scholarly journals Absorption and Elimination of Oat Avenanthramides in Humans after Acute Consumption of Oat Cookies

2017 ◽  
Vol 2017 ◽  
pp. 1-7 ◽  
Author(s):  
Tianou Zhang ◽  
Jing Shao ◽  
Yike Gao ◽  
Chi Chen ◽  
Dan Yao ◽  
...  
Keyword(s):  
Half Life ◽  
Plasma Concentrations ◽  
Elimination Rate ◽  
Pharmacokinetic Parameters ◽  
Oral Ingestion ◽  
Blood Samples ◽  
Oral Consumption ◽  
Maximal Plasma ◽  
Oat Flour ◽  
Antioxidant Effects

Background. Avenanthramides (AVA) are a group of diphenolic acids found only in oats that have anti-inflammatory and antioxidant effects. Absorption of AVAs in humans after oral consumption of natural oat flour is unknown.Objective. To examine the appearance of AVAs in plasma after oral ingestion of oat cookies and estimate key pharmacokinetic parameters.Methods. Male and female nonobese participants (n=16) consumed three cookies made with oat flour containing high (229.6 mg/kg, H-AVA) or low (32.7 mg/kg, L-AVA) amounts of AVAs, including AVA-A, AVA-B, and AVA-C. Blood samples were collected at 0, 0.5, 1, 2, 3, 5, and 10 h after ingestion. Plasma total (conjugated and free) AVA concentrations were quantified using UPLC-MS, and pharmacokinetic parameters for each AVA were estimated.Results. AVAs reached peak concentrations in plasma between 2 and 3 h for the H-AVA group and between 1 and 2 h for the L-AVA group. Maximal plasma concentrations for AVAs were higher in the H-AVA than in the L-AVA group. AVA-B demonstrated a longer half-life and slower elimination rate than AVA-A and AVA-C.Conclusions. AVAs found naturally in oats are absorbed in the plasma after oral administration in humans. AVA-B has the slowest elimination rate and the longest half-life compared to AVA-A and AVA-C, while AVA-C demonstrated the lowest plasma concentrations. This study is registered with ClinicalTrials.gov identifierNCT02415374.

Concentration–Effect Relation of Succinylcholine Chloride during Propofol Anesthesia

2002 ◽  
Vol 97 (5) ◽  
pp. 1082-1092 ◽  
Author(s):  
Julie J. Roy ◽  
François Donati ◽  
Daniel Boismenu ◽  
France Varin
Keyword(s):  
Rate Constant ◽  
Plasma Concentrations ◽  
Elimination Rate ◽  
Quantitative Model ◽  
Concentration Effect ◽  
Pharmacokinetic Parameters ◽  
Effect Compartment ◽  
Duration Of Action ◽  
Arterial Blood ◽  
Effect Relation

Background The pharmacokinetics and pharmacodynamics of succinylcholine were studied simultaneously in anesthetized patients to understand why the drug has a rapid onset and short duration of action. A quantitative model describing the concentration-effect relation of succinylcholine was proposed. The correlation between hydrolysis in plasma and elimination was also examined. Methods Before induction of anesthesia, blood was drawn for analysis in seven adults. Anesthesia was induced with propofol and remifentanil. Single twitch stimulation was applied at the ulnar nerve every 10 s, and the force of contraction of the adductor pollicis was measured. Arterial blood was drawn frequently after succinylcholine injection to characterize the front-end kinetics. Plasma concentrations were measured by mass spectrometry, and pharmacokinetic parameters were derived using compartmental and noncompartmental approaches. Pharmacokinetic-pharmacodynamic relations were estimated. Results The mean degradation rate constant in plasma (1.07 +/- 0.49 min(-1)) was not different from the elimination rate constant (0.97 +/- 0.30 min(-1)), and an excellent correlation (r2 = 0.94) was observed. Total body clearance derived using noncompartmental (37 +/- 7 ml x min(-1) x kg(-1)) and compartmental (37 +/- 9 ml x min(-1) x kg(-1)) approaches were similar. The plasma-effect compartment equilibration rate constant (k(eo)) was 0.058 +/- 0.026 min(-1), and the effect compartment concentration at 50% block was 734 +/- 211 ng/ml. Conclusion Succinylcholine is a low-potency drug with a very fast clearance that equilibrates relatively slowly with the effect compartment. Its disappearance is greatly accountable by a rapid hydrolysis in plasma.

Cefazolin pharmacokinetics in cats under surgical conditions

2016 ◽  
Vol 19 (10) ◽  
pp. 992-997 ◽  
Author(s):  
Gabriela A Albarellos ◽  
Laura Montoya ◽  
Sabrina M Passini ◽  
Martín P Lupi ◽  
Paula M Lorenzini ◽  
...  
Keyword(s):  
Half Life ◽  
Subcutaneous Tissue ◽  
Plasma Concentrations ◽  
Pharmacokinetic Profile ◽  
Intravenous Dose ◽  
Pharmacokinetic Parameters ◽  
Antibiotic Administration ◽  
Single Intravenous Dose ◽  
Tissue Concentrations ◽  
Surgical Conditions

Objectives The aim of this study was to determine the plasma pharmacokinetic profile, tissue concentrations and urine elimination of cefazolin in cats under surgical conditions after a single intravenous dose of 20 mg/kg. Methods Intravenous cefazolin (20 mg/kg) was administered to nine young mixed-breed cats 30 mins before they underwent surgical procedures (ovariectomy or orchiectomy). After antibiotic administration, samples from blood, some tissues and urine were taken. Cefazolin concentrations were determined in all biological matrices and pharmacokinetic parameters were estimated. Results Initial plasma concentrations were high (Cp(0), 134.80 ± 40.54 µg/ml), with fast and moderately wide distribution (distribution half-life [t½(d)] 0.16 ± 0.15 h; volume of distribution at steady state [V(d[ss])] 0.29 ± 0.10 l/kg) and rapid elimination (body clearance [ClB], 0.21 ± 0.06 l/h/kg; elimination half-life [t½], 1.18 ± 0.27 h; mean residence time 1.42 ± 0.36 h). Thirty to 60 mins after intravenous administration, cefazolin tissue concentrations ranged from 9.24 µg/ml (subcutaneous tissue) to 26.44 µg/ml (ovary). The tissue/plasma concentration ratio ranged from 0.18 (muscle) to 0.58 (ovary). Cefazolin urine concentrations were high with 84.2% of the administered dose being eliminated in the first 6 h postadministration. Conclusions and relevance Cefazolin plasma concentrations remained above a minimum inhibitory concentration of ⩽2 µg/ml up to 4 h in all the studied cats. This suggests that a single intravenous dose of 20 mg/kg cefazolin would be adequate for perioperative prophylactic use in cats.

Pharmacokinetics of Intermittent Intraperitoneal Cefazolin in Continuous Ambulatory Peritoneal Dialysis Patients

1999 ◽  
Vol 19 (1) ◽  
pp. 65-70 ◽  
Author(s):  
Harold J. Manley ◽  
George R. Bailie ◽  
Rupesh D. Asher ◽  
George Eisele ◽  
Reginald F. Frye
Keyword(s):  
Body Weight ◽  
Peritoneal Dialysis ◽  
Continuous Ambulatory Peritoneal Dialysis ◽  
Rate Constant ◽  
Half Life ◽  
Elimination Rate ◽  
Pharmacokinetic Parameters ◽  
Number Of Patients ◽  
The Mean ◽  
Concentration Levels

Objective To investigate the pharmacokinetic parameters of intermittent intraperitoneal (IP) cefazolin, and recommend a cefazolin dosing regimen in continuous ambulatory peritoneal dialysis (CAPD) patients. Design Prospective nonrandomized open study. Setting CAPD outpatient clinic in Albany, New York. Patients Seven volunteer CAPD patients without peritonitis. Three of the patients were nonanuric while 4 were anuric. Interventions Cefazolin (15 mg/kg total body weight) was given to each patient during the first peritoneal exchange. Blood and dialysate samples were collected at times 0, 0.5, 1, 2, 3, 6 (end of the first antibiotic-containing dwell), 24, and 48 hours after the administration of IP cefazolin. Urine samples were collected in nonanuric patients over the study period. Results The mean ± SD amount of cefazolin dose absorbed from the dialysate after the 6-hour dwell was 69.7% ± 8.0% of the administered dose. The cefazolin absorption rate constant from dialysate to serum was 0.21 ± 0.1 /hr (absorption half-life 3.5 ± 0.8 hr). The mean serum concentrations reached at 24 and 48 hours were 52.4 ± 3.7 mg/L and 30.3 ± 5.9 mg/L, respectively. The mean dialysate cefazolin concentrations reached at 24 and 48 hours were 15.1 ± 3.4 mg/L and 7.9 ± 1.4 mg/L, respectively. The cefazolin serum elimination rate constant was 0.02 ± 0.01 /hr (elimination half-life 31.5 ± 8.8 hr). The total cefazolin body clearance was 3.4 ± 0.6 mL/min. In the 3 nonanuric patients the mean renal clearance of cefazolin was 0.6 ± 0.4 mL/min. The peritoneal clearance of cefazolin was 1.0 ± 0.3 mL/min. The systemic volume of distribution of cefazolin was 0.2 ± 0.05 L/kg. No statistical difference was detected in pharmacokinetic parameters between anuric and nonanuric patients, although this may be due to the small number of patients in each group. Conclusion A single daily dose of cefazolin dosed at 15 mg/kg actual body weight in CAPD patients is effective in achieving serum concentration levels greater than the minimum inhibitory concentration for sensitive organisms over 48 hours, and dialysate concentration levels over 24 hours. Caution is warranted in extrapolation of dosing recommendations to patients who maintain a significant degree of residual renal function.

scholarly journals The Effects of Formaldehyde on Cytochrome P450 Isoform Activity in Rats

2017 ◽  
Vol 2017 ◽  
pp. 1-7 ◽  
Author(s):  
Min Xu ◽  
Huaqiao Tang ◽  
Qian Rong ◽  
Yuanli Zhang ◽  
Yinglun Li ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Plasma Concentrations ◽  
Pharmacokinetic Parameters ◽  
Control Group ◽  
High Dose ◽  
Blood Samples ◽  
Time Points ◽  
Indoor Pollutant ◽  
Carcinogenic Effects

Formaldehyde (FA) is an occupational and indoor pollutant. Long-term exposure to FA can irritate the respiratory mucosa, with potential carcinogenic effects on the airways. The effects of acute FA poisoning on the activities of CYP450 isoforms CYP1A2, CYP2C11, CYP2E1, and CYP3A2 were assessed by determining changes in the pharmacokinetic parameters of the probe drugs phenacetin, tolbutamide, chlorzoxazone, and testosterone, respectively. Rats were randomly divided into three groups: control, low FA dose (exposure to 110 ppm for 2 h for 3 days), and high FA dose (exposure to 220 ppm for 2 h for 3 days). A mixture of the four probe drugs was injected into rats and blood samples were taken at a series of time points. Plasma concentrations of the probe drugs were measured by HPLC. The pharmacokinetic parameters t1/2, AUC(0-t), and Cmax of tolbutamide, chlorzoxazone, and testosterone increased significantly in the high dose versus control group (P<0.05), whereas the CL of chlorzoxazone and testosterone decreased significantly (P<0.05). However, t1/2, AUC(0-t), and Cmax of phenacetin decreased significantly (P<0.05), whereas the CL of phenacetin increased significantly (P<0.05) compared to controls. Thus, acute FA poisoning suppressed the activities of CYP2C11, CYP2E1, and CYP3A2 and induced the activity of CYP1A2 in rats. And the change of CYP450 activity caused by acute FA poisoning may be associated with FA potential carcinogenic effects on the airways.

Propranolol Plasma Concentrations and Plasmapheresis

1981 ◽  
Vol 15 (12) ◽  
pp. 993-996 ◽  
Author(s):  
Robert L. Talbert ◽  
Yan Yan Wong ◽  
Douglas B. Duncan
Keyword(s):  
Hemolytic Uremic Syndrome ◽  
Rate Constant ◽  
Half Life ◽  
Plasma Concentrations ◽  
Elimination Rate ◽  
Elimination Rate Constant ◽  
Before And After ◽  
Uremic Syndrome ◽  
The Mean

Propranolol plasma concentrations were determined in a patient with hemolytic-uremic syndrome undergoing plasmapheresis before and after the procedure on three occasions. The mean half-life and elimination rate constant during plasmapheresis were estimated to be 25.6 percent of the values obtained without plasmapheresis. These changes suggest that plasmapheresis may influence propranolol disposition.

Pharmacokinetics and investigation of optimal dose ertapenem in intermittent hemodialysis patients

2018 ◽  
Vol 34 (10) ◽  
pp. 1766-1772 ◽  
Author(s):  
Lama M Hsaiky ◽  
Francine D Salinitri ◽  
Judy Wong ◽  
Sin-Ling T Jennings ◽  
Neha H Desai ◽  
...  
Keyword(s):  
Half Life ◽  
Plasma Concentrations ◽  
Area Under The Curve ◽  
Optimal Dose ◽  
Hemodialysis Patients ◽  
Pharmacokinetic Parameters ◽  
Intermittent Hemodialysis ◽  
Pharmacokinetic Studies ◽  
Open Label ◽  
Serious Adverse Events

Abstract Background Previous pharmacokinetic studies demonstrated an increase in serum ertapenem concentrations with decreasing kidney function, including patients receiving renal replacement therapy. This study evaluated the pharmacokinetic parameters of ertapenem in patients receiving hemodialysis. Methods This prospective, single-center, open-label study examined the pharmacokinetics of a single intravenous (IV) dose of ertapenem 1 g in seven hospitalized noninfected patients undergoing hemodialysis. Blood samples were collected prior to ertapenem administration and at 0.5, 1, 2, 6, 12 and 48 hours (h) after administration. Ertapenem concentrations were determined by validated liquid chromatography mass spectrometry assay. Results Following an IV bolus of 1 g ertapenem, plasma concentrations declined relatively slowly with a mean ±standard deviation (SD) elimination half-life of 19.3 ±6.6 h. Plasma concentrations were similar in all subjects, with maximum mean plasma concentration observed of 343±48 µg/mL postdose. The mean ±SD values for systemic plasma clearance (CL) and volume of distribution at steady state (Vss) were 2±0.5 mL/min and 3295±1187 mL, respectively. The area under the curve for 0 h–∞ (AUCinf) was 7494 ±1424 h•µg/mL. No gender effect was observed and no serious adverse events were reported. Conclusions Ertapenem half-life was prolonged in hemodialysis patients. Considering the nonrenal clearance and the expected 70% removal with high-efficacy hemodialysis, the dose of 1 g ertapenem, three times weekly, after hemodialysis may produce pharmacodynamically sufficient exposure for potential antimicrobial efficacy. Further studies are warranted to assess the clinical efficacy and safety of this dose with prolonged duration of therapy.

scholarly journals Plasma Concentrations of Boswellic Acids in Fasting Healthy Humans Supplemented with a Water-Soluble Boswellia Extract (78% AKBA) vs. Reference Boswellia Extract (30% AKBA) (P06-005-19)

2019 ◽  
Vol 3 (Supplement_1) ◽  
Author(s):  
Barbara Davis ◽  
Krishanu Sengupta ◽  
Venkata Krishnaraju Alluri ◽  
Trimurtulu Golakoti
Keyword(s):  
Plasma Concentrations ◽  
Water Soluble ◽  
Pharmacokinetic Analysis ◽  
Pharmacokinetic Parameters ◽  
Open Label ◽  
Oral Ingestion ◽  
Post Dose ◽  
Geometric Means ◽  
Funding Sources ◽  
Healthy Humans

Abstract Objectives A randomized, open label, balanced, two-way crossover study compared the oral bioavailability and pharmacokinetic profiles of two Boswellia products standardized to 3-O-acetyl-11-Keto-β-boswellic acid (AKBA). Methods Twenty-two fasted male participants completed the study. They received a single oral-dose of water-soluble Boswellia extract 78% (LI51202F1) or the standard Boswellia extract 30% (5-Loxin) at 30 mg AKBA equivalent with 240 mL water on 2 separate occasions 12 days apart. Plasma AKBA and KBA were analyzed using a LC-MS/MS in pre- (0 hr) and post-dose (00.50, 01.00, 01.50, 02.00, 02.50, 03.00, 04.00, 08.00, 12.00 and 24.00 hrs) blood samples. Pharmacokinetic analysis was performed using WinNonlin® version 7.0 (Pharsight corporation, USA). Results Comparative analysis of the pharmacokinetic parameters showed LI51202F1 had higher (111.11%) Cmax for AKBA vs. 5-Loxin. The bioavailability indicated by Geometric means of AUC0-t and AUC0-∞ were 25.49% and 16.13% higher in LI51202F1 than 5-Loxin. Conclusions The present study demonstrates that oral ingestion of water soluble and standard Boswellia extracts resulted in similar bioavailability. Interestingly, the water-soluble version exhibited higher Cmax and AUC values, which could be attributed to the improved solubility of LI51202F1. Funding Sources Laila Nutraceuticals.

scholarly journals Effects of Vitamin D Plus Calcium Supplements on Pharmacokinetics of Isoflavones in Thai Postmenopausal Women

2011 ◽  
Vol 2011 ◽  
pp. 1-7 ◽  
Author(s):  
Supanimit Teekachunhatean ◽  
Paveena Pongnad ◽  
Noppamas Rojanasthein ◽  
Maleeya Manorot ◽  
Chaichan Sangdee
Keyword(s):  
Vitamin D ◽  
Single Dose ◽  
Plasma Concentration ◽  
Postmenopausal Women ◽  
Plasma Concentrations ◽  
Pharmacokinetic Parameters ◽  
Calcium Supplements ◽  
Maximal Plasma Concentration ◽  
Maximal Plasma ◽  
To Receive

The objective of this study was to determine the effects of vitamin D3plus calcium supplements (D3-calcium) on pharmacokinetics of isoflavones in Thai postmenopausal women. This study was an open-labeled, randomized three-phase crossover study. Twelve healthy subjects were randomized to receive one of the following regimens: (a) a single dose of isoflavones, (b) a single dose of isoflavones, and D3-calcium, or (c) continuous D3-calcium for 7 days followed by a single dose of isoflavones on the 8th day. After a washout period, subjects were switched to receive the 2 remaining regimens according to their randomized sequences. Blood samples were collected before dose and at specific time points until 32 hours after isoflavone administration. Plasma was treated with β-glucuronidase/sulfatase to hydrolyze glucuronide and sulfate conjugates of daidzein and genistein. Plasma concentrations of daidzein and genistein were determined by high performance liquid chromatography. The estimated pharmacokinetic parameters of isoflavones were time to maximal plasma concentration (Tmax), maximal plasma concentration (Cmax), half-life (t1/2) and area under the plasma concentration-time curve (AUC).Tmaxof daidzein and genistein after regimen B was significantly longer than that of regimen A. Other pharmacokinetic parameters of daidzein and genistein obtained following the three regimens were not significantly different.

scholarly journals Absorption and pharmacokinetics of grapefruit flavanones in beagles

2007 ◽  
Vol 98 (1) ◽  
pp. 86-92 ◽  
Author(s):  
Maria de Lourdes Mata-Bilbao ◽  
Cristina Andrés-Lacueva ◽  
Elena Roura ◽  
Olga Jáuregui ◽  
Elvira Escribano ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Biological Activities ◽  
Plasma Concentrations ◽  
Oral Intake ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Blood Samples ◽  
Dog Plasma ◽  
Citrus Flavonoids ◽  
L 14

The present study evaluated the pharmacokinetics of three different grapefruit flavanone forms in dog plasma and demonstrated their absorption after an oral intake of a grapefruit extract; pharmacokinetic parameters of these forms were also determined. Ten healthy beagles were administered 70 mg citrus flavonoids as a grapefruit extract contained in capsules, while two additional dogs were used as controls and given an excipient. The grapefruit flavanone naringin, along with its metabolites naringenin and naringenin glucuronide, was detected in dog plasma. Blood samples were collected between 0 and 24 h after administration of the extract. Naringin reached its maximun plasma concentration at around 80 min, whereas naringenin and naringenin glucuronide reached their maximun plasma concentrations at around 20 and 30 min, respectively. Maximum plasma concentrations of naringin, naringenin and naringenin glucuronide (medians and ranges) were 0·24 (0·05–2·08), 0·021 (0·001–0·3) and 0·09 (0·034–0·12) μmol/l, respectively. The areas under the curves were 23·16 l (14·04–70·62) min × μmol/for nariningin, 1·78 (0·09–4·95) min × μmol/l for naringenin and 22·5 (2·74–99·23) min × μmol/l for naringenin glucuronide. The median and range values for mean residence time were 3·3 (1·5–9·3), 2·8 (0·8–11·2) and 8·0 (2·3–13·1) h for naringin, naringenin and naringenin glucuronide, respectively. The results of the present study demonstrate the absorption of grapefruit flavanones via the presence of their metabolites in plasma, thus making an important contribution to the field since the biological activities ascribed to these compounds rely on their specific forms of absorption.

scholarly journals Randomized, Open-Label, Two-Way Crossover Study To Compare The Bioequivalence Of Two Formulations Of Esomeprazole In Healthy Male Volunteers

KYAMC Journal ◽  
2017 ◽  
Vol 4 (1) ◽  
pp. 326-330
Author(s):  
Uttam Kumar Sarker ◽  
Mir Misbahuddin ◽  
Md Shariful Hasan Ripon ◽  
Md Rabiul Islam
Keyword(s):  
Half Life ◽  
Plasma Concentrations ◽  
Bioequivalence Study ◽  
Relative Bioavailability ◽  
Hplc Method ◽  
Pharmacokinetic Parameters ◽  
Test Drug ◽  
Healthy Male ◽  
Open Label ◽  
Reference Drug

A crossover-randomized bioequivalence study of two oral formulations of esomeprazole (40 mg) capsules were carried out in 16 healthy male Bangladeshi volunteers. The test and reference formulations were PRONEX™ (Drug International Ltd, Bangladesh) and NEXIUM™ (AstraZeneca AB, Sweden), respectively. Each tablet was administered with 150 mL of water to subjects after overnight fasting on 2 treatment days separated by 1 week washout period. After dosing, serial blood samples were collected for a period of 24 hours. The plasma concentrations of esomeprazole were estimated using a validated HPLC method. The pharmacokinetic parameters Cmax, Tmax, AUC0g24h, t1/2, and Kel were determined. The mean (± SD) AUC0g24h for esomeprazole of test drug PRONEXTM for 16 volunteers was 1509 (± 546) ng.hr/mL whereas it was 1622 (± 589) ng.hr/mL for esomeprazole of NEXIUMTM. The relative bioavailability (PRONEXTM/NEXIUMTM ratio) was 93%. The Cmax, tmax, half-life of elimination (t1/2) and the rate of elimination (Kel) of esomeprazole of test drug were 1653 (± 706) ng/mL, 2.13 (± 0.81) hours, 2.00 (± 0.61) hour and 0.3465 respectively. The Cmax, tmax, half-life of elimination (t1/2) and the rate of elimination (Kel) of esomeprazole of reference drug were 1820 (± 877) ng/mL, 2.80 (± 0.67) hours, 2.14 (± 0.55) hour and 0.3238 respectively. The 90% CI for the test and reference drugs were found within the acceptance range of 80-125%. In conclusion, PRONEX™ is bioequivalent to NEXIUM ™ in terms of absorption.KYAMC Journal Vol. 4, No.-1, July 2013, Page 326-330

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