2019
DOI: 10.5599/admet.704
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Harmonizing solubility measurement to lower inter-laboratory variance – progress of consortium of biopharmaceutical tools (CoBiTo) in Japan

Abstract: <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 e… Show more

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Cited by 14 publications
(14 citation statements)
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“…The apparent solubility of albendazole in the buffer was determined as 0.74 μg/mL or 2.8 µM. This value is in excellent agreement with reported intrinsic solubility and in good agreement with earlier reported values of 0.80 and 0.85 µg/mL, respectively, at the same pH but different buffer composition 24 . Other reported values differ to a greater extent, but they were measured at 25 °C in water without pH control 15,16 .…”
Section: Apparent Solubilities Of Albendazole In the Presence Of Hp-β-cd And Biomimetic Mediasupporting
confidence: 91%
“…The apparent solubility of albendazole in the buffer was determined as 0.74 μg/mL or 2.8 µM. This value is in excellent agreement with reported intrinsic solubility and in good agreement with earlier reported values of 0.80 and 0.85 µg/mL, respectively, at the same pH but different buffer composition 24 . Other reported values differ to a greater extent, but they were measured at 25 °C in water without pH control 15,16 .…”
Section: Apparent Solubilities Of Albendazole In the Presence Of Hp-β-cd And Biomimetic Mediasupporting
confidence: 91%
“…Figure 1 illustrates the variability in pH-dependent solubility data reported for darunavir, as a representative example, which was analyzed by six different laboratories. Laboratory-specific interpretation of experimental parameters that were deliberately kept flexible in the globally harmonized protocol to enable wide spread adoption across various resource settings [ 15 ] introduces unavoidable variability in absolute solubility data, ranging between 20-50 %. However, it is important to note that intra-laboratory variability was always ≤5 % and the final solubility classification of darunavir as a “low solubility” drug was consistent among all laboratories.…”
Section: Resultsmentioning
confidence: 99%
“…a salt form coverts to a free form in the pH-controlled region). In drug discovery and development, the solubility of a drug substance is usually measured in well-buffered media after a sufficient incubation time to achieve equilibrium [108][109][110][111]. The small intestinal pH (about pH 6.5) is in the pH-controlled region in most cases.…”
Section: Example 3: Salt Dissolutionmentioning
confidence: 99%
“…In addition, in silico models for the physicochemical properties of a drug are not so accurate as to be used for PBPK modelling [ 120 ]. Solubility measurements are not as easy as a modeler might imagine [ 109 , 111 , 121 ]. The p K a values change between 25 °C and 37 °C [ 122 , 123 ].…”
Section: Part 2: Scientific Literacy For Physiologically-based Pharma...mentioning
confidence: 99%
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