Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Furosemide

Granero, Gladys E.; Longhi, Marcela R.; Mora, María Julia; Junginger, Hans E.; Midha, K. K.; Shah, Vinod P.; Stavchansky, Salomon A; Dressman, Jennifer B.; Barends, D. M.

doi:10.1002/jps.22030

Cited by 119 publications

(106 citation statements)

References 66 publications

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“…For those drugs, accounting for the GI physiological factors affecting the solubility, dissolution and precipitation along the GI tract is absolutely necessary, especially when it comes to the prediction and understanding of their regional intestinal absorption (4,25,(83)(84)(85). However, for our simulations, that assumption seemed reasonable as the majority of the drugs listed in Table II can be classified as highly soluble (BCS classes 1 and 3), with the exception of furosemide, which is poorly soluble weak acid (pKa=3.9), yet its solubility is expected to be high at the intestinal pH range (6-7.4) (85,86).…”

Section: Discussionmentioning

confidence: 87%

Translating Human Effective Jejunal Intestinal Permeability to Surface-Dependent Intrinsic Permeability: a Pragmatic Method for a More Mechanistic Prediction of Regional Oral Drug Absorption

Olivares‐Morales

Lennernäs

Aarons

et al. 2015

AAPS J

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Abstract. Regional intestinal effective permeability (P eff ) values are key for the understanding of drug absorption along the whole length of the human gastrointestinal (GI) tract. The distal regions of the GI tract (i.e. ileum, ascending-transverse colon) represent the main sites for GI absorption when there is incomplete absorption in the upper GI tract, e.g. for modified release formulations. In this work, a new and pragmatic method for the estimation of (passive) intestinal permeability in the different intestinal regions is being proposed, by translating the observed differences in the available mucosal surface area along the human GI tract into corrections of the historical determined jejunal P eff values. These new intestinal P eff values or Bintrinsic^P eff (P eff,int ) were subsequently employed for the prediction of the ileal absorption clearance (CL abs,ileum ) for a set of structurally diverse compounds. Additionally, the method was combined with a semimechanistic absorption PBPK model for the prediction of the fraction absorbed (f abs ). The results showed that P eff,int can successfully be employed for the prediction of the ileal CL abs and the f abs . P eff,int also showed to be a robust predictor of the f abs when the colonic absorption was allowed in the PBPK model, reducing the overprediction of f abs observed for lowly permeable compounds when using the historical P eff values. Due to its simplicity, this approach provides a useful alternative for the bottom-up prediction of GI drug absorption, especially when the distal GI tract plays a crucial role for a drug's GI absorption.KEY WORDS: intestinal permeability; oral drug absorption; physiologically based pharmacokinetic modelling.

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Section: Discussionmentioning

confidence: 87%

Translating Human Effective Jejunal Intestinal Permeability to Surface-Dependent Intrinsic Permeability: a Pragmatic Method for a More Mechanistic Prediction of Regional Oral Drug Absorption

Olivares‐Morales

Lennernäs

Aarons

et al. 2015

AAPS J

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“…Lasix name derived from lasts six (hours) referring to its duration of action [5]. The solubility of furosemide is 0.01825 mg/ ml at room temperature and the solubility increases from 0.18 mg/ml at pH 2.3 to 13.36 mg/ml at pH10 [6].…”

Section: Introductionmentioning

confidence: 99%

Spectrofluorometric determination of furosemide in some pharmaceutical product using acriflavine as a reagent

Qader

Fakhre²

2017

AIP Conference Proceedings

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“…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%

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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Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Furosemide

Cited by 119 publications

References 66 publications

Translating Human Effective Jejunal Intestinal Permeability to Surface-Dependent Intrinsic Permeability: a Pragmatic Method for a More Mechanistic Prediction of Regional Oral Drug Absorption

Translating Human Effective Jejunal Intestinal Permeability to Surface-Dependent Intrinsic Permeability: a Pragmatic Method for a More Mechanistic Prediction of Regional Oral Drug Absorption

Spectrofluorometric determination of furosemide in some pharmaceutical product using acriflavine as a reagent

Stabilisation of amorphous furosemide increases the oral drug bioavailability in rats

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