“…This iteration is done by replacing dx 1,3 and V cor in the Eqs. (15), (16) and (19) to recalculate x L 1;3 until a non-variant value of V cor is acquired. The obtained values of correlation volume V cor and dx 1,3 are listed in Tables S12-S15 of Supplementary material for {methanol (1) + water (2)}, {n-propanol (1) + water (2)}, {acetonitrile (1) + water (2)} and {1,4-dioxane (1) + water (2)} solvent mixtures, respectively.…”
Section: Preferential Solvation Of Ribavirinmentioning
confidence: 99%
“…Because of its activity against both RNA and DNA viruses [8], it is recommended for the treatment of some infectious disorders including herpes [9], respiratory syncytial viral disease, and acute respiratory infections caused by adenovirus [10]. At present, ribavirin is also part of a combination therapy for the treatment of hepatitis C [11][12][13][14][15][16] and Lassa fever [14,15]. Furthermore, it has been evaluated for severe acute respiratory syndrome (SARS) and as an anti-cancer drug with successful results for the treatment of leukemia and breast cancer [16][17][18].…”
Section: Introductionmentioning
confidence: 99%
“…At present, ribavirin is also part of a combination therapy for the treatment of hepatitis C [11][12][13][14][15][16] and Lassa fever [14,15]. Furthermore, it has been evaluated for severe acute respiratory syndrome (SARS) and as an anti-cancer drug with successful results for the treatment of leukemia and breast cancer [16][17][18]. Due to its good properties, ribavirin has been received great attention.…”
a b s t r a c tThe equilibrium solubility of ribavirin in solvent mixtures of {methanol (1) + water (2)}, {n-propanol (1) + water (2)}, {acetonitrile (1) + water (2)} and {1,4-dioxane (1) + water (2)} was determined experimentally by using isothermal dissolution equilibrium method within the temperature range from (278.15 to 318.15) K under atmospheric pressure (101.1 kPa). At the same temperature and mass fraction of methanol (n-propanol, acetonitrile or 1,4-dioxane), the mole fraction solubility of ribavirin is greater in (methanol + water) than in the other three solvent mixtures. The preferential solvation parameters were derived from their thermodynamic solution properties by means of the inverse Kirkwood-Buff integrals. The preferential solvation parameters for methanol, n-propanol, acetonitrile or 1,4-dioxane (dx 1,3 ) were negative in the four solvent mixtures with a very wide compositions, which indicated that ribavirin was preferentially solvated by water. Temperature had little effect on the preferential solvation magnitudes. The higher solvation by water could be explained in terms of the higher acidic behaviour of water interacting with the Lewis basic groups of the ribavirin. Besides, the solubility of the drugs was mathematically represented by using the Jouyban-Acree model, van't Hoff-Jouyban-Acree model and Apelblat-Jouyban-Acree model obtaining average relative deviations lower than 1.57% for correlative studies. It is noteworthy that the solubility data presented in this work contribute to expansion of the physicochemical information about the solubility of drugs in binary solvent mixtures and also allows the thermodynamic analysis of the respective dissolution and specific solvation process.
“…This iteration is done by replacing dx 1,3 and V cor in the Eqs. (15), (16) and (19) to recalculate x L 1;3 until a non-variant value of V cor is acquired. The obtained values of correlation volume V cor and dx 1,3 are listed in Tables S12-S15 of Supplementary material for {methanol (1) + water (2)}, {n-propanol (1) + water (2)}, {acetonitrile (1) + water (2)} and {1,4-dioxane (1) + water (2)} solvent mixtures, respectively.…”
Section: Preferential Solvation Of Ribavirinmentioning
confidence: 99%
“…Because of its activity against both RNA and DNA viruses [8], it is recommended for the treatment of some infectious disorders including herpes [9], respiratory syncytial viral disease, and acute respiratory infections caused by adenovirus [10]. At present, ribavirin is also part of a combination therapy for the treatment of hepatitis C [11][12][13][14][15][16] and Lassa fever [14,15]. Furthermore, it has been evaluated for severe acute respiratory syndrome (SARS) and as an anti-cancer drug with successful results for the treatment of leukemia and breast cancer [16][17][18].…”
Section: Introductionmentioning
confidence: 99%
“…At present, ribavirin is also part of a combination therapy for the treatment of hepatitis C [11][12][13][14][15][16] and Lassa fever [14,15]. Furthermore, it has been evaluated for severe acute respiratory syndrome (SARS) and as an anti-cancer drug with successful results for the treatment of leukemia and breast cancer [16][17][18]. Due to its good properties, ribavirin has been received great attention.…”
a b s t r a c tThe equilibrium solubility of ribavirin in solvent mixtures of {methanol (1) + water (2)}, {n-propanol (1) + water (2)}, {acetonitrile (1) + water (2)} and {1,4-dioxane (1) + water (2)} was determined experimentally by using isothermal dissolution equilibrium method within the temperature range from (278.15 to 318.15) K under atmospheric pressure (101.1 kPa). At the same temperature and mass fraction of methanol (n-propanol, acetonitrile or 1,4-dioxane), the mole fraction solubility of ribavirin is greater in (methanol + water) than in the other three solvent mixtures. The preferential solvation parameters were derived from their thermodynamic solution properties by means of the inverse Kirkwood-Buff integrals. The preferential solvation parameters for methanol, n-propanol, acetonitrile or 1,4-dioxane (dx 1,3 ) were negative in the four solvent mixtures with a very wide compositions, which indicated that ribavirin was preferentially solvated by water. Temperature had little effect on the preferential solvation magnitudes. The higher solvation by water could be explained in terms of the higher acidic behaviour of water interacting with the Lewis basic groups of the ribavirin. Besides, the solubility of the drugs was mathematically represented by using the Jouyban-Acree model, van't Hoff-Jouyban-Acree model and Apelblat-Jouyban-Acree model obtaining average relative deviations lower than 1.57% for correlative studies. It is noteworthy that the solubility data presented in this work contribute to expansion of the physicochemical information about the solubility of drugs in binary solvent mixtures and also allows the thermodynamic analysis of the respective dissolution and specific solvation process.
“…Therefore, further efforts will be focused on the development of immobilized enzyme. Recently, Rivero et al reported successful immobilization of E. coli ATCC 12407 in agarose matrix [16]. Moreover, immobilization on fused silica Open Tubular Capillary [22], aldehyde-agarose [23], and MagReSyn epoxide microspheres [24,25], in calcium alginate, agar, and kcarrageenan matrix [18], was described in the literature.…”
Section: International Journal Of Chemical Engineeringmentioning
confidence: 99%
“…All the methods for synthesis of Ribavirin available at the moment could be divided into chemical [4][5][6][7] and microbiological [8][9][10][11][12][13][14][15][16] approaches. Typical procedure for chemical synthesis includes condensation of the 1,2,3,5-tetra-O-acetyl--D-ribofuranose 1 with 1,2,4-triazolecarboxylic acid esters 2 followed by treatment of the resulting compound 3 with methanolic ammonia solution (Scheme 1).…”
Ribavirin is an important antiviral drug, which is used for treatment of many diseases. The pilot-scale chemoenzymatic process for synthesis of the active pharmaceutical ingredient Ribavirin was developed with 32% overall yield and more than 99.5% purity. The described method includes the chemical synthesis of 1,2,4-triazole-3-carboxamide, which is a key intermediate and enzyme-catalyzed transglycosylation reaction for preparation of the desired product. 1,2,4-Triazole-3-carboxamide was synthesized from 5-amino-1,2,4-triazole-3-carboxylic acid by classical Chipen-Grinshtein method. Isolated fromE. сoliBL21(DE3)/pERPUPHHO1 strain the purine nucleoside phosphorylase was used as a biocatalytical system. All steps of this process were optimized and scaled.
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