scholarly journals Pharmacokinetics Evaluation of Acamprosate Tablets in Healthy Human Volunteers

2021 ◽  
pp. 79-88
Author(s):  
Kiran S. Chaudhari ◽  
Milind Bagul ◽  
Ketan Shah
Keyword(s):  
Human Subjects ◽  
Bioequivalence Study ◽  
Healthy Male Subject ◽  
Pharmacokinetic Property ◽  
Pharmacokinetic Data ◽  
Open Label ◽  
Healthy Human ◽  
Entire Study ◽  
Fasting Condition ◽  
Single Dosing

Pharmacokinetic data of acamprosate tablets was not accessible on large number of human. Rationale to examine the pharmacokinetic properties of acamprosate calcium in healthy male subject, on single or multiple dosage administration, to evaluate the bioequivalence of two formulations of acamprosate calcium tablets in fast or fed environment. This work engross the study of pharmacokinetic property of Acamprosate calcium tablets in single dosing under fasting condition. Methods: Bioequivalence study of delayed release acamprosate tablets 333 mg for a randomized, single dose, open label, two treatment, two periods, two sequences and crossover design in 12 healthy, adult human subjects under fasting condition was conducted. The wash out period within the each treatment and each stage was 1 week. The quantification of acamprosate was done by LCMS/MS method. Accessibility was evaluated by monitoring adverse events, physical examinations and ECG and laboratory tests. Results: The entire study was conducted by using 12 male subjects to fulfill all stages in the study. The pharmacokinetic calculations for test and reference formulations are as follows: single dosing, Tmax 8.54 ± 5.24 and 10.71 ± 5.41 h, Cmax 146.06 ± 99.73 and 115.01 ±86.26 ng · mL−1, AUC0-t 1391.95 ± 731.24 and 1557.03 ± 960.98 ng·mL−1·h, AUC0–∞ 1987.40 ± 962.84 and 2720.21 ± 1931.79 ng·mL−1·h, respectively. In all three stages, 90% CIs for the test/reference ratio of AUC0–t and AUC0–∞ was to be found within 80% –125% of acamprosate calcium. Conclusions: As per regulatory guidelines, pharmacokinetics parameters for acamprosate calcium were found to be within the acceptance criteria.

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.

scholarly journals BIOEQUIVALENCE STUDY OF AZELNIDIPINE 16 MG TABLET TO EVALUATE PHARMACOKINETIC PROFILE OF SINGLE DOSE IN HEALTHY, ADULT, HUMAN VOLUNTEERS UNDER FASTING CONDITION

2021 ◽  
pp. 154-159
Author(s):  
DIBYA DAS ◽  
DHIMAN HALDER ◽  
ANIRBANDEEP BOSE ◽  
CHIRANJIT SAHA ◽  
HIMANGSHU SEKHAR MAJI ◽  
...  
Keyword(s):  
Single Dose ◽  
Healthy Volunteers ◽  
Plasma Sample ◽  
Reference Product ◽  
Bioequivalence Study ◽  
Pharmacokinetic Parameters ◽  
Open Label ◽  
Entire Study ◽  
Test Product ◽  
Fasting Condition

Objective: The present study's objective is to conduct a comparative bioavailability study with a special emphasis on the test product's bioequivalence using a standard reference product as a comparator. Methods: Before initiating the bioequivalent study, the plasma sample analysis method was developed and validated by using LC-MS/MS method. The entire study was conducted as a single-dose crossover randomized bioequivalence study with open-label, two treatment, two-period, and two sequences on 24 healthy volunteers under fasting condition. With proper informed consent process the oral dose of the Reference product (R) or Test product (T) was administered on healthy volunteers at 0 h during each period of the study. After the drug's oral administration, a certain quantity of blood sample was collected, and the plasma sample was separated using a cold centrifuge. The plasma samples were analysed by using the validated LC-MS/MS method. The pharmacokinetic parameters, statistical data and ANOVA of the test and reference product were evaluated. Results: The Cmax, Auc0-t, AUC0-∞ and tmax of the test product were found to be 6.29 ng/ml, 117.0 ng. h/ml, 161.67 ng. h/ml and 3.33 h. respectively. And the Cmax, Auc0-t, AUC0-∞ and tmax of reference product were found 6.59 ng/ml, 123.21 ng. h./ml, 172.20 ng. h/ml and 3.38 h respectively. Relative bioavailability was found 94.96%. The overall results show that the 90% confidence intervals (Log-Transformed and Untransformed) for Cmax, AUC0-t and AUC0-∞ for Azelnidipine were within the acceptable limit of 80%-125%. Conclusion: The entire study's conclusion can be drawn as the test product was bioequivalent with the reference product's comparator.

scholarly journals A Comparative Pharmacokinetic Evaluation of a Bioavailable Curcumin Formulation Curene® with Curcumin Formulation Containing Turmeric Volatile Oil and Standard Curcuminoids 95% in Healthy Human Subjects

2019 ◽  
Vol 9 (2) ◽  
pp. 134
Author(s):  
Sanjib Kumar Panda ◽  
Somashekara ◽  
Vivek A. Parachur ◽  
Nilima Mohanty ◽  
Tathastu Swain ◽  
...  
Keyword(s):  
Human Subjects ◽  
Health Benefits ◽  
Volatile Oil ◽  
Relative Bioavailability ◽  
Healthy Male ◽  
Open Label ◽  
Healthy Human ◽  
Comparative Pharmacokinetic ◽  
Reference Treatment ◽  
Healthy Human Subjects

Background: Curcumin, a major active component of turmeric, which is one of the most studied botanicals for its numerous health benefits and higher safety profile. In spite of its potent clinical health benefits, its applications are circumscribed due to its poor bioavailability. The current study was carried out to compare the oral bioavailbility of newly developed bioavailable curcumin formulation Curene® with Curcumin formulation containing turmeric volatile oil (CP-01) and Standard Curcuminoids 95% in healthy human volunteers.Methods: In this current open-label, randomized, three treatments, single oral dose, single period, parallel, comparative pharmacokinetics study, 12 healthy male volunteers participated. The test product Curene® (T), reference products CP-01(Reference treatment-R1) and Standard Curcuminoids 95% (Reference treatment-R2) were orally administrated as a single dose of 3 grams per subject. Plasma samples were withdrawn from each subject at predetermined timepoints and samples were analyzed by LC-MS/MS. Results: Based on the pharmacokinetics data, the relative bioavailability (Free Curcumin; AUC0-t) of Curene® was found to be ~112.7 times more when compared to the standard Curcuminoids (R2).Conclusion: The oral bioavailability of Curene® was found to be significantly higher compared to CP-01and Standard Curcuminoids (95%) furthermore, it was also found to be safe in healthy human subjects under the study conditions.

scholarly journals Quantification of Paroxetine in Human Plasma by Liquid Chromatography Coupled with Electrospray Ionization Tandem Mass Spectrometry

2010 ◽  
Vol 93 (1) ◽  
pp. 141-149 ◽  
Author(s):  
Hiten J Shah ◽  
Mohan L Kundlik ◽  
Abhijit Kakad ◽  
Nitesh K Patel ◽  
Ankit Pandya ◽  
...  
Keyword(s):  
Electrospray Ionization ◽  
Human Plasma ◽  
Solid Phase ◽  
Human Subjects ◽  
Internal Standard ◽  
Bioequivalence Study ◽  
Selected Reaction Monitoring ◽  
Healthy Human ◽  
Healthy Human Subjects ◽  
Imipramine Hydrochloride

Abstract A rapid LC coupled with electrospray ionization (ESI) MS/MS method was developed and validated for the quantification of paroxetine in heparinized human plasma. The plasma samples were prepared by the solid-phase extraction method without drying or reconstitution. Elution was done with 0.5 mL 0.2 (v/v) formic acid in methanolacetonitrile (65 + 35, v/v). The analyte and the internal standard (IS; imipramine hydrochloride) were chromatographed on a BDS Hypersil C18 column. The analyte was analyzed by LC/MS/MS with only 1.7 min run time. An ESI interface was chosen for ionization of the analyte from the sample matrix. Selected reaction monitoring mode for detection of paroxetine and the IS were achieved by using m/z 330.17/192.10 and 281.13/86.14, respectively. The LC retention times for paroxetine and imipramine were 0.94 and 1.05 min, respectively. The method was linear in the concentration range of 0.580.0 ng/mL with r ≥0.9995. Recovery of paroxetine and imipramine ranged from 90 to 95. The assay has been successfully applied to bioequivalence study samples for estimation of paroxetine in healthy human subjects.

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.

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