Molecular Basis of Crystal Morphology-Dependent Adhesion Behavior of Mefenamic Acid During Tableting

Waknis, Vrushali; Chu, Elza; Schlam, Roxana F.; Sidorenko, Alexander; Badawy, Sherif; Yin, Shawn; Narang, Ajit S.

doi:10.1007/s11095-013-1149-6

Cited by 45 publications

(35 citation statements)

References 35 publications

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“…The weakest bonding (per molecule) is likely to be that between the stacks. This agrees with vacuum crystal shape simulations within the Material studio software, using the attachment energy method 39 . The shape of Form I crystals is plate-like and the axis of the stacks is parallel to the big flat slow growing surface.…”

supporting

confidence: 82%

Promotion of Mefenamic Acid Nucleation by a Surfactant Additive, Docusate Sodium

Bodnár

Hudson

Rasmuson

2018

Crystal Growth & Design

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The influence of docusate sodium (DOSS) on the nucleation of mefenamic acid (MEF) has been studied in different dimethylacetamide (DMA)-water mixtures. A series of induction time experiments were conducted under moderate supersaturations, varying the solvent composition and the concentration of DOSS. In 40 % DMA-60 % water, the presence of 0.1 mg/mL and 0.2 mg/mL DOSS increased the nucleation rate. Evaluating the results by the classical nucleation theory reveals that the pre-exponential factor (A) increases by approximately 50 % while the interfacial energy is essentially uninfluenced. It is also found that the crystal growth rate becomes higher in the presence of DOSS. It is thus hypothesized that transport and desolvation of MEF molecules is facilitated in the presence of DOSS. With increasing amount of DMA in the binary solvent mixture, the influence of DOSS appears to decrease.

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supporting

confidence: 82%

Promotion of Mefenamic Acid Nucleation by a Surfactant Additive, Docusate Sodium

Bodnár

Hudson

Rasmuson

2018

Crystal Growth & Design

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“…Properties of the API, such as small particle size [8, 9] and needle-like morphology [10, 11] can lead to processing limitations such as poor flowability [12], difficulties with blending [9] as well as undesirable adhesion [13] to surfaces such as tablet punches or feeder walls [14]. These issues are addressed by selecting an appropriate processing route and/or by adding agents like glidants, lubricants or surfactants [15–18].…”

Section: Introductionmentioning

confidence: 99%

A Review of Disintegration Mechanisms and Measurement Techniques

2017

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Pharmaceutical solid dosage forms (tablets or capsules) are the predominant form to administer active pharmaceutical ingredients (APIs) to the patient. Tablets are typically powder compacts consisting of several different excipients in addition to the API. Excipients are added to a formulation in order to achieve the desired fill weight of a dosage form, to improve the processability or to affect the drug release behaviour in the body. These complex porous systems undergo different mechanisms when they come in contact with physiological fluids. The performance of a drug is primarily influenced by the disintegration and dissolution behaviour of the powder compact. The disintegration process is specifically critical for immediate-release dosage forms. Its mechanisms and the factors impacting disintegration are discussed and methods used to study the disintegration in-situ are presented. This review further summarises mathematical models used to simulate disintegration phenomena and to predict drug release kinetics.

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“…This work seeks to outline some of the recent progress on the application of emerging computer modelling technologies for the design strategy of advanced functional particulate products [7]. The paper highlights the opportunity for bridging across the chemical, analytical and manufacturing disciplines with a particular focus on understanding punch sticking.…”

Section: Introductionmentioning

confidence: 99%

Effects of crystal habit on the sticking propensity of ibuprofen—A case study

Hooper

Clarke

Docherty

et al. 2017

International Journal of Pharmaceutics

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This study demonstrates the effect of active pharmaceutical ingredient (API) particle habit on the sticking propensity of ibuprofen. Four diverse crystal habits with similar physico chemical properties are reported and the sticking propensity was found to increase with shape regularity. The surface energy of the extreme habits were shown to be different where particles that were more regular in shape exhibited surface energies of 9mJ/m higher than those that were needle-like in habit. Computational and experimental data reveals that the increase in surface energy of the regular shaped particles can be attributed to the increase in the specific (polar) component, which is due to greater presence of faces which contain the carboxylic acid functionality at the surface. The increase in the specific energy component is shown to correlate with the sticking propensity of ibuprofen. It is proposed that investigation of the chemical causality of sticking, for this API and others, using the techniques demonstrated in this paper will be of increasing importance.

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Molecular Basis of Crystal Morphology-Dependent Adhesion Behavior of Mefenamic Acid During Tableting

Cited by 45 publications

References 35 publications

Promotion of Mefenamic Acid Nucleation by a Surfactant Additive, Docusate Sodium

Promotion of Mefenamic Acid Nucleation by a Surfactant Additive, Docusate Sodium

A Review of Disintegration Mechanisms and Measurement Techniques

Effects of crystal habit on the sticking propensity of ibuprofen—A case study

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