scholarly journals Development of a Novel Controlled-Release Tablet of Pregabalin: Formulation Variation and Pharmacokinetics in Dogs and Humans

2020 ◽  
Vol Volume 14 ◽  
pp. 445-456
Author(s):  
Kyung Hun Kim ◽  
Seo Hyun Lim ◽  
Cho Rok Shim ◽  
Junsung Park ◽  
Woo Heon Song ◽  
...  
Keyword(s):  
Controlled Release ◽  
Release Tablet

scholarly journals Influence of Splitting on Dissolution Properties of Metoprolol Tablets

2009 ◽  
Vol 9 (3) ◽  
pp. 245-249 ◽  
Author(s):  
Edina Vranić ◽  
Alija Uzunović
Keyword(s):  
Controlled Release ◽  
Extended Release ◽  
Release Formulation ◽  
Extended Release Formulation ◽  
Dissolution Properties ◽  
Tablet Formulations ◽  
Score Line ◽  
Adequate Design ◽  
Release Tablet

The objective of this work was to compare several profiles of dissolution data for metoprolol controlled release tablet formulations in order to identify possible changes in dissolution profiles of whole and scored tablets. Adequate design of score lines (on one or both sides) as well as the technology of preparation of tablet mixtures ensure forming a score line of adequate thickness, shape, size, curvature. According to the obtained results, this type of extended release formulation is eligible for splitting and use in therapy either as a whole or scored tablets.

An in Vivo Single- and Multiple-Dose Study of Several Marketed Brands of Conventional and Controlled-Release Theophylline

1984 ◽  
Vol 18 (2) ◽  
pp. 147-153 ◽  
Author(s):  
Jeffrey A. Kotzan ◽  
Joseph V. Vallner ◽  
James T. Stewart ◽  
Irwin L. Honigberg ◽  
W.J. Brown
Keyword(s):  
Single Dose ◽  
Controlled Release ◽  
Multiple Dose ◽  
Healthy Adult ◽  
Dosage Forms ◽  
Adult Males ◽  
Single Dose Study ◽  
Multiple Dose Study ◽  
Dose Study ◽  
Release Tablet

In a single-dose study, 18 healthy adult males consumed each of six dosage forms of theophylline. A conventional-release tablet, a syrup, and four competing brands of controlled-release theophylline were studied. Serial serum samples were obtained and analyzed via high pressure liquid chromatography (HPLC). After achieving steady state, 15 healthy adult males consumed each of five dosage forms of theophylline in a multiple-dose study. Serial blood samples were obtained between 0 and 72 hours and subjected to analysis with HPLC. The results indicated that the controlled-release products were not bioequivalent, although they achieved longer time-to-peak values than did the immediate-release syrup and the conventional-release tablet. A single sustained-release product was uniquely different on most pharmacokinetic parameters when compared with the remaining three controlled-release products. In general, the dosage form variation exceeded the individual subject variation on the single-dose study, but the opposite was true for the multiple-dose study.

A Multiple-Dose Pharmacokinetic Comparison of Naproxen as a Once-Daily Controlled-Release Tablet and a Twice-Daily Conventional Tablet

1987 ◽  
Vol 27 (4) ◽  
pp. 325-329 ◽  
Author(s):  
Teck L. Ling ◽  
James P. Yee ◽  
Albert Cohen ◽  
Charles Hsiao ◽  
Mario A. Gonzalez ◽  
...  
Keyword(s):  
Controlled Release ◽  
Multiple Dose ◽  
Once Daily ◽  
Conventional Tablet ◽  
Release Tablet

scholarly journals Development and Optimization of Gastro-Retentive Controlled-Release Tablet of Calcium-Disodium Edentate and its In Vivo Gamma Scintigraphic Evaluation

2015 ◽  
Vol 16 (6) ◽  
pp. 1270-1280 ◽  
Author(s):  
Neeraj Kumar ◽  
Sandeep Soni ◽  
Thakuri Singh ◽  
Amit Kumar ◽  
Farhan Jalees Ahmad ◽  
...  
Keyword(s):  
Controlled Release ◽  
Gastro Retentive ◽  
Release Tablet

scholarly journals Increased Bioavailability of β-Alanine by a Novel Controlled-Release Powder Blend Compared to a Slow-Release Tablet

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1517
Author(s):  
Lydia de Salazar ◽  
Ignacio Segarra ◽  
Francisco Javier López-Román ◽  
Antonio Torregrosa-García ◽  
Silvia Pérez-Piñero ◽  
...  
Keyword(s):  
Single Dose ◽  
Controlled Release ◽  
Side Effects ◽  
Sustained Release ◽  
Pharmacokinetic Analysis ◽  
Prediction Ability ◽  
Powder Blend ◽  
Sustained Release Tablet ◽  
Sensory Score ◽  
Release Tablet

Background: β-Alanine is a sport supplement with increasing popularity due to its consistent ability to improve physical performance, with the downside of requiring several weeks of supplementation as imposed to the maximum daily and single dose tolerated without side effects (i.e., paresthesia). To date, the only alternative to overcome this problem has been use of a sustained-release tablet, while powders are the most commonly used format to deliver several grams of amino acids in a single dose. In this study we assessed the bioavailability, pharmacokinetics and paresthesia effect of β-alanine after administration in a novel controlled-released powder blend (test) versus a sustained-release tablet (reference). Methods: Twelve subjects (25.6 ± 3.2 y, 50% female) participated in a randomized, single-blind, crossover study. Each participant was administered orally the test (β-alanine 8 g, l-histidine 300 mg, carnosine 100 mg) or the reference product (10 tablets to reach β-alanine 8 g, Zinc 20 mg) with a 1-week washout period. β-Alanine plasma concentrations (0–8 h) were determined by LC-MS/MS and model-independent pharmacokinetic analysis was carried out. Paresthesia intensity was evaluated using a Visual Analog Score (VAS) and the categorical Intensity Sensory Score (ISS). Results: The CMAX and AUC0→∞ increased 1.6- and 2.1-fold (both p < 0.001) in the test product, respectively, which yielded 2.1-fold higher bioavailability; Ka decreased in the test (0.0199 ± 0.0107 min−1) versus the reference (0.0299 ± 0.0121 min−1) product (p = 0.0834) as well as V/F and Cl/F (both p < 0.001); MRT0→last increased in the test (143 ± 19 min) versus reference (128 ± 16 min) formulation (p = 0.0449); t1/2 remained similar (test: 63.5 ± 8.7 min, reference: 68.9 ± 9.8 min). Paresthesia EMAX increased 1.7-fold using the VAS (p = 0.086) and the ISS (p = 0.009). AUEC increased 1.9-fold with the VAS (p = 0.107) and the ISS (p = 0.019) reflecting scale intrinsic differences. Pharmacokinetic-pharmacodynamic analysis showed a clockwise hysteresis loop without prediction ability between CMAX, AUC0→∞ and EMAX or AUEC. No side effects were reported (except paresthesia). Conclusions: The novel controlled-release powder blend shows 100% higher bioavailability of β-alanine, opening a new paradigm that shifts from chronic to short or mid-term supplementation strategies to increase carnosine stores in sports nutrition.

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