Prediction of the impact of lubrication on tablet compactibility

Puckhaber, Daniel; Finke, Jan Henrik; David, Sarah; Serratoni, M.; Zafar, Umair; John, Edgar; Juhnke, Michael; Kwade, Arno

doi:10.1016/j.ijpharm.2022.121557

Cited by 24 publications

(9 citation statements)

References 42 publications

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“…This combination gives a balance of cohesion and adhesion in direct compression where lactose exhibits brittle fracture and cellulose exhibits plastic deformation [ 28 ]. Increasing lubricant amount and its mixing time tended to decrease tablet hardness [ 29 ] so the lubricant amount of only 0.5% and the lubrication time of 2 min were chosen. Magnesium stearate was selected as lubricant.…”

Section: Resultsmentioning

confidence: 99%

Synthesis of Celecoxib-Eutectic Mixture Particles via Supercritical CO2 Process and Celecoxib Immediate Release Tablet Formulation by Quality by Design Approach

et al. 2022

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Significant improvements in the wettability and dissolution rate of celecoxib (CEL), a poorly soluble selective cyclooxygenase-2 (COX-2) inhibitor, have been shown by Huyn et al., 2019 by combining the binary pharmaceutical compositions including CEL and one of the two co-formers, adipic acid (ADI) and saccharin (SAC), into eutectic mixtures (EM). Purpose: In this study, we developed a therapeutic eutectic system for CEL which is a promising approach for oral delivery to enhance bioavailability. CEL EM were synthesized by novel techniques including supercritical CO2 techniques and new tablet formulations were purposed. Methods: CEL EM were synthesized by evaporation crystallization method, spray drying, supercritical fluid (SCF) techniques. The CEL EM particles were then characterized by differential scanning calorimetry, powder X-ray diffraction, Fourier-transform infrared spectroscopy, scanning electron microscope, and particle size analysis. Dissolution studies were carried out. With a quality by design approach, a statistical method through design of experiment and data analysis by JMP® (SAS institute) was applied to CEL EM immediate release tablet formulation development. Results: CEL EM produced by spray drying technique, supercritical fluid (SCF) techniques were identified and characterized. The enhancement of dissolution was observed for SCF processed samples. The design space for CEL-ADI EM IR tablet and control limits for individual parameters were determined.

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Section: Resultsmentioning

confidence: 99%

Synthesis of Celecoxib-Eutectic Mixture Particles via Supercritical CO2 Process and Celecoxib Immediate Release Tablet Formulation by Quality by Design Approach

et al. 2022

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“…This can be related to the brittle nature of lactose. During compaction, lactose particles break, which provides new surfaces for the bonding of the tablet [44]. The bonding capability of lactose particles is therefore not limited by the outer surface, which can be covered by the lubricant.…”

Section: Batch Modementioning

confidence: 99%

Lubricant Sensitivity of Direct Compression Grades of Lactose in Continuous and Batch Tableting Process

Hebbink,

Janssen,

Kok

et al. 2023

Pharmaceutics

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Modern pharmaceutical manufacturing based on Quality by Design and digitalisation is revolutionising the pharmaceutical industry. Continuous processes are promoted as they increase efficiency and improve quality control. Compared to batch blending, continuous blending is easier to scale and provides advantages for achieving blend homogeneity. One potential challenge of continuous blending is the risk of over-lubrication. In this study, blending homogeneity and lubricant sensitivity are investigated for both batch and continuous processes. Given their distinct chemical structures and morphologies, anhydrous lactose and granulated lactose are expected to exhibit varying sensitivities to changes in process settings across both technologies. The findings suggest that both lactose grades provide highly stable blends that can be safely utilised in both batch and continuous modes. Optimisation should focus on process variables, such as the quality of loss-in-weight feeders used for dosing low doses of ingredients. The most significant process parameter for lubricant sensitivity was the type of lactose used. Anhydrous lactose produced harder tablets than the more porous granulated lactose but was more sensitive to lubrication at the same settings. The magnesium stearate content and its interaction with the type of lactose are also critical factors, with magnesium stearate having a counterproductive impact on tabletability.

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“…A detailed mechanism and dynamic processes has been documented elsewhere. 6 The rate at which drugs are released from tablets from these products could be influenced by a variety of factors within the GI tract. Bayer introduced a reformulation of aspirin, which was based on "pro-release technology" utilizing microparticles that are 90% smaller than the particle size of previously used aspirin tablets.…”

Section: Introductionmentioning

confidence: 99%

“…The process of compacting APIs into tablet form generally categorized as die-filling as well as ejection steps. A detailed mechanism and dynamic processes has been documented elsewhere . The rate at which drugs are released from tablets from these products could be influenced by a variety of factors within the GI tract.…”

Section: Introductionmentioning

confidence: 99%

Tabletized Nanomedicine: From the Current Scenario to Developing Future Medicine

Tiwari,

Kolli,

Chauhan

et al. 2024

ACS Nano

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The limitations of conventional therapeutic treatments prevailed in the development of nanotechnology-based medical formulations, termed nanomedicine. Nanomedicine is an advanced medicine that often consists of therapeutic agent(s) embedded in biodegradable or biocompatible nanomaterial-based formulations. Among nanomedicine approaches, tablet (oral) nanomedicine is still under development. In tabletized nanomedicine, the dynamic interplay between nanoformulations and the intricate milieu of the gastrointestinal tract simulates a pivotal role, particularly accentuating the influence exerted upon the luminal, mucosal, and epithelial cells. In this work, we document the perspectives and opportunities of nanoformulations toward the development of tabletized nanomedicine. This review also unveils the notion of integrating nanomedicine within a tablet formulation, which facilitates the controlled release of drugs, biomolecules, and agent(s) from the formulation to achieve a better therapeutic response. Finally, an attempt was made to explore current trends in nanomedicine technology such as bacteriophage, probiotic, and oligonucleotide tabletized nanomedicine and the combination of nanomedicine with imaging agents, i.e., nanotheranostics.

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Prediction of the impact of lubrication on tablet compactibility

Cited by 24 publications

References 42 publications

Synthesis of Celecoxib-Eutectic Mixture Particles via Supercritical CO2 Process and Celecoxib Immediate Release Tablet Formulation by Quality by Design Approach

Synthesis of Celecoxib-Eutectic Mixture Particles via Supercritical CO2 Process and Celecoxib Immediate Release Tablet Formulation by Quality by Design Approach

Lubricant Sensitivity of Direct Compression Grades of Lactose in Continuous and Batch Tableting Process

Tabletized Nanomedicine: From the Current Scenario to Developing Future Medicine

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