scholarly journals Pharmacokinetics of Tinidazole in Chinese subjects: Comparison of Mongolian, Korean, Hui, Uighur and Han nationalities

2009 ◽  
Vol 12 (2) ◽  
pp. 175 ◽  
Author(s):  
Xin-Yu Chang ◽  
Tao Guo ◽  
Dong-Ya Xia
Keyword(s):  
Oral Dose ◽  
Single Oral Dose ◽  
Half Life ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Elimination Rate ◽  
Area Under The Curve ◽  
Elimination Half ◽  
Pharmacokinetic Properties ◽  
Chinese Subjects

ABSTRACT - Purpose. This study investigated the pharmacokinetics of tinidazole in subjects of five different Chinese nationalities (Han, Mongolian, Korean, Hui, and Uighur). Methods. Fifty healthy subjects (five male and five female of each nationality) were recruited for the study, and each received 1 g tinidazole. A total of 14 blood samples were collected over a 72-hour period after administration. Results. Pharmacokinetic profiles, including area under the curve from time zero to infinity (AUC0-inf), peak plasma concentration (Cmax), time to reach Cmax (tmax), oral clearance (CL/F), elimination rate constant (Ke), and elimination half-life (t1/2), were determined following a single oral dose of tinidazole. The respective pharmacokinetic properties of Han, Mongolian, Korean, Hui, and Uighur nationalities were: half-life (h): 16.94±2.40, 16.40±1.79, 16.63±1.82, 16.81±1.56, 14.34±1.92; Cmax (μg/mL): 19.04±2.42, 19.22±4.93, 20.83±3.33, 20.25±4.05, 18.81±3.10; AUC0-inf (h•μg/mL): 483.13±65.65, 479.70±99.74, 511.07±53.47, 514.25±130.78, 388.58±37.37. The t1/2 and AUC0-inf of Uighur subjects were significantly lower (p =0.023, 0.011) and the CL/F and Ke were significantly higher (p = 0.003, 0.013) than those of other nationalities. After normalization by weight, the differences in AUC0-inf and CL/F between Uigur subjects and those of other races were still significant. Conclusions. The results indicate that ethnicity had significant impact on the pharmacokinetics of tinidazole after a single oral dose in healthy volunteers of different nationalities in China.

BIOLOGICAL HALF-LIFE OF CAFFEINE IN PIGS

1970 ◽  
Vol 50 (1) ◽  
pp. 49-54 ◽  
Author(s):  
H. M. CUNNINGHAM
Keyword(s):  
Oral Dose ◽  
Water Content ◽  
Single Oral Dose ◽  
Plasma Levels ◽  
Half Life ◽  
Intramuscular Injection ◽  
Peak Plasma ◽  
Growing Pigs ◽  
Sufficient Time ◽  
Biological Half Life

Five experiments were conducted with growing pigs to determine the biological half-life of caffeine after injection or various periods of ingestion. Peak plasma caffeine levels were reached within 5 hr after a single oral dose and 2 hr after intramuscular injection, and then declined with a biological half-life of about 12 hr. The caffeine content of tissues was approximately proportional to their water content and 6% of orally administered caffeine was excreted in the urine. Upon continuous ingestion of caffeine, peak plasma levels were reached within 2 days, indicating that accumulation was quite limited. When 1.5 g of caffeine per kg of feed was fed from weaning to market weight, the withdrawal of caffeine 2 days prior to slaughter was sufficient time to insure that caffeine levels in the liver, muscle, kidney and backfat were below 1 μg/g.

scholarly journals Interaction between Grapefruit Juice and Praziquantel in Humans

2002 ◽  
Vol 46 (5) ◽  
pp. 1614-1616 ◽  
Author(s):  
Nelly Castro ◽  
Helgi Jung ◽  
Roberto Medina ◽  
Dinora González-Esquivel ◽  
Mario Lopez ◽  
...  
Keyword(s):  
Water Treatment ◽  
Oral Dose ◽  
Single Oral Dose ◽  
Half Life ◽  
Maximum Concentration ◽  
Grapefruit Juice ◽  
Time Curve ◽  
Elimination Half Life ◽  
Concentration Time ◽  
Elimination Half

ABSTRACT After a single oral dose of praziquantel with 250 ml of grapefruit juice, the area under the concentration-time curve and the maximum concentration in plasma of praziquantel (C max) were significantly increased (C max for water treatment, 637.71 ± 128.5 ng/ml; and C max for grapefruit juice treatment, 1,037.65 ± 305.7 ng/ml, P < 0.05). No statistically significant differences were found in the time to maximum concentration of drug in plasma or elimination half-life.

scholarly journals Plasma appearance and disappearance of an oral dose of 25-hydroxyvitamin D2in healthy adults

2011 ◽  
Vol 107 (8) ◽  
pp. 1128-1137 ◽  
Author(s):  
Kerry S. Jones ◽  
Inez Schoenmakers ◽  
Les J. C. Bluck ◽  
Shujing Ding ◽  
Ann Prentice
Keyword(s):  
Vitamin D ◽  
Plasma Concentration ◽  
Oral Dose ◽  
Half Life ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Post Dose ◽  
Vitamin D Metabolism ◽  
Blood Samples ◽  
Potential Biomarker

25-Hydroxyvitamin D (25(OH)D) half-life is a potential biomarker for investigating vitamin D metabolism and requirements. We performed a pilot study to assess the approach and practical feasibility of measuring 25(OH)D half-life after an oral dose. A total of twelve healthy Gambian men aged 18–23 years were divided into two groups to investigate the rate and timing of (1) absorption and (2) plasma disappearance after an 80 nmol oral dose of 25(OH)D2. Fasting blood samples were collected at baseline and, in the first group, every 2 h post-dose for 12 h, at 24 h, 48 h and on day 15. In the second group, fasting blood samples were collected on days 3, 4, 5, 6, 9, 12, 15, 18 and 21. Urine was collected for 2 h after the first morning void at baseline and on day 15. 25(OH)D2plasma concentration was measured by ultra-performance liquid chromatography-tandem MS/MS and corrected for baseline. Biomarkers of vitamin D, Ca and P metabolism were measured at baseline and on day 15. The peak plasma concentration of 25(OH)D2was 9·6 (sd0·9) nmol/l at 4·4 (sd1·8) h. The terminal slope of 25(OH)D2disappearance was identified to commence from day 6. The terminal half-life of plasma 25(OH)D2was 13·4 (sd2·7) d. There were no significant differences in plasma 25(OH)D3, total 1,25(OH)2D, parathyroid hormone, P, Ca and ionised Ca and urinary Ca and P between baseline and day 15 and between the two groups. The present study provides data on the plasma response to oral 25(OH)D2that will underpin and contribute to the further development of studies to investigate 25(OH)D half-life.

scholarly journals The effects of oral administration of Cola nitida on the pharmacokinetic profile of metoclopramide in rabbits

2020 ◽  
Vol 21 (1) ◽  
Author(s):  
Cecilia Nwadiuto Amadi ◽  
Wisdom Izuchukwu Nwachukwu
Keyword(s):  
Drug Interaction ◽  
Plasma Concentration ◽  
Oral Administration ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Elimination Rate ◽  
Area Under The Curve ◽  
Pharmacokinetic Profile ◽  
Pharmacokinetic Parameters ◽  
Cola Nitida

Abstract Background Cola nitida is commonly chewed in many West African cultures to ease hunger pangs and sometimes for their stimulant and euphoriant qualities. Metoclopramide is a known substrate for P-gp, SULT2A1 and CYP2D6 and studies have revealed that caffeine- a major component of Cola nitida can induce P-glycoprotein (P-gp), SULT2A1 and SULT1A1, hence a possible drug interaction may occur on co-administration. The aim of this study was to investigate the pharmacokinetic interactions of Cola nitida and metoclopramide in rabbits. Methods The study was performed in two stages using five healthy male rabbits with a 1-week washout period between treatments. Stage one involved oral administration of metoclopramide (0.5 mg/kg) alone while in the second stage, metoclopramide (0.5 mg/kg) was administered concurrently with Cola nitida (0.7 mg/kg). Blood samples were collected after each stage at predetermined intervals and analyzed for plasma metoclopramide concentration using HPLC. Results Compared with control, the metoclopramide/Cola nitida co-administration produced a decrease in plasma concentration of metoclopramide at all the time intervals except at the 7th hour. The following pharmacokinetic parameters were also decreased: area under the curve (51%), peak plasma concentration (39%), half-life (51%); while an increase in elimination rate constant (113%) and clearance rate (98%) were noted indicating rapid elimination of the drug. A minimal decrease in absorption rate (10%) was also observed. Conclusions The results of this study reveal a possible herb-drug interaction between Cola nitida and metoclopramide.

Buccal Absorption of Fentanyl Is pH-Dependent in Dogs 

1995 ◽  
Vol 82 (3) ◽  
pp. 759-764 ◽  
Author(s):  
James B Streisand ◽  
Jie Zhang ◽  
Suyi Niu ◽  
Scott McJames ◽  
Remco Natte ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Buccal Mucosa ◽  
Half Life ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Elimination Half Life ◽  
Arterial Blood ◽  
Buccal Absorption ◽  
Elimination Half ◽  
Fentanyl Administration

Background Analgesia and sedation have been achieved noninvasively by fentanyl administration through the oral and nasal mucosa. In theory, the transmucosal bioavailability and absorption of fentanyl could be improved by converting more fentanyl to the unionized form by adjusting the surrounding pH. The authors tested this hypothesis in dogs. Methods Under general anesthesia, each of six mongrel dogs was given fentanyl on repeated occasions, first intravenously (once), then by application to the buccal mucosa (six times). Buccal fentanyl administration was accomplished by placement of a pH-buffered solution of fentanyl into a specially constructed cell, which was clamped to the dog's buccal mucosa for 60 min. Fentanyl solutions with pHs of 6.6, 7.2, and 7.7 were studied to span a tenfold difference in the unionized fraction of fentanyl. Femoral arterial blood samples were sampled frequently and analyzed for fentanyl using a radioimmunoassay. Peak plasma concentration and the time of its occurrence for each buccal study were noted from the plasma concentration verses time profile. Terminal elimination half-life, bioavailability, and permeability coefficients were calculated using standard pharmacokinetic techniques. Results The variables peak plasma concentration, bioavailability, and permeability coefficient increased three- to fivefold as the pH of the fentanyl buccal solution increased and more fentanyl molecules became unionized. There was no difference in terminal elimination half-life after intravenous fentanyl (244 +/- 68 min) or buccal fentanyl administration (pH 7.7, 205 +/- 89 min; pH 7.2, 205 +/- 65 min; pH 6.6, 196 +/- 48 min). In all buccal studies regardless of pH, time to peak plasma concentration occurred within 10 min of removal of the fentanyl solutions from the buccal mucosa. Conclusions The buccal absorption, bioavailability, and permeability of fentanyl are markedly increased as the pH of the fentanyl solution becomes more basic. Most likely, this is because of an increase in the fraction of unionized fentanyl.

scholarly journals Plasma disposition of cefoperazone after single intravenous and intramuscular administrations in camels (Camelus dromedarius)

2018 ◽  
Vol 66 (3) ◽  
pp. 444-450
Author(s):  
Mohamed Aboubakr ◽  
Ahmed Soliman ◽  
Kamil Uney ◽  
Muammer Elmas
Keyword(s):  
Half Life ◽  
High Performance ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Volume Of Distribution ◽  
Camelus Dromedarius ◽  
Promising Alternative ◽  
Elimination Half Life ◽  
Elimination Half ◽  
Total Body

The plasma disposition of cefoperazone was investigated after intravenous (IV) and intramuscular (IM) administrations of 20 mg/kg as a single dose in six camels (Camelus dromedarius) in a crossover design. Blood plasma samples were analysed by high-performance liquid chromatography (HPLC). After IV administration, elimination half-life (t1/2β), volume of distribution at steady state (Vdss), total body clearance (Cltot) and mean residence time (MRT) of cefoperazone were 1.95 h, 0.38 L/kg, 0.17 L/h/kg and 2.16 h, respectively. After IM administration of cefoperazone, peak plasma concentration (Cmax) was 21.95 μg/mL and it was obtained at (tmax) 1.23 h. Absorption half-life (t1/2ab), elimination half-life and mean absorption time were 0.45 h, 2.84 h and 2.07 h, respectively. The bioavailability of cefoperazone was 89.42%. The lack of local reaction or any other adverse effects and the very good bioavailability following IM administration indicate that cefoperazone might be a promising alternative treatment for a variety of infectious diseases in camels.

scholarly journals Pharmacokinetics of cefquinome in goats after intramuscular administration alone and with meloxicam

2020 ◽  
Vol 9 (4) ◽  
pp. 518
Author(s):  
Saber El Hanbally ◽  
Hanem El Gendy ◽  
Hanem El Gendy ◽  
Mohamed El Hewaity ◽  
Mohamed El Hewaity
Keyword(s):  
Dose Rate ◽  
Half Life ◽  
Area Under Curve ◽  
Total Body Clearance ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Intramuscular Administration ◽  
Elimination Half ◽  
Total Body ◽  
Body Clearance

Background: Nonsteroidal anti-inflammatory drugs and antibiotics are commonly prescribed together. We aimed to study the kinetic profile of cefquinome (2 mg/kg b.wt.) following intramuscular administration of it alone and co-administered with meloxicam (0.2 mg/kg b.wt.) in goats.Methods: Five Egyptian Baladi goats, each goat was injected intramuscularly at the dose rate of 2 mg/kg b.wt. Cefquinome into the deep gluteal muscle of hindquarter alone and then after fifteen days washout period, these animals also injected intramuscularly at the dose rate of 2 mg/kg b.wt. Cefquinome preceded with meloxicam at the dose rate of 0.2 mg/kg b.wt. The serum concentrations of cefquinome were detected by high performance liquid chromatography, two compartment model.Results: Following a single dose intramuscular administration of cefquinome alone, peak plasma concentration (1.71±0.0189 μg/ml) was obtained at 1.59±0.0038 h. The absorption half-life (t1/2ab), total body clearance (Cltot), elimination half-life (t1/2el) and area under curve (area under concentration (AUC(0-inf)) of cefquinome were 0.4±0.0028 h, 0.068±0.78 l/h/kg, 9.21±0.178h and 29.36±0.78 µg.h.ml-1, respectively. Following a single dose intramuscular co-administration of cefquinome and meloxicam, peak plasma concentration (1.60±0.0124 μg/ml) was obtained at 1.49±0.0092 h. The absorption half-life (t1/2ab), total body clearance (Cltot), elimination half-life (t1/2el) and area under curve (AUC(0-inf)) of cefquinome were 0.396±0.006 h, 0.094±0.25 l/h/kg, 6.5±0.221 h and 21.38±0.696 µg/h/ml, respectively. Non significant alters were reported in the parameters following co-administration of Cefquinome with meloxicam.Conclusions: From our results, may be concluded that intramuscular administration of meloxicam may be successfully co-administrated with cefquinome for combating bacterial infections with an inflammatory condition in goats without any antagonistic effect.

Pharmacokinetics of the Bronchodilator Tulobuterol in Man after Repeated Oral Doses

1986 ◽  
Vol 14 (5) ◽  
pp. 223-227 ◽  
Author(s):  
L F Chasseaud ◽  
S G Wood
Keyword(s):  
Plasma Levels ◽  
Half Life ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Repeated Administration ◽  
Elimination Half Life ◽  
Time To Peak ◽  
Final Study ◽  
Elimination Half ◽  
Repeated Dosing

Plasma levels and elimination half-life of tulobuterol, a new beta-adrenergic agonist, were determined in ten healthy male volunteers after repeated dosing with 2mg, twice daily, for seven days. Peak plasma levels attained (2.8 ±0.8 ng/ml), the time to peak plasma concentration (1.0 ±0.3 hr) and the elimination half-life (2.4 ±0.4 hr) were generally unchanged from the first to the final study dose. This suggests that tulobuterol does not accumulate in plasma after repeated administration of a dose regimen known to be clinically effective.

scholarly journals Emulsification by TPGS or Quillaja Extract Increased Absorption and Affected Metabolism of Berberine in Humans

2021 ◽  
Vol 5 (Supplement_2) ◽  
pp. 381-381
Author(s):  
Yavuz Yagiz ◽  
Gary Wang ◽  
Liwei Gu
Keyword(s):  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Area Under The Curve ◽  
Total Content ◽  
Compartment Model ◽  
Analysis Of Covariance ◽  
High Tech ◽  
Pharmacokinetic Parameters ◽  
Funding Sources ◽  
Human Volunteers

Abstract Objectives Berberine is a botanical alkaloid used widely for the prevention of several diseases. However, the absorption rate of berberine is less than 1% in human. The objectives of this study were to determine whether emulsification by TPGS or Quillaja extract affect the absorption and metabolism of orally ingested berberine in human volunteers. Methods Twelve healthy subjects (7 male and 5 females, 21–50-year-old) participated this study. Each subject received 800 mg berberine in a powder form or emulsified with TPGS or Quillaja extract using a randomized crossover design with one-week washout period. Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, and 12 hours after dose. Plasma was hydrolyzed with glucuronidase and sulfatase before total content of berberine and its metabolites were analyzed on LC/MS/MS. Free forms of metabolites were determined in plasma without hydrolysis. Pharmacokinetic parameters were calculated using a non-compartment model before they were compared by analysis of covariance. Results The area under the curve (AUC) and peak plasma concentration (Cmax) of berberine was 6.6 μM.hr and 0.9 μM in participants received berberine powder. They were increased to 18.3 μM.hr and 4.5 μM by TPGS emulsification and 28 μM.hr and 5.1 μM by Quillaja extract emulsification, respectively. Berberrubine and demethylberberine were major metabolites of berberine. The AUC of free Berberrubine and demethylberberine was increased by 1.9 fold and 1.6 fold by TPGS and 5.9 folds and 2.7 folds by Quillaja extract, respectively, compared to berberine powder. Participants received berberine powder had AUC of 254 μM.hr and Cmax of 33 μM for total berberrubine. TPGS emulsification increased these values to 425 μM.hr and 54 μM, while Quillaja extract increased them to 341 μM.hr and 44 μM, respectively. Significant increases of AUC and Cmax were also observed for total demethylberberine by TPGS or Quillaja extract emulsification. Conclusions Emulsification of berberine with TPGS or Quillaja extract significantly increased the absorption of berberine and its metabolites in human compared to berberine supplement without emulsifiers. Funding Sources Florida High Tech Corridor Council and Designs for Health.

scholarly journals Single-Dose Pharmacokinetics of Meropenem during Continuous Venovenous Hemofiltration

1998 ◽  
Vol 42 (9) ◽  
pp. 2417-2420 ◽  
Author(s):  
Florian Thalhammer ◽  
Peter Schenk ◽  
Heinz Burgmann ◽  
Ibrahim El Menyawi ◽  
Ursula M. Hollenstein ◽  
...  
Keyword(s):  
High Performance ◽  
Peak Plasma ◽  
Continuous Venovenous Hemofiltration ◽  
Drug Concentrations ◽  
Elimination Half ◽  
Pharmacokinetic Properties ◽  
Severe Infections ◽  
Total Body ◽  
Trough Levels ◽  
Body Clearance

ABSTRACT The pharmacokinetic properties of meropenem were investigated in nine critically ill patients treated by continuous venovenous hemofiltration (CVVH). All patients received one dose of 1 g of meropenem intravenously. High-flux polysulfone membranes were used as dialyzers. Meropenem levels were measured in plasma and ultrafiltrate by high-performance liquid chromatography. The total body clearance and elimination half-life were 143.7 ± 18.6 ml/min and 2.46 ± 0.41 h, respectively. The post- to prehemofiltration ratio of meropenem was 0.24 ± 0.06. Peak plasma drug concentrations measured 60 min postinfusion were 28.1 ± 2.7 μg/ml, and trough levels after 6 h of CVVH were 6.6 ± 1.5 μg/ml. The calculated total daily meropenem requirement in these patients with acute renal failure and undergoing CVVH was 2,482 ± 321 mg. Based on these data, we conclude that patients with severe infections who are undergoing CVVH can be treated effectively with 1 g of meropenem every 8 h.

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