Dual-drug co-crystal synthesis for synergistic in vitro effect of three key first-line antiretroviral drugs

Ngilirabanga, Jean Baptiste; Rosa, Paulo; Aucamp, Marique; Kippie, Yunus; Samsodien, Halima

doi:10.1016/j.jddst.2020.101958

Cited by 6 publications

(2 citation statements)

References 30 publications

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“…Naproxen solubility was increased by 2.2, 1.6, and 2.38 times in the case of N1, N2, and N3 co-crystals, respectively, when compared with pure naproxen solubility. This may be attributed to the co-crystal high energy that made co-crystal behave in a similar manner to amorphous form when dissolved in water by maintaining a supersaturated state which leads to giving a higher saturated solubility in comparison with their starting materials (36,37) .…”

Section: Saturation Solubility Studymentioning

confidence: 99%

Development of novel paracetamol/naproxen co-crystals with an improvement in naproxen solubility.

Al-Dulaimi

Al-Kotaji²,

Abachi

2022

IJPS

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Co-crystals are new solid forms of drugs that could resolve more than one problem associated with drugs formulations like solubility, stability, bioavailability, mechanical and tableting properties. A preliminary theoretical study for estimating the possible bonding between the co-crystal components (paracetamol and naproxen) was performed using the ChemOffice program. The results revealed a high possibility for bonding between paracetamol and naproxen and indicated the ability of molecular mechanics study to predict the co-crystal design. In this work, four different methods were used for the preparation of three different ratios 1:1, 2:1, and 1:2 of paracetamol:naproxen co-crystals. The four methods are liquid-assisted grinding, solvent evaporation method, ultrasonic-assisted co-crystallization, and microwave-assisted co-crystallization. The characterization of the prepared co-crystal was performed by Fourier transform infrared spectroscopy, Thermogravimetric Analysis, Differential scanning calorimetry, Powder X-Ray diffraction, and Field emission scanning electron microscopy. The results showed that the most successful method for co-crystal production was solvent evaporation methods. The FTIR and DSC results indicated the formation of paracetamol-naproxen co-crystals when prepared by using the solvent evaporation method in the three ratios 1:1 (N1), 2:1 (N2), and 1:2 (N3). Moreover, the PXRD results confirm the previous conclusions. A solubility study was conducted to compare the water solubility of pure paracetamol and naproxen with co-crystals solubility. The naproxen solubility was improved by more than two times in (1:1) and (1:2) paracetamol/naproxen co-crystals. To conclude, this work succeeded in formation of new paracetamol/naproxen co-crystals, which can be considered as a new promising technique for formulation of these two drugs with an obvious enhancement in naproxen solubility and crystallinity. This could be exploited in preparation of tablets with possible enhancement in dissolution and bioavailability, however, further work is needed to prove this assumption.

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Section: Saturation Solubility Studymentioning

confidence: 99%

Development of novel paracetamol/naproxen co-crystals with an improvement in naproxen solubility.

Al-Dulaimi

Al-Kotaji²,

Abachi

2022

IJPS

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“…The average volume of the thermal ellipsoids of the CH 2 carbon atoms of the cyclopropyl groups were calculated at a 50% ellipsoid probability and, as shown in Table 1, is largest in 1 and decreases in the cocrystals, suggesting the occurrence of reduced dynamics of the cyclopropyl group in the cocrystals. While there are additional cocrystals with 1 reported in the literature, 46,47 we have restricted our investigations to the structures available in the CSD. 40 Selected experimental X-ray parameters have been summarized in Table 2.…”

Section: I) X-ray Diffractionmentioning

confidence: 99%

Taming the dynamics in a pharmaceutical by cocrystallization: investigating the impact of the coformer by solid-state NMR

et al. 2021

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Molecular complexes of drug combinations: A review of cocrystals, salts, coamorphous systems and amorphous solid dispersions

Li,

Wang,

et al. 2023

International Journal of Pharmaceutics

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Dual-drug co-crystal synthesis for synergistic in vitro effect of three key first-line antiretroviral drugs

Cited by 6 publications

References 30 publications

Development of novel paracetamol/naproxen co-crystals with an improvement in naproxen solubility.

Development of novel paracetamol/naproxen co-crystals with an improvement in naproxen solubility.

Taming the dynamics in a pharmaceutical by cocrystallization: investigating the impact of the coformer by solid-state NMR

Molecular complexes of drug combinations: A review of cocrystals, salts, coamorphous systems and amorphous solid dispersions

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