Bioavailability of aspirin and salicylamide following oral co-administration in human volunteers

1991 ◽  
Vol 69 (10) ◽  
pp. 1436-1442 ◽  
Author(s):  
Mohamed S. Abdel-Rahman ◽  
Alluru S. Reddi ◽  
Frederick A. Curro ◽  
Rita M. Turkall ◽  
Abdelrazak M. Kadry ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Plasma Levels ◽  
Maximum Concentration ◽  
Peak Concentration ◽  
Area Under The Curve ◽  
Active Ingredients ◽  
Time Curve ◽  
Human Volunteers ◽  
Kinetics Of ◽  
Peak Value

BC® powder (I) is a commercially available analgesic containing the active ingredients aspirin and salicylamide. The kinetics of I, BC® powder minus aspirin (II), and BC® powder minus salicylamide (III) were evaluated in 13 volunteers. Ten minutes after administration of I, aspirin reached a maximum concentration of 12.9 μg/mL, while salicylamide concentration reached a peak value of 3.4 μg/mL. However, when III was administered, aspirin was not detected at 10 min and only reached a concentration of 0.4 μg/mL at 2 and 6 h. Furthermore, the area under the plasma concentration versus time curve for aspirin when III was administered was sixfold less compared with treatment with I. The area under the curve for aspirin metabolites was significantly different in I versus III. After treatment with II, a delay in salicylamide peak concentration was observed. Gentisamide was not detected throughout the study. This study demonstrates that salicylamide significantly enhances plasma levels of aspirin with potential therapeutic implications.Key words: aspirin, BC® powder, bioavailability, salicylamide.

The Pharmacokinetics of a Single Dose of Calcitriol Administered Subcutaneously in Continuous Ambulatory Peritoneal Dialysis Patients

1993 ◽  
Vol 13 (2) ◽  
pp. 122-125 ◽  
Author(s):  
Rafael Selgas ◽  
Maria-E. Martinez ◽  
Blanca Miranda ◽  
Maria-Auxiliadara Baja ◽  
Jase-Raman Ramera ◽  
...  
Keyword(s):  
Single Dose ◽  
Peritoneal Dialysis ◽  
Continuous Ambulatory Peritoneal Dialysis ◽  
Plasma Levels ◽  
Subcutaneous Administration ◽  
Area Under The Curve ◽  
Serum Levels ◽  
Mean Value ◽  
Ionized Calcium ◽  
Kinetics Of

Objectives To evaluate the kinetics of calcitriol (1,25(OH)2D3) administered subcutaneously. Study Design Calcitriol kinetics and efficacy after subcutaneous administration were studied in 13 CAPD patients with varying degrees of increased plasma levels of parathyroid hormone (i-PTH). A single dose of 2 μg of calcitriol was administered subcutaneously, and its serum levels at baseline and after 1,2,6,12, and 24 hours were determined. Plasma ionized calcium and i-PTH were also determined at these periods. Results Serum calcitriol levels reached peak levels of 60 and 70 pg/mL at 1 and 2 hours after administration, respectively. These levels decreased thereafter, but remained above baseline values during 24 hours. The mean value of the area under the curve (AUC) was 809±226 pg/mL/hour. Plasma i-PTH levels showed a slight decrease after 1 and 2 hours, returning to baselime levels after this period. Plasma ionized calcium did not show significant changes during the study. A slight pain at the site of injection was mentioned by some patients. Conclusions The subcutaneous route for calcitriol administration achieves theoretically adequate plasma levels in continuous ambulatory peritoneal dialysis (CAPD) patients. This is important when paremteral administration of calcitriol is considered in the treatment of secondary hyperparathyroidism.

Pharmacokinetics of an immunomodulating dose of levamisole in weaned pigs

2013 ◽  
Vol 61 (3) ◽  
pp. 376-382
Author(s):  
Jelena Šuran ◽  
Dubravka Flajs ◽  
Maja Peraica ◽  
Andreja Prevendar Crnić ◽  
Marcela Šperanda ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Area Under The Curve ◽  
Maximum Plasma ◽  
Weaned Pigs ◽  
Time Curve ◽  
Treatment Groups ◽  
Parallel Design ◽  
Concentration Time ◽  
Plasma Concentration Time Curve ◽  
Crossbred Pigs

Levamisole has been shown to stimulate the immune response in immunocompromised humans and animals. However, its use as an adjuvant in immunocompromised weaned pigs prone to colibacillosis has only been experimentally tested but not yet officially approved. Therefore, the aim of these studies was to study the pharmacokinetics (PK) of an immunomodulating dose of levamisole in weaned pigs. For that purpose, 20 weaned crossbred pigs were divided into two treatment groups. In this parallel-design study, a single dose of levamisole (2.5 mg/kg body weight) was administered by the intramuscular (i.m.) or oral (p.o.) route. Statistically significant differences between the i.m. and p.o. routes in terminal beta rate constant (β), maximum plasma concentration (Cmax), area under the curve (AUC) for plasma concentration-time curve from time zero to infinity (AUC0-inf), area under the plasma concentration-time curve from time 0 to the last quantifiable time point (AUC0-t) were determined. Further research is needed to establish a relationship between the PK and the immunomodulating effect of levamisole in pigs.

scholarly journals Studies of the Toxicological Potential of Capsinoids, XII: Pharmacokinetic Study of Capsinoid-Containing CH-19 Sweet Extract in Rats

2010 ◽  
Vol 29 (2_suppl) ◽  
pp. 15S-21S ◽  
Author(s):  
Yoshiaki Shirai ◽  
Satoko Ueno ◽  
Akira Nakayama ◽  
Kiyoko Ikeuchi ◽  
Kazuyuki Ubukata ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Portal Vein ◽  
Pharmacokinetic Study ◽  
Maximum Concentration ◽  
Medium Chain Triglyceride ◽  
Systemic Circulation ◽  
Blood Levels ◽  
Vanillyl Alcohol ◽  
Systemic Blood ◽  
Time Curve

Pharmacokinetics of the main capsinoid components of CH-19 Sweet extract (capsiate, dihydrocapsiate, and nordihydrocapsiate) were investigated in rats receiving a single gavage dose of extract containing 10 or 100 mg of capsinoids per kilogram in medium-chain triglyceride. Resultant blood levels of these capsinoids and a capsinoid metabolite, vanillyl alcohol, were measured in portal vein and systemic blood. Capsinoids were never detected. Portal compartment vanillyl alcohol concentrations and area under the plasma concentration versus time curve increased approximately with dose, whereas the time to maximum concentration of vanillyl alcohol was independent of dose (30 minutes post dosing), suggesting that precipitation in the stomach or intestines was unlikely. Vanillyl alcohol levels were just barely detectable in systemic plasma (5 minutes post dosing). Significant levels of vanillyl alcohol conjugates, sulfate, and glucuronide were detected in the systemic blood. Given that the orally administered capsinoids were never detected in the portal vein or systemic circulation, these compounds must be broken down (chemically or enzymatically) to vanillyl alcohol.

scholarly journals Total Intravenous Versus Inhalation Anesthesia in Patients Undergoing Laparoscopic Cholecystectomies. Effects on Two Proinflammatory Cytokines Serum Levels: Il-32 and TNF-Alfa.

2016 ◽  
Vol 2 (1) ◽  
pp. 44-50
Author(s):  
Adina Hadade ◽  
Daniela Ionescu ◽  
Teodora Mocan ◽  
Alexandru Necula ◽  
Victor Cristea
Keyword(s):  
Plasma Concentration ◽  
Proinflammatory Cytokines ◽  
Plasma Levels ◽  
Area Under The Curve ◽  
Secondary Outcome ◽  
Anesthetic Techniques ◽  
Inhalation Anesthesia ◽  
Tnf Α ◽  
Group 2 ◽  
Group 1

Abstract Introduction: It has been reported that as compared with total intravenous anesthesia (TIVA), inhalation anesthesia is increasing the postoperative level of proinflammatory interleukins. The aim of the study is to investigate if there is an in-vivo relationship between proinflammatory cytokines, Interleukin- 32 (IL-32) and Tumour necrosis factor - α (TNF- α), in patients undergoing laparoscopic cholecystectomies with two different anesthetic techniques, TIVA or inhalation anesthesia. Material and Methods: Twenty two consecutive patients undergoing laparoscopic cholecystectomies were prospectively randomized into two groups: Group 1: TIVA with target-controlled infusion (TIVA-TCI) (n=11) and Group 2: isoflurane anesthesia (ISO) (n=11). IL-32 and TNF-α were determined before the induction of anesthesia (T1), before incision (T2) and at 2h (T3) and 24h (T4) postoperatively. Our primary outcome was to compare plasma levels of IL-32 and TNF- α concentrations (expressed as area-under-the-curve) over 24 hours between study groups. Our secondary outcome was to establish whether there is a correlation between plasma levels of IL-32 and of TNF-α at each time point between the two groups. Results: Area-under-the-curve (AUC) of IL-32 plasma concentration was 7.53 in Group 1 (TIVA) versus 3.80 in Group 2 (ISO), p= 1. For TNF-α, AUC of plasma concentration was 733.9 in Group 1 (TIVA) and 668.7 in Group 2 (ISO), p= 0.066. There were no significant differences in plasma concentrations of both IL-32 and TNF- α between the groups. Conclusions: IL-32 expression in response to minor surgery is very low. There were no significant difference between plasma levels ofTNF- α and IL-32 after TIVA versus inhalation anesthesia during the first 24 hours postoperatively. Further studies are needed on larger groups to investigate whether there can be a correlation between these interleukins after 2 different anesthetic techniques and the impact of this correlation on postoperative outcome.

scholarly journals ABT-773: Pharmacokinetics and Interactions with Ranitidine and Sucralfate

2003 ◽  
Vol 47 (3) ◽  
pp. 1129-1131 ◽  
Author(s):  
M. W. Pletz ◽  
V. Preechachatchaval ◽  
J. Bulitta ◽  
M. Allewelt ◽  
O. Burkhardt ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Half Life ◽  
Maximum Concentration ◽  
Time Curve ◽  
Concentration Time ◽  
Plasma Concentration Time Curve

ABSTRACT We assessed the pharmacokinetics and interaction of ABT-773 in 12 volunteers receiving ABT-773 alone or concomitantly with ranitidine or sucralfate. Data for 150 mg of ABT-773 were as follows: the maximum concentration of the drug in plasma (C max) was 318 ng/ml, its half-life was 5.66 h, and its area under the plasma concentration-time curve from 0 h to ∞ (AUC0-∞) was 1,662 ng · h/ml. Coadministration of ranitidine, reduced the C max (−25.7%) and AUC0-∞ (−15.8%) significantly. Sucralfate had no impact on the bioavailability of ABT-773.

scholarly journals A Rapid and Sensitive UHPLC-MS/MS Method for Determination of 2, 3, 8-Trimethylellagic, a Potent Active Compound from Sanguisorba officinalis L., and Its Application in the Pharmacokinetic Study within Thrombocytopenia Rats

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Yuqing Wang ◽  
Jianming Wu ◽  
Yunxia Li ◽  
Jing Yang ◽  
Long Wang ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Maximum Concentration ◽  
High Performance ◽  
Internal Standard ◽  
Pharmacokinetic Parameters ◽  
Time Curve ◽  
Concentration Time ◽  
Relative Standard ◽  
Plasma Concentration Time Curve

To investigate the pharmacokinetics of 2, 3, 8-trimethylellagic (TMEA) in rats in vivo and determine the possible effects of the pathological conditions and compatibility, a rapid and sensitive ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method for quantitative determination was developed. TMEA and Artemetin (internal standard, IS) were separated on an Acquity Shim-pack GIST column with a total running time of 7 min using gradient elution at a flow rate of 0.3 mL/min. The intraday and interday relative standard deviations were <9.50%, and the relative error of accuracy was between −5.70% and 2.96%. The calibration curve of TMEA demonstrated good linearity with r2 = 0.9996, with the average recovery changing from 94.77% to 102.47% and the matrix effect from 93.16% to 100.15%. Compared with the normal group, the area under the plasma concentration-time curve from time 0 to the last time of quantifiable concentration (AUC(0 − t)), area under the plasma concentration-time curve from time 0 extrapolated to infinite time (AUC(0 − ∞)), and the maximum concentration (Cmax) of TMEA increased, whereas the time of maximum concentration (Tmax) and apparent clearance (CL/F) remarkably decreased in the TMEA group. With significantly reduced CL/F, AUC(0 − t), AUC(0 − ∞), and Cmax for TMEA were increased approximately one time after combining with 3, 7-Di-O-methylducheside A (DOMA). AUC(0 − t) and Cmax for TMEA in the 2, 3, 8-trimethylellagic-3, 8-dimethoxyellagic acid-2-oxyglucoside (TMEA-DMAG) group were significantly lower than that in the TMEA group with clearly prolonged Tmax and increased CL/F. These findings indicate that the changes in the pharmacokinetic parameters of TMEA may be caused by pathological and combination conditions.

scholarly journals Pharmacokinetics of fucoxanthinol in human plasma after the oral administration of kombu extract

2011 ◽  
Vol 107 (11) ◽  
pp. 1566-1569 ◽  
Author(s):  
Takashi Hashimoto ◽  
Yoshiaki Ozaki ◽  
Masashi Mizuno ◽  
Masaru Yoshida ◽  
Yosuke Nishitani ◽  
...  
Keyword(s):  
Oral Administration ◽  
Human Plasma ◽  
Peripheral Blood ◽  
Maximum Concentration ◽  
Active Metabolite ◽  
Human Subjects ◽  
Area Under The Curve ◽  
The Other ◽  
Half Time ◽  
Human Volunteers

Dietary fucoxanthin has been reported to exert several physiological functions, and fucoxanthinol is considered to be the primary active metabolite of fucoxanthin. However, there is no information about the pharmacokinetics of fucoxanthinol in human subjects. In the present study, eighteen human volunteers were orally administered kombu extract containing 31 mg fucoxanthin, and their peripheral blood was collected 5 min before and 0·5, 1, 2, 4, 8 and 24 h after the treatment. Plasma fucoxanthinol concentrations were measured by HPLC, and the pharmacokinetics of fucoxanthinol were as follows: maximum concentration, 44·2 nmol/l; time at maximum concentration, 4 h; terminal half-time, 7·0 h; area under the curve (AUC) for 1–24 h, 578·7 nmol/l × h; AUC(∞), 663·7 nmol/l × h. In addition to fucoxanthinol, we also attempted to detect amarouciaxanthin A, a hepatic metabolite of fucoxanthinol, using HPLC, but it was not present in the volunteers' plasma. On the other hand, a peak that was suspected to represent the cis-isomer of fucoxanthinol was found in the HPLC chromatogram. By comparing the present results with those of a previous study using mice, we found that the bioavailability and metabolism of fucoxanthinol differ between human subjects and mice.

scholarly journals Kill Rate and Evaluation of Ex Vivo PK/PD Integration of Cefquinome Against Actinobacillus pleuropneumoniae

2021 ◽  
Vol 8 ◽  
Author(s):  
Longfei Zhang ◽  
Hongbing Xie ◽  
Hongjuan Wang ◽  
Huanzhong Ding ◽  
Gaiping Zhang ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Maximum Concentration ◽  
Ex Vivo ◽  
Area Under The Curve ◽  
Actinobacillus Pleuropneumoniae ◽  
Time Curve ◽  
Concentration Time ◽  
Dosage Regimens ◽  
Kill Rate

We wished to study the detailed and precise antibacterial activity of cefquinome against Actinobacillus pleuropneumoniae (APP) in vitro and ex vivo. We analyzed the relationships between kill rate and cefquinome concentration in broth and between pharmacokinetic/pharmacodynamic (PK/PD) parameters and antibacterial effect in serum and tissue cage fluid (TCF) of piglets. Cefquinome exhibited time-dependent antibacterial activity against APP according to the kill rate. The maximum kill rate was 0.48 log10 CFU/mL/h at the 0-9-h period in broth. In the ex vivo PK/PD study, the maximum concentration (Cmax), time to reach the maximum concentration (Tmax), terminal half-life (T1/2β), and area under the concentration time curve (AUCinfinity) were 5.65 μg/ml, 0.58 h, 2.24 h, and 18.48 μg·h/ml in serum and 1.13 μg/ml, 2.60 h, 12.22 h, and 20.83 μg·h/ml in TCF, respectively. The values of area under the curve during 24 h/minimum inhibitory concentration (AUC24h/MIC) for bacteriostatic, bactericidal, and bacterial eradication effects were 18.94, 246.8, and 1013.23 h in serum and 4.20, 65.81, and 391.35 h in TCF, respectively. Our findings will provide a valuable basis for optimization of dosage regimens when applying cefquinome to treat APP infection.

scholarly journals The pharmacokinetic interaction between nasally administered naloxone and the opioid remifentanil in human volunteers

2021 ◽  
Author(s):  
Ida Tylleskar ◽  
Sissel Skarra ◽  
Arne Kristian Skulberg ◽  
Ola Dale
Keyword(s):  
Maximum Concentration ◽  
Intranasal Administration ◽  
Area Under The Curve ◽  
Pharmacokinetic Interaction ◽  
Intramuscular Administration ◽  
Nasal Administration ◽  
Pharmacokinetic Studies ◽  
Remifentanil Infusion ◽  
Human Volunteers ◽  
Significant Difference

Abstract Purpose Remifentanil has been shown to increase the bioavailability of nasally administered naloxone. The aim of this study was to explore the nature of this observation. Methods We analysed samples from three pharmacokinetic studies to determine the serum concentrations of naloxone-3-glucuronide (N3G), the main metabolite of naloxone, with or without exposure to remifentanil. To enable direct comparison of the three studies, the data are presented as metabolic ratios (ratio of metabolite to mother substance, N3G/naloxone) and dose-corrected values of the area under the curve and maximum concentration (Cmax). Results Under remifentanil exposure, the time to maximum concentration (Tmax) for N3G was significantly higher for intranasal administration of 71 min compared to intramuscular administration of 40 min. The dose-corrected Cmax of N3G after intranasal administration of naloxone under remifentanil exposure was significantly lower (4.5 ng/mL) than in subjects not exposed to remifentanil (7.8–8.4 ng/mL). The metabolic ratios after intranasal administration rose quickly after 30–90 min and were 2–3 times higher at 360 min compared to intravenous and intramuscular administration. Remifentanil exposure resulted in a much slower increase of the N3G/naloxone ratio after intranasal administration compared to intranasal administration with the absence of remifentanil. After remifentanil infusion was discontinued, this effect gradually diminished. From 240 min there was no significant difference between the ratios observed after intranasal naloxone administration. Conclusion Remifentanil increases the bioavailability of naloxone after nasal administration by reducing the pre-systemic metabolism of the swallowed part of the nasal dose.

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