Bumetanide (BUM) is a loop diuretic of the sulfamyl category, (3-(butylamino)-4-phenoxy-5-sulfamoylbenzoic acid) most often used to treat heart failure. Most often used in the people whom high dose of furosemide or other diuretics are ineffective.
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The main differences between bumetanide and furosemide are the bioavailability and potency. Mostly 60 percent of furosemide is absorbed in the intestine, and these are substantial inter and intra-individual differences in the bioavailability (range 10-90%). About 80 percent of bumetanide is absorbed, and these absorption does not change when it is taken with food. It is said to be a more diuretics, meaning that the predictable absorption is reflected in a more predictable effect. Bumetanide drug are 40 times more potent than furosemide for patients with normal renal function. It is sometimes used for weight loss because, use as a diuretic, and removes water from body. The study of solid state chemistry of pharmaceutical solid focuses on all disciplines right from drug discovery to successful marketing. A clear understanding of the molecular structure can lead to a better design and control of the drug performance. Moreover, interest in the subject of pharmaceutical solids stems in the part from FDA’s substance guideline that states appropriate analytical procedures to be used to detect polymorphic, cocrystals, hydrated or amorphous forms of the drug substance. Solid forms are usually more stable than liquid counterpart. The main factors which affect the oral route absorption are aqueous solubility, physical/chemical stability, and permeability. The fundamental parameters, i.e. aqueous solubility and gastrointestinal permeability which define oral drug absorption are used as the basis for the BCS classification scheme. These biopharmaceutical classes are defined as below figure.-01 Solubility and permeability parameters defined by FDA and according to it, ‘A drug substance is considered highly soluble when the highest strength is soluble in 250 mL or less of aqueous media within the pH range of 1- 6.8 at 37 ?± 1?°C’ and ‘A drug substance is considered to be highly permeable when the systemic Bioavailability or the extent of absorption in the humans is determined to be 85 percent or more in to the administered dose based on a mass balance determination (along with evidence showing stability of the drug in the GI tract ) or in comparison to an intravenous reference dose’.
1 Bumetanide is the diuretics agent, belongs to BCS class II. A survey by Lin et al.3 revealed that almost 40% of marketed medicines and 90% of emerging new chemical entities suffer from poor solubility which allows them to be eliminated from the gastrointestinal tract before they get completely dissolved and absorbed into the blood circulation, thus results in low bioavailability, less potency, and higher dose strength. For these classes of drugs, higher dose strength would be required to ensure therapeutic concentration in blood but it may lead to adverse or toxic effects on the recipient’s body.
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