Application of percolation threshold to disintegration and dissolution of ibuprofen tablets with different microcrystalline cellulose grades

Queiroz, Ana Luiza P.; Wood, Barbara A.; Faisal, Waleed; Farag, Fatma; Garvie-Cook, Hazel; Glennon, Brian; Vučen, Sonja; Crean, Abina M.

doi:10.1016/j.ijpharm.2020.119838

Cited by 10 publications

(3 citation statements)

References 41 publications

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“…In any case, it can be seen that the type of co-amorphous material clearly influences the disintegration time of the tablets as a whole and becomes dominant when there is above 20% of the co-amorphous material in the tablet. The percolation threshold is usually found in this range, and the current observation is in good agreement with a recent study that reported a step-change change in dissolution and disintegration behavior upon passing the percolation threshold [ 33 ]. In the current study, the salt-forming co-amorphous system still enabled disintegration, while the non-salt-forming system prevented disintegration.…”

Section: Resultssupporting

confidence: 92%

Compaction Behavior of Co-Amorphous Systems

2023

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Co-amorphous systems have been shown to be a promising strategy to address the poor water solubility of many drug candidates. However, little is known about the effect of downstream processing-induced stress on these systems. The aim of this study is to investigate the compaction properties of co-amorphous materials and their solid-state stability upon compaction. Model systems of co-amorphous materials consisting of carvedilol and the two co-formers aspartic acid and tryptophan were produced via spray drying. The solid state of matter was characterized using XRPD, DSC, and SEM. Co-amorphous tablets were produced with a compaction simulator, using varying amounts of MCC in the range of 24 to 95.5% (w/w) as a filler, and showed high compressibility. Higher contents of co-amorphous material led to an increase in the disintegration time; however, the tensile strength remained rather constant at around 3.8 MPa. No indication of recrystallization of the co-amorphous systems was observed. This study found that co-amorphous systems are able to deform plastically under pressure and form mechanically stable tablets.

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Section: Resultssupporting

confidence: 92%

Compaction Behavior of Co-Amorphous Systems

2023

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“…The rapid release of sildenafil could be explained as follows: initially, the dissolution medium rapidly penetrated the pores of prepared tablets that come in contact with PGS. The swelling of PGS was observed followed by the mechanical fragmentation of tablets into small agglomerates that resulted in the rapid release of sildenafil due to the availability of a higher surface area for dissolution [35]. Besides, fluid-bed produced low density and high porous granules that rapidly eroded, disintegrated, and rapidly released sildenafil from the tablet [12].…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

Exploitation of Design-of-Experiment Approach for Design and Optimization of Fast-Disintegrating Tablets for Sublingual Delivery of Sildenafil Citrate with Enhanced Bioavailability Using Fluid-Bed Granulation Technique

et al. 2021

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Sildenafil citrate undergoes first-pass metabolism, resulting in poor oral bioavailability at 25–41% of the administered dose. This study aimed to design and optimize fast-disintegrating tablets for the sublingual delivery of sildenafil citrate to improve bioavailability and facilitate rapid onset of action. The design-of-experiment (DoE) approach using 32 full factorial design was conducted to develop a new formulation of sildenafil fast-disintegrating sublingual tablets (FDSTs) using the fluid-bed granulation technique. The levels of partially pre-gelatinized starch (5–15%) and microcrystalline cellulose (10–60%) were selected as independent formulation variables. The prepared FDSTs were investigated for physical properties. Further, the optimum formulation was chosen for in vivo study in rabbits. Regression analysis showed that independent variables have a significant (p < 0.05) influence on critical attributes of FDSTs. The optimized formulation showed acceptable mechanical strength (friability <1.0%) with very fast disintegration (14.561 ± 0.84 s) and dissolution (94.734 ± 2.76% after 15 min). Further, the optimized formulation demonstrated a significant increase (p < 0.01) in Cmax and AUC0–∞ with short tmax compared to the market product (Viagra®). Based on these results, using the DoE approach, a high level of assurance was achieved for FDSTs’ product quality and performance.

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“…Good packaging is an important condition to protect drugs from deliquescence. [ 60 ] Figure 8d shows the changes in the time ( T 100% ) required for the complete disintegration of ibuprofen tablets in water at 37 °C with the preservation time in different packaging preservation processes. The T 100% of ibuprofen in the unpackaged group (WP) decreased gradually with the prolongation of storage time.…”

Section: Resultsmentioning

confidence: 99%

Poly(lactic acid) based Pearl Layer Moistureproof Membrane for Flexible Laminated Packaging

Zhao

Wang

et al. 2023

Macromol. Rapid Commun.

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The development of bio-based polymer materials, such as polylactic acid (PLA) -based polymers, is an effective strategy to reduce dependence on petrochemical-based polymers. However, the preparation of bio-based polymers with high barrier properties is a major challenge. To overcome this challenge, a nacreous layer structure with a ' brick and mud ' pattern is mimicked to improve the overall performance of the material. In this paper, Poly ( L -lactic acid) (PLLA) and Polypropylene Glycol (PPG) was combined to prepare bio-based polyurethane (PU-PLLA), which is used as the slurry structure of nacreous layer. The bio-based biomimetic composite membrane (PU-PLLA/BN) is then obtained by adding boron nitride (BN, brick structure of pearl layer) to it. The water vapor permeability test results show that the permeability of PU-PLLA material can be reduced by more than 50% by 5 wt.% BN, which is because the addition of BN can increase the length and tortuosity of the gas molecular diffusion path in the composite. Therefore, this pearl-inspired PU-PLLA/BN film has excellent moisture resistance, which opens up a broad road for the practical application of PLLA in flexible laminated packaging.

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Application of percolation threshold to disintegration and dissolution of ibuprofen tablets with different microcrystalline cellulose grades

Cited by 10 publications

References 41 publications

Compaction Behavior of Co-Amorphous Systems

Compaction Behavior of Co-Amorphous Systems

Exploitation of Design-of-Experiment Approach for Design and Optimization of Fast-Disintegrating Tablets for Sublingual Delivery of Sildenafil Citrate with Enhanced Bioavailability Using Fluid-Bed Granulation Technique

Poly(lactic acid) based Pearl Layer Moistureproof Membrane for Flexible Laminated Packaging

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