Physicochemical characterization and dissolution of norfloxacin/cyclodextrin inclusion compounds and PEG solid dispersions

Guyot, M.; Fawaz, F; Bildet, J.; Bonini, F.; Lagueny, Anne-Marie

doi:10.1016/0378-5173(95)00039-l

Cited by 101 publications

(60 citation statements)

References 22 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…It involves the use of polymers (e.g., Poloxamers (10), some grades of polyethylene glycols (11)) which melt at relatively low temperatures (60-90°C) (12). This technique along with hot melt extrusion allows mixing of drug and polymer at a molecular level without the use of organic solvents.…”

Section: Introductionmentioning

confidence: 99%

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407

2016

View full text Add to dashboard Cite

ABSTRACT. Aim of current research was to prepare ibuprofen-poloxamer 407 binary mixtures using fusion method and characterize them for their physicochemical and performance properties. Binary mixtures of ibuprofen and poloxamer were prepared in three different ratios (1:0.25, 1:0.5, and 1:0.75, respectively) using a water-jacketed high shear mixer. In vitro dissolution and saturation solubility studies were carried out for the drug, physical mixtures, and formulations for all ratios in de-ionized water, 0.1 N HCl (pH = 1.2), and phosphate buffer (pH = 7.2). Thermal and physical characterization of samples was done using modulated differential scanning calorimetry (mDSC), X-ray powder diffraction (XRD), and infrared spectroscopy (FTIR). Flow properties were evaluated using a powder rheometer. Maximum solubility enhancement was seen in acidic media for fused formulations where the ratio 1:0.75 had 18-fold increase. In vitro dissolution studies showed dissolution rate enhancement for physical mixtures and the formulations in all three media. The most pronounced effect was seen for formulation (1:0.75) in acidic media where the cumulative drug release was 58.27% while for drug, it was 3.67%. Model independent statistical methods and ANOVA based methods were used to check the significance of difference in the dissolution profiles. Thermograms from mDSC showed a characteristic peak for all formulations with T peak of around 45°C which suggested formation of a eutectic mixture. XRD data displayed that crystalline nature of ibuprofen was intact in the formulations. This work shows the effect of eutectic formation and micellar solubilization between ibuprofen and poloxamer at the given ratios on its solubility and dissolution rate enhancement.

show abstract

Section: Introductionmentioning

confidence: 99%

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407

2016

View full text Add to dashboard Cite

show abstract

“…Upon complexation, a significant shift in the characteristic peaks of the guest molecule, either to higher or lower frequency, was observed by some authors (20,21). Disappearance and broadening of the peaks of the guest also proves interaction between the drug and b-CD molecules (18).…”

Section: Irmentioning

confidence: 95%

“…The peak position (angle of diffraction) is an indication of crystal structure and peak heights are measures of sample crystallinity in a diffractogram (17). Formation of an amorphous state proves that the drug was dispersed in molecular state with CD (18). Various authors have reported the formation of a diffuse diffraction pattern, appearance of new peaks and disappearance of characteristic peaks of the guest as evidences for formation of inclusion complexes of the drug with CD (19).…”

Section: X-ray Diffractionmentioning

confidence: 99%

Physicochemical characterization and in vitro dissolution behaviour of celecoxib-β-cyclodextrin inclusion complexes

Sinha¹,

Anitha²,

Ghosh³

et al. 2007

Acta Pharmaceutica

View full text Add to dashboard Cite

Cyclodextrins are chemically and physically stable molecules formed by the enzymatic modification of starch (1). They are cyclomalto oligosaccharides composed of six, seven or eight a-D-glucopyranose units (a-, b-, g-CD, respectively). Their hollow structure enables them to host a variety of molecules (guests) partially or entirely in their hydrophobic caving. These inclusion complexes exist both in aqueous solution and in solid state. As a result of complexation of compounds by cyclodextrins, the apparent solubility of the molecule can be altered (2), stability of the compound in the presence of light and oxidizing conditions is increased (3) and volatility of compounds is decreased (4). Many scientists have studied the cyclodextrin complexes of various NSAIDs such as valdecoxib, diclofenac, piroxicam, ketoprofen, etc. and have showed their superiority over physical mixtures (5-8).Celecoxib, 4-[(5-(4-methyl phenyl)-3-trifluoro methyl)-1H-pyrazol-1-yl] benzene sulfonamide is a non steroidal anti-inflammatory drug that is a specific inhibitor of COX-2 enzyme. Celecoxib is widely used in the treatment of rheumatoid and osteoarthritis. According to the biopharmaceutical classification system, celecoxib belongs to class II type In this study, attempts were made to investigate the effects of b-cyclodextrin (b-CD) on the aqueous solubility and dissolution rate of celecoxib. Inclusion complexes were prepared by the kneading method and characterized by SEM, NMR, IR, DSC, and X-ray powder diffraction. Dissolution rate of the complexes was significantly greater than that of the corresponding physical mixtures and pure drug, indicating that the formation of inclusion complex increased the solubility of the poorly soluble drug celecoxib.

show abstract

“…It is therefore to improve the aqueous solubility of NFLX to enhance its extent of absorption (18)(19)(20). One study on inclusion complexes of NFLX investigated the influence of dispersion in PEG 6000 and complexation with hydroxypropyl-β-cyclodextrin (HP-β-CD) in systems obtained by freeze-drying (21). The effect of solid dispersions and CD complexation on the bioavailability of NFLX was reported-by Fawaz and coworkers (22).…”

Section: Introductionmentioning

confidence: 99%

Influence of β-cyclodextrin on the Properties of Norfloxacin Form A

et al. 2014

View full text Add to dashboard Cite

Abstract. Cyclodextrins are able to form host-guest complexes with hydrophobic molecules to result in the formation of inclusion complexes. The complex formation between norfloxacin form A and β-cyclodextrin was studied by exploring its structure affinity relationship in an aqueous solution and in the solid state. Kneading, freeze-drying, and physical mixture methods were employed to prepare solid complexes of norfloxacin and β-cyclodextrin. The solubility of norfloxacin significantly increased upon complexation with β-cyclodextrin as demonstrated by a solubility isotherm of the A L type along with the results of an intrinsic dissolution study. The complexes were also characterized in the solid stated by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier-transform infrared (FT-IR) spectroscopy, X-ray diffractometry, scanning electron microscopy (SEM), and solid-state nuclear magnetic resonance (ssNMR) spectrometry. The thermal analysis showed that the thermal stability of the drug is enhanced in the presence of β-cyclodextrin. Finally, the microbiological studies showed that the complexes have better potency when compared with pure drug.

show abstract

Physicochemical characterization and dissolution of norfloxacin/cyclodextrin inclusion compounds and PEG solid dispersions

Cited by 101 publications

References 22 publications

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407

Physicochemical characterization and in vitro dissolution behaviour of celecoxib-β-cyclodextrin inclusion complexes

Influence of β-cyclodextrin on the Properties of Norfloxacin Form A

Contact Info

Product

Resources

About