Update on Fenofibrate

Guay, David R.P.

doi:10.1111/j.1527-3466.2002.tb00098.x

Cited by 45 publications

(20 citation statements)

References 68 publications

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“…32 Fenofibrate belongs to a Biopharmaceutics Classification System (BCS) class II drug (low solubility and high permeability), and its poor aqueous solubility limits the oral absorption of fenofibrate. 33,34 Therefore, in this study, ALC formulation was developed to improve the drug release profiles of fenofibrate. Single-factor analysis was used to optimize the formulation variables for the preparation of ALC formulation based on drug release profiles.…”

Section: Optimization Of Formulation Variablesmentioning

confidence: 99%

Aminoclay–lipid hybrid composite as a novel drug carrier of fenofibrate for the enhancement of drug release and oral absorption

Yang

Shao

Han

2016

IJN

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This study aimed to prepare the aminoclay–lipid hybrid composite to enhance the drug release and improve the oral bioavailability of poorly water-soluble fenofibrate. Antisolvent precipitation coupled with an immediate freeze-drying method was adopted to incorporate fenofibrate into aminoclay–lipid hybrid composite (ALC). The optimal composition of the ALC formulation was determined as the ratios of aminoclay to krill oil of 3:1 (w/w), krill oil to fenofibrate of 2:1 (w/w), and antisolvent to solvent of 6:4 (v/v). The morphological characteristics of ALC formulation were determined using scanning electron microscopy, differential scanning calorimetry, and X-ray powder diffraction, which indicated microcrystalline state of fenofibrate in ALC formulation. The ALC formulation achieved almost complete dissolution within 30 minutes, whereas the untreated powder and physical mixture exhibited less than 15% drug release. Furthermore, ALC formulation effectively increased the peak plasma concentration ( C max ) and area under the curve (AUC) of fenofibric acid (an active metabolite) in rats by approximately 13- and seven-fold, respectively. Furthermore, ALC formulation exhibited much lower moisture sorption behavior than the lyophilized formulation using sucrose as a cryoprotectant. Taken together, the present findings suggest that ALC formulation is promising for improving the oral absorption of poorly soluble fenofibrate.

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Section: Optimization Of Formulation Variablesmentioning

confidence: 99%

Aminoclay–lipid hybrid composite as a novel drug carrier of fenofibrate for the enhancement of drug release and oral absorption

Yang

Shao

Han

2016

IJN

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“…Since fenofibrate was first made commercially available, its main drawback has been the low bioavailability of the active metabolite, fenofibric acid, when the prodrug is taken orally on an empty stomach 8,[12][13][14][15][16][17][18] . Fenofibrate is virtually insoluble in water and is highly lipophilic, hence it is poorly absorbed when taken orally, especially under fasting conditions 2,9 .…”

Section: Description Of the Studymentioning

confidence: 99%

Untitled

2013

IJPSR

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Bioequivalence studies should be conducted for two products marketed by different licensees, containing same active ingredient(s), must be shown to be therapeutically equivalent to one another order to be considered interchangeable. The bioequivalence of two formulations of the same drug can be determined based on the absence of significant differences in primary pharmacokinetic properties of bioavailability, such as pharmacokinetic parameters like C max , T max , AUC 0-t, and AUC 0-∞ . The pharmacokinetic parameters derived from the plasma concentration-time curve are subjected to ANOVA. So we need to check ANOVAs for all pharmacokinetic parameters. Instead of that we can use multivariate analysis of variance (MANOVA) as it contains ANOVA results and further give more information regarding significance. From the results we can see that we get the same values like ANOVA and additionally we get 4 different tests for significance. Wilk's Lambda shows that 6.9%, 14.1% and 20% of the variance of the dependent variable (C max , T max , AUC 0-t, and AUC 0-∞ ) is accounted for by the differences between drugs, phase and interaction respectively. Pillai's Trace, Hotelling's Trace and Roy's largest root says that the data lead to statistical insignificance. So from these results we can suggest MANOVA instead of ANOVA in bioequivalence and control the increase risk of Type I error.

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“…It has a lipid-water distribution coefficient of 5.24 and aqueous solubility of less than 0.5 mg/liter with half life of 20 hours. Due to its virtual aqueous insolubility it is poorly absorbed from digestive tract leading to consequences of incomplete, irregular oral bioavailability [4]. The therapeutic dose required to be administered must thus be increased to obviate the disadvantage.…”

Section: Introductionmentioning

confidence: 99%

Enhancement of Bioavailability of Fenofibrate with Alpha Tocopherol and Phospholipids as Solubilizers

Indira¹

2012

JBB

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The purpose of this study was to investigate the effect of different solubilizers namely alpha tocopherol, soy phosphatidylcholine 70, Phospholipon 80H, and Phospholipon 90H on the bioavailability of sustained release fenofibrate pellets using fluid bed coating by applying Taguchi design to optimize the type and concentration of solubilizer at four levels namely 0.5%, 1%, 1.5%, and 2%. The pellets were prepared by loading the fenofibrate blended with other excipients onto the core sugar pellets with the aid of the binder solution. Taguchi experimental runs with alpha tocopherol 1% and Phospholipon 90H 2% (test) showed significant differences in in vitro dissolution behavior of drug compared to the pure drug. The pharmacokinetics of pure drug and test was evaluated in healthy male Wistar rats and found that t 1/2 was reduced significantly (4.36 and 4.02 hours) while AUC 0-t (32.14 ± 6.38 μg h/ml, 36.94 ± 6.2 μg h/ml), C max (8.7 ± 2.31 μg/ml, 9.8 ± 2.2 μg/ml) were improved markedly compared to the pure drug with t 1/2 (7.339314 ± 3.1 hours), AUC 0-t (11.89 ± 8.13 μg h/ml), and C max (5.137 ± 3.37 μg/ml). The extent of the mean plasma exposure of fenofibrate was 2.7 and 3.1 fold higher in animals treated with test. The ANOVA results revealed that type and concentration of solubilizer are crucial for enhancement of in vitro dissolution profile. Hence use of solubilizers may be the promising way to improve the oral bioavailability of fenofibrate. Enhancement of Bioavailability of MethodsDrug loading: Drug was loaded onto sugar spheres using fluidized bed processor . The sugar spheres were loaded into the fluidized bed processor and warmed for about 10 -15 minutes. Binder solution was prepared by dissolving Povidone K30 and sugar in purified water under constant stirring. Unmicronized fenofibrate which was pre blended and pulverized (0.5 mm screen pulverizer) with other excipients was incorporated intermittently into the solution under constant stirring. The obtained solution was loaded onto the circulating sugar spheres (800 μm). The wet spheres were dried simultaneously during the process of circulation in wurster chamber. The process was continued till the complete solution was consumed. The various processing variables namely inlet air temperature (40-45°C), outlet air temperature (30-33°C), product temperature (36-40°C), chamber humidity (58-60%), air flow (85 m 3 /hr), compressed air pressure (1.5-3.0 kg/cm 2 )The peristaltic pump rpm (10-35) and spray rate (2 ml/min) were optimized in the preliminary trials.Design of experiment to optimize drug loaded fenofibrate pellets: Taguchi L16 design of experiment was used to study the effect of two variables namely, type of solubilizer and concentration of solubilizer at four different levels as given in Table 1 and Table 2. All the experimental runs were analyzed using Minitab statistical software package (version 15). Characterization methodsInfrared Spectroscopy analysis of drug and excipients: FT-IR spectra were obtained using FT-IR spectrometer (Model Nic...

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Update on Fenofibrate

Cited by 45 publications

References 68 publications

Aminoclay–lipid hybrid composite as a novel drug carrier of fenofibrate for the enhancement of drug release and oral absorption

Aminoclay–lipid hybrid composite as a novel drug carrier of fenofibrate for the enhancement of drug release and oral absorption

Untitled

Enhancement of Bioavailability of Fenofibrate with Alpha Tocopherol and Phospholipids as Solubilizers

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Update on Fenofibrate

Cited by 45 publications

References 68 publications

Aminoclay&ndash;lipid hybrid composite as a novel drug carrier of fenofibrate for the enhancement of drug release and oral absorption

Aminoclay&ndash;lipid hybrid composite as a novel drug carrier of fenofibrate for the enhancement of drug release and oral absorption

Untitled

Enhancement of Bioavailability of Fenofibrate with Alpha Tocopherol and Phospholipids as Solubilizers

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Product

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Aminoclay–lipid hybrid composite as a novel drug carrier of fenofibrate for the enhancement of drug release and oral absorption

Aminoclay–lipid hybrid composite as a novel drug carrier of fenofibrate for the enhancement of drug release and oral absorption