The biorelevant simulation of gastric emptying and its impact on model drug dissolution and absorption kinetics

Vrbanac, Helena; Trontelj, Jurij; Berglez, Sandra; Petek, Boštjan; Opara, Jerneja; Jereb, Rebeka; Krajcar, Dejan; Legen, Igor

doi:10.1016/j.ejpb.2020.02.002

Cited by 16 publications

(7 citation statements)

References 31 publications

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“…Some models focus primarily on changes in the gastric volumes after co-administration of formulation with water (32)(33)(34)(35)(36). To increase physiological relevance, some in vitro models also simulate the gastric motility patterns during MMC cycles (37)(38)(39)(40). The complexity of these non-compendial models thus depends mainly on the number of physiological factors simulated.…”

Section: Resultsmentioning

confidence: 99%

Forecasting the effect of water gastric emptying patterns on model drug release in an in vitro glass-bead flow-through system

Felicijan,

Bogataj

2024

Acta Pharmaceutica

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Oral solid dosage forms are most frequently administered with a glass of water which empties from the stomach relatively fast, but with a certain variability in its emptying kinetics. The purpose of this study was thus to simulate different individual water gastric emptying (GE) patterns in an in vitro glass-bead flow-through dissolution system. Further, the effect of GE on the dissolution of model drugs from immediate-release tablets was assessed by determining the amount of dissolved drug in the samples pumped out of the stomach compartment. Additionally, different HCl solutions were used as dissolution media to assess the effect of the variability of pH of the gastric fluid on the dissolution of three model drugs: paracetamol, diclofenac sodium, and dipyridamole. The difference in fast and slow GE kinetics resulted in different dissolution profiles of paracetamol in all studied media. For diclofenac sodium and dipyridamole tablets, the effect of GE kinetics was well observed only in media, where the solubility was not a limiting factor. Therefore, GE kinetics of co-ingested water influences the drug release from immediate-release tablets, however, in certain cases, other parameters influencing drug dissolution can partly or fully hinder the expression of this effect.

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Section: Resultsmentioning

confidence: 99%

Forecasting the effect of water gastric emptying patterns on model drug release in an in vitro glass-bead flow-through system

Felicijan,

Bogataj

2024

Acta Pharmaceutica

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“…Obviously, if the drug is released in the gastrointestinal tract, it will be emptied, making it still difficult to absorb. 31 However, combined with the results of pharmacokinetic experiments and cellular uptake, the absorption was enhanced, indicating that the nanoparticles were absorbed into the gastrointestinal cells in a whole form. This was also confirmed in the study of the uptake mechanism.…”

Section: In Vitro Releasementioning

confidence: 99%

Preparation and In Vitro and In Vivo Evaluation Of Panax Notoginseng Saponins-loaded Nanoparticles Coated with Trimethyl Chitosan Derivatives

Chen¹,

Zhao²,

et al. 2022

Journal of Pharmaceutical Sciences

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“…[166] Recently, Vrbanac et al introduced an advanced gastric simulator (AGS) system to mimic the motility of the human stomach, which could be used to provide more realistic drug release data. [313] As shown in Figure 20A, this AGS apparatus was composed of four major elements, including a pyloric valve, constriction mechanisms (simulating the mixing and grinding of ingested food), step motors, and a flexible vessel. The temperature of the chamber was adjusted to 37 ± 0.5 °C.…”

Section: Which Checkpoints Need To Be Passed For New Formulations To ...mentioning

confidence: 99%

“…Red arrows mark direction of the contraction movement. B) In vitro drug release profiles of the tested formulations with different dissolution methodologies: slow and fast gastric emptying (upper diagrams) and dissolution in USP2 apparatus (lower diagram).Reproduced with permission [313]. Copyright 2020, Elsevier.…”

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confidence: 99%

Future Nanotechnology‐Based Strategies for Improved Management of Helicobacter pylori Infection

Kamankesh,

Yadegar,

Llopis‐Lorente

et al. 2023

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Helicobacter pylori (H. pylori) is a recalcitrant pathogen, which can cause gastric disorders. During the past decades, polypharmacy‐based regimens, such as triple and quadruple therapies have been widely used against H. pylori. However, polyantibiotic therapies can disturb the host gastric/gut microbiota and lead to antibiotic resistance. Thus, simpler but more effective approaches should be developed. Here, some recent advances in nanostructured drug delivery systems to treat H. pylori infection are summarized. Also, for the first time, a drug release paradigm is proposed to prevent H. pylori antibiotic resistance along with an IVIVC model in order to connect the drug release profile with a reduction in bacterial colony counts. Then, local delivery systems including mucoadhesive, mucopenetrating, and cytoadhesive nanobiomaterials are discussed in the battle against H. pylori infection. Afterward, engineered delivery platforms including polymer‐coated nanoemulsions and polymer‐coated nanoliposomes are poposed. These bioinspired platforms can contain an antimicrobial agent enclosed within smart multifunctional nanoformulations. These bioplatforms can prevent the development of antibiotic resistance, as well as specifically killing H. pylori with no or only slight negative effects on the host gastrointestinal microbiota. Finally, the essential checkpoints that should be passed to confirm the potential effectiveness of anti‐H. pylori nanosystems are discussed.

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The biorelevant simulation of gastric emptying and its impact on model drug dissolution and absorption kinetics

Cited by 16 publications

References 31 publications

Forecasting the effect of water gastric emptying patterns on model drug release in an in vitro glass-bead flow-through system

Forecasting the effect of water gastric emptying patterns on model drug release in an in vitro glass-bead flow-through system

Preparation and In Vitro and In Vivo Evaluation Of Panax Notoginseng Saponins-loaded Nanoparticles Coated with Trimethyl Chitosan Derivatives

Future Nanotechnology‐Based Strategies for Improved Management of Helicobacter pylori Infection

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