Physicochemical characterization of furosemide modifications

Matsuda, Yoshihisa; Tatsumi, Etsuko

doi:10.1016/0378-5173(90)90185-7

Cited by 105 publications

(85 citation statements)

References 22 publications

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“…Furosemide, a loop diuretic, is widely used orally for treatment of hypertension and oedema (Goud et al, 2011;Matsuda et al, 1990). Furosemide is classified as class IV in the Biopharmaceutics Classification System (BCS), hence it has a low aqueous solubility in the physiological pH range (5-20 µg/ml) and at the same time, a poor intestinal permeability.…”

Section: Introductionmentioning

confidence: 99%

“…Furosemide is classified as class IV in the Biopharmaceutics Classification System (BCS), hence it has a low aqueous solubility in the physiological pH range (5-20 µg/ml) and at the same time, a poor intestinal permeability. The compound has weak acidic properties, two pKa values of 9.9 and 3.5 and is reported to be able to exist in seven different solid state forms: four polymorphs (I, II, III, IV), two solvates (IV-DMS and V-dioxane) and one amorphous form (Goud et al, 2011;Granero et al, 2010;Matsuda et al, 1990). The poor solubility of furosemide together with a tendency to undergo site-specific absorption in the stomach and upper small intestine, leads to a highly variable bioavailability of orallyadministered furosemide in humans (20-60%) (Iannuccelli et al, 2000).…”

Section: Introductionmentioning

confidence: 99%

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Stabilisation of amorphous furosemide increases the oral drug bioavailability in rats

Nielsen

Rades

2015

International Journal of Pharmaceutics

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A glass solution of the amorphous sodium salt of furosemide (ASSF) and polyvinylpyrrolidone (PVP) (80:20 w/w%) was prepared by spray drying. It was investigated if PVP was able to stabilise ASSF during storage and dissolution and whether this influenced the in vivo performance of the glass solution after oral dosing to rats. The glass solution had a glass transition temperature of 121.3±0.5°C, which was significantly higher than that of the pure drug (101.2°C). ASSF in the glass solution was stable for at least 168 days when stored at 20°C and 0% relative humidity. The glass solution exhibited fast dissolution in simulated intestinal medium, pH 6.5; the intrinsic dissolution rate was found to be 10.1±0.6 mg/cm 2 /min, which was significantly faster than the pure ASSF. When investigating the stability during dissolution in stimulated intestinal medium at pH 6.5, the ASSF in the glass solution showed signs of crystallinity after 1 min of dissolution, but crystallised to a lesser extent than pure ASSF. The stabilising effect of PVP on ASSF, led to improved relative oral bioavailability in rats of 263%, when compared to the pure ASSF.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Stabilisation of amorphous furosemide increases the oral drug bioavailability in rats

Nielsen

Rades

2015

International Journal of Pharmaceutics

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Section: Furosemidementioning

confidence: 99%

“…When the solubilities of furosemide polymorphs are compared, the metastable form II is found to be the most soluble (Matsuda et al, 1990). This API has been observed to undergo photolytic degradation from which the metastable forms suffer more than the thermodynamically stable form I (Matsuda et al, 1990;Villiers et al1992). To differentiate furosemide polymorphic forms in pharmaceutical formulations, several dissolution mediums were tested, which resulted in a recommended medium at pH 2.2 due to its ability to differentiate the commercialized form (form I) from the other forms (II and III) (Maggio et al, 2009).…”

Section: Furosemidementioning

confidence: 99%

Polymorphism: an evaluation of the potential risk to the quality of drug products from the Farmácia Popular Rede Própria

Santos

Reis

Jacon

et al. 2014

Braz. J. Pharm. Sci.

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Polymorphism in solids is a common phenomenon in drugs, which can lead to compromised quality due to changes in their physicochemical properties, particularly solubility, and, therefore, reduce bioavailability. Herein, a bibliographic survey was performed based on key issues and studies related to polymorphism in active pharmaceutical ingredient (APIs) present in medications from the Farmácia Popular Rede Própria. Polymorphism must be controlled to prevent possible ineffective therapy and/or improper dosage. Few mandatory tests for the identification and control of polymorphism in medications are currently available, which can result in serious public health concerns.Uniterms: Polymorphism. Medicines/quality control. Medicines/solubility. Medicines/bioavailability.O polimorfismo em sólidos é um fenômeno frequente em fármacos e pode levar a problemas na qualidade dos medicamentos por alterar suas propriedades físico-químicas, em especial a solubilidade e, consequentemente, a biodisponibilidade. Nesse trabalho realizou-se levantamento bibliográfico sobre os principais estudos e problemas relacionados ao polimorfismo em fármacos presentes nos medicamentos disponibilizados pela Farmácia Popular do Brasil. O polimorfismo deve ser controlado a fim de evitar possível ineficácia terapêutica e/ou dosagem inapropriada dos medicamentos. Destacamos que são poucos os ensaios obrigatórios para identificação e controle desse fenômeno em medicamentos, o que pode acarretar grande problema de saúde pública. Unitermos:Polimorfismo. Medicamentos/controle de qualidade. Medicamentos/solubilidade. Medicamentos/biodisponibilidade.

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“…Furosemide is a loop-diuretic and is mainly used for oral treatment of hypertension and oedema (Matsuda et al 1990). The employment of an amorphous sodium salt of furosemide (ASSF) has been previously shown to significantly improve aqueous solubility and dissolution rate in comparison to furosemide in a crystalline acid form (Nielsen et al 2013a).…”

Section: Introductionmentioning

confidence: 99%