ArticleMolecular pharmaceutics2021
Amorphous Drug-Polymer Salt with High Stability under Tropical Conditions and Fast Dissolution: The Case of Clofazimine and Poly(acrylic acid).
Article in Molecular pharmaceutics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Crystal engineering for poorly water-soluble drugs: From design to applications.Acta pharmaceutica Sinica. B · 2026Review
- Recent Techniques to Improve Amorphous Dispersion Performance with Quality Design, Physicochemical Monitoring, Molecular Simulation, and Machine Learning.Pharmaceutics · 2025Review
- The Implications of Drug-Polymer Interactions on the Physical Stability of Amorphous Solid Dispersions.Pharmaceutical research · 2023Review
- Effects of Additives on the Physical Stability and Dissolution of Polymeric Amorphous Solid Dispersions: a Review.AAPS PharmSciTech · 2023Review
- Enteric coating of tablets containing an amorphous solid dispersion of an enteric polymer and a weakly basic drug: A strategy to enhance in vitro release.International journal of pharmaceutics · 2023Article
- Advances in the development of amorphous solid dispersions: The role of polymeric carriers.Asian journal of pharmaceutical sciences · 2023Review
- Amorphous Drug-Polymer Salts: Maximizing Proton Transfer to Enhance Stability and Release.Molecular pharmaceutics · 2023Article
- pH-Dependent supersaturation from amorphous solid dispersions of weakly basic drugs.Pharmaceutical research · 2022Article
- Combining enabling formulation strategies to generate supersaturated solutions of delamanid: In situ salt formation during amorphous solid dispersion fabrication for more robust release profiles.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2022Article
- Amorphous Form of Carvedilol Phosphate-The Case of Divergent Properties.Molecules (Basel, Switzerland) · 2021Article
- Amorphous Drug-Polymer Salts.Pharmaceutics · 2021Article
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6 authors.
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Abstract
We report that the stability of amorphous clofazimine (CFZ) against crystallization is vastly improved by salt formation with a polymer without sacrificing dissolution rate. A simple slurry method was used to produce the amorphous salt of CFZ with poly(acrylic acid) (PAA) at 75 wt % drug loading. The synthesis was performed under a mild condition suitable for thermally unstable drugs and polymers. Salt formation was confirmed by visible spectroscopy and glass temperature elevation. The amorphous salt at 75 wt % drug loading is remarkably stable against crystallization at 40 °C and 75% RH for at least 180 days. In contrast, the amorphous solid dispersion containing the un-ionized CFZ dispersed in poly(vinylpyrrolidone) crystallized in 1 week under the same condition. The high stability of the amorphous drug-polymer salt is a result of the absence of a drug-polymer crystalline structure, reduced driving force for crystallizing the free base, and reduced molecular mobility. Despite the elevated stability, the amorphous drug-polymer salt showed fast dissolution and high solution concentration in two biorelevant media (SGF and FaSSIF). Additionally, the amorphous CFZ-PAA salt has improved tabletability and powder flow relative to crystalline CFZ. The CFZ-PAA example suggests a general method to prepare amorphous drugs with high physical stability under tropical conditions and fast dissolution.
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