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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

Saturation solubility data of FNO and FNO-nicotinamide cocrystals.Saturation solubility data performed in 0.5 % sodium lauryl sulphate. FNO is fenofibrate; fenofibrate and nicotinamide co-crystals were prepared using PM- physical mixture, SC- solvent co-crystallization, SD- solvent drop method, KN- kneading and AN- antisolvent addition method.
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Figure 1: Saturation solubility data of FNO and FNO-nicotinamide cocrystals.Saturation solubility data performed in 0.5 % sodium lauryl sulphate. FNO is fenofibrate; fenofibrate and nicotinamide co-crystals were prepared using PM- physical mixture, SC- solvent co-crystallization, SD- solvent drop method, KN- kneading and AN- antisolvent addition method.

Mentions: Table 2, summarized experimentally determined solubility of FNO in 0.5% SLS solution. The prepared co-crystals with nicotinamide have shown significantly higher solubility compared to their physical mixture and FNO alone. It is to be expected that FNO would dissolve better in co-crystal form due to a reduction in the crystallinity of FNO and hydrogen bond formation between FNO and the coformer. The co-crystals prepared by antisolvent addition method demonstrated higher solubility than that of FNO and other cocrystals (fig. 1) because addition of an antisolvent which reduces the solute solubility in the resultant system, or changing the solute by chemical reaction producing another substance with much lower solubility[9].


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)

Saturation solubility data of FNO and FNO-nicotinamide cocrystals.Saturation solubility data performed in 0.5 % sodium lauryl sulphate. FNO is fenofibrate; fenofibrate and nicotinamide co-crystals were prepared using PM- physical mixture, SC- solvent co-crystallization, SD- solvent drop method, KN- kneading and AN- antisolvent addition method.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 1: Saturation solubility data of FNO and FNO-nicotinamide cocrystals.Saturation solubility data performed in 0.5 % sodium lauryl sulphate. FNO is fenofibrate; fenofibrate and nicotinamide co-crystals were prepared using PM- physical mixture, SC- solvent co-crystallization, SD- solvent drop method, KN- kneading and AN- antisolvent addition method.
Mentions: Table 2, summarized experimentally determined solubility of FNO in 0.5% SLS solution. The prepared co-crystals with nicotinamide have shown significantly higher solubility compared to their physical mixture and FNO alone. It is to be expected that FNO would dissolve better in co-crystal form due to a reduction in the crystallinity of FNO and hydrogen bond formation between FNO and the coformer. The co-crystals prepared by antisolvent addition method demonstrated higher solubility than that of FNO and other cocrystals (fig. 1) because addition of an antisolvent which reduces the solute solubility in the resultant system, or changing the solute by chemical reaction producing another substance with much lower solubility[9].

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