Mechanical Activation by Ball Milling as a Strategy to Prepare Highly Soluble Pharmaceutical Formulations in the Form of Co-Amorphous, Co-Crystals, or Polymorphs

LM Martínez, J Cruz-Angeles, M Vázquez-Dávila… - Pharmaceutics, 2022 - mdpi.com
Almost half of orally administered active pharmaceutical ingredients (APIs) have low
solubility, which affects their bioavailability. In the last two decades, several alternatives …

[HTML][HTML] Cocrystals of tuberculosis antibiotics: Challenges and missed opportunities

E Khanfar, S Nagy, A Széchenyi - International journal of pharmaceutics, 2022 - Elsevier
Cocrystals have been extensively used to improve the physicochemical properties and
bioavailability of active pharmaceutical ingredients. Cocrystals of anti-tuberculosis …

Pharmaceutical salts of fenbendazole with organic counterions: structural analysis and solubility performance

AO Surov, NA Vasilev, MV Vener… - Crystal Growth & …, 2021 - ACS Publications
In this work, three new pharmaceutical salts of fenbendazole (FNB), a benzimidazole-based
anthelmintic drug, with sulfonic acids have been obtained and thoroughly investigated by …

Crystal structure, solubility, and pharmacokinetic study on a hesperetin cocrystal with piperine as coformer

Y Liu, F Yang, X Zhao, S Wang, Q Yang, X Zhang - Pharmaceutics, 2022 - mdpi.com
Hesperetin (HES) is a key biological active ingredient in citrus peels, and is one of the
natural flavonoids that attract the attention of researchers due to its numerous therapeutic …

Simultaneous improvement of dissolution behavior and oral bioavailability of antifungal miconazole via cocrystal and salt formation

KV Drozd, AN Manin, DE Boycov, GL Perlovich - Pharmaceutics, 2022 - mdpi.com
Miconazole shows low oral bioavailability in humans due to poor aqueous solubility,
although it has demonstrated various pharmacological activities such as antifungal, anti …

[HTML][HTML] A minimalist and robust chemo-photothermal nanoplatform capable of augmenting autophagy-modulated immune response against breast cancer

H Ming, B Li, H Tian, L Zhou, J Jiang, T Zhang, L Qiao… - Materials Today Bio, 2022 - Elsevier
Previously used in anti-fungal therapy, itraconazole has now been shown to be successful in
treating advanced breast cancer (NCT00798135). However, its poor solubility still restricts its …

[HTML][HTML] Leveraging the use of in vitro and computational methods to support the development of enabling oral drug products: An InPharma commentary

C Reppas, M Kuentz, A Bauer-Brandl, S Carlert… - European Journal of …, 2023 - Elsevier
Due to the strong tendency towards poorly soluble drugs in modern development pipelines,
enabling drug formulations such as amorphous solid dispersions, cyclodextrins, co-crystals …

In Silico Screening as a Tool to Prepare Drug-Drug Cocrystals of Ibrutinib-Ketoconazole: a Strategy to Enhance Their Solubility Profiles and Oral Bioavailability

DD Kara, PD Bangera, CH Mehta, K Tanvi… - AAPS …, 2023 - Springer
Ibrutinib (IBR) is a biopharmaceutical classification system (BCS) class II drug and an
irreversible Bruton's tyrosine kinase (BTK) inhibitor. IBR has an extremely low oral …

Pharmaceutical multicomponent crystals of antifungal drugs with improved dissolution performance

KV Drozd, AN Manin, DE Boycov… - Crystal Growth & …, 2021 - ACS Publications
New multicomponent crystals of climbazole (CLB) with fumaric acid (FumAc) and
tioconazole (TCL) with oxalic (OxlAc), malonic (MlnAc), fumaric, and dl-tartaric (TartAc) acids …

[HTML][HTML] Two novel palbociclib-resorcinol and palbociclib-orcinol cocrystals with enhanced solubility and dissolution rate

C Duan, W Liu, Y Tao, F Liang, Y Chen, X Xiao… - Pharmaceutics, 2021 - mdpi.com
Palbociclib (PAL) is an effective anti-breast cancer drug, but its use has been partly
restricted due to poor bioavailability (resulting from extremely low water solubility) and …