Brief overview of solubility methods: Recent trends in equilibrium solubility measurement and predictive models

2018 ◽  
Vol 27 ◽  
pp. 3-10 ◽  
Author(s):  
Árpád Könczöl ◽  
Gergő Dargó
Keyword(s):  
Predictive Models ◽  
Equilibrium Solubility ◽  
Solubility Measurement ◽  
Recent Trends

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

ADMET & DMPK ◽  
2019 ◽  
Vol 7 (3) ◽  
pp. 183-195 ◽  
Author(s):  
Asami Ono ◽  
Naoya Matsumura ◽  
Takahiro Kimoto ◽  
Yoshiyuki Akiyama ◽  
Satoko Funaki ◽  
...  
Keyword(s):  
Shake Flask ◽  
Water Soluble ◽  
Equilibrium Solubility ◽  
Poorly Water Soluble Drugs ◽  
Solubility Measurement ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Proprietary Protocol

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.

scholarly journals Equilibrium solubility measurement of ionizable drugs – consensus recommendations for improving data quality

ADMET & DMPK ◽  
2016 ◽  
Vol 4 (2) ◽  
pp. 117 ◽  
Author(s):  
Alex Avdeef ◽  
Elisabet Fuguet ◽  
Antonio Llinàs ◽  
Clara Ràfols ◽  
Elisabeth Bosch ◽  
...  
Keyword(s):  
Solid State ◽  
Data Quality ◽  
Solution Chemistry ◽  
Equilibration Time ◽  
Equilibrium Solubility ◽  
Factors Affecting ◽  
Solubility Measurement ◽  
Type Water ◽  
Reported Data

<p class="ADMETabstracttext">This commentary addresses data quality in equilibrium solubility measurement in aqueous solution. Broadly discussed is the “gold standard” shake-flask (SF) method used to measure equilibrium solubility of ionizable drug-like molecules as a function of pH. Many factors affecting the quality of the measurement are recognized. Case studies illustrating the analysis of both solution and solid state aspects of solubility measurement are presented. Coverage includes drug aggregation in solution (sub-micellar, micellar, complexation), use of mass spectrometry to assess aggregation in saturated solutions, solid state characterization (salts, polymorphs, cocrystals, polymorph creation by potentiometric method), solubility type (water, buffer, intrinsic), temperature, ionic strength, pH measurement, buffer issues, critical knowledge of the pK<sub>a</sub>, equilibration time (stirring and sedimentation), separating solid from saturated solution, solution handling and adsorption to untreated surfaces, solubility units, and tabulation/graphic presentation of reported data. The goal is to present cohesive recommendations that could lead to better assay design, to result in improved quality of measurements, and to impart a deeper understanding of the underlying solution chemistry in suspensions of drug solids.</p>

Equilibrium solubility measurement of compounds with low dissolution rate by Higuchi's Facilitated Dissolution Method. A validation study

2017 ◽  
Vol 106 ◽  
pp. 133-141 ◽  
Author(s):  
Krisztina Takács-Novák ◽  
Maria Urac ◽  
Péter Horváth ◽  
Gergely Völgyi ◽  
Bradley D. Anderson ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Validation Study ◽  
Equilibrium Solubility ◽  
Dissolution Method ◽  
Solubility Measurement
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