ArticlePharmaceutical research2023
Optimisation of Pharmaceutical Cocrystal Dissolution Performance through a Synergistic Precipitation Inhibition.
Article in Pharmaceutical research, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 16 citations in OpenAlex.
- From triggers to interfaces: polymer-stabilized nano-co-crystals for robust mesalazine delivery in UC.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2026Review
- Novel Cocrystal of Quercetagetin: In vitro and in vivo Insights into Biopharmaceutical Performance.Pharmaceutical research · 2026Article
- Polymorphism Control of Carbamazepine Based on Deep Eutectic Solvents.Pharmaceutical research · 2026Article
- Pharmaceutical Cocrystals in Drug-Delivery Technologies: Advances from Rational Design to Therapeutic Applications.Pharmaceutics · 2026Review
- ML-Driven Pharmaceutical Cocrystal Technology: Advances in Screening, Property Prediction and Applications.AAPS PharmSciTech · 2026Review
- Advances in Pharmaceutical Cocrystals and Nano-Cocrystals: Strategies for Enhancing Solubility and Translating to Clinical Use.AAPS PharmSciTech · 2025Review
- Insight into the Precipitation Inhibition of Polymers within Cocrystal Formulations in Solution Using Experimental and Molecular Modeling Techniques.Crystal growth & design · 2025Article
- Supersaturated Liquid Formulation of Pazopanib Hydrochloride Loaded with Synergistic Precipitation Inhibitors.Molecules (Basel, Switzerland) · 2024Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
objectivesPolymeric excipients play an important role in a cocrystal formulation to act as precipitation inhibitors to maximize the potential. Otherwise, a stable form of the parent drug will be recrystallized on the dissolving cocrystal surface and/or in the bulk solution during the cocrystal dissolution process, negating the solubility advantage. The objectives of this work were to investigate the potential of using combined polymers to maximise the dissolution performance of surface precipitation pharmaceutical cocrystals.
methodsThe dissolution performance of a highly soluble flufenamic acid and nicotinamide (FFA-NIC) cocrystal has been systematically studied with predissolved or powder mixed with a single polymer, including a surface precipitation inhibitor [i.e., copolymer of vinylpyrrolidone (60%) /vinyl acetate (40%) (PVP-VA)] and two bulk precipitation inhibitors [i.e., polyethylene glycol (PEG) and Soluplus (SLP)], or binary polymers combinations.
resultsA single polymer of PVP-VA prevented the FFA surface precipitation for an enhanced dissolution performance of FFA-NIC cocrystal. Unfortunately, it cannot sustain the supersaturated FFA concentration in the bulk solution. A combination of two polymers of PVP-VA and SLP has shown a synergistic inhibition effect to enhance the dissolution advantage of FFA-NIC cocrystal.
conclusionsThe dissolution of a cocrystal with surface precipitation of the parent drug can be described as: i) the cocrystal surface contacting the dissolution medium; ii) the cocrystal surface dissolving; iii) the parent drug precipitation on the dissolving surface; and iv) the parent drug particles redissolving. A combination of two types of polymers can be used to maximise the cocrystal performance in solution.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.