scholarly journals Formulation of Sustained Release Hydrophilic Matrix Tablets of Tolcapone with the Application of Sedem Diagram: Influence of Tolcapone’s Particle Size on Sustained Release

Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 674 ◽  
Author(s):  
Anna Nardi-Ricart ◽  
Isaac Nofrerias-Roig ◽  
Marc Suñé-Pou ◽  
Pilar Pérez-Lozano ◽  
Montse Miñarro-Carmona ◽  
...  
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Potent Inhibitor ◽  
High Viscosity ◽  
Matrix Tablets ◽  
Formulation Development ◽  
Methyl Transferase ◽  
Diagram Method ◽  
Hydrophilic Matrix ◽  
Amyloid Polyneuropathy

Hydrophilic matrix tablets are a type of sustained release dosage form characterized by distributing a drug in a matrix that is usually polymeric. Tolcapone is a drug that inhibits the enzyme catechol-O-methyl transferase. In recent years, it has been shown that tolcapone is a potent inhibitor of the amyloid aggregation process of the transthyretin protein, and acts by stabilizing the structure of the protein, reducing the progression of familial amyloid polyneuropathy. The main objective of this study was to obtain a sustained release tablet of tolcapone for oral administration with a preferred dosage regimen of 1 administration every 12 or 24 h and manufactured, preferably, by direct compression. The SeDeM Diagram method has been used for the formulation development of hydrophilic matrix tablets. Given the characteristics of tolcapone, the excipient selected for the formation of the polymeric matrix was a high viscosity hydroxypropylmethylcellulose (Methocel® K100M CR). A decrease in the particle size of tolcapone resulted in a slower dissolution release of the formulation when the concentration of the polymer Methocel® K100M CR was below 29%. These surprising and novel results have given rise to patent number WO/2018/019997.

scholarly journals In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
High Viscosity ◽  
Matrix Tablets ◽  
Release Studies ◽  
The Matrix ◽  
Vitro Release

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

Sustained-release hydrophilic matrix tablets of zileuton: formulation and in vitro/in vivo studies

1997 ◽  
Vol 45 (3) ◽  
pp. 249-256 ◽  
Author(s):  
Yihong Qiu ◽  
Howard Cheskin ◽  
Jackie Briskin ◽  
Kevin Engh
Keyword(s):  
Sustained Release ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Hydrophilic Matrix

Formulation development and in vitro Evaluation of sustained release matrix tablets of Cefpodoxime proxetil

2021 ◽  
pp. 273-278
Author(s):  
A. Bhavani ◽  
B. Hemalatha ◽  
K. Padmalatha
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
Oral Dosage ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Formulation Development ◽  
Cefpodoxime Proxetil

The present focus is on the development of sustained release formulations due to its inherent boons. There are several advantages of sustained release drug delivery over conventional dosage forms like improved patient compliance, reduction in fluctuation and increased safety margin of potent drug. The present study was aimed to prepare a sustained drug delivery system to design a controlled release oral dosage form of Cefpodoxime proxetil. The sustained release matrix tablets of Cefpodoxime proxetil were prepared by wet granulation and evaluated for different parameters such as weight variation, drug content, thickness, hardness, friability and In vitro release studies. The in vitro dissolution study was carried out for 12 hours using USP (Type- II) paddle apparatus in hydrochloride (0.1N) as dissolution media for first 2 hours and phosphate buffer (pH 6.8) for next 10 hours. Based on the in vitro dissolution data, formulation F8 was selected as the best formulation from Cefpodoxime proxetil formulations (F1 – F9) as the drug release was retarded up to 12 hours with 96.29 % and followed zero order release kinetics & drug release mechanism was diffusion.

scholarly journals Formulation and evaluation of sustained release diclofenac sodium matrix tablets produced using Brachystegia eurycoma gum

2020 ◽  
Vol 17 (1) ◽  
pp. 34-43
Author(s):  
Sinodukoo E. Okafo ◽  
John A. Avbunudiogba ◽  
Ejiro Ejomafuvwe
Keyword(s):  
Sustained Release ◽  
Diclofenac Sodium ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Content Uniformity ◽  
Drug Release Profile ◽  
Hydrophilic Matrix ◽  
Weight Content ◽  
The Matrix ◽  
Hardness Values

This study was carried out to evaluate sustained release diclofenac sodium matrix tablets formulated using Brachystegia eurycoma gum (BEG) as matrix polymer. BEG was isolated by acetone -precipitation of the filtrate obtained from the maceration of powdered dried seeds of Brachystegia eurycoma in distilled water. Diclofenac sodium matrix tablets were produced by non-aqueous wet granulation method using BEG as the hydrophilic matrix former. The tablets were evaluated using official and unofficial tests such as; uniformity of weight, content uniformity, dissolution test, tablets diameter, thickness, hardness and friability tests. The drug release profile of the matrix tablets were compared to that formulated using a standard matrix former, hydroxypropylmethylcellulose (HPMC). Hardness values ranged from 6.12 ± 1.80 to 9.73 ± 1.39 kgf, friability from 0.31 ± 0.00 to 1.00 ± 0.00%. The drug content ranged from 98 to 101 %. The percentage drug released from the matrix tablets after 10 h was between 71.27 and 98.73 % except for formulation BF3 that released 32.56 %. This study showed that sustained release diclofenac sodium matrix tablets were  successfully formulated using Brachystegia eurycoma gum as the matrix former and the tablets were comparable to that formulated with HPMC. Keywords: Brachystegia eurycoma gum; Diclofenac sodium; Matrix tablets; Sustained release

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