Effects of polymers on the crystallinity of nanonized meloxicam during a co-grinding process

Mártha, Csaba; Kürti, Levente; Farkas, Gyöngyi; Jójárt-Laczkovich, Orsolya; Szalontai, Balázs; Glässer, Erik; Deli, Mária A.; Szabó‐Révész, Piroska

doi:10.1016/j.eurpolymj.2013.03.006

Cited by 16 publications

(13 citation statements)

References 14 publications

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“…Ground extrudates (0.4 mm < d p < 0.8 mm ) equivalent to 8 mg of spironolactone were placed in the dissolution vessel, which had been filled with 900 ml of 0.1 M hydrochloric acid maintained at (37.0 ± 0.5)°C and stirred at 100 rpm. Samples were taken after 0, 1, 2, 3, 4, 5, 6,7,8,9,10,15,20,25,30,45, 60, 75, 90, 105 and 120 min (washing period prior to sampling was 30 s) and were analyzed on-line using a Hewlett-Packard HP 8453G UV-VIS spectrophotometer (Palo Alto, USA) at 242 nm, using a diode array detector, then added back to the dissolution vessel.…”

Section: In Vitro Drug Dissolutionmentioning

confidence: 99%

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Effect of supercritical CO₂plasticization on the degradation and residual crystallinity of melt-extruded spironolactone

Vígh

Sauceau

Fages

et al. 2014

Polym. Adv. Technol.

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Immediate-release solid dispersions of a slowly dissolving active pharmaceutical ingredient, spironolactone, were prepared by supercritical-CO 2 -assisted melt extrusion (a solvent-free and continuous manufacturing technology) using Eudragit E as matrix. Through optimizing process parameters (i.e. temperature, melt throughput, pressure and CO 2 flow), stable foams with high porosity, homogeneous structure and thin (even submicronic) walls could be prepared, as revealed by scanning electron microscopy. The samples were found to be rigid enough to mill, enabling further processing, as is necessary to formulate tablets. The influence of extrusion temperature and melt throughput on residual drug crystallinity was measured using non-invasive confocal Raman mapping coupled with chemometric analysis, while the influence on the degree of drug degradation was determined using high performance liquid chromatography. The plasticizing effect of supercritical CO 2 was shown to reasonably improve the purity of the prepared solid dispersions by enabling high-yield production at lower temperature ranges. At the same time, shorter residence time and lower temperature slightly increased residual drug crystallinity. The obtained foamy structures ensured immediate drug dissolution in an acidic medium.

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Section: In Vitro Drug Dissolutionmentioning

confidence: 99%

“…Dissolution of the API from the resulting solid suspensions or solid solutions can be faster for several reasons. First, the solubility of the amorphous form is higher than that of the crystalline forms . Second, matrix polymers can ensure better wettability and also solubilize drug molecules, thus improving their apparent solubility.…”

Section: Introductionmentioning

confidence: 99%

Effect of supercritical CO₂plasticization on the degradation and residual crystallinity of melt-extruded spironolactone

Vígh

Sauceau

Fages

et al. 2014

Polym. Adv. Technol.

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“…In our earlier studies, we investigated the applicability of the combined wet milling technique, 20 – 23 and these preliminary studies showed that for the nanonization of Mel, PVA as a stabilizer agent and an increased milling time (>50 min) were required. The influence of milling time was also studied on the particle size distribution, crystallinity, and dissolution rate of Mel.…”

Section: Introductionmentioning

confidence: 99%

Optimization of a combined wet milling process in order to produce poly(vinyl alcohol) stabilized nanosuspension

Gyovai

Jójárt-Laczkovich

Katona

et al. 2018

DDDT

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PurposeThe article reports a wet milling process, where the planetary ball mill was combined with pearl milling technology to reach nanosize range of meloxicam (Mel; 100–500 nm). The main purpose was to increase the dissolution rate and extent of a poorly water-soluble Mel as nonsteroidal anti-inflammatory drug as well as to study its permeability across cultured intestinal epithelial cell layers.MethodsViscosity of milled dispersion and particle size distribution and zeta potential of Mel were investigated and differential scanning calorimeter and X-ray powder diffractometer were used to analyse the structure of the suspended Mel. Finally in vitro dissolution test and in vitro cell culture studies were made.ResultsIt was found that the ratio of predispersion and pearls 1:1 (w/w) resulted in the most effective grinding system (200-fold particle size reduction in one step) with optimized process parameters, 437 rpm and 43 min. Nanosuspension (1% Mel and 0.5% poly[vinyl alcohol]) as an intermediate product showed a stable system with 2 weeks of holding time. This optimized nanosuspension enhanced the penetration of Mel across cultured intestinal epithelial cell layers without toxic effects.ConclusionThe dissolution rate of Mel from the poly(vinyl alcohol) stabilized nanosuspension justified its applicability in the design of innovative per oral dosage form (capsule) in order to ensure/give a rapid analgesia.

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“…It can cause polymorphic transformations, e.g., the amorphous form of a crystalline API may appear 20, 21. This is especially true for co‐grinding 22, 23, when an appropriate excipient is used which is able to reduce the free energy of the system and the energy demand of the amorphization process. This can lead to a major decrease in crystallinity 24.…”

Section: Introductionmentioning

confidence: 99%

Effect of Co‐Grinding on Crystallinity of Clopidogrel Bisulfate

2014

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A high energy input during pharmaceutical formulation is capable of decreasing the crystallinity of compounds in the product. The presence of the amorphous form can cause serious problems at any stage of the formulation. Crystallinity changes of a model powder mixture containing clopidogrel bisulfate (CLP) and a colloidal silicon dioxide as additive were investigated during a long-time co-grinding process. The crystallinity of CLP was reduced sigmoidally by co-grinding with longer co-grinding time. X-ray powder diffraction and differential scanning calorimetry examinations confirmed that the product had become totally amorphous after four hours of grinding. Thermogravimetric results proved that no major mass reduction happened and FT-IR changes referred to formulation of a secondary bond between the components.

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Effects of polymers on the crystallinity of nanonized meloxicam during a co-grinding process

Cited by 16 publications

References 14 publications

Effect of supercritical CO₂plasticization on the degradation and residual crystallinity of melt-extruded spironolactone

Effect of supercritical CO₂plasticization on the degradation and residual crystallinity of melt-extruded spironolactone

Optimization of a combined wet milling process in order to produce poly(vinyl alcohol) stabilized nanosuspension

Effect of Co‐Grinding on Crystallinity of Clopidogrel Bisulfate

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Effects of polymers on the crystallinity of nanonized meloxicam during a co-grinding process

Cited by 16 publications

References 14 publications

Effect of supercritical CO2plasticization on the degradation and residual crystallinity of melt-extruded spironolactone

Effect of supercritical CO2plasticization on the degradation and residual crystallinity of melt-extruded spironolactone

Optimization of a combined wet milling process in order to produce poly(vinyl alcohol) stabilized nanosuspension

Effect of Co‐Grinding on Crystallinity of Clopidogrel Bisulfate

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Effect of supercritical CO₂plasticization on the degradation and residual crystallinity of melt-extruded spironolactone

Effect of supercritical CO₂plasticization on the degradation and residual crystallinity of melt-extruded spironolactone