Global testing of a consensus solubility assessment to enhance robustness of the WHO biopharmaceutical classification system

Gigante, Valeria; Pauletti, Giovanni M.; Kopp, Sabine; Xu, Minghze; González‐Álvarez, Isabel; Merino, Virginia; McIntosh, Michelle Paula; Wessels, Anita; Lee, Beom‐Jin; Rezende, Kênnia Rocha; Scriba, Gerhard K. E.; Jadaun, Gaurav P. S.; Bermejo, Marival

doi:10.5599/admet.850

Cited by 7 publications

(7 citation statements)

References 29 publications

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“…Because the bioequivalence cannot be established if there is a difference (8-10). (37). Generic versions of drugs must show bioequivalence (BE) to the corresponding brandname versions before they may be sold (38).…”

Section: Figure 3: Bcs Class Drug Biowaviersmentioning

confidence: 99%

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BCS Class II Drug & Its Solubility Enhancement: A Review

Bajpai¹,

Singh²,

Bisht³

et al. 2022

J. Res. Appl. Sci. Biotechnol.

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The objective of this review article is to summarize literature data pertinent to potential excipient effects on intestinal drug permeability and transit. Despite the use of excipients in drug products for decades, considerable research efforts have been directed towards evaluating their potential effects on drug bioavailability. Potential excipient concerns stem from drug formulation changes (e.g., scale-up and post-approval changes, development of a new generic product). Regulatory agencies have established in vivo bioequivalence standards and, as a result, may waive the in vivo requirement, known as a biowaiver, for some oral products. Biowaiver acceptance criteria are based on the in vitro characterization of the drug substance and drug product using the Biopharmaceutics Classification System (BCS). Various regulatory guidance documents have been issued regarding BCS-based biowaivers, such that the current FDA guidance is more restrictive than prior guidance, specifically about excipient risk. In particular, sugar alcohols have been identified as potential absorption-modifying excipients. These biowaivers and excipient risks are discussed here.

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Section: Figure 3: Bcs Class Drug Biowaviersmentioning

confidence: 99%

“…Replacement therapies and other essential pharmaceuticals, as well as backup measures in case of shortages. [37,38], are examples of medication treatment services that should be readily available without interruption, in our opinion.…”

Section: Higher Drug Consumption During Pandemicmentioning

confidence: 99%

BCS Class II Drug & Its Solubility Enhancement: A Review

Bajpai¹,

Singh²,

Bisht³

et al. 2022

J. Res. Appl. Sci. Biotechnol.

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show abstract

“…However, using them to measure a new chemical’s solubility with useful accuracy is still a practical problem . The gold standard of saturation shake-flask measurement is low throughput, and it would take state-of-the-art techniques to achieve a low interlaboratory variability . Factors like crystallinity, polymorphism, compound purity, particle size, and so forth all impact interlaboratory reproducibility.…”

Section: Introductionmentioning

confidence: 99%

Building Machine Learning Small Molecule Melting Points and Solubility Models Using CCDC Melting Points Dataset

Zhu

Polyakov

Bajjuri

et al. 2023

J. Chem. Inf. Model.

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Predicting solubility of small molecules is a very difficult undertaking due to the lack of reliable and consistent experimental solubility data. It is well known that for a molecule in a crystal lattice to be dissolved, it must, first, dissociate from the lattice and then, second, be solvated. The melting point of a compound is proportional to the lattice energy, and the octanol−water partition coefficient (log P) is a measure of the compound's solvation efficiency. The CCDC's melting point dataset of almost one hundred thousand compounds was utilized to create widely applicable machine learning models of small molecule melting points. Using the general solubility equation, the aqueous thermodynamic solubilities of the same compounds can be predicted. The global model could be easily localized by adding additional melting point measurements for a chemical series of interest.

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“…The single particle analysis was useful to study local recrystallization occurring on the particle surface, providing crucial information to understand surface chemistry effects during storage and dissolution. Dissolution was also studied by Gigante et al [14] who set out to perform a global evaluation of the WHO harmonised protocol for equilibrium solubility experiments. The study focused on measurement of 16 compounds for which the biopharmaceutics classification had previously been performed.…”

mentioning

confidence: 99%

“…Dissolution was also studied by Gigante et al . [ 14 ] who set out to perform a global evaluation of the WHO harmonised protocol for equilibrium solubility experiments. The study focused on measurement of 16 compounds for which the biopharmaceutics classification had previously been performed.…”

mentioning

confidence: 99%