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Formulation and Solid State Characterization of Nicotinamide-based Co-crystals of Fenofibrate.

Shewale S, Shete AS, Doijad RC, Kadam SS, Patil VA, Yadav AV - Indian J Pharm Sci (2015 May-Jun)

Bottom Line: Fenofibrate and nicotinamide as a coformer in 1:1 molar ratio were used to formulate molecular complexes by kneading, solution crystallization, antisolvent addition and solvent drop grinding methods.In vitro dissolution study showed that the formation of co-crystals improves the dissolution rate of fenofibrate.Nicotinamide forms the co-crystals with fenofibrate, theoretically and practically.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Satara College of Pharmacy, Degaon, Satara-415 004, India.

ABSTRACT
The present investigation deals with formulation of nicotinamide-based co-crystals of fenofibrate by different methods and solid-state characterization of the prepared co-crystals. Fenofibrate and nicotinamide as a coformer in 1:1 molar ratio were used to formulate molecular complexes by kneading, solution crystallization, antisolvent addition and solvent drop grinding methods. The prepared molecular complexes were characterized by powder X-ray diffractometry, differential scanning calorimetry, Fourier transform infrared spectroscopy, nuclear magnetic resonance spectroscopy and in vitro dissolution study. Considerable improvement in the dissolution rate of fenofibrate from optimized co-crystal formulation was due to an increased solubility that is attributed to the super saturation from the fine co-crystals is faster because of large specific surface area of small particles and prevention of phase transformation to pure fenofibrate. In vitro dissolution study showed that the formation of co-crystals improves the dissolution rate of fenofibrate. Nicotinamide forms the co-crystals with fenofibrate, theoretically and practically.

No MeSH data available.


Related in: MedlinePlus

PXRD patterns of FNO, nicotinamide and co-crystals after 6 months of storage.Powder X-Ray diffraction patterns after 6 months of storage under stability testing conditions from (a) fenofibrate (FNO) (b) physical mixture (c) antisolvent addition (d) kneading (e) solution crystallization method (f) solvent drop grinding and (g) nicotinamide.
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Figure 8: PXRD patterns of FNO, nicotinamide and co-crystals after 6 months of storage.Powder X-Ray diffraction patterns after 6 months of storage under stability testing conditions from (a) fenofibrate (FNO) (b) physical mixture (c) antisolvent addition (d) kneading (e) solution crystallization method (f) solvent drop grinding and (g) nicotinamide.

Mentions: The pure FNO and co-crystals prepared by various methods were charged on accelerated stability and monitored for appearance, drug content and in vitro dissolution study at 6 months. The obtained data were mentioned in Tables 3 and 4. Also it was subjected to FTIR and X-ray diffraction study. The stability study reveals no significant variation in appearance, drug content and in vitro dissolution study of pure FNO drug and prepared cocrystals up to six months. Also there were no significant changes in FTIR and XRD spectra of co-crystals after six months as shown in figs. 7 and 8, respectively[13].


Formulation and Solid State Characterization of Nicotinamide-based Co-crystals of Fenofibrate.

Shewale S, Shete AS, Doijad RC, Kadam SS, Patil VA, Yadav AV - Indian J Pharm Sci (2015 May-Jun)

PXRD patterns of FNO, nicotinamide and co-crystals after 6 months of storage.Powder X-Ray diffraction patterns after 6 months of storage under stability testing conditions from (a) fenofibrate (FNO) (b) physical mixture (c) antisolvent addition (d) kneading (e) solution crystallization method (f) solvent drop grinding and (g) nicotinamide.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4502148&req=5

Figure 8: PXRD patterns of FNO, nicotinamide and co-crystals after 6 months of storage.Powder X-Ray diffraction patterns after 6 months of storage under stability testing conditions from (a) fenofibrate (FNO) (b) physical mixture (c) antisolvent addition (d) kneading (e) solution crystallization method (f) solvent drop grinding and (g) nicotinamide.
Mentions: The pure FNO and co-crystals prepared by various methods were charged on accelerated stability and monitored for appearance, drug content and in vitro dissolution study at 6 months. The obtained data were mentioned in Tables 3 and 4. Also it was subjected to FTIR and X-ray diffraction study. The stability study reveals no significant variation in appearance, drug content and in vitro dissolution study of pure FNO drug and prepared cocrystals up to six months. Also there were no significant changes in FTIR and XRD spectra of co-crystals after six months as shown in figs. 7 and 8, respectively[13].

Bottom Line: Fenofibrate and nicotinamide as a coformer in 1:1 molar ratio were used to formulate molecular complexes by kneading, solution crystallization, antisolvent addition and solvent drop grinding methods.In vitro dissolution study showed that the formation of co-crystals improves the dissolution rate of fenofibrate.Nicotinamide forms the co-crystals with fenofibrate, theoretically and practically.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, Satara College of Pharmacy, Degaon, Satara-415 004, India.

ABSTRACT
The present investigation deals with formulation of nicotinamide-based co-crystals of fenofibrate by different methods and solid-state characterization of the prepared co-crystals. Fenofibrate and nicotinamide as a coformer in 1:1 molar ratio were used to formulate molecular complexes by kneading, solution crystallization, antisolvent addition and solvent drop grinding methods. The prepared molecular complexes were characterized by powder X-ray diffractometry, differential scanning calorimetry, Fourier transform infrared spectroscopy, nuclear magnetic resonance spectroscopy and in vitro dissolution study. Considerable improvement in the dissolution rate of fenofibrate from optimized co-crystal formulation was due to an increased solubility that is attributed to the super saturation from the fine co-crystals is faster because of large specific surface area of small particles and prevention of phase transformation to pure fenofibrate. In vitro dissolution study showed that the formation of co-crystals improves the dissolution rate of fenofibrate. Nicotinamide forms the co-crystals with fenofibrate, theoretically and practically.

No MeSH data available.


Related in: MedlinePlus