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

Nardi-Ricart, Anna; Nofrerias-Roig, Isaac; Suñé-Pou, Marc; Pérez-Lozano, Pilar; Carmona, Montserrat Miñarro; García-Montoya, Encarna; Grau, Josep R. Ticó; Boronat, Raul Insa; Suñé-Negre, Josep M.

doi:10.3390/pharmaceutics12070674

Cited by 20 publications

(10 citation statements)

References 27 publications

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“…The SeDeM Expert System proposes three indexes to determine whether a powder is acceptable for direct compression: parametric index (PI), parametric profile index (PPI) and good compression index (GCI). Values higher than 0.5, 5, and 5, respectively, indicate that the substance can be processed through direct compression [ 27 , 37 ]. The three indexes were calculated according to this method.…”

Section: Resultsmentioning

confidence: 99%

A Biodegradable Copolyester, Poly(butylene succinate-co-ε-caprolactone), as a High Efficiency Matrix Former for Controlled Release of Drugs

et al. 2021

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A biodegradable copolyester, poly(butylene succinate-co-ε-caprolactone) (PBS_CL), was used for first time as an excipient for pharmaceutical dosage forms using direct compression and hot processing techniques (ultrasound-assisted compression (USAC) and hot melt extrusion (HME)). Robust binary systems were achieved with hot processing techniques, allowing a controlled release of the drug. With only 12% v/v of PBS_CL, controlled release forms were obtained using USAC whereas in HME over 34% v/v of excipient is necessary. Amounts over 23% v/v allowed a long-extended release for more than 72 h following diffusional kinetic. Thanks to the high melting point of theophylline and the physicochemical properties of PBS_CL selected and synthesized, the structure of the excipient inside the USAC tablets and HME filaments corresponds to a continuum medium. A percolation threshold around 23% v/v was estimated, which agrees with a continuum percolation model. The polymer shows a high excipient efficiency value using HME and USAC. A nanostructured matrix with wall thicknesses lower than 0.1 µm was obtained. This leads to a very effective coating of the drug particles by the excipient, providing a slow and reproducible release. The present study therefore supports the use of PBS_CL, for the preparation of controlled release dosage forms using hot processing techniques.

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Section: Resultsmentioning

confidence: 99%

A Biodegradable Copolyester, Poly(butylene succinate-co-ε-caprolactone), as a High Efficiency Matrix Former for Controlled Release of Drugs

et al. 2021

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“…The active substance dissolves in the aqueous medium and diffuses out of the matrix by way of the water-filled capillaries 16 . The materials used as matrix formers include hydrogenated vegetable oil, hydrogenated cottonseed oil, hydrogenated soy oil, microcrystalline wax, carnauba wax, as well as hydroxypropyl methylcellulose (HPMC) 17 .…”

Section: Formulation and Evaluation Of Sustained Release Matrix Tablets Of Aceclofenacmentioning

confidence: 99%

Formulation and Evaluation of Sustained Release Matrix Tablets of Aceclofenac

Singh

Shrivastava

Kumar³

et al. 2021

Borneo J Pharm

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This study aimed to improve the dissolution rate of aceclofenac and release the drug in a controlled manner over a period of 24 hours. Matrix tablets were prepared by direct compression method, using hydrophilic polymers (HPMC/guar gum). Matrix tablets were prepared by wet granulation method using different hydrophilic polymers (HPMC/guar gum). Tablets were evaluated for in vitro drug release profile in phosphate buffer with pH 6.8 (without enzymes). The thickness and hardness of prepared tablets were 3.23 ± 0.035 to 3.28 ± 0.008 mm and 3.26 ± 0.115 to 3.60 ± 0.200 kg/cm2, respectively. The friability was within the acceptable limits of pharmacopoeial specifications (0.31 to 0.71%), which indicates the good mechanical strength of the tablets. Drug release was retarded with an increase in polymer concentration due to the gelling property of polymers. The in vitro drug release from the proposed system was best explained by Higuchi’s model, indicating that drug release from tablets displayed a diffusion-controlled mechanism. The results clearly indicate that guar gum could be a potential hydrophilic carrier in developing oral controlled drug delivery systems. Based on the study results, formulations F8 was selected as the best formulation.

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“…Knowledge of the particle size distribution for drug formulations is critical in ensuring that batch-to-batch consistency is maintained throughout the development process. 44,45 2.3. Antitubercular Efficacy of SnPPIX-TIF In Vivo.…”

Section: In Vitro and In Vivo Gelationmentioning

confidence: 99%

A Long-Acting Thermoresponsive Injectable Formulation of Tin Protoporphyrin Sustains Antitubercular Efficacy in a Murine Infection Model

Adeleke

Fisher

Moore

et al. 2020

ACS Pharmacol. Transl. Sci.

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Tuberculosis is the leading cause of death from a single infectious agent, ranking above the human immunodeficiency virus (HIV). Effective treatment using antibiotics is achievable, but poor patient compliance constitutes a major challenge impeding successful pharmacotherapeutic outcomes. This is often due to the prolonged treatment periods required and contributes significantly to the rising incidence of drug resistance, which is a major cause of tuberculosis mortality. Thus, innovative interventions capable of encouraging compliance and decreasing lengthy and frequent dosing are needed. Previously, aqueous tin protoporphyrin IX (SnPPIX), a heme oxygenase-1 inhibitor, administered as multiple daily intraperitoneal (IP) injections, showed considerable antitubercular efficacy and treatment shortening capabilities as a host-directed therapy in infected mice. Since daily IP injection is a clinically impractical administration approach, this proof-of-concept study aims to develop a novel, sustained action injectable formulation of SnPPIX for safe intramuscular (IM) administration. Herein, a SnPPIX-loaded poloxamer-poly(acrylic acid)-based thermoresponsive injectable formulation (SnPPIX-TIF) is designed for effective IM delivery. Results show SnPPIX-TIF is microparticulate, syringeable, injectable, and exhibits complete in vitro / in vivo gelation. Administered once weekly, SnPPIX-TIF significantly prolonged absorption and antimicrobial efficacy in infected mice. In addition, SnPPIX-TIF is well-tolerated in vivo ; results from treated animals show no significant histopathologic alterations and were indistinguishable from the untreated control group, thus supporting its biocompatibility and preclinical safety. Overall, the IM delivery of the thermoresponsive injectable formulation safely sustains antitubercular effect in an infected murine model and decreases the number of injections required, signifying a potentially practical approach for future clinical translation.

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

Cited by 20 publications

References 27 publications

A Biodegradable Copolyester, Poly(butylene succinate-co-ε-caprolactone), as a High Efficiency Matrix Former for Controlled Release of Drugs

A Biodegradable Copolyester, Poly(butylene succinate-co-ε-caprolactone), as a High Efficiency Matrix Former for Controlled Release of Drugs

Formulation and Evaluation of Sustained Release Matrix Tablets of Aceclofenac

A Long-Acting Thermoresponsive Injectable Formulation of Tin Protoporphyrin Sustains Antitubercular Efficacy in a Murine Infection Model

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