Bioavailability of d-pseudoephedrine and Azatadine from a Repeat Action Tablet Formulation

1982 ◽  
Vol 10 (2) ◽  
pp. 122-125
Author(s):  
C Lin ◽  
J Lim ◽  
S Symchowicz
Keyword(s):  
Plasma Concentration ◽  
Tablet Formulation ◽  
Maximum Plasma Concentration ◽  
Maximum Plasma ◽  
Gas Liquid Chromatography ◽  
Time Curve ◽  
Conventional Tablet ◽  
Cumulative Urinary Excretion ◽  
Significant Difference ◽  
Curve Maximum

The objective of this study was to compare in man the bioavailability of d-pseudoephedrine and azatadine from a repeat action tablet* formulation and from conventional tablets. The repeat action tablet, containing 1 mg of azatadine maleate in the coat, and 60 mg of d-pseudoephedrine sulfate in both the coat and the core, was given at 0 hour. A conventional tablet of 60 mg of d-pseudoephedrine sulfate was given at 0 and 4 hours and a conventional tablet of 1 mg of azatadine maleate was given at 0 hour. The plasma levels of d-pseudoephedrine were measured by gas-liquid chromatography and the amount of azatadine in the urine was determined by a mass fragmentographic procedure. The results showed that there were no statistically significant differences in the measured bioavailability parameters (area under plasma concentration-time curve, maximum plasma concentration and time to reach maximum plasma concentration) for pseudoephedrine from repeat action tablets and conventional d-pseudoephedrine sulfate tablets; neither was there any statistically significant difference in the cumulative urinary excretion of azatadine from the repeat action tablets and conventional azatadine maleate tablets (p > 0·10). These data clearly demonstrate the bioequivalence of the repeat action tablets and the conventional tablets of d-pseudoephedrine and azatadine.

Comparative Bioavailability of d-pseudoephedrine from a Conventional d-pseudoephedrine Sulfate Tablet and from a Repeat Action Tablet

1982 ◽  
Vol 10 (2) ◽  
pp. 126-128
Author(s):  
C Lin ◽  
J Lim ◽  
S Symchowicz
Keyword(s):  
Plasma Concentration ◽  
Tablet Formulation ◽  
Maximum Plasma ◽  
Time Curve ◽  
Tablet Form ◽  
Conventional Tablet ◽  
Concentration Time ◽  
Equivalent Quantity ◽  
Significant Difference ◽  
Comparative Bioavailability

The bioavailability of a single dose of d-pseudoephedrine sulfate administered to male volunteers in repeat action tablet* form (60 mg d-pseudoephedrine sulfate in the coat and 60 mg d-pseudoephedrine sulfate in the core) was compared with the bioavailability of an equivalent quantity of the drug given as two 60 mg conventional tablets, one given at 0 hour and the second 6 hours later. There was no significant difference (p > 0·10) between the conventional tablets and the repeat action tablet formulation in area under the plasma concentration-time curve and the maximum plasma concentration of d-pseudoephedrine. Based on the data, we conclude that the repeat action tablet formulation and the conventional tablet are bioequivalent.

Comparative Bioavailability of a Microsize and Ultramicrosize Griseofulvin Formulation in Man

1982 ◽  
Vol 10 (4) ◽  
pp. 274-277 ◽  
Author(s):  
C Lin ◽  
J Lim ◽  
C DiGiore ◽  
R Gural ◽  
bS Symchowicz
Keyword(s):  
Plasma Concentration ◽  
Maximum Plasma Concentration ◽  
Maximum Plasma ◽  
Healthy Male ◽  
Time Curve ◽  
Concentration Time ◽  
Comparative Bioavailability ◽  
Plasma Concentration Time Curve ◽  
Randomized Crossover Study ◽  
Curve Maximum

The bioavailability of 500 mg of a microsize formulation of griseofulvin has been compared to two new ultramicrosize griseofulvin formulations, two 165 mg tablets and a 330 mg tablet, in sixteen healthy, male, volunteers in a randomized crossover study design. Based on the griseofulvin plasma levels measured at specified times over a 48-hour period, the major bioavailability parameters (i.e., area under plasma concentration-time curve, maximum plasma concentration, and time to reach maximum plasma concentration) were determined and statistically evaluated. The results showed that one 330 mg ultramicrosize tablet is bioequivalent to two 165 mg ultramicrosize griseofulvin tablets and that either ultramicrosize griseofulvin dosage regimen is bioequivalent to 500 mg of the microsize griseofulvin formulation.

scholarly journals Multiple-Dose Safety, Tolerability, and Pharmacokinetics of Oral Nemonoxacin (TG-873870) in Healthy Volunteers

2010 ◽  
Vol 54 (1) ◽  
pp. 411-417 ◽  
Author(s):  
David T. Chung ◽  
Cheng-Yuan Tsai ◽  
Shu-Jen Chen ◽  
Li-Wen Chang ◽  
Chi-Hsin R. King ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Healthy Volunteers ◽  
Bacterial Infections ◽  
Maximum Plasma Concentration ◽  
Maximum Plasma ◽  
Time Curve ◽  
Once Daily ◽  
Concentration Time ◽  
Atypical Pathogens ◽  
Plasma Concentration Time Curve

ABSTRACT Nemonoxacin (TG-873870) is a novel nonfluorinated quinolone with broad-spectrum activities against Gram-positive and Gram-negative aerobic, anaerobic, and atypical pathogens, as well as against methicillin-resistant Staphylococcus aureus, vancomycin-resistant S. aureus, and multiple-resistant bacterial pathogens. We conducted a randomized, double-blind, placebo-controlled, dose-escalating study to ascertain the safety, tolerability, and pharmacokinetics of nemonoxacin. We enrolled 46 healthy volunteers and used a once-daily oral-dosing range of 75 to 1,000 mg for 10 days. Additionally, the food effect was evaluated in subjects in the 500-mg cohort. Nemonoxacin was generally safe and well tolerated, with no significant changes in the clinical laboratory tests or electrocardiograms. Adverse effects, including headache, contact dermatitis, and rash, were mild and resolved spontaneously. Nemonoxacin was rapidly absorbed within 2 h postdosing, and generally, a steady state was reached after 3 days. The maximum plasma concentration and the area under the plasma concentration-time curve were dose proportional over the dosing range. The elimination half-life was approximately 7.5 h and 19.7 h on days 1 and 10, respectively. Approximately 37 to 58% of the drug was excreted in the urine. Food affected the pharmacokinetics, with decreases in the maximum plasma concentration and area under the plasma concentration-time curve of 46% and 27%, respectively. However, the free AUC/MIC90 of nemonoxacin was more than 100 under both the fasting and fed conditions, predicting the efficacy of nemonoxacin against most of the tested pathogens. In conclusion, the results support further clinical investigation of once-daily nemonoxacin administration for antibiotic-sensitive and antibiotic-resistant bacterial infections.

The Pharmacokinetics of Loratadine in Normal Geriatric Volunteers

1988 ◽  
Vol 16 (1) ◽  
pp. 50-60 ◽  
Author(s):  
J. Hilbert ◽  
V. Moritzen ◽  
A. Parks ◽  
E. Radwanski ◽  
G. Perentesis ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
High Performance ◽  
The Elderly ◽  
Maximum Plasma Concentration ◽  
Pharmacokinetic Analysis ◽  
Maximum Plasma ◽  
Open Label ◽  
Post Dose ◽  
Time Curve ◽  
Concentration Time

The pharmacokinetics of loratadine, a non-sedating anti-histamine, were studied in 12 normal geriatric volunteers. In an open label fashion, each volunteer received one 40 mg loratadine capsule. Blood was collected prior to and at specified times (up to 120 h) after dosing. Plasma loratadine concentrations were determined by a specific radioimmunoassay and those of an active metabolite, descarboethoxyloratadine, by high performance liquid chromatography. Concentrations of loratadine in the disposition phase were fitted to a biexponential equation and those of descarboethoxyloratadine to either a monoexponential or biexponential equation for pharmacokinetic analysis. Loratadine was rapidly absorbed, reaching a maximum plasma concentration of 50.5 ng/ml at 1.5 h after dosing. The disposition half-lives of loratadine in the distribution and elimination phases were 1.5 and 18.2 h, respectively. The area under the plasma concentration–time curve, was 146.7 h·ng/ml. Descarboethoxyloratadine had a maximum plasma concentration of 28.0 ng/ml at 2.9 h post-dose and an area under the concentration–time curve of 394.9 h·ng/ml. Its disposition half-lives in the distribution and elimination phases were 2.8 and 17.4 h, respectively. Comparison of these data with those from a previous study of loratadine in young adults showed no clear differences in the disposition half-lives between the two groups. The clearance of loratadine tends to be lower in the elderly, but inter-individual variation within each age group appears greater than any age effect.

Pharmacokinetic interaction between linagliptin and tadalafil in healthy Egyptian males using a novel LC–MS method

Bioanalysis ◽  
2019 ◽  
Vol 11 (14) ◽  
pp. 1321-1336 ◽  
Author(s):  
Sara S Mourad ◽  
Eman I El-Kimary ◽  
Magda A Barary ◽  
Dalia A Hamdy
Keyword(s):  
Plasma Concentration ◽  
Pharmacokinetic Interaction ◽  
Volume Of Distribution ◽  
Maximum Plasma Concentration ◽  
Maximum Plasma ◽  
Qtc Interval ◽  
Qtc Prolongation ◽  
Open Label ◽  
Time Curve ◽  
Concentration Time

Aim: Assessment of pharmacokinetic interaction between linagliptin (LNG) and tadalafil (TDL) in healthy males. Methods: First, a novel LC–MS method was developed; second, a Phase IV, open-label, cross-over study was performed. Volunteers took single 20-mg TDL dose on day 1 followed by wash out period of 2 weeks then multiple oral dosing of 5-mg/day LNG for 13 days. On day 13, volunteers were co-administered 20-mg TDL. Results: LNG and TDL single doses did not affect QTc interval. Smoking did not alter pharmacokinetics/pharmacodynamics of LNG and TDL. Co-administration of LNG with TDL resulted in TDL longer time to reach maximum plasma concentration (Tmax), decreased oral clearance (Cl/F) and oral volume of distribution (Vd/F), increased its maximum plasma concentration (Cmax), area under concentration-time curve (AUC), muscle pain and QTc prolongation. Conclusion: LNG and TDL co-administration warrants monitoring and/or TDL dose adjustment.

Comparative Human Bioavailability Study of Macrocrystalline Nitrofurantoin and Two Prolonged-Action Hydroxymethylnitrofurantoin Preparations

1988 ◽  
Vol 22 (12) ◽  
pp. 959-964 ◽  
Author(s):  
Pieter J.M. Guelen ◽  
Johannes B.J. Boerema ◽  
Tom B. Vree
Keyword(s):  
Plasma Concentration ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Prolonged Action ◽  
Time Curve ◽  
Significant Difference ◽  
Bioavailability Study ◽  
Total Body ◽  
Single Blind ◽  
Healthy Females

This single-blind crossover study compared the human bioavailability of macrocrystalline nitrofurantoin (Furadantine MC) and two prolonged-action hydroxymethylnitrofurantoin formulations (Urfadyn PL, bid, and Uridurine, tid), based on plasma nitrofurantoin concentrations and urinary nitrofurantoin excretion. The drugs were administered to 16 healthy females for a single day according to the recommended daily dosages. For comparison, Furadantine MC was administered both at the qid dosage recommended by the manufacturer and at tid dosage. Pharmacokinetic parameters determined were maximum plasma concentration after first dose, minimum plasma concentration after first dose, area under the plasma concentration-time curve (AUC), cumulative renal excretion over 30 hours (ARE), overall renal clearance, total body clearance, and bioavailability relative to Furadantine MC qid, based on plasma AUC (F) and ARE (Fren). F for Furadantine MC 100 mg tid was 108 ± 25 percent (mean ± SD); for Uridurine 100 mg tid and Urfadyn PL 100 mg bid, F equalled 86 ± 33 percent and 53 ± 20 percent (p<0.05), respectively. A similar relationship was observed between Fren for Furadantine MC 100 mg qid and the respective Fren of Furadantine MC 100 mg tid, Uridurine 100 mg tid, and Urfadyn PL 100 mg bid. No significant difference was found between the respective F and Fren of each of the drugs studied. Although bioavailability was comparable for Furadantine MC tid and qid, the single-day design of these studies precludes inferring that these dosage schedules are therapeutically equivalent. However, the significantly lower relative bioavailabilities for the prolonged-action hydroxymethylnitrofurantoin formulations suggest that Urfadyn PL 100 mg bid and Uridurine 100 mg tid are not pharmacokinetically equivalent to Furadantine MC.

Efficacy of guar gum-based ronidazole capsules as a treatment for Tritrichomonas foetus infection in cats

2016 ◽  
Vol 19 (2) ◽  
pp. 177-184 ◽  
Author(s):  
Aurélien Grellet ◽  
Seyf Eddine Makhlouf ◽  
Loic Desquilbet ◽  
Fani Hovhannessian ◽  
Cassandre Boogaerts ◽  
...  
Keyword(s):  
Clinical Trial ◽  
Placebo Group ◽  
Plasma Concentration ◽  
Guar Gum ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Maximum Plasma Concentration ◽  
Maximum Plasma ◽  
Tritrichomonas Foetus ◽  
Significant Difference

Objectives The aims of the study were to determine the in vitro drug release of guar gum-coated capsules of ronidazole, and to evaluate the pharmacokinetics and efficacy of this formulation for the treatment of cats naturally infected with Tritrichomonas foetus. Methods The pharmacokinetics of ronidazole were evaluated in five healthy cats and five cats infected with T foetus. In a second step, the clinical efficacy of these capsules was evaluated by a controlled, randomised, double-blind clinical trial performed in 47 infected cats from French catteries. In this study, cats were randomly allocated to either the ronidazole treatment group (n = 25) or a placebo group (n = 22). Ronidazole (30 mg/kg) q24h for 14 days was administered to the treated cats. After 14 days of treatment, the presence of T foetus was tested by conventional PCR assay. Results In the pharmacokinetic study, a delayed peak plasma concentration was observed in healthy and infected cats, with no significant difference between these two groups (mean geometric mean of 9 h for time to maximum plasma concentration [Tmax], 21.6 µg/ml for time to maximum plasma concentration [Cmax] and 467.4 μg/h/ml for the area under the curve [AUC] in healthy cats; and 9.4 h for Tmax, 17.1 µg/ml for Cmax and 481 μg/h/ml for AUC in infected cats). In the clinical trial, T foetus was detected in 16% of cats from the treated group and 82% of cats from the placebo group at the end of the study ( P <0.001). No clinical signs of adverse drug reactions were observed. Conclusions and relevance Oral administration of guar gum-coated capsules of ronidazole at a dose of 30 mg/kg once daily for 14 days delays the peak plasma concentration and eradicates infection in most cases.

Preparation and pharmacokinetics of cefquinome sulfate liposomes in goats

2018 ◽  
Author(s):  
Haigang Wu ◽  
Jinni Liu ◽  
Gugangke Xu ◽  
Zhaowei Ye ◽  
Jicheng Liu and Benchi Yi
Keyword(s):  
Plasma Concentration ◽  
Particle Diameter ◽  
Entrapment Efficiency ◽  
Maximum Plasma Concentration ◽  
Maximum Plasma ◽  
Average Particle ◽  
Average Particle Diameter ◽  
Ethanol Injection ◽  
Elimination Half ◽  
Time Point

We evaluated the pharmacokinetics of cefquinome sulfate (CEF) liposomes in eight healthy goats following intramuscular administration at 4 mg/kg. The average particle diameter of CEF liposomes prepared by the ethanol injection method was 335nm with a CEF entrapment efficiency of 69.56%. The elimination half-life (t1/2b) of CEF liposomes was 33.04h compared with 16.21 h for CEF injected without carrier (p less than 0.05). The area under the concentration curve (AUC) for CEF liposomes was approximately three-times greater than for CEF alone (P less than 0.05). The time-point of maximum plasma concentration of the drug (Tp) and the maximum plasma concentration (Cmax) were 4.38 h and 1.99 ìg/mL for CEF liposomes, compared with 1.86 h and 3.55 ìg/mL for CEF without carrier, respectively. 

scholarly journals Plasma appearance and correlation between coffee and green tea metabolites in human subjects

2010 ◽  
Vol 104 (11) ◽  
pp. 1635-1640 ◽  
Author(s):  
Mathieu Renouf ◽  
Philippe Guy ◽  
Cynthia Marmet ◽  
Karin Longet ◽  
Anne-Lise Fraering ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Green Tea ◽  
Phenolic Acids ◽  
Human Subjects ◽  
Coffee Consumption ◽  
Maximum Plasma Concentration ◽  
Maximum Plasma ◽  
Isoferulic Acid ◽  
Long Time ◽  
High Level

Coffee and green tea are two of the most widely consumed hot beverages in the world. Their respective bioavailability has been studied separately, but absorption of their respective bioactive phenolics has not been compared. In a randomised cross-over design, nine healthy subjects drank instant coffee and green tea. Blood samples were collected over 12 h and at 24 h to assess return to baseline. After green tea consumption, ( − )-epigallocatechin (EGC) was the major catechin, appearing rapidly in the plasma; ( − )-EGC gallate (EGCg) and ( − )-epicatechin (EC) were also present, but ( − )-EC gallate and C were not detected. Dihydroferulic acid and dihydrocaffeic acid were the major metabolites that appeared after coffee consumption with a long time needed to reach maximum plasma concentration, suggesting metabolism and absorption in the colon. Other phenolic acid equivalents (caffeic acid (CA), ferulic acid (FA) and isoferulic acid (iFA)) were detected earlier, and they peaked at lower concentrations. Summations of the plasma area under the curves (AUC) for the measured metabolites showed 1·7-fold more coffee-derived phenolic acids than green tea-derived catechins (P = 0·0014). Furthermore, we found a significant correlation between coffee metabolites based on AUC. Inter-individual differences were observed, but individuals with a high level of CA also showed a correspondingly high level of FA. However, no such correlation was observed between the tea catechins and coffee phenolic acids. Correlation between AUC and maximum plasma concentration was also significant for CA, FA and iFA and for EGCg. This implies that the mechanisms of absorption for these two classes of compounds are different, and that a high absorber of phenolic acids is not necessarily a high absorber of catechins.

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