Right filter-selection for phase separation in equilibrium solubility measurement

Völgyi, Gergely; Csicsák, Dóra; Takács‐Novák, Krisztina

doi:10.1016/j.ejps.2018.06.031

Cited by 14 publications

(9 citation statements)

References 18 publications

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“…Lipophilic drugs tend to adsorb to the filter material [ 44 , 45 , 46 ]. A hydrophilic type filter (e.g., hydrophilic PVDF and PES) is recommended for unionized species [ 28 ].…”

Section: Resultsmentioning

confidence: 99%

Harmonizing solubility measurement to lower inter-laboratory variance – progress of consortium of biopharmaceutical tools (CoBiTo) in Japan

et al. 2019

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<p class="ADMETabstracttext">The purpose of the present study was to harmonize the protocol of equilibrium solubility measurements for poorly water-soluble drugs to lower inter-laboratory variance. The “mandatory” and “recommended” procedures for the shake-flask method were harmonized based on the knowledge and experiences of each company and information from the literature. The solubility of model drugs was measured by the harmonized protocol (HP) and the non-harmonized proprietary protocol of each company (nonHP). Albendazole, griseofulvin, dipyridamole, and glibenclamide were used as model drugs. When using the nonHP, the solubility values showed large inter-laboratory variance. In contrast, inter-laboratory variance was markedly reduced when using the HP.</p>

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“…Lipophilic drugs tend to adsorb to the filter material [ 44 , 45 , 46 ]. A hydrophilic type filter (e.g., hydrophilic PVDF and PES) is recommended for unionized species [ 28 ].…”

Section: Resultsmentioning

confidence: 99%

Harmonizing solubility measurement to lower inter-laboratory variance – progress of consortium of biopharmaceutical tools (CoBiTo) in Japan

et al. 2019

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“…As a base with p K a = 6.36, it is more soluble in pH = 5.0 media than in buffers of pH = 6.5, because in the first case 95.8% of the molecules are protonated, which results in an increased polarity and therefore an increased aqueous solubility [ 20 , 24 ]. The solubilizing effect of the SIF powder is prevailing in both the FaSSIF and FeSSIF full buffers, resulting in a higher solubility of the compound than in the blank buffers.…”

Section: Resultsmentioning

confidence: 99%

The Effect of the Particle Size Reduction on the Biorelevant Solubility and Dissolution of Poorly Soluble Drugs with Different Acid-Base Character

et al. 2023

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Particle size reduction is a commonly used process to improve the solubility and the dissolution of drug formulations. The solubility of a drug in the gastrointestinal tract is a crucial parameter, because it can greatly influence the bioavailability. This work provides a comprehensive investigation of the effect of the particle size, pH, biorelevant media and polymers (PVA and PVPK-25) on the solubility and dissolution of drug formulations using three model compounds with different acid-base characteristics (papaverine hydrochloride, furosemide and niflumic acid). It was demonstrated that micronization does not change the equilibrium solubility of a drug, but it results in a faster dissolution. In contrast, nanonization can improve the equilibrium solubility of a drug, but the selection of the appropriate excipient used for nanonization is essential, because out of the two used polymers, only the PVPK-25 had an increasing effect on the solubility. This phenomenon can be explained by the molecular structure of the excipients. Based on laser diffraction measurements, PVPK-25 could also inhibit the aggregation of the particles more effectively than PVA, but none of the polymers could hold the nanonized samples in the submicron range until the end of the measurements.

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“…Thus, aliquots were taken and centrifuged at 14000 rpm for 15 min using a MicroGen 16-type (Herolab GmbH, Germany) centrifuge. To avoid dissolved ABZ absorption of syringe mounted membrane filters and to increase precision and reproducibility, membrane filtering has been ignored, only centrifugation had been utilized for phase separation [62]. Complete phase separation has been confirmed by transmittance analysis and Dynamic Light Scattering particle sizing methods.…”

Section: Thermodynamic Solubility Studiesmentioning

confidence: 99%

Study on Optimization of Wet Milling Process for the Development of Albendazole Containing Nanosuspension with Improved Dissolution

Fülöp

Jakab

Tóth

et al. 2020

Period. Polytech. Chem. Eng.

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The main objective of this work was to show the potential of the optimization of top-down wet planetary bead milling process parameters (milling speed, process time and size of the milling medium) by Design Of Experiments (DOE) approach for the development of albendazole (ABZ) containing nanosuspension with improved dissolution. In addition, the influence of process parameters (capacity of milling container, applied volume of milling beads, size of the milling medium, milling speed, milling time) on ABZ polymorphic transition has also been investigated. The optimized, milled formula yielded ~ 145.39 times reduction in mean particle size (182.200 ± 1.3130 nm) compared to unmilled dispersion, which demonstrated 13.50 times gain in mean dissolution rate value compared to the unmilled dispersion in medium at pH = 1.2. No lag time values were observed in the dissolution kinetics of the nanosuspension in comparison with the unmilled samples. Moreover, maximal mean solubility value was also improved by 1.45 times compared to the unmilled suspension, in medium at pH = 6.8, supporting the significance of the Ostwald-Freundlich equation. Diffraction pattern comparisons have indicated a polymorphic transition of albendazole to Form II, which was more pronounced in smaller container at high milling speed values and prolonged operations.

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Right filter-selection for phase separation in equilibrium solubility measurement

Cited by 14 publications

References 18 publications

Harmonizing solubility measurement to lower inter-laboratory variance – progress of consortium of biopharmaceutical tools (CoBiTo) in Japan

Harmonizing solubility measurement to lower inter-laboratory variance – progress of consortium of biopharmaceutical tools (CoBiTo) in Japan

The Effect of the Particle Size Reduction on the Biorelevant Solubility and Dissolution of Poorly Soluble Drugs with Different Acid-Base Character

Study on Optimization of Wet Milling Process for the Development of Albendazole Containing Nanosuspension with Improved Dissolution

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