Abstract
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.
Highlights
Modified release pharmaceutical forms are designed with the aim of modifying the rate or the site of release of a drug, with respect to the immediate release pharmaceutical forms of the same active ingredient [1].Sustained-release or extended-release forms are types of modified-release dosage forms characterized by an initial release of the drug in enough quantities to produce therapeutic action or even a small excess
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%
The six diluent excipients chosen were characterized following the methodology of SeDeM Diagram with the objective of choosing the excipient with the capacity of correcting the deficient parameters of tolcapone
Summary
Sustained-release or extended-release forms are types of modified-release dosage forms characterized by an initial release of the drug in enough quantities to produce therapeutic action or even a small excess. This excess is never harmful to the organism but it allows the slow release of the drug to continue, sometimes with a speed that is not always equal to the speed of elimination [2]. The drug is distributed in a matrix that is usually polymeric. This matrix hinders the access of the solution medium to the surface of the particles and make the drug diffusion towards the outside matrix difficult [3]
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