Saccharin

Zubair, Muhammad; Hassan, M. M. A.

doi:10.1016/s0099-5428(08)60200-2

Cited by 12 publications

(4 citation statements)

References 32 publications

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“…The numbering is according to Figure 1. The tentative assignments of SAC and FQs moieties were based on the individual spectra obtained with SAC and the respective FQ in addition to published information 27–29. Integration of signals allowed establishing a stoichiometric ratio 1:1 FQ/SAC suggesting that complete reaction of the individual components occurred.…”

Section: Resultsmentioning

confidence: 99%

“…The assignments for SAC were done by comparing with the solution spectrum reported in Ref 27. and taking into account the NQS data.…”

Section: Resultsmentioning

confidence: 99%

“…These values have been directly extracted from the highest level in each correlation of the 2D HETCOR experiment. The positions of the aromatic protons of SAC at 7.9 ppm were taken as reference for all the 1 H spectra 27. The error in the determination of the solid state 1 H chemical shifts is 0.5 ppm.…”

Section: Resultsmentioning

confidence: 99%

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Characterization of the Solubility and Solid-State Properties of Saccharin Salts of Fluoroquinolones

Romañuk

Manzo

Linck

et al. 2009

Journal of Pharmaceutical Sciences

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Section: Resultsmentioning

confidence: 99%

“…The assignments for SAC were done by comparing with the solution spectrum reported in Ref 27. and taking into account the NQS data.…”

Section: Resultsmentioning

confidence: 99%

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Characterization of the Solubility and Solid-State Properties of Saccharin Salts of Fluoroquinolones

Romañuk

Manzo

Linck

et al. 2009

Journal of Pharmaceutical Sciences

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“…The effect of cocrystal reactant properties on moisture sorption and cocrystal formation was studied by replacing NCT with SAC as the cocrystal reactant. NCT is highly hygroscopic and water soluble while SAC is nonhygroscopic, is ionizable (p K a =1.8), and has lower aqueous solubility than NCT. The DRH of the SAC/fructose blend shown in Table is similar to that of pure fructose.…”

Section: Resultsmentioning

confidence: 99%

Mechanisms by Which Moisture Generates Cocrystals

2007

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The purpose of this study is to determine the mechanisms by which moisture can generate cocrystals when solid particles of cocrystal reactants are exposed to deliquescent conditions (when moisture sorption forms an aqueous solution). It is based on the hypothesis that cocrystallization behavior during water uptake can be derived from solution chemistry using models that describe cocrystal solubility and reaction crystallization of molecular complexes. Cocrystal systems were selected with active pharmaceutical ingredients (APIs) that form hydrates and include carbamazepine, caffeine, and theophylline. Moisture uptake and crystallization behavior were studied by gravimetric vapor sorption, X-ray powder diffraction, and on-line Raman spectroscopy. Results indicate that moisture uptake generates cocrystals of carbamazepine-nicotinamide, carbamazepine-saccharin, and caffeine or theophylline with dicarboxylic acid ligands (oxalic acid, maleic acid, glutaric acid, and malonic acid) when solid mixtures with cocrystal reactants deliquesce. Microscopy studies revealed that the transformation mechanism to cocrystal involves (1) moisture uptake, (2) dissolution of reactants, and (3) cocrystal nucleation and growth. Studies of solid blends of reactants in a macro scale show that the rate and extent of cocrystal formation are a function of relative humidity, moisture uptake, deliquescent material, and dissolution rates of reactants. It is shown that the interplay between moisture uptake and dissolution determines the liquid phase composition, supersaturation, and cocrystal formation rates. Differences in the behavior of deliquescent additives (sucrose and fructose) are associated with moisture uptake and composition of the deliquesced solution. Our results show that deliquescence can transform API to cocrystal or reverse the reaction given the right conditions. Key indicators of cocrystal formation and stability are (1) moisture uptake, (2) cocrystal aqueous solubility, (3) solubility and dissolution of cocrystal reactants, and (4) transition concentration.

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Synthetische nichtnutritive Süßstoffe

et al. 1998

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Süßen (fast) ohne Kalorien ist mit den heute verfügbaren hochwirksamen Süßstoffen wie Aspartam 1, Saccharin 2 und Acesulfam‐K 3 alltäglich geworden. Entsprechend groß ist der Markt für diese nichtnutritiven synthetischen Verbindungen. Neben den Eigenschaften und großtechnischen Synthesen der Handelsprodukte werden auch einige Süßstoffe im fortgeschrittenen Entwicklungsstadium vorgestellt.

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Saccharin

Cited by 12 publications

References 32 publications

Characterization of the Solubility and Solid-State Properties of Saccharin Salts of Fluoroquinolones

Characterization of the Solubility and Solid-State Properties of Saccharin Salts of Fluoroquinolones

Mechanisms by Which Moisture Generates Cocrystals

Synthetische nichtnutritive Süßstoffe

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