ArticlePharmaceutics2022
Crystal Structure, Solubility, and Pharmacokinetic Study on a Hesperetin Cocrystal with Piperine as Coformer.
Article in Pharmaceutics, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 54 citations in OpenAlex.
- Research progress on the metabolic fate of citrus flavonoids and strategies to improve bioavailability.Food chemistry: X · 2026Review
- Flavonoids in Medicine and Food Homology Substances: Structure-Activity Relationship, Application Challenges, and Cutting-Edge Technological Breakthroughs.Foods (Basel, Switzerland) · 2026Review
- Integrative green synthesis and molecular simulation of ibrutinib cocrystals for enhanced biopharmaceutical performance and in vivo pharmacokinetics.International journal of pharmaceutics: X · 2025Article
- Flavonoid-Based Cocrystals: A Comprehensive Study on Their Synthesis, Characterization, Physicochemical Properties and Applications.Molecules (Basel, Switzerland) · 2025Review
- Carrier-free nanoparticles-new strategy of improving druggability of natural products.Journal of nanobiotechnology · 2025Review
- Modification of biopharmaceutical parameters of flavonoids: a review.Frontiers in chemistry · 2025Review
- Evaluation of Pharmacokinetic Feasibility of Febuxostat/L-pyroglutamic Acid Cocrystals in Rats and Mice.Pharmaceutics · 2023Article
- In Silico Screening as a Tool to Prepare Drug-Drug Cocrystals of Ibrutinib-Ketoconazole: a Strategy to Enhance Their Solubility Profiles and Oral Bioavailability.AAPS PharmSciTech · 2023Article
- Citrus By-Products as a Valuable Source of Biologically Active Compounds with Promising Pharmaceutical, Biological and Biomedical Potential.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Article
- Nano-hesperetin attenuates ketamine-induced schizophrenia-like symptoms in mice: participation of antioxidant parameters.Psychopharmacology · 2023Article
- Stachydrine, a Bioactive Equilibrist for Synephrine, Identified from FourMolecules (Basel, Switzerland) · 2023Article
- Cocrystal of phloretin with isoniazid: preparation, characterization, and evaluation.RSC advances · 2023Article
- Amorphous System of Hesperetin and Piperine-Improvement of Apparent Solubility, Permeability, and Biological Activities.International journal of molecular sciences · 2023Article
- A Review of Coformer Utilization in Multicomponent Crystal Formation.Molecules (Basel, Switzerland) · 2022Review
- A DFT study on the structure activity relationship of the natural xanthotoxin-based pharmaceutical cocrystals.Journal of molecular modeling · 2022Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
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 bioactivities that have been identified in vitro. As a bioenhancer, piperine (PIP) can effectively improve the absorption of insoluble drugs in vivo. In the present study, a cocrystal of HES and PIP was successfully obtained through solution crystallization. The single-crystal structure was illustrated and comprehensive characterization of the cocrystal was conducted. The cocrystal was formed by two drug molecules at a molar ratio of 1:1, which contained O-H-O hydrogen bonds between the carbonyl and ether oxygen of PIP and the phenolic hydroxyl group of HES. In addition, a solubility experiment was performed on powder cocrystal in simulated gastrointestinal fluid, and the result revealed that the cocrystal improves the dissolution behavior of HES compared with that of the pure substance. Furthermore, HES's bioavailability in the cocrystal was six times higher than that of pristine drugs. These results may provide an efficient oral formulation for HES.
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Registered trials
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