Pharmacokinetic Evaluation of Two Brands of Linezolid Tablets in Healthy Human Volunteers

2010 ◽  
Vol 3 (2) ◽  
pp. 933-939
Author(s):  
Parameshwar P ◽  
Y N Rao ◽  
Shobha J C ◽  
Y N Reddy ◽  
V M Reddy
Keyword(s):  
Lower Limit ◽  
Bioequivalence Study ◽  
Hplc Method ◽  
Pharmacokinetic Parameters ◽  
Healthy Human ◽  
Blood Samples ◽  
Upper Limit ◽  
Human Volunteers ◽  
Significant Difference ◽  
Healthy Adult Male

The aim of a  randomized, balanced, two treatment, two-period, two-sequence, single-dose, crossover pilot bioavailability and bioequivalence study conducted in 12 healthy adult male volunteers under fasting conditions was to compare steady state pharmacokinetics of Linezolid 600mg tablets of Dr.Reddy’s Laboratories Ltd, and Zyvox ® (Linezolid) 600mg tablets of Pharmacia & Upjohn Company, USA. The subjects were dosed once during the study and the pre-dose blood samples were collected within 1 hr prior to dosing. The concentrations of Linezolid from the blood samples were quantified by validated HPLC method and pharmacokinetic parameters were computed. 90% Confidence intervals of reference Vs test for Cmax  lower limit 87.23 and upper limit 109.24, AUC0-t lower limit 86.20 and upper limit 109.17, AUCO-α lower limit 85.48 and upper limit 111.54. Analysis of variance (ANOVA) did not show significant difference to these parameters. Based on the results obtained, both the formulations have exhibited the same rate and extent of absorption, indicating switch ability in clinical practice.

Effect of silymarin pretreatment on the bioavailability of domperidone in healthy human volunteers

2014 ◽  
Vol 29 (4) ◽  
Author(s):  
Shravan Kumar Yamsani ◽  
Madhusudan Rao Yamsani
Keyword(s):  
Oral Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Rat Intestine ◽  
Healthy Human ◽  
P Glycoprotein ◽  
Human Volunteers ◽  
Significant Difference

AbstractThe aim of this study was to investigate the effect of silymarin pretreatment on domperidone oral bioavailability in humans.The rats were pretreated with silymarin for 7 days. The transport of domperidone across the rat intestine (duodenum, jejunum, ileum, and colon) was studied by usingIn the everted sac and non-everted sac study with silymarin pretreatment, domperidone transport increased from the duodenum, jejunum, ileum, and colon. The silymarin pretreatment increased the bioavailability of domperidone. There was a statistically significant difference in the pharmacokinetic parameters CThe significant difference in absorption of domperidone on pretreatment with silymarin is due to the inhibition of P-glycoprotein and CYP3A. Silymarin, which inhibits CYP3A4, should be contraindicated for domperidone.

scholarly journals Bioequivalence study of different brands of vildagliptin in healthy human subjects

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Mahaveer Sharma ◽  
S. S. Agrawal
Keyword(s):  
Single Dose ◽  
Healthy Volunteers ◽  
Geometric Mean ◽  
Bioequivalence Study ◽  
Pharmacokinetic Parameters ◽  
Open Label ◽  
Healthy Human ◽  
Single Dose Study ◽  
Dipeptidyl Peptidase 4 ◽  
Significant Difference

Abstract Background Vildagliptin is a dipeptidyl peptidase-4 inhibitor used to treat diabetes mellitus. No bioequivalence study data have been published for the Indian population comparing bioequivalence of vildagliptin brands Galvus, Zomelis, and Jalra. This study aimed to evaluate the bioequivalence between three brands of vildagliptin 50 mg tablet (test 1, Zomelis; test 2, Jalra; and reference, Galvus) and to compare these test formulations with the reference formulation to meet the regulatory requirements of bioequivalence of CDSCO, India. The study was conducted in the clinical research center of the college after enrolling 12 healthy volunteers. This study was a single-dose, randomized, open-label, balanced, three treatment, three period, under fasting condition in 12 adult healthy volunteers. After overnight fasting, the subjects received a single dose of either of any three brands of the vildagliptin tablet (T1—test 1; T2—test 2; and R—reference). The washout period was 7 days. Randomization was in the way of T1T2R in the first period, T2T1R in the second period, and RT1T2 in the third period. Blood samples were collected, after that drug concentration in the plasma was measured with the help of HPLC. Outcome measures 90% confidence interval of the geometric mean ratios (test/reference) for the LnCmax, LnAUC0-t, and LnAUC0-∞ was calculated. Results The AUC0-t was 1390.03, 1401.50, and 1409.37 ng h/ml for the T1, T2, and R, respectively. Cmax was 287.89, 287.41, and 285.17 ng/ml for the T1, T2, and R, respectively. AUC0-∞ was 1452.03, 1467.59, and 1473.53 ng h/ml for the T1, T2, and R, respectively. No significant difference was observed in the pharmacokinetic parameters between the T1, T2, and R. The geometric mean ratios for T1/R for LnCmax, LnAUC0-t, and LnAUC0-∞ were 1.0014 (90% CI, 1.0002–1.0026), 0.9992 (90% CI, 0.9971–1.0013), and 0.9994 (90% CI, 0.9973–1.0016), respectively. For the T2/R, geometric mean ratios for LnCmax, LnAUC0-t, and LnAUC0-∞ were 1.0003 (90% CI, 0.9992–1.0013), 0.9988 (90% CI, 0.9969–1.0008), and 0.9985 (90% CI, 0.9961–1.0010), respectively. Conclusion In this single-dose study involving Indian healthy volunteers under fasting conditions, the three brands of vildagliptin (Zomelis, Jalra, and Galvus) were bioequivalent as per the bioequivalence criterion of CDSCO, India.

scholarly journals Comparative Bioavailabilitv Studv of Two Brands of Terbutaline Sulphate Tablets in Healthy Human Volunteers

2004 ◽  
Vol 72 (3) ◽  
pp. 227-237
Author(s):  
Nahla S. Barakat ◽  
Nawal M. Khalafallah ◽  
Said A. Khalil
Keyword(s):  
Single Dose ◽  
Reference Product ◽  
Hplc Method ◽  
Fasting State ◽  
Unchanged Drug ◽  
Healthy Human ◽  
Terbutaline Sulphate ◽  
Human Volunteers

The purpose of this study was to evaluate the bioavailability of locally produced 2.5 mg terbutaline sulphate tablets (brand A ) relative to a reference product, Bricanyl 2.5 mg tablets (brand 6). The study was a single dose 5 mg randomized crossover one in 15 healthy volunteers in the fasting state. Urine was collected at intervals of 24 h. Total terbutaline excreted in urine as unchanged drug and as conjugates (sulphate and glucuronide) was determined by a developed and validated HPLC method. In-vitro characteristics of both brands were similar. Based on percent of the dose excreted in urine, the oral bioavailability ranged from 33.5% to 75.8% for both brands. Statistics were applied to judge bioequivalence according to USP 24 in-vivo bioequivalence guidance. Results indicated that brand A and B were bioequivalent and hence interchangeable in medical practice.

Bioavailability and pharmacokinetic study of Metformin 500 mg tablet (SR formulations) in healthy human volunteers

2017 ◽  
Vol 3 (3) ◽  
pp. 354-358
Author(s):  
Ashish Kumar ◽  
Pradeep Singh ◽  
Garima Mishra
Keyword(s):  
Bioequivalence Study ◽  
Metformin Hydrochloride ◽  
Reference Standard ◽  
Reference Formulation ◽  
Open Label ◽  
Healthy Human ◽  
Fasting Condition ◽  
Test Formulation ◽  
Acceptable Range ◽  
Human Volunteers

Bioavailability and Bioequivalence studies have become an important part of the clinical research in India. This study was performed to find out the safety and efficacy of two Metformin 500 mg tablet (SR formulations). This study was an open label, balanced, randomized, two treatment, two periods, two sequences, single dose, cross over bioequivalence study under fasting condition. Metformin Hydrochloride (SR) 500 mg tablet was the Test formulation and Dibeta SR tablet [containing Metformin Hydrochloride (SR) 500 mg] was the Reference standard. Volunteers were randomly given a single oral dose of the test and the reference formulation under fasting condition, with a washout period of 07 days. Drug concentration in the plasma samples were quantified by using a validated method on LC/MS/MS. Win Nonlin Version 5.2 software was used for statistical calculations. Cmax, AUC0-t and AUC0-∞ values of the test formulation and reference standard were 89.13%, 87.46%, 88.29%, and 112.44%, 123.85% and 123.87%, respectively. Cmax, AUC0-t and AUC0- ∞ values of the test formulation and reference standard fall within the acceptable range of 80–125%. So, the present study concludes that the test formulation is bioequivalent to the reference standard.

Bioequivalence study of two commercial amoxicillin suspension formulations in healthy human volunteers

2014 ◽  
Vol 52 (05) ◽  
pp. 425-430 ◽  
Author(s):  
Gilson C.N. Franco ◽  
Sinvaldo Baglie ◽  
Ana P.B. Ruenis ◽  
Luiz M. Franco ◽  
Karina Cogo ◽  
...  
Keyword(s):  
Bioequivalence Study ◽  
Healthy Human ◽  
Human Volunteers

scholarly journals Bioequivalence study of cefepime intramuscular injection

2014 ◽  
Vol 8 (2) ◽  
pp. 237-240
Author(s):  
Monchana Jullangkoon ◽  
Sutep Jaruratanasirikul ◽  
Nanchanit Aeinlang
Keyword(s):  
Intramuscular Injection ◽  
Bioequivalence Study ◽  
Generation Cephalosporin ◽  
Fourth Generation ◽  
Pharmacokinetic Parameters ◽  
Reference Formulation ◽  
Photodiode Array Detection ◽  
Serious Adverse Events ◽  
Pharmaceutical Firms ◽  
Significant Difference

Abstract Background: Cefepime, a fourth generation cephalosporin, is a broad spectrum antibiotic effective against both Gram positive and Gram negative bacteria. It is available from several pharmaceutical firms in southeast Asia. We studied bioequivalence of two products. Objective: To assess the bioequivalence of two cefepime formulations: Cefamax 1 g intramuscular (Siam Pharmaceutical, Bangkok, Thailand) as the test formulation and Maxipime 1 g (Bristol-Myers Squibb, Bangkok, Thailand) as the reference formulation. Methods: The study was conducted as an open, randomized, two-period crossover trial with a 1 week washout period in 18 healthy volunteers. Each subject received a single dose of 1 g intramuscular injection of the test or reference formulation. Blood samples were collected via an intravascular catheter at several time points over a 12 h period. Plasma cefepime concentrations were quantified by HPLC with photodiode array detection at 280 nm. The statistical comparisons for pharmacokinetic parameters were made using a paired t test. Results: There was no significant difference in the logarithmically transformed values of Cmax, AUC0-12, and AUC0-∞ between Cefamax and Maxipime using an analysis of variance (ANOVA). The 90% confidence intervals (CIs) of Cmax, AUC0-12, and AUC0-∞ between the two formulations were 91.17-105.78, 90.29-97.63, and 88.89-96.57, respectively. All subjects had good tolerance and no serious adverse events were observed. Conclusion: Cefamax 1 g intramuscular formulation is bioequivalent to Maxipime 1 g intramuscular formulation based on 90% CIs for Cmax, AUC0-12, and AUC0-∞ within 80%-125%.

scholarly journals A Liquid Chromatography-Tandem Mass Spectrometry Method for Evaluation of Two Brands of Enalapril 20 mg Tablets in Healthy Human Volunteers

2017 ◽  
Vol 2017 ◽  
pp. 1-8
Author(s):  
Wael Abu Dayyih ◽  
Mohammed Hamad ◽  
Ahmad Abu Awwad ◽  
Eyad Mallah ◽  
Zainab Zakarya ◽  
...  
Keyword(s):  
Enzyme Inhibitor ◽  
Internal Standard ◽  
Pharmacokinetic Parameters ◽  
Healthy Human ◽  
Chronic Heart Disease ◽  
Chromatography Tandem Mass Spectrometry ◽  
Human Volunteers ◽  
Treatment Of Hypertension ◽  
Liquid Chromatography Tandem Mass ◽  
Enalapril And Enalaprilat

Enalapril is an angiotensin-converting enzyme inhibitor used for treatment of hypertension and chronic heart disease. Enalaprilat is its active metabolite responsible for the activity. This study aimed to develop and validate a method for enalapril and enalaprilat analysis and to determine the bioequivalence of two tablet formulae of enalapril. LC-MS/MS bioanalytical method was developed and validated and then applied to evaluate the bioavailability of two enalapril formulae. Antihyperglycemic sitagliptin was used as internal standard (IS). The method was accurate for the within- and between-days analysis, and precise CV% was <5%, being linear over the calibration range 1.0–200.0 ng/ml. Stability was >85% and the LOD was 0.907 and 0.910 ng/ml for enalapril and enalaprilat, respectively, and LLOQ was 1 ng/ml. The pharmacokinetic parameters Cmax, tmax, AUC0–72, and AUC0–∞ values of enalapril and enalaprilat of the two formulae were calculated and nonsignificant differences were found. A linearity, specific, accurate, and precise method was developed and applied for the analysis of enalapril and enalaprilat in human plasma after oral administration of two formulae of enalapril 20 mg tablets in healthy volunteers. Depending on the statistical analysis it was concluded that the two enalapril formulae were bioequivalent.

scholarly journals Allium sativumL. Improves Visual Memory and Attention in Healthy Human Volunteers

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Sara Tasnim ◽  
Parsa Sanjana Haque ◽  
Md. Sazzadul Bari ◽  
Md. Monir Hossain ◽  
Sardar Mohd. Ashraful Islam ◽  
...  
Keyword(s):  
Executive Function ◽  
Verbal Memory ◽  
Visual Memory ◽  
Neuropsychological Test ◽  
Healthy Human ◽  
Beneficial Effects ◽  
Memory And Attention ◽  
Human Volunteers ◽  
Short Period ◽  
Significant Difference

Studies have shown thatAllium sativumL. (AS) protects amyloid-beta peptide-induced apoptosis, prevents oxidative insults to neurons and synapses, and thus prevent Alzheimer’s disease progression in experimental animals. However, there is no experimental evidence in human regarding its putative role in memory and cognition. We have studied the effect of AS consumption by healthy human volunteers on visual memory, verbal memory, attention, and executive function in comparison to control subjects taking placebo. The study was conducted over five weeks and twenty volunteers of both genders were recruited and divided randomly into two groups: A (AS) and B (placebo). Both groups participated in the 6 computerized neuropsychological tests of the Cambridge Neuropsychological Test Automated Battery (CANTAB) twice: at the beginning and after five weeks of the study. We found statistically significant difference (p<0.05) in several parameters of visual memory and attention due to AS ingestion. We also found statistically nonsignificant (p>0.05) beneficial effects on verbal memory and executive function within a short period of time among the volunteers. Study for a longer period of time with patients suffering from neurodegenerative diseases might yield more relevant results regarding the potential therapeutic role of AS.

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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