Solid solution polymorphs afford two highly soluble co-drug forms of tolbutamide and chlorpropamide

Spoletti, Enrico; Verma, Vivek; Cappuccino, Chiara; Lusi, Matteo

doi:10.1039/d3cc04725c

Chem. Commun.

2023

DOI: 10.1039/d3cc04725c

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Solid solution polymorphs afford two highly soluble co-drug forms of tolbutamide and chlorpropamide

Enrico Spoletti,

Vivek Verma,

Chiara Cappuccino

et al.

Abstract: Tolbutamide and chloropropamide form two co-drug solid solutions that show a rare case of monotropic polymorphism at any composition. Both forms are kinetically stable and with faster dissolution rate than the pure drugs.

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2024

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Cited by 3 publications

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An analysis of multidrug multicomponent crystals as tools for drug development

Kavanagh

2024

Journal of Controlled Release

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An analysis of multidrug multicomponent crystals as tools for drug development

Kavanagh

2024

Journal of Controlled Release

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Drug–Drug Cocrystal Alloy and Nanoformulation of Cytarabine: Optimized Biopharmaceutical Property and Synergistic Antitumor Efficacy

Yu,

Li,

et al. 2024

Mol. Pharmaceutics

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An integrated strategy by combining cocrystallization with nanotechnology is developed to optimize in vitro/vivo performances of marine antitumor drug cytarabine (ARA) and further obtain innovative insights into the exploitation of cocrystal alloy nanoformulation. Therein, the optimization of properties and synergistic effects of ARA mainly depends on assembling with uracil (U) and antitumor drug 5-fluorouracil (FU) into the same crystal by cocrystallization technology, while the long-term efficacy is primarily maintained by playing the superiority of nanotechnology. Along this line, the first cocrystal alloy of ARA, viz., ARA-FU-U (0.6:0.4), is successfully obtained and then transformed into a nanocrystal. Single-crystal X-ray diffraction analysis demonstrates that this cocrystal alloy consists of two isomorphic cocrystals of ARA, namely, ARA-FU and ARA-U, in 0.6:0.4 ratio. An R 2 2 (8) hydrogen-bonding cyclic system formed by a cytosine fragment of ARA with U or FU can protect and stabilize the amine group on ARA, laying the foundation for regulating its properties. The in vitro/in vivo properties of the cocrystal alloy and its nanocrystals are investigated by theoretical and experimental means. It reveals that both the alloy and nanocrystal can improve physicochemical properties and promote drug absorption, thus bringing to optimized pharmacokinetic behaviors. The nanocrystal produces superior effects than the alloy that helps to extend therapeutic time and action. Particularly, relative to the corresponding binary cocrystal, the synergistic antitumor activity of ARA and FU in the cocrystal alloy is heightened obviously. It may be that U contributes to reducing the degradation of FU, specifically increasing its concentration in tumors to enhance the synergistic effects of FU and ARA. These findings provide new thoughts for the application of cocrystal alloys in the marine drug field and break fresh ground for cocrystal alloy formulations to optimize drug properties.

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Impurity retention and pharmaceutical solid solutions: visualizing the effect of impurities on dissolution and growth using dyed crystals

Nong,

Schleper,

Martin

et al. 2024

CrystEngComm

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Solid solution polymorphs afford two highly soluble co-drug forms of tolbutamide and chlorpropamide

Abstract: Tolbutamide and chloropropamide form two co-drug solid solutions that show a rare case of monotropic polymorphism at any composition. Both forms are kinetically stable and with faster dissolution rate than the pure drugs.

Cited by 3 publications

References 37 publications

An analysis of multidrug multicomponent crystals as tools for drug development

An analysis of multidrug multicomponent crystals as tools for drug development

Drug–Drug Cocrystal Alloy and Nanoformulation of Cytarabine: Optimized Biopharmaceutical Property and Synergistic Antitumor Efficacy

Impurity retention and pharmaceutical solid solutions: visualizing the effect of impurities on dissolution and growth using dyed crystals

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