Influence of screw configuration and processing parameters on the dissolution of ketoprofen in polymer blends

Restrepo‐Uribe, Laura; Ioannidis, Nicolas; Escobar, María del Pilar Noriega

doi:10.1002/app.49407

Cited by 5 publications

(4 citation statements)

References 34 publications

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“…Kollidon ® SR is a copolymer consisting of polyvinyl acetate linked to polyvinylpyrrolidone and, accordingly, exhibits two glass transition temperatures (~30 °C and 128–180 °C). The variability of the second glass transition temperature is a consequence of inconsistent moisture content, residual monomers, and molecular masses [ 21 ]. Therefore, the slight shift of the peaks generated by the presence of Kollidon ® SR in the filament and tablet samples compared to those acquired by analyzing the physical mixture is most likely caused by the alteration of the moisture content following thermal processing.…”

Section: Resultsmentioning

confidence: 99%

Development of a Bilayer Tablet by Fused Deposition Modeling as a Sustained-Release Drug Delivery System

Crișan,

Porfire,

Iurian

et al. 2023

Pharmaceuticals

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Three-dimensional printing by fused deposition modeling (FDM) coupled with hot-melt extrusion (HME) is a point of convergence of research efforts directed toward the development of personalized dosage forms. In addition to the customization in terms of shapes, sizes, or delivered drug doses, the modulation of drug release profiles is crucial to ensure the superior efficacy and safety of modern 3D-printed medications compared to those of conventional ones. Our work aims to solidify the groundwork for the preparation of 3D-printed tablets that ensure the sustained release of diclofenac sodium. Specifically, we achieved the fast release of a diclofenac sodium dose to allow for the prompt onset of its pharmacological effect, further sustaining by the slow release of another dose to maintain the effect over a prolonged timeframe. In this regard, proper formulation and design strategies (a honeycomb structure for the immediate-release layer and a completely filled structure for the sustained-release layer) were applied. Secondarily, the potential of polyvinyl alcohol to function as a multifaceted polymeric matrix for both the immediate and slow-release layers was explored, with the objective of promoting the real-life applicability of the technique by downsizing the number of materials required to obtain versatile pharmaceutical products. The present study is a step forward in the translation of HME-FDM-3DP into a pharmaceutical manufacturing methodology.

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Section: Resultsmentioning

confidence: 99%

Development of a Bilayer Tablet by Fused Deposition Modeling as a Sustained-Release Drug Delivery System

Crișan,

Porfire,

Iurian

et al. 2023

Pharmaceuticals

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“…KOL showed three endothermic peaks at 44 • C, 89 • C, and 115 • C, respectively, according to the DSC curve for the first heating run within the 25-250 • C temperature range, as shown in Figure 3a. According to the DSC curve obtained in the second heating run (Figure 8c), this excipient underwent two glass transitions at temperatures of 43 • C and 172 • C, as it is a copolymer of polyvinyl acetate (PVA) and polyvinylpyrrolidone [41]. The F1b, F2b, and F3b formulations have a single peak at 338 °C in the third stage, within the 326-359 °C temperature range, which proves an excellent compatibility of the excipients used [38].…”

Section: Dsc Resultsmentioning

confidence: 82%

“…KOL showed three endothermic peaks at 44 °C, 89 °C, and 115 °C, respectively, according to the DSC curve for the first heating run within the 25-250 °C temperature range, as shown in Figure 3a. According to the DSC curve obtained in the second heating run (Figure 8c), this excipient underwent two glass transitions at temperatures of 43 °C and 172 °C, as it is a copolymer of polyvinyl acetate (PVA) and polyvinylpyrrolidone [41].…”

Section: Dsc Resultsmentioning

confidence: 99%

New Hydrophilic Matrix Tablets for the Controlled Released of Chlorzoxazone

Creteanu,

Lisa,

Vasile

et al. 2024

IJMS

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The modified release of active substances such as chlorzoxazone from matrix tablets, based on Kollidon®SR and chitosan, depends both on the drug solubility in the dissolution medium and on the matrix composition. The aim of this study is to obtain some new oral matrix tablet formulations, based on Kollidon®SR and chitosan, in order to optimize the low-dose oral bioavailability of chlorzoxazone, a non-steroidal anti-inflammatory drug of class II Biopharmaceutical Classification System. Nine types of chlorzoxazone matrix tablets were obtained using the direct compression method by varying the components ratio as 1:1, 1:2, and 1:3 chlorzoxazone/excipients, 20–40 w/w % Kollidon®SR, 3–7 w/w % chitosan while the auxiliary substances: Aerosil® 1 w/w %, magnesium stearate 0.5 w/w % and Avicel® up to 100 w/w % were kept in constant concentrations. Pharmaco-technical characterization of the tablets included the analysis of flowability and compressibility properties (flow time, friction coefficient, angle of repose, Hausner ratio, and Carr index), and pharmaco-chemical characteristics (such as mass and dose uniformity, thickness, diameter, mechanical strength, friability, softening degree, and in vitro release profiles). Based on the obtained results, only three matrix tablet formulations (F1b, F2b, and F3b, containing 30 w/w % KOL and 5 w/w % CHT, were selected and further tested. These formulations were studied in detail by Fourier-transform infrared spectrometry, X-ray diffraction, thermogravimetry, and differential scanning calorimetry. The three formulations were comparatively studied regarding the release kinetics of active substances using in vitro release testing. The results were analyzed by fitting into four representative mathematical models for the modified-release oral formulations. In vitro kinetic study revealed a complex mechanism of release occurring in two steps of drug release, the first step (0–2 h) and the second (2–36 h). Two factors were calculated to assess the release profile of chlorzoxazone: f1—the similarity factor, and f2—the factor difference. The results have shown that both Kollidon®SR and chitosan may be used as matrix-forming agents when combined with chlorzoxazone. The three formulations showed optima pharmaco-technical properties and in vitro kinetic behavior; therefore, they have tremendous potential to be used in oral pharmaceutical products for the controlled delivery of chlorzoxazone. In vitro dissolution tests revealed a faster drug release for the F2b sample.

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“…KOL showed three endothermic peaks at 44ºC, 89ºC, and 115ºC, respectively, according to the DSC cube for the first heating stage within the 25 -250ºC temperature range, as shown in Figure 3a. According to the DSC curve obtained in the second heating stage (figure 8c), this excipient underwent two glass transition temperatures at 43ºC and 172ºC, as it is a copolymer of polyvinyl acetate (PVA) and polyvinylpyrrolidone [43,44].…”

Section: X-ray Diffraction Analysismentioning

confidence: 99%

Formulation and Evaluation of Hydrophilic Matrix Tablets for Controlled Released Chlorzoxazone Delivery

Creteanu,

Lisa,

Vasile

et al. 2024

Preprint

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The release of the active substance from the matrix modified-release tablets based on Kollidon®SR and chitosan depends on its solubility in the dissolution medium and on the composition of the matrix-forming polymers. The study is based on new oral matrix tablets based on Kollidon®SR and chitosan, formulated to optimize the low oral bioavailability of chlorzoxazone, a non-steroidal anti-inflammatory drug, a class II Biopharmaceutical Classification System. Nine types of chlorzoxazone matrix tablets were obtained using the direct compression method, and their combination at 1:1, 1:2, 1:3 chlorzoxazone/ excipients, 20%-40% (w/w) Kollidon®SR, 3-7% (w/w) chitosan and the auxiliary substances were formulated in constant concentrations. Pharmaco-technical characterization included the analysis of flowability and compressibility properties (flow time, friction coefficient, angle of repose, Hausner ratio, Carr Index), and of pharmaco-chemical characteristics (mass and dose uniformity, thickness, diameter, mechanical strength, Friability, degree of softening, in vitro release profile) of the tablets. Based on the initial evaluation of the pharmaco-technical analysis, pharmaco-chemical characteristics, and in vitro release profile, only three matrix tablet formulations (F1b, F2b, and F3b) were further tested. They were evaluated through Fourier-transform infrared spectrometry, X-ray Diffraction, thermogravimetry, differential scanning calorimetry, and in vitro dissolution tests. The three formulations were comparatively studied regarding the release kinetics of active substances using in vitro release testing. The results were analyzed by fitting into four representative mathematical models for the modified release oral formulations. In vitro kinetic study reveals a complex mechanism of release occurring in the first (0 - 2 hours) and second (2.0 hours – 36 hours) steps of drug release. Two factors have been calculated to assess the release profile of chlorzoxazone: f1 - the similarity factor and f2 - the factor difference. The results have shown that both Kollidon®SR and chitosan may be used as matrix-forming agents when combined with chlorzoxazone. In vitro dissolution tests revealed the F2b sample, data suggesting a faster drug release. The three formulations showed optimum pharmaco-technical properties and in vitro kinetic study, and they had tremendous potential to be used in oral pharmaceutical products for the controlled delivery of chlorzoxazone.

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Influence of screw configuration and processing parameters on the dissolution of ketoprofen in polymer blends

Cited by 5 publications

References 34 publications

Development of a Bilayer Tablet by Fused Deposition Modeling as a Sustained-Release Drug Delivery System

Development of a Bilayer Tablet by Fused Deposition Modeling as a Sustained-Release Drug Delivery System

New Hydrophilic Matrix Tablets for the Controlled Released of Chlorzoxazone

Formulation and Evaluation of Hydrophilic Matrix Tablets for Controlled Released Chlorzoxazone Delivery

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