28395-05-3Relevant academic research and scientific papers
METHODS AND COMPOSITIONS FOR TREATING EDEMA REFRACTORY TO ORAL DIURETICS
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Paragraph 0140; 0141, (2021/06/11)
The present invention features methods and compositions for the intranasal, sublingual, and subcutaneous administration of bumetanide for the treatment of subjects suffering from edema refractory to oral diuretics.
Sodium and potassium salts of bumetanide trihydrate: Impact of counterion on structure, aqueous solubility and dehydration kinetics
Ong, Winston,Cheung, Eugene Y.,Schultz, Karen A.,Smith, Cartney,Bourassa, James,Hickey, Magali B.
experimental part, p. 2428 - 2434 (2012/07/27)
A form of bumetanide potassium trihydrate that is structurally similar to bumetanide sodium trihydrate was identified. Structural analysis indicated however that the change from sodium to potassium salt resulted in meaningful changes in the packing arrangement and even greater changes on physicochemical properties. The potassium trihydrate salt was five times more soluble in water relative to the sodium trihydrate salt (27 mg mL-1vs. 5.6 mg mL -1). Both salts underwent complete dehydration to their corresponding anhydrate forms following exposure to low humidity or elevated temperature. Arrhenius plots for the dehydration between 20-30 °C yielded a lower activation barrier for the potassium trihydrate compared to the sodium trihydrate (14.9 kcal mol-1vs. 19.9 kcal mol-1), translating into a 15-20-fold difference in the rate of dehydration. Such a 5.0 kcal mol-1 gap suggests that the H2O molecules are more tightly bound in the sodium trihydrate compared to potassium trihydrate. These differences in solubility and rate of dehydration further illustrate that changes to chemical composition can have a meaningful and unpredictable impact on the physicochemical properties of closely related pharmaceutical salt forms. The Royal Society of Chemistry 2012.
3-Amino, 4-thio-substituted, 5-sulphamyl-benzoic acid derivatives
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, (2008/06/13)
This invention relates to new, therapeutically active compounds of the general formula SPC1 In which A represents one of the groupings EQU1 R2 --O--, R2 --S--, R2 --OS--, and R2 --O2 S--, R1, R2, R3, and R4 each represents hydrogen, an aliphatic radical, a cycloaliphatic radical, or an aromatically, cycloaliphatically, or heterocyclically substituted aliphatic radical, in addition to which R2 and R3 may each represent an aromatic or heterocyclic radical, and when A is EQU2 R1 and R2 may be linked to form a 5- to 8-membered heterocyclic ring system, which may have one or more nitrogen atoms, sulphur atoms, or oxygen atoms in addition to the nitrogen atom linked to R1 and R2 ; R5 is hydrogen or lower alkyl; and R6 is hydrogen or lower alkyl or acyl; to salts, esters, and amides of the said compounds; and to methods for the production of the compounds.
