fasting condition
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2021 ◽  
Author(s):  
Ping SHI ◽  
Xin LIU ◽  
Ting LI ◽  
Fei-fei SUN ◽  
Yan-ping LIU ◽  
...  

Abstract Objective To evaluate the pharmacokinetics and bioequivalence between Sitagliptin Phosphate/metformin Hydrochloride Tablets (test formulation) at a single dose of 50mg/850mg and Sitagliptin Phosphate/metformin Hydrochloride Tablets (reference formulation, JANUMET®) at a single dose of 50mg/850mg in healthy Chinese subjects.Methods The study was designed as a randomized, open-lable, two-period double-crossover trial. A total of 24 volunteers under fasting condition and 24 subjects under fed condition were given a single oral dose of 50mg/850mg Sitagliptin Phosphate/metformin Hydrochloride Tablets of test and reference, respectively. Liquid chromatography Tandem mass spectrometry (LC-MS/MS) method was used to determine the concentrations of sitagliptin and metformin in the plasma of subjects. The pharmacokinetic parameters were calculated by WinNonlin 7.0 program and the bioequivalence was evaluated by SAS 9. 4program. Results The 90% confidential interval (CI) of geometric mean ratio under fasting condition for Cmax, AUC0-t and AUC0-∞ of sitagliptin between the test group and the reference group were 101.70%-120.62%, 99.81%-105.61%, 100.27%-106.12% and metformin were 90.39%-111.48%, 94.76%-109.12%, 95.76%-110.38%. The 90% CI of geometric mean ratio under fed condition for Cmax, AUC0-t and AUC0-∞ between the test group and the reference group were 102.12%-117.31%, 100.80%-107.81%, 100.82%-107.78% and metformin were 95.53%-105.22%, 92.76%-103.07%, 93.40%-104.14%. Both were generally well tolerated.Conclusion The two formulations of Sitagliptin Phosphate/metformin Hydrochloride Tablets were bioequivalent under fasting and fed condition in healthy Chinese subjects.Trial registration Clinical Trial Registry (trial ID: NCT04877106).


Author(s):  
Sabine Daemen ◽  
Nynke van Polanen ◽  
Lena Bilet ◽  
Esther Phielix ◽  
Esther Moonen-Kornips ◽  
...  

Intramyocellular lipid (IMCL) content is an energy source during acute exercise. Non-esterified fatty acid (NEFA) levels can compete with IMCL utilization during exercise. IMCL content is stored as lipid droplets (LDs) that vary in size, number, subcellular distribution and in coating with LD protein PLIN5. Little is known about how these factors are affected during exercise and recovery. Here, we aimed to investigate the effects of acute exercise with and without elevated NEFA levels on intramyocellular LD size and number, intracellular distribution and PLIN5 coating, using high-resolution confocal microscopy. In a cross-over study, 9 healthy lean young men performed a 2h moderate intensity cycling protocol in the fasted (high NEFA levels) and glucose-fed state (low NEFA levels). IMCL and LD parameters were measured at baseline, directly after exercise and 4h post-exercise. We found that total IMCL content was not changed directly after exercise (irrespectively of condition), but IMCL increased 4h post-exercise in the fasting condition, which was due to an increased number of LDs rather than changes in size. The effects were predominantly detected in type I muscle fibers and in LDs coated with PLIN5. Interestingly, subsarcolemmal, but not intermyofibrillar IMCL content, was decreased directly after exercise in the fasting condition and was replenished during the 4h recovery period. In conclusion, acute exercise affects IMCL storage during exercise and recovery, particularly in type I muscle fibers, in the subsarcolemmal region and in the presence of PLIN5. Moreover, the effects of exercise on IMCL content are affected by plasma NEFA levels.


Author(s):  
DIBYA DAS ◽  
DHIMAN HALDER ◽  
ANIRBANDEEP BOSE ◽  
CHIRANJIT SAHA ◽  
HIMANGSHU SEKHAR MAJI ◽  
...  

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.


Author(s):  
Kiran S. Chaudhari ◽  
Milind Bagul ◽  
Ketan Shah

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.


2021 ◽  
pp. 155005942110009
Author(s):  
Christoph Bamberg ◽  
Vera Flasbeck ◽  
Georg Juckel ◽  
Martin Brüne

Serotonin is an important neuromodulator involved in many physiological processes including mood and satiety. In the brain, serotonin is manufactured from tryptophan, as serotonin itself cannot cross the blood–brain barrier. Previous research has shown that blood-tryptophan levels increase upon ingestion of carbohydrates and decrease upon protein consumption. How this translates into serotonin availability is as yet under-researched. Therefore, we examined the effect of fasting versus consuming carbohydrates or protein on central serotonergic activity using a repeated-measures crossover design in a sample of 37 healthy men. The loudness dependence of auditory-evoked potentials (LDAEP) serves as a noninvasive method to study central serotonergic activity. Blood-glucose levels and mood changes were also monitored before and after the nutritional intervention. The intervention had a significant nutrition-specific effect on LDAEP and blood-glucose levels. A significant difference emerged between the fasting condition and satiety, with LDAEP being lower during satiety, irrespective of the type of food. Thus, this indicator of serotonergic activity increased after food consumption, which was further related to mood improvement. Moreover, the LDAEP differed between the 2 measurements only for the carbohydrate testing day, suggesting that LDAEP can be selectively modulated by the type of nutrition consumed. Our data further indicate a high intraindividual stability of LDAEP, as the electrophysiological signals were very similar in the fasting condition across the 2 testing days. Together, these findings demonstrate that the LDAEP can serve as a biological marker for central serotonergic activity, while at the same time being sensitive to nutritional changes.


2021 ◽  
Vol 11 (1) ◽  
pp. 48-59
Author(s):  
Mahavir Singh ◽  
Lalit Singh Ranawat

Oral drug delivery is the most preferred route for the various drug molecules among all other routes of drug delivery, because ease of administration which lead to better patient compliance. So, oral extended release drug delivery system becomes a very promising approach for those drugs that are given orally but having the shorter half-life and high dosing frequency. Extended release Extended-release systems allow for the drug to be released over prolonged time periods. By extending the release profile of a drug, the frequency of dosing can be reduced. The study was an open label, balanced, randomized, three-treatment, three-period, three-sequence, single oral dose, crossover, bioequivalence study in normal healthy adult human subjects under fasting condition, with a screening period of 28 days prior to IMP administration in Period-I. In each study period, 27 blood samples, including one pre-dose blood sample, were collected from each subject except for the discontinued / withdrawn subjects to analyze the pharmacokinetic profile of the two test products (T1 and T2) as well as the reference product. The pharmacokinetic parameters were calculated from the plasma concentration vs. time profile by non-compartmental model using Phoenix® WinNonlin® Version 6.4 (Certara L.P.) for Metoprolol. Out of 18 subjects enrolled, data of 13 subjects were analyzed. Mean Cmax is 31.634 ± 22.6007 ng/mL, 31.241 ± 20.6090 ng/mL and 31.773 ± 23.1819 ng/mL, mean AUCo-t is722.992 ± 584.3793 ng hr/mL, 658.192 ± 492.3416 ng hr/mL and 706.219 ± 546.5064 ng hr/mL, mean AUC0-inf is 751.204 ± 631.9623 ng hr/mL, 676.939 ± 519.1306 ng hr/mL and729.505 ± 578.1691 ng hr/mL for test product (T1), test product (T2) and reference product (R).Test Products (T1 and T2) when compared with the Reference Product-R meets the bioequivalence criteria with respect to Cmax, AUC0-t and AUC0-∞ for Metoprolol under fasting condition as per criteria set in the protocol.


2020 ◽  
Author(s):  
Li Xin ◽  
Chenjing Wang ◽  
Ting Li ◽  
Yanping Liu ◽  
Shuqin Liu ◽  
...  

Abstract Background: Levamlodipine, a calcium channel blocker, is used in treatment of hypertension. To compare the pharmacokinetic parameters between levamlodipine test formulation at a single dose of 5 mg and amlodipine reference formulation at a single dose of 10 mg, the bioequivalence study was carried out.Methods: A single-dose randomized, open-label, two-period crossover study was designed in healthy Chinese subjects. 48 subjects were divided into fasting and high-fat meal group equally. The subjects randomly received the test or reference formulations at the rate of 1:1. Following a 21-day washout period, the alternative formulations were received. The blood samples were collected at 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14, 24, 36, 48, 72, 96, 120, 144, 168 hours later. Liquid chromatography-tandem mass spectrometry (LC-MS/MS) was applied to determine levamlodipine in the plasma samples.Results: Within equivalence limits between 80 ~ 125%, the test formulation and the reference formulation were bioequivalent, with the 90% confidence intervals (CIs) for the ratio of geometric means of Cmax, AUC0-t, and AUC0-∞. The data were shown as Cmax (89.59% ~ 101.61%), AUC0-t (87.83% ~ 94.87%) and AUC0-∞ (86.28% ~ 93.49%) under fasting condition, Cmax (90.93% ~ 102.37%), AUC0–t (95.75% ~ 104.93%) and AUC0–∞ (95.36% ~ 105.33%) under high-fat meal condition. Serious adverse event was not observed.Conclusions: The trial confirmed that levamlodipine at a single dose of 5 mg and amlodipine at a single dose of 10 mg were bioequivalent under both fasting condition and high-fat meal condition.Trial registration: Cinicaltrials, NCT04411875. Registered 3 June 2020 - Retrospectively registered, https://register.clinicaltrials.gov/prs/app/action/SelectProtocol?sid=S0009W1Q&selectaction=Edit&uid=U00050YQ&ts=3&cx=-6iqkm8


Author(s):  
Ye Htut Linn ◽  
Myat Myat Soe ◽  
K Khine Thu ◽  
Thida Tun ◽  
Mi Kun Kaw San ◽  
...  

Background: Tramadol is one of the most commonly used analgesics, thanks to its efficacy and safety. It is widely used in Myanmar for postoperative and cancer pain control. The use of generic drugs has been steadily increasing worldwide, mostly in developing countries. Generic drugs should have efficacy and safety comparable to their innovators or other approved generic products. Objectives: This study aims to compare the bioequivalence of locally producing, Tramadol BPI® capsule (test product) with the Tramazac® capsule (reference product) in healthy Myanmar volunteers. Methods: The bioequivalence was determined in 16 healthy Myanmar volunteers after a single oral administration of 100 mg tramadol (under fasting condition) in a randomized, openlabel, two-period, and two-treatment crossover study with a two-week washout period. Blood samples were collected at specified times, and plasma tramadol concentrations were measured with a validated high-performance liquid chromatography method with a fluorescence detector. Pharmacokinetic parameters were determined using the plasma concentration-time data in a noncompartmental model. Results: The analysis of variance of the logarithmically transformed parameters (maximum plasma concentration (Cmax), Area Under the concentration-time Curve from the time of administration to the last measured concentration (AUC0-t), and to infinity (AUC0-∞) revealed no sequence, period, and formulation effects between the test and reference products. Significant differences were found between the subjects within the sequence for both AUC0-t, and AUC0-∞, indicating a substantial intersubject variation. The geometric mean ratio of test/reference and their 90% confidence intervals were within the ASEAN (Association of Southeast Asian Nations) bioequivalence acceptance interval of 80% to 125%. Conclusion: Tramadol BPI® and Tramazac® capsules, after a single oral administration of 100 mg, were bioequivalent in respect of their rate and extent of absorption under fasting condition.


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