Influence of crystal habit on the compression and densification mechanism of ibuprofen

Martino, Piera Di; Beccerica, Moira; Joiris, E; Palmieri, Gianni; Gayot, A.; Martelli, Sante

doi:10.1016/s0022-0248(02)01523-3

Cited by 39 publications

(19 citation statements)

References 18 publications

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“…Ibuprofen RDTs had sufficient hardness even when prepared with 88.7 MPa compression pressure. Low melting point (75-77°C) of ibuprofen could be responsible for particle-particle fusion while compressing ibuprofen RDTs, leading to stronger tablets (33,34). The suggested single disintegrant for ibuprofen RDT was CCS (≥4.5% at compression pressure 88.7 MPa) or disintegrant composite combinations for ibuprofen RDTs were SSG-CP (compression pressure range, 88.7-239.4 MPa), MCC-CP (compression pressure range, 88.7-239.4 MPa), MCC-CCS (compression pressure range, 88.7-133 MPa), SSG-CCS (compression pressure range, 88.7-133 MPa) and CP-CCS (compression pressure range, 88.7-239.4 MPa).…”

Section: Formulation Optimizationmentioning

confidence: 99%

Functionality of Disintegrants and Their Mixtures in Enabling Fast Disintegration of Tablets by a Quality by Design Approach

Desai

Liew

et al. 2014

AAPS PharmSciTech

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Abstract. Investigation of the effect of disintegrants on the disintegration time and hardness of rapidly disintegrating tablets (RDTs) was carried out using a quality by design (QbD) paradigm. Ascorbic acid, aspirin, and ibuprofen, which have different water solubilities, were chosen as the drug models. Disintegration time and hardness of RDTs were determined and modeled by executing combined optimal design. The generated models were validated and used for further analysis. Sodium starch glycolate, croscarmellose sodium, and crospovidone were found to lengthen disintegration time when utilized at high concentrations. Sodium starch glycolate and crospovidone worked synergistically in aspirin RDTs to decrease disintegration time. Sodium starch glycolate-crospovidone mixtures, as well as croscarmellose sodium-crospovidone mixtures, also decreased disintegration time in ibuprofen RDTs at high compression pressures as compared to the disintegrants used alone. The use of sodium starch glycolate in RDTs with highly water soluble active ingredients like ascorbic acid slowed disintegration, while microcrystalline cellulose and crospovidone drew water into the tablet rapidly and quickened disintegration. Graphical optimization analysis demonstrated that the RDTs with desired disintegration times and hardness can be formulated with a larger area of design space by combining disintegrants at difference compression pressures. QbD was an efficient and effective paradigm in understanding formulation and process parameters and building quality in to RDT formulated systems.

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Section: Formulation Optimizationmentioning

confidence: 99%

Functionality of Disintegrants and Their Mixtures in Enabling Fast Disintegration of Tablets by a Quality by Design Approach

Desai

Liew

et al. 2014

AAPS PharmSciTech

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“…Crystallization can therefore prove to be a very important tool in modifying the external structure of a crystal drug for the production of a particular dosage form (i.e. suspensions [4] or tablets [5][6][7]). Since during crystallization a great number of variables (i.e.…”

Section: Introductionmentioning

confidence: 99%

Influence of solvent and crystallization method on the crystal habit of metronidazole

Martino¹,

Censi

Malaj

et al. 2007

Cryst. Res. Technol.

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In the present study, metronidazole was crystallized in several solvents, according to both the "cooling crystallization" and the "crystallization by non-solvent addition". Particle properties, such as crystal habit, elongation ratio, and mean particle size, were determined by SEM analysis. Structural changes and development of polymorphic forms were excluded by both Differential Scanning Calorimetry (DSC) and XRay Powder Diffractometry (XRPD). Crystal habit (and thus elongation ratio) was typically influenced by both the solvent polarity index and the crystallization method: solvents with higher polarity index tended to promote acicular or stick-shaped crystals with a high elongation ratio, while isodimensional crystals were promoted by decreasing the polarity index, as was particle aggregation.

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“…By increasing the confidence and reducing uncertainty in the drug-related parameters affecting dissolution rate via separately modeling experimental pH-solubility profile, one may redirect an available semimechanistic dissolution model, such as the DLM, to work in an estimation mode and unveil formulationrelated factors controlling dissolution kinetics. In this context, the P-PSD for formulations containing plastic-elastic drugs such as ibuprofen 22,25 is based on the effective surface area concept, which is a geometrical controlling factor for a chemical reaction involving fine particulate materials. 26 Even though not an ideal physiologically and mechanistically based biopharmaceutics modeling approach, 27 the semimechanistic IVIVE approach still allows one to leverage experimentally obtained particle size distributions for plastic-elastic materials (e.g., starting values for P-PSD modeling) to investigate the interplay between drug-, formulation-, and GIrelated properties and ultimately to derive individual intraluminal dissolution profiles, which are essential to inform IVIVCs and virtual bioequivalence trials.…”

Section: Discussionmentioning

confidence: 99%

Integrating Drug- and Formulation-Related Properties With Gastrointestinal Tract Variability Using a Product-Specific Particle Size Approach: Case Example Ibuprofen

Cristofoletti

Hens

Patel

et al. 2019

Journal of Pharmaceutical Sciences

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Keywords:absorption dissolution physiologically based pharmacokinetic (PBPK) modeling in vitro-in vivo (IVIVC) correlation(s) mechanistic modeling particle size a b s t r a c tIn the present study, an in vitroein vivo extrapolation of dissolution integrated to a physiologically based pharmacokinetics modeling approach, considering a product-specific particle size distribution and a selfbuffering effect of the drug, is introduced and appears to be a promising translational modeling strategy to support drug product development, manufacturing changes and setting clinically relevant specifications for immediate release formulations containing ibuprofen and other weak acids with similar properties.

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Influence of crystal habit on the compression and densification mechanism of ibuprofen

Cited by 39 publications

References 18 publications

Functionality of Disintegrants and Their Mixtures in Enabling Fast Disintegration of Tablets by a Quality by Design Approach

Functionality of Disintegrants and Their Mixtures in Enabling Fast Disintegration of Tablets by a Quality by Design Approach

Influence of solvent and crystallization method on the crystal habit of metronidazole

Integrating Drug- and Formulation-Related Properties With Gastrointestinal Tract Variability Using a Product-Specific Particle Size Approach: Case Example Ibuprofen

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