Bioavailability of norfloxacin from PEG 6000 solid dispersion and cyclodextrin inclusion complexes in rabbits

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

doi:10.1016/0378-5173(95)04387-x

Cited by 30 publications

(11 citation statements)

References 8 publications

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“…β-CD exhibits a complex spectrum with multiple sharp resonances for each type of carbon atom, typical of a crystalline system. The 13 C CP-MAS spectrum of NFLX matches well with that previously reported (22).…”

Section: Solid-state Nmr (Ssnmr)supporting

confidence: 78%

“…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). Dua and coworkers investigated the possibility of improving the solubility and dissolution rate of NFLX in the presence of solubilizing agents such as ascorbic acid and citric acid incorporated into β-CD (23).…”

Section: Introductionmentioning

confidence: 99%

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

et al. 2014

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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.

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Section: Solid-state Nmr (Ssnmr)supporting

confidence: 78%

Section: Introductionmentioning

confidence: 99%

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

et al. 2014

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“…This pattern was similar to AUC, except for the unusual behavior of DHA-PVPK25. The t 1/2 of the prepared solid dispersions were substantially lower than plain DHA and was statistically significantly different from the DHA solution (Table III), dissimilar to norfloxacin (Fawaz et al, 1996). The pharmacokinetic parameters of DHA-HPβCD complexes were comparable to DHA-PVPK30 solid dispersions, but the advantage of the former complex is that it was more stable (up to 1 year) than the latter complex at room temperature (data not shown).…”

Section: Pharmacokinetic Studiesmentioning

confidence: 66%

“…Studies on PVPassociated solid dispersions of pharmaceuticals have revealed inhibited crystallization and enhanced solubility; examples include bicalutamide (Andrews et al, 2010), AM (Ansari et al, 2010), piroxicam (Wu et al, 2009), DHA (Ansari and Sunderland, 2008), lamotrigine (Shinde et al, 2008), valdecoxib (Ambike et al, 2004), carbamazepine (Sethia andSquillante, 2004), artemisinin (Nijlen et al, 2003), camptothecin (Kang et al, 2002). Similar studies reported increased bioavailability of ketoconazole (Heo et al, 2005), artemisinin (Wong and Yuen, 2001), norfloxacin (Fawaz et al, 1996), lonidamine (Palmieri et al, 2002) and nifedipine (Emara et al, 2002).…”

Section: Introductionmentioning

confidence: 83%

Improving the solubility and bioavailability of dihydroartemisinin by solid dispersions and inclusion complexes

et al. 2011

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Dihydroartemisinin (DHA) is a poorly water-soluble drug that displays low bioavailability after oral administration. Attempts have been made to improve the solubility of DHA. Yet, no information is available concerning improved bioavailability. This study aimed to improve the water solubility of DHA by two systems: solid dispersions with polyvinylpyrrolidone (PVPK30, PVPK25, PVPK15) and inclusion complexes with hydroxypropyl-β-cyclodextrin (HPβCD), as well as improving the bioavailability of both systems. The phase transition of DHA with hydrophilic polymers was evaluated by X-ray diffraction (XRD) and differential scanning calorimetery (DSC). DHA became amorphous in DHA-HPβCD complexes and showed more amorphous behavior in XRD analyses with rise in molecular weight of PVP. Melting onset temperature of DHA decreased, while DSC thermograms revealed the peak area and enhanced enthalpy change (DH) in solid dispersions as well as inclusion complexes. DHA solubility was enhanced 84-fold in DHA-HPβCD complexes and 50-times in DHA-PVPK30. The improved solubility using the four polymers was in the following order: HPβCD > PVPK30 > PVPK25 > PVPK15. Values of area under curve (AUC) and half life (t(1/2)) of DHA-PVPK30 were highest followed by DHA-HPβCD, DHA-PVPK15 and DHA-PVPK25. V(d)/f of DHA-PVPK30 was 7-fold. DHA-HPβCD, DHA-PVPK15 and DHA-PVPK25 showed significantly different pharmacokinetic parameters compared with DHA solutions. The 95% confidence interval was meaningful in AUC and t(1/2). Pharmacokinetic parameters revealed that all four-test preparations were significantly more bioavailable than DHA alone.

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“…Therefore, technologies aimed at improving their rate and extent of dissolution of poorly water-soluble drugs are continuously being developed [1]. Different methods to improve the water-solubility have been described in literature, such as the inclusion of drugs in cyclodextrins [2][3][4][5], solid dispersions [6], self-emulsifying drug delivery systems [7], nanocrystals [8,9] and coacervation.…”

Section: Introductionmentioning

confidence: 99%

Formulation of poorly water-soluble drugs via coacervation – A pilot study using febantel

Jaeghere

Geest

Bocxlaer

et al. 2013

European Journal of Pharmaceutics and Biopharmaceutics

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In this study febantel was dissolved under increased temperature in a non-ionic surfactant Lutrol L44®, and subsequently mixed into an aqueous maltodextrin solution. After 8h under static conditions, coacervation or phase separation took place. 1 H-NMR spectra and HPLC analysis showed that the upper phase contained mainly all febantel, while no febantel was detected in the lower phase. Fluorescent microscopy showed that maltodextrin is distributed in the lower phase. Coacervation proved to be a promising formulation technology for certain poorly water-soluble drugs, such as febantel. The coacervate phase showed an increase in in vitro dissolution kinetics, compared to Rintal® granules. These results were confirmed in an in vivo study performed on dogs. Febantel and fenbendazole showed a significant increase in plasma concentration compared to Rintal® granules. Further studies have to be performed to transform coacervates into a solid dosage form and to prove broad applicability to other poorly soluble drugs.

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Bioavailability of norfloxacin from PEG 6000 solid dispersion and cyclodextrin inclusion complexes in rabbits

Cited by 30 publications

References 8 publications

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

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

Improving the solubility and bioavailability of dihydroartemisinin by solid dispersions and inclusion complexes

Formulation of poorly water-soluble drugs via coacervation – A pilot study using febantel

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