The role of solid state properties on the dissolution performance of flufenamic acid

Maestrelli, Francesca; Rossi, Patrizia; Paoli, Paola; Luca, Enrico De; Mura, Paola

doi:10.1016/j.jpba.2019.113058

Cited by 11 publications

(19 citation statements)

References 21 publications

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“…Two different batches of flufenamic acid (2-{ [3-(trifluoromethyl) phenyl] amino} benzoic acid), FFA) were used: a batch donated by S.I.M.S. (FFA SIMS) (Florence, Italy) (purity 99.97% [13]) and another batch provided by TCI EUROPE N.V. (FFA TCI) (Zwijndrecht, Belgium) (purity 99.99% [13]). CDs were from Merck Life Science S.r.l.…”

Section: Methodsmentioning

confidence: 99%

“…In vitro dissolution studies of the prepared solid products were performed using a modified dispersed amount method [13]. Briefly, a sample amount corresponding to 200 mg of FFA was added to 75 mL of phosphate buffer (pH 6.8) at 37 • C and gently stirred (100 rpm) by a three-blade propeller.…”

Section: Characterisation Of Drug: CD Binary Systemsmentioning

confidence: 99%

“…The influence of polymorphism on bioavailability of poorly hydro-soluble drugs has been amply demonstrated [12]. A different intrinsic dissolution rate was observed between two FFA samples from two different firms, even using the same powder granulometric fraction [13]. An enhancement of FFA solubility and dissolution rate could be particularly useful to overcome all the issues associated with its poor-solubility, leading to an increased and more reproducible bioavailability and enabling the development of more effective and robust solid dosage forms of the drug, strongly reducing risks of bio-inequivalence issues.…”

Section: Introductionmentioning

confidence: 99%

“…All tablets were fully characterised by classic tests (drug content, mean weight, diameter, thickness, friability, hardness, disaggregation time and dissolution rate). Moreover, the effect of using FFA powder samples obtained from two different suppliers was also evaluated, considering the unexpected differences in their intrinsic dissolution rate previously detected as well as in the different wettability of the surface of their compacts [13]. For this reason, possible differences in wettability of the obtained tablets were also investigated, since they could be an additional factor responsible for differences in drug dissolution rate.…”

Section: Introductionmentioning

confidence: 99%

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Role of Cyclodextrins and Drug Solid State Properties on Flufenamic Acid Dissolution Performance from Tablets

et al. 2022

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Flufenamic acid (FFA) is a non-steroidal anti-inflammatory drug characterised by a low solubility and problems of variable dissolution rate and bio-inequivalence. Different FFA batches, obtained by different suppliers, showed different powder characteristics (particle size, shape and surface properties) that may affect its dissolution behaviour from solid dosage forms. Aim of this work was the improvement of FFA solubility and dissolution rate by the use of cyclodextrins (CDs) and the obtainment of an effective tablet formulation by direct compression. Several CDs have been tested, both in solution and in solid state and several binary systems drug-CDs have been obtained with different techniques, with the scope to select the most effective system. Grinding technique with randomly methylated-β-cyclodextrin (RAMEB) was the only one that allowed the complete drug amorphization, together with the highest improvement in drug dissolution rate, and was then selected for tablets formulation. Conventional and immediate release tablets were obtained and fully characterised for technological properties. In both cases an improved and well reproducible drug dissolution performance was obtained, independently from the FFA supplier and thus no more affected by the differences observed between the original FFA crystalline samples.

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Section: Methodsmentioning

confidence: 99%

Section: Characterisation Of Drug: CD Binary Systemsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Role of Cyclodextrins and Drug Solid State Properties on Flufenamic Acid Dissolution Performance from Tablets

et al. 2022

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“…X-ray crystallography is the key to studying structure-property relationships and single crystal X-ray diffraction (SCXRD) is the method of choice for molecular and crystal structure determination when crystals are available, as well as X-ray powder diffraction (XRPD), which provides an alternative valuable tool for the characterization of crystalline powder materials [10]. Both of these techniques [11][12][13][14][15], complemented by differential scanning calorimetry [16][17][18], solid state NMR [19], IR-UV and Raman spectroscopy [20][21][22] and modelling [23][24][25][26][27][28][29], can be successfully used to characterize the solid state features and behavior (e.g., phase stability, polymorphism, phase transformation) of a large variety of compounds including APIs' key precursors, well-known APIs as well as new promising active pharmaceutical compounds.…”

Section: Introductionmentioning

confidence: 99%

A Combined Crystallographic and Computational Study on Dexketoprofen Trometamol Dihydrate Salt

et al. 2020

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Dexketoprofen trometamol is the tromethamine salt of dexketoprofen [(2S)-2-(3-benzoylphenyl)propanoic acid-2-amino-2-(hydroxymethyl)propane-1,3-diol], a nonsteroidal anti-inflammatory drug (NSAID) used for the treatment of moderate- to strong-intensity acute pain. The crystal structure of the hitherto sole known hydrate phase of dexketoprofen trometamol (DK-T_2H2O), as determined by single-crystal X-ray diffraction, is presented. The water molecules are arranged in dimers included in isolated sites and sandwiched between piles of trometamol cations. The molecular and crystal structures of DK-T_2H2O are analyzed and compared to those of the parent anhydrous crystal form DK-T_A. In both the crystal structures, all the potential H-bond donors and acceptor of the dexketoprofen and trometamol ions are engaged, and both the species crystallize in the P21 space group. However, during the DK-T_A➔DK-T_2H2O hydration process, the unique symmetry axis is not conserved, i.e., the ions are arranged in a different way with respect to the screw axis, even if the two crystal structures maintain structural blocks of DK anions and T cations. Quantum mechanical solid-state calculations provide some hints for the possible intermediate structure during the crystalline–crystalline hydration/dehydration process.

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Thermal characterization and stability evaluation of leishmanicidal selenocyanate and diselenide derivatives

Etxebeste

Durán

Sanmartín

et al. 2021

J Therm Anal Calorim

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The role of solid state properties on the dissolution performance of flufenamic acid

Cited by 11 publications

References 21 publications

Role of Cyclodextrins and Drug Solid State Properties on Flufenamic Acid Dissolution Performance from Tablets

Role of Cyclodextrins and Drug Solid State Properties on Flufenamic Acid Dissolution Performance from Tablets

A Combined Crystallographic and Computational Study on Dexketoprofen Trometamol Dihydrate Salt

Thermal characterization and stability evaluation of leishmanicidal selenocyanate and diselenide derivatives

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