Pharmacokinetics and Bioequivalence of 2 Immediate‐Release Tofacitinib Tablet Formulations in Chinese Healthy Volunteers Under Fasting and Fed Conditions

2020 ◽  
Author(s):  
Xin Li ◽  
Lihua Liu ◽  
Yang Deng ◽  
Yuan Li ◽  
Ping Zhang ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Immediate Release ◽  
Tablet Formulations

scholarly journals Dissolution efficiency and bioequivalence study using urine data from healthy volunteers: a comparison between two tablet formulations of cephalexin

2015 ◽  
Vol 51 (2) ◽  
pp. 383-392
Author(s):  
Cristina Helena dos Reis Serra ◽  
Kyung Hee Chang ◽  
Thaisa Marinho Dezani ◽  
Valentina Porta ◽  
Sílvia Storpirtis
Keyword(s):  
Urinary Excretion ◽  
Healthy Volunteers ◽  
High Performance ◽  
Bioequivalence Study ◽  
Immediate Release ◽  
International Standards ◽  
Pharmacokinetic Parameters ◽  
Tablet Formulations ◽  
Dissolution Efficiency

<p>The aim of the present study was to assess the bioequivalence of two cephalexin tablet formulations available in the Brazilian market (product A as reference formulation and product B as test formulation). Dissolution efficiency (DE%) was calculated for both formulations to evaluate their <italic>in vitro</italic>biopharmaceutical features. The oral bioequivalence study was performed in twenty-four healthy volunteers in a crossover design. Single oral dose (tablet containing 500 mg of cephalexin) of each product was administered with two weeks of washout period. Urinary concentrations of cephalexin were measured by high-performance liquid chromatography (HPLC) method and pharmacokinetics parameters were estimated by urinary excretion data. The bioequivalence was determined by the following parameters: the cumulative amount of cephalexin excreted in the urine, the total amount of cephalexin excreted in the urine and the maximum urinary excretion rate of cephalexin. DE values of immediate-release cephalexin tablets (500 mg) were 68.69±4.18% for product A and 71.03±6.63% for product B. Regarding the dissolution test of the two brands (A and B) analysed, both were in compliance with the official pharmacopeial specifications, since the dissolution of both formulations was superior to 80% of the amount declared in the label after 45 minutes of test (A=92.09%±1.84; B=92.84%±1.08). The results obtained indicated that the products A and B are pharmaceutical equivalents. Confidence intervals for the pharmacokinetic parameters were in compliance with the international standards, indicating that products A and B can be considered bioequivalents and, therefore, interchangeable.</p>

scholarly journals Reduced gastric injury with a novel, liquid lipid-aspirin formulation: results from a pooled, patient level analysis of two randomized endoscopy studies In healthy volunteers

2020 ◽  
Vol 41 (Supplement_2) ◽  
Author(s):  
D.L Bhatt ◽  
J Scheiman ◽  
D.J Angiolillo ◽  
P.G Steg ◽  
G.D Dangas ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Primary Outcome ◽  
Immediate Release ◽  
Platelet Inhibition ◽  
Gastric Injury ◽  
Funding Source ◽  
Private Company ◽  
Patient Level ◽  
Repeat Endoscopy ◽  
Initiation Of Therapy

Abstract Background Gastrointestinal (GI) toxicity from aspirin is high at the time of initiation of therapy. Objective The current analysis aimed to determine rates of endoscopically detected gastroduodenal erosions and ulcers after 7 days of either immediate release aspirin (IR-ASA) or a novel, pharmaceutical lipid-aspirin complex (PL-ASA) liquid formulation that has an antiplatelet effect similar to IR-ASA. Methods Two randomized, single blind, multicenter active control studies comparing upper GI damage after 7 days of 325 mg PL-ASA or IR-ASA in healthy volunteers not taking a gastroprotectant and who had a negative baseline endoscopy were pooled at the patient level. The primary outcome was the composite of &gt;5 erosions and/or ≥1 ulcer (≥3 mm deep) assessed by a treatment-blinded reviewer at repeat endoscopy on day 7. Results Out of 451 randomized subjects (mean age 57 years, 47% males), 441 completed the 7-day endoscopy and represent the full analysis set. PL-ASA significantly reduced the primary outcome by 34% compared with IR-ASA (25.7% vs. 39%, p=0.0032) (figure). Notably, for ulcers there was a 61% reduction with PL-ASA (6.0% vs. 14.8%, p=0.0018) (Figure 1). The mean number of gastric erosions per patient was also reduced with PL-ASA (2.8±7.3 vs. 4.2±7.5, p&lt;0.0001), while erosions in the duodenum were not different (1.4±7.1 vs. 0.9±2.3, p=0.45). Conclusion The novel PL-ASA liquid capsules reduced rates of GI injury compared with IR-ASA tablets. The combination of reliable platelet inhibition with less GI injury makes PL-ASA an attractive new aspirin therapy option. Figure 1 Funding Acknowledgement Type of funding source: Private company. Main funding source(s): PLx Pharma

Bioequivalence of Two Tablet Formulations of Atenolol after Single Oral Administration in Healthy Volunteers

2011 ◽  
Vol 50 (03) ◽  
pp. 243-247
Author(s):  
Ioannis Niopas ◽  
Athanasios Daftsios ◽  
Ioannis Xanthakis ◽  
Nicolaos Nikolaidis ◽  
Samuel Njau
Keyword(s):  
Oral Administration ◽  
Healthy Volunteers ◽  
Single Oral Administration ◽  
Tablet Formulations

Evaluation of the Bio equivalence and Pharmacokinetics of Two Lisinopril Tablet Formulations after Single Oral Administration in Healthy Volunteers

2011 ◽  
Vol 54 (01) ◽  
pp. 15-19
Author(s):  
Manolis Georgarakis ◽  
Andreas Tsakalof ◽  
Fotini Zougrou ◽  
Georgios Kontopoulos ◽  
Iakovos Tsiptsios
Keyword(s):  
Oral Administration ◽  
Healthy Volunteers ◽  
Single Oral Administration ◽  
Tablet Formulations

scholarly journals Potential and Comparative Tablet Disintegrant Properties of Pectin Obtained from Five Okra Genotypes in Ghana

Scientifica ◽  
2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Frederick William Akuffo Owusu ◽  
Mariam El Boakye-Gyasi ◽  
Jacob Kwaku Agbenorhevi ◽  
Marcel Tunkumgnen Bayor ◽  
Kwabena Ofori-Kwakye
Keyword(s):  
Immediate Release ◽  
Dissolution Profile ◽  
Maize Starch ◽  
Dissolution Tests ◽  
The World ◽  
Weight Test ◽  
Pharmaceutical Industries ◽  
Tablet Formulations ◽  
Low Levels ◽  
Paracetamol Tablet

Okra pectin has been studied as a potential excipient in tablet formulations for pharmaceutical industries. Okra is widely grown and available in Ghana and other parts of the world. The prospective use of pectin from okra genotypes grown in Ghana as tablet disintegrants has not been reported. This study aims to determine the potential and comparative disintegrating properties of pectin from five okra genotypes (Abelmoschus esculentus L.) in Ghana using uncoated immediate release paracetamol tablet formulations. The yield of the pectin from the various genotypes ranged between 6.12 and 18.84% w/w. The extracted pectins had pH ranging from slightly acidic to almost neutral (6.39–6.92). Pectin from the various genotypes exhibited good swelling indexes (˃200%), varying solubility in different solvents, and low moisture content (˂20%). Elemental analysis of the extracted pectin from the various genotypes revealed very low levels of toxic metals and micronutrients. Pectin from the various genotypes was evaluated as disintegrants within concentrations of 5–10% w/w (F1–F18). Their disintegrating properties were compared to that of maize starch BP. All the formulated batches of uncoated immediate release paracetamol tablets (F1–F18) passed the following: uniformity of weight test, uniformity of dimensions, hardness, friability (˂1%), and drug content (95–105%). Significant differences ( p ≤ 0.05 ) were observed between the hardness of the maize starch tablets and tablets formulated from pectin of the various genotypes. Pectin from all genotypes other than PC5 exhibited good disintegrating properties (DT ˂ 15 min) and subsequently passed the dissolution profile test (≥70% release in 45 minutes). Tablets formulated with PC5 as disintegrants at all concentrations (5% w/w (F5), 7.5% w/w (F11), and 10% w/w (F17)) failed the disintegration and dissolution tests. Ultimately, pectins extracted from PC1, PC2, PC3, and PC4 can be commercially exploited as disintegrants in immediate release tablets.

scholarly journals 81 Bioequivalence of a Manipulation-Resistant Immediate-Release Amphetamine Sulfate Formulation Compared with Reference Standard

CNS Spectrums ◽  
2019 ◽  
Vol 24 (1) ◽  
pp. 216-216
Author(s):  
Steve Caras ◽  
Terrilyn Sharpe
Keyword(s):  
Single Dose ◽  
Healthy Volunteers ◽  
Peak Concentration ◽  
Immediate Release ◽  
Open Label ◽  
Time Curve ◽  
Time To Peak ◽  
Amphetamine Sulfate ◽  
Quantifiable Concentration ◽  
Funding Acknowledgements

AbstractStudy ObjectivesWe compared the bioavailability of racemic amphetamine (d-amphetamine and l-amphetamine) from a manipulation-resistant immediate-release (IR) amphetamine sulfate capsule (AR19) versus amphetamine sulfate IR tablets (reference).MethodIn this open-label, randomized, two-period, two-treatment, two-sequence, crossover study, 36 healthy volunteers aged 18–45 received a single dose (20-mg capsule) of AR19 in one period and a single dose (2 x 10-mg tablets) of reference in another period, after a 10-hour overnight fast. Each drug administration was separated by a washout period of at least 6days. Bioequivalence for d- and l-amphetamine was assessed using time to peak concentration (Tmax), peak concentration in plasma (Cmax), and area under the plasma concentration–time curve from time-zero to the time of the last quantifiable concentration (AUClast) and extrapolated to infinity (AUCinf).ResultsAll 36 volunteers completed both treatment sequences. Mean (standard deviation; SD) Tmax for d- and l-amphetamine was similar for AR19 (2.84[1.05]; 3.05[1.22], respectively) and reference (2.52[0.75]; 2.75[1.00], respectively). The geometric least-squares mean ratios and 90% confidence intervals were within the boundary of 80%–125% for bioequivalence for Cmax (d-amphetamine, 98.35% [96.12–100.64]; l-amphetamine, 98.82% [96.42–101.28]), AUClast (d-amphetamine, 99.45% [96.92–102.05]; l-amphetamine, 99.29% [96.55–102.10]), and AUCinf (d-amphetamine, 99.50%[96.77–102.30]; l-amphetamine, 99.23% [96.06–102.50]). A total of 13 mild adverse events were reported by 7 volunteers (AEs; AR19, n=5; reference, n=8). No serious AEs were reported.ConclusionAR19 was well tolerated and was bioequivalent to reference when administered as a 20-mg dose in healthy volunteers.Funding Acknowledgements: This study was funded by Arbor Pharmaceuticals, LLC.

Bioequivalency of single doses of desloratadine administered as syrup and tablet formulations in healthy volunteers in China

2007 ◽  
Vol &NA; ◽  
pp. S104-S105
Author(s):  
Xue-Ning Li ◽  
Hong-Rong Xu ◽  
Wei-Li Chen
Keyword(s):  
Healthy Volunteers ◽  
Tablet Formulations

Bioequivalence study of two perindopril erbumine tablet formulations in healthy volunteers

2011 ◽  
Vol 61 (04) ◽  
pp. 234-238 ◽  
Author(s):  
Effi Setiawati ◽  
Siti Deniati ◽  
Danang Yunaidi ◽  
Lucia Handayani ◽  
Iwan Santoso ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
Bioequivalence Study ◽  
Perindopril Erbumine ◽  
Tablet Formulations
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