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Pharmaceutics
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Matrix Tablets for Oral Controlled Release
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Matrix Tablets for Oral Controlled Release

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: closed (20 March 2022) | Viewed by 24963

Special Issue Editor

Prof. Dr. Peter Timmins

E-Mail Website1 Website2
Guest Editor
Department of Pharmacy, University of Huddersfield, Queensgate, Huddersfield HD1 3DH, UK
Interests: oral drug delivery; modified release technologies; hydrophilic matrix tablets; poorly water-soluble drugs; amorphous solid dispersions; pharmaceutical polymers
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

It is now more than half a century since the first publications describing the design of hydrophilic matrix tablets for oral controlled release appeared.  The value of the technology is clear from the number of clinically important therapies based on matrix tablet technology that have been introduced into medicine over that time.  Significant advances in the understanding of the factors controlling drug release from matrix tablets have been made, better assuring a Quality by Design approach in the development of such products.  Nevertheless, there is still much to explore in further building out  that understanding,  particularity with the compounds now emerging from drug discovery with very poor aqueous solubility, and with pH dependent solubility coupled with a drug dissociation constant within the physiological pH range, making control of release independent of environmental pH in the gastrointestinal tract challenging.  In addition, newer, improved versions of the polymers utilized in fabricating matrix tablets are becoming available, and how their properties influence drug release, product quality and product manufacturing need to be determined.

This Special Issue of Pharmaceutics will aim to cover the latest advances in the area of matrix tablets for oral controlled release.

Prof. Dr. Peter Timmins
Guest Editor

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Keywords

  • matrix tablet
  • oral controlled release
  • polymer
  • drug release
  • dissolution

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Published Papers (5 papers)

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Research

16 pages, 6596 KiB  
Article
Application of Focus Variation Microscopy and Dissolution Imaging in Understanding the Behaviour of Hydrophilic Matrices
by Adam Ward, Benedict Brown, Karl Walton, Peter Timmins, Barbara R. Conway and Kofi Asare-Addo
Pharmaceutics 2020, 12(12), 1162; https://doi.org/10.3390/pharmaceutics12121162 - 28 Nov 2020
Cited by 6 | Viewed by 3382
Abstract
Hydrophilic matrix systems can be found in a wide range of extended release pharmaceutical formulations. The main principle of these systems is that upon contact with water, the hydrophilic component swells to form a hydrated gel layer which controls drug release. The following [...] Read more.
Hydrophilic matrix systems can be found in a wide range of extended release pharmaceutical formulations. The main principle of these systems is that upon contact with water, the hydrophilic component swells to form a hydrated gel layer which controls drug release. The following work demonstrates an explorative study into the use of dissolution imaging and focus variation microscopy with hydrophilic polymers. This study investigated the surface properties of xanthan gum (XG), polyethylene oxide (PEO), and hypromellose (hydroxypropyl methylcellulose, HPMC) compacts with each of these three hydrophilic polymers from one of each classification of natural, semi-synthetic, or synthetic polymer using a focus variation instrument. The auto correlation length (Sal) showed all surface profiles from the compacts displayed a value below 0.1 mm, indicating that only high frequency components (i.e., roughness) were considered and that the analysis had been successful. The developed interfacial area ratio (Sdr) displayed values below 5% in line with ISO guidelines for all the polymers studied with their texture aspect ratio values (Str) > 0.5, indicating uniformity of the surfaces of the produced compacts. Of the various parameters studied, areal material ratio (Smr2) predicted XG to wet and hydrate quicker than PEO, with PEO also wetting and hydrating quicker than the HPMC. The dissolution imaging and initial swelling studies proved to concur with the findings from the areal material ratio (Smr2) parameter, suggesting porosity was not an indicator for the ease with which water ingress occurs. This study suggests the Smr2 surface parameter to potentially predict wetting and initial hydration of hydrophilic polymers, however care should be taken as this study consists of a selected number of hydrophilic polymers. Full article
(This article belongs to the Special Issue Matrix Tablets for Oral Controlled Release)
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20 pages, 10091 KiB  
Article
Imaging of the Effect of Alcohol-Containing Media on the Performance of Hypromellose Hydrophilic Matrix Tablets: Comparison of Direct Compression and Regular Grades of Polymer
by Nihad Mawla, Sarah Hanley, Karl Walton, Waseem Kaialy, Tariq Hussain, Adam Ward, Jonathan Brown, Barbara R. Conway, Peter Timmins and Kofi Asare-Addo
Pharmaceutics 2020, 12(9), 889; https://doi.org/10.3390/pharmaceutics12090889 - 18 Sep 2020
Cited by 5 | Viewed by 4114
Abstract
As the ingestion of drug products with alcohol could have adverse effects on the release of drugs from dosage forms, it is important to understand the mechanisms underpinning the influence on drug release by evaluating the effect of alcohol-containing media on the behaviour [...] Read more.
As the ingestion of drug products with alcohol could have adverse effects on the release of drugs from dosage forms, it is important to understand the mechanisms underpinning the influence on drug release by evaluating the effect of alcohol-containing media on the behaviour of pharmaceutical excipients. In this work, the effect of hydroalcoholic media containing up to 40% v/v absolute ethanol was evaluated, employing both the regular (CR) and direct compression grades (DC) of hypromellose. X-ray microtomography (XµT) and magnetic resonance imaging (MRI) were used as complementary techniques in determining the influence of the media composition on the ability of the CR and DC polymers to form and evolve the gel layer that controls drug release. Particle and powder properties of the polymer were characterised to determine any relationship to performance in hydroalcoholic media. Triboelectrification results showed the CR grade formulation to charge electropositively whereas the DC grade charged electronegatively. The flow properties also showed the DC grade to have a superior flow as compared to its CR counterpart. Differences in particle morphology between the grades influenced charging and flow behaviour of the powders; however, it did not seem to impact significantly either on the mechanical strength or the drug release properties of the compacted formulation using the model drug propranolol HCl. XµT and MRI imaging were successfully used as complementary techniques in determining the gel layer/hydration layer thickness measurements as the layer developed, as well as following ingress of hydroalcoholic media and its impact on the dry core. The result showed that although differences were present in the gel layer thickness potentially due to differences in particle morphology, this also did not impact significantly on the dissolution process, especially in acidic and hydroalcoholic media. Full article
(This article belongs to the Special Issue Matrix Tablets for Oral Controlled Release)
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18 pages, 3011 KiB  
Article
Formulation of Sustained Release Hydrophilic Matrix Tablets of Tolcapone with the Application of Sedem Diagram: Influence of Tolcapone’s Particle Size on Sustained Release
by Anna Nardi-Ricart, Isaac Nofrerias-Roig, Marc Suñé-Pou, Pilar Pérez-Lozano, Montse Miñarro-Carmona, Encarna García-Montoya, Josep R. Ticó-Grau, Raul Insa Boronat and Josep M. Suñé-Negre
Pharmaceutics 2020, 12(7), 674; https://doi.org/10.3390/pharmaceutics12070674 - 17 Jul 2020
Cited by 19 | Viewed by 4672
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 [...] Read more.
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. Full article
(This article belongs to the Special Issue Matrix Tablets for Oral Controlled Release)
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24 pages, 6133 KiB  
Article
A Direct Compression Matrix Made from Xanthan Gum and Low Molecular Weight Chitosan Designed to Improve Compressibility in Controlled Release Tablets
by Deeb Abu Fara, Suha M. Dadou, Iyad Rashid, Riman Al-Obeidi, Milan D. Antonijevic, Babur Z. Chowdhry and Adnan Badwan
Pharmaceutics 2019, 11(11), 603; https://doi.org/10.3390/pharmaceutics11110603 - 12 Nov 2019
Cited by 12 | Viewed by 5520
Abstract
The subject of our research is the optimization of direct compression (DC), controlled release drug matrices comprising chitosan/xanthan gum. The foregoing is considered from two main perspectives; the use of low molecular weight chitosan (LCS) with xanthan gum (XG) and the determination of [...] Read more.
The subject of our research is the optimization of direct compression (DC), controlled release drug matrices comprising chitosan/xanthan gum. The foregoing is considered from two main perspectives; the use of low molecular weight chitosan (LCS) with xanthan gum (XG) and the determination of important attributes for direct compression of the mixtures of the two polymers. Powder flow, deformation behaviour, and work of compression parameters were used to characterize powder and tableting properties. Compression pressure and LCS content within the matrix were investigated for their influence on the crushing strength of the tablets produced. Response surface methodology (RSM) was applied to determine the optimum parameters required for DC of the matrices investigated. Results confirm the positive contribution of LCS in enhancing powder compressibility and crushing strength of the resultant compacts. Compactibility of the XG/LCS mixtures was found to be more sensitive to applied compression pressure than LCS content. LCS can be added at concentrations as low as 15% w/w to achieve hard compacts, as indicated by the RSM results. The introduction of the plasticity factor, using LCS, to the fragmenting material XG was the main reason for the high volume reduction and reduced porosity of the polymer mixture. Combinations of XG with other commonly utilized polymers in controlled release studies such as glucosamine, hydroxypropyl methylcellulose (HPMC), Na alginate (ALG), guar gum, lactose and high molecular weight (HMW) chitosan were also used; all the foregoing polymers failed to reduce the matrix porosity beyond a certain compression pressure. Application of the LCS/XG mixture, at its optimum composition, for the controlled release of two model drugs (metoprolol succinate and dyphylline) was examined. The XG/LCS matrix at 15% w/w LCS content was found to control the release of metoprolol succinate and dyphylline. The former preparation confirmed the strong influence of compression pressure on changing the drug release profile. The latter preparation showed the ability of XG/LCS to extend the drug release at a fixed rate for 12 h of dissolution time after which the release became slightly slower. Full article
(This article belongs to the Special Issue Matrix Tablets for Oral Controlled Release)
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15 pages, 4156 KiB  
Article
Swelling of Zein Matrix Tablets Benchmarked against HPMC and Ethylcellulose: Challenging the Matrix Performance by the Addition of Co-Excipients
by Alberto Berardi, Safwan Abdel Rahim, Lorina Bisharat and Marco Cespi
Pharmaceutics 2019, 11(10), 513; https://doi.org/10.3390/pharmaceutics11100513 - 4 Oct 2019
Cited by 17 | Viewed by 5216
Abstract
Zein is an insoluble, yet swellable, biopolymer that has been extensively studied for its applications in drug delivery. Here, we screened the effect of co-excipients on the swelling and drug release of zein tablets. All throughout the study the behavior of zein was [...] Read more.
Zein is an insoluble, yet swellable, biopolymer that has been extensively studied for its applications in drug delivery. Here, we screened the effect of co-excipients on the swelling and drug release of zein tablets. All throughout the study the behavior of zein was benchmarked against that of hydroxypropyl methylcellulose (HPMC) and ethylcellulose (EC). Tablets containing either zein, HPMC, or EC alone or in combination with co-excipients, namely lactose, dicalcium phosphate (DCP), microcrystalline cellulose (MCC), polyvinylpyrrolidone (PVP), or sodium lauryl sulfate (SLS) were prepared by direct compression. Matrix swelling was studied by taking continuous pictures of the tablets over 20 h, using a USB microscope connected to a PC. The overall size change and the axial and radial expansion of the tablets were automatically extrapolated from the pictures by image analysis. Moreover, drug release from tablets containing ternary mixtures of zein, co-excipients and 10% propranolol HCl was also studied. Results showed that zein matrices swelled rapidly at first, but then a plateau was reached, resulting in an initial rapid drug burst followed by slow drug release. HPMC tablets swelled to a greater extent and more gradually, providing a more constant drug release rate. EC did not practically swell, giving a nearly constant drug release pattern. Among the additives studied, only MCC increased the swelling of zein up to nearly three-fold, and thus suppressed drug burst from zein matrices and provided a nearly constant drug release over the test duration. Overall, the incorporation of co-excipients influenced the swelling behavior of zein to a greater extent compared to that of HPMC and EC, indicating that the molecular interactions of zein and additives are clearly more complex and distinct. Full article
(This article belongs to the Special Issue Matrix Tablets for Oral Controlled Release)
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