Novel Furosemide Cocrystals and Selection of High Solubility Drug Forms

Goud, N. Rajesh; Gangavaram, Swarupa; Suresh, Kuthuru; Pal, Sharmistha; Manjunatha, Sulur G.; Nambiar, Sudhir; Nangia, Ashwini

doi:10.1002/jps.22805

Cited by 148 publications

(150 citation statements)

References 54 publications

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“…for peptides, proteins and low permeable drugs. Furosemide is a loop diuretic and widely used orally for hypertension and oedema (Goud et al, 2011;Matsuda et al, 1990), and therefore a rapid absorption will often be beneficial for the patients, but in case of other drug candidates where a prolonged release may be required other polymers than Eudragit L100 can be utilised as coating agents. …”

Section: In Situ Closed-loop Rat Intestinal Perfusionmentioning

confidence: 99%

Polymeric microcontainers improve oral bioavailability of furosemide

Nielsen

Melero

Keller

et al. 2016

International Journal of Pharmaceutics

117

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Microcontainers with an inner diameter of 223 µm are fabricated using the polymer SU-8, and evaluated in vitro, in situ and in vivo for their application as an advanced oral drug delivery system for the poorly water soluble drug furosemide. An amorphous sodium salt of furosemide (ASSF) is filled into the microcontainers followed by applying a lid using Eudragit L100. It is possible to control the drug release in vitro, and in vitro absorption studies show that the microcontainers are not a hindrance for absorption of ASSF. In situ perfusion studies in rats are performed with ASSF-filled microcontainers coated with Eudragit and compared to a furosemide solution. The absorption rate constant of ASSF confined in microcontainers is found to be significantly different from the solution, and by light microscopy, it is observed that the microcontainers are engulfed by the intestinal mucus. An oral bioavailability study in rats is performed with ASSF confined in microcontainers coated with Eudragit and a control group with ASSF in Eudragit-coated capsules. A relative bioavailability of 220% for the ASSF in microcontainers compared to ASSF in capsules is found. These studies indicate that the microcontainers could serve as a promising oral drug delivery system.

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Section: In Situ Closed-loop Rat Intestinal Perfusionmentioning

confidence: 99%

Polymeric microcontainers improve oral bioavailability of furosemide

Nielsen

Melero

Keller

et al. 2016

International Journal of Pharmaceutics

117

View full text Add to dashboard Cite

show abstract

“…The increasing interest in PCCs is due to the fact that they display intermolecular motifs and crystal structures different from the pure API components and consequently can exhibit diverse specific physical properties, e.g. API dissolution rate and solubility (Nehm et al, 2006;Good & Rodríguez-Hornedo, 2009;Goud et al, 2012), API pharmacokinetics (Cheney et al, 2010;Shan et al, 2014;Suresh et al, 2014Suresh et al, , 2016, bioavailability (Bak et al, 2008;Jung et al, 2010) and permeability (Ferretti et al, 2015;Dalpiaz et al, 2017), efficiency and safety of the API native solid form, available in pharmaceutical formulations, and processability and stability of the sole crystalline form of PCC with a unique structure (Newman & Wenslow, 2016;Battini et al, 2014;Trask, 2007) …”

Section: Introductionmentioning

confidence: 99%

New pharmaceutical salts containing pyridoxine

2017

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Two mixed crystals were obtained by crystallizing the active pharmaceutical ingredient pyridoxine [systematic name: 4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol, PN] with (E)-3-(4-hydroxy-3-methoxyphenyl)prop-2-enoic acid (ferulic acid) and 4-hydroxy-3,5-dimethoxybenzoic acid (syringic acid). PN and the coformers crystallize in the form of pharmaceutical salts in a 1:1 stoichiometric ratio, namely 3-hydroxy-4,5-bis(hydroxymethyl)-2-methylpyridin-1-ium (E)-3-(4-hydroxy-3-methoxyphenyl)prop-2-enoate, C 8 H 12 NO 3 + ÁC 9 H 9 O 5 À , and 3-hydroxy-4,5-bis(hydroxymethyl)-2-methylpyridin-1-ium 4-hydroxy-3,5-dimethoxybenzoate monohydrate, C 8 H 12 NO 3 + ÁC 10 H 11 O 5 À ÁH 2 O, the proton exchange between PN and the acidic partner being supported by the differences of the pK a values of the two components and by the C-O bond lengths of the carboxylate groups. Besides complex hydrogen-bonding networks, -interactions between aromatic moieties have been found to be important for the packing architecture in both crystals. Hirshfeld surface analysis was used to explore the intermolecular interactions in detail and compare them with the interactions found in similar pyridoxine/carboxylic acid salts.

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“…application of the fundamental concepts presented in this paper explains to examine the ability of hansen solubility parameter to predict the formation of cocrystals systems and pharmaceutical properties of cocrystals, in particular solubility, dissolution, and stability (3). Several research reports of cocrystals show their ability to improve physicochemical including solubility, dissolution, stability, tabletability and pharmacokinetic characteristics especially bioavailability of active pharmaceutical ingredients (4)(5)(6)(7)(8). Cocrystal synthesis can work as green technique becoming avenue for pharmaceutical industry (9).…”

Section: Introductionmentioning

confidence: 99%