palmitate ◽  
Time Profile ◽  
Intramuscular Administration ◽  
Pharmacokinetic Modelling ◽  
Concentration Time

scholarly journals Predicting Method for the Human Plasma Concentration–Time Profile of a Monoclonal Antibody from the Half-life of Non-human Primates

2020 ◽  
Vol 43 (5) ◽  
pp. 823-830 ◽  
Author(s):  
Genki Nakamura ◽  
Kazuhisa Ozeki ◽  
Miho Nagayasu ◽  
Takeru Nambu ◽  
Takayuki Nemoto ◽  
...  
Keyword(s):  
Monoclonal Antibody ◽  
Plasma Concentration ◽  
Human Plasma ◽  
Half Life ◽  
Time Profile ◽  
Concentration Time

scholarly journals Comparison of Dissolution Profile and Plasma Concentration-time Profile of the Thalidomide Formulations Made by Japanese, Mexican and British Companies

2008 ◽  
Vol 128 (10) ◽  
pp. 1449-1457 ◽  
Author(s):  
Yukiyoshi FUJITA ◽  
Koujirou YAMAMOTO ◽  
Tohru AOMORI ◽  
Hirokazu MURAKAMI ◽  
Ryuya HORIUCHI
Keyword(s):  
Plasma Concentration ◽  
Time Profile ◽  
Dissolution Profile ◽  
Concentration Time

scholarly journals Effects of Intestinal Microecology on Metabolism and Pharmacokinetics of Oral Wogonoside and Baicalin

2017 ◽  
Vol 12 (4) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Shihua Xing ◽  
Mengyue Wang ◽  
Ying Peng ◽  
Xiaobo Li
Keyword(s):  
Plasma Concentration ◽  
Herbal Medicine ◽  
Intestinal Microbiota ◽  
Time Profile ◽  
Flavonoid Glycosides ◽  
Pharmacokinetic Parameters ◽  
Clinical Use ◽  
Scutellaria Baicalensis Georgi ◽  
Concentration Time ◽  
The Difference

Baicalin and wogonoside are two of the most abundant flavonoid glycosides in the root of Scutellaria baicalensis Georgi, which is a widely used peroral herbal medicine with anticancer, antiviral, antibacterial and anti-inflammatory properties. In the present study, the effects of intestinal microecology on the metabolism and pharmacokinetics of orally administered baicalin and wogonoside were investigated by UPLC-QTOF/MS measurement of the difference in metabolites between normal and antibiotic-pretreated rats. In the antibiotic-pretreated rats, the plasma concentration-time profile and pharmacokinetic parameters of the two flavonoid glycosides and their relevant aglycone forms were significantly changed compared with those in normal rats. Further, hydrolysis and glucuronidated metabolites were not detected in the cecum contents and urine samples from antibiotic-pretreated rats. These results suggested that intestinal microbiota may play a key role in the pharmacokinetics and metabolism of peroral baicalin and wogonoside. According to our findings, it is recommended that the root of S. baicalensis should not be co-administered with antibiotics in clinical use.

scholarly journals Improvement of the Bioavailability and Glycaemic Metabolism of Cinnamon Oil in Rats by Liquid Loadable Tablets

2012 ◽  
Vol 2012 ◽  
pp. 1-6 ◽  
Author(s):  
Chunchao Han ◽  
Bo Cui
Keyword(s):  
Insulin Secretion ◽  
Blood Glucose ◽  
Plasma Concentration ◽  
Time Profile ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Pharmacokinetic Parameters ◽  
Cinnamon Oil ◽  
Concentration Time

The purpose of this study is to investigate the bioavailability and glycaemic metabolism of cinnamon oil (CIO) carried by liquid-loadable tablets (CIO-LLTs), the carrier of a CIO self-emulsifying formulation (CIO-LS). The results of tests performed to evaluate the physical properties of the CIO-LLT complied with Chinese Pharmacopeia (2010). The release profile suggested that the CIO-LLT preserved the enhancement of in vitro dissolution of cio. After orally administration, the plasma concentration-time profile and pharmacokinetic parameters suggested that a significant increase (P<0.0001) in theCmax, AUC andFwere observed in the CIO-LLT. The blood glucose and the HbA1c were significantly decreased in alloxan-induced hyperglycemic rats (P<0.05,P<0.01, resp.), while the level of insulin secretion was markedly elevated in alloxan-induced hyperglycemic rats (P<0.05). The alloxan-damaged pancreaticβ-cells of the rats were partly recovered gradually after the rats were administered with CIO-LLT 45 days later. CIO-LLT could improve the bioavailability and glycaemic metabolism of CIO.

scholarly journals Physiologically Based Pharmacokinetic Modeling of Cefadroxil in Mouse, Rat, and Human to Predict Concentration–Time Profile at Infected Tissue

2021 ◽  
Vol 12 ◽  
Author(s):  
Zhongxia Tan ◽  
Youxi Zhang ◽  
Chao Wang ◽  
Le Sun
Keyword(s):  
Plasma Concentration ◽  
Pbpk Model ◽  
Oral Absorption ◽  
Time Profile ◽  
Infected Tissue ◽  
Dose Selection ◽  
Pbpk Models ◽  
Physiologically Based Pharmacokinetic ◽  
Concentration Time ◽  
Physiologically Based

The aim of this study was to develop physiologically based pharmacokinetic (PBPK) models capable of simulating cefadroxil concentrations in plasma and tissues in mouse, rat, and human. PBPK models in this study consisted of 14 tissues and 2 blood compartments. They were established using measured tissue to plasma partition coefficient (Kp) in mouse and rat, absolute expression levels of hPEPT1 along the entire length of the human intestine, and the transporter kinetic parameters. The PBPK models also assumed that all the tissues were well-stirred compartments with perfusion rate limitations, and the ratio of the concentration in tissue to the unbound concentration in plasma is identical across species. These PBPK models were validated strictly by a series of observed plasma concentration–time profile data. The average fold error (AFE) and absolute average fold error (AAFE) values were all less than 2. The models’ rationality and accuracy were further demonstrated by the almost consistent Vss calculated by the PBPK model and noncompartmental method, as well as the good allometric scaling relationship of Vss and CL. The model suggests that hPEPT1 is the major transporter responsible for the oral absorption of cefadroxil in human, and the plasma concentration–time profiles of cefadroxil were not sensitive to dissolution rate faster than T85% = 2 h. The cefadroxil PBPK model in human is reliable and can be used to predict concentration–time profile at infected tissue. It may be useful for dose selection and informative decision-making during clinical trials and dosage form design of cefadroxil and provide a reference for the PBPK model establishment of hPEPT1 substrate.

scholarly journals P85 Prediction of raltegravir plasma concentration in HIV paediatric patients using physiologically-based pharmacokinetic model

2019 ◽  
Vol 104 (6) ◽  
pp. e52.2-e53
Author(s):  
F Salem ◽  
K Abduljalil ◽  
T Johnson
Keyword(s):  
Plasma Concentration ◽  
Geometric Mean ◽  
Time Profile ◽  
Metabolic Enzyme ◽  
List Type ◽  
Physiologically Based Pharmacokinetic ◽  
Concentration Time ◽  
Paediatric Patients ◽  
Age Related ◽  
Rate Of Absorption

BackgroundRaltegravir is a drug used to treat patients with HIV infection. Understanding the disposition kinetics including the ontogeny of the major metabolic enzyme (UGT1A1) is important in prediction of raltaeravir pharmacokinetics in paediatric patients.MethodsSim-Raltegravir compound file in Simcyp simulator version 18 was used to predict pharmacokinetics in paediatric subjects aged 4 weeks to 6 months, 0.5 to 2, 2 to 6 and 6 to 12 years. Details of trial design were matched as closely as possible with a clinical study.1 Rate of absorption and variability in first order absorption model within Simcyp were set to the reported values. Predicted plasma concentration time profiles with 5th and 95th percentile were compared with observations.ResultsThe predicted vs. observed geometric mean area under plasma concentration-time profile of raltegravir was 18.4 vs. 22.3 µM.h in subjects 4 weeks to 6 months and 16.5 vs. 19.8 µM.h in those 0.5 to 2 years old. In 2 to 6 and 6 to 12 year olds around 80% and 85% of observed data were within 5th and 95th percentile of the predictions.ConclusionThe results show that the UGT1A1 ontogeny profile in the Simcyp version 18 adequately addressed age-related differences in pharmacokinetics of raltegravir.ReferenceRizk, M., et al, J Clin Pharmacol 2015; 55(7):748–56Disclosure(s)Nothing to disclose

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