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In vitro profiling of fenofibrate solid dispersion mediated tablet formulation to treat high blood cholesterol - 01/03/23

Profilage in vitro de la formulation de comprimés médiés par une dispersion solide de fénofibrate pour traiter l'hypercholestérolémie

Doi : 10.1016/j.pharma.2022.08.009 
U. Atneriya a, D. Kapoor b, J. Sainy a, R. Maheshwari c, 1,
a School of Pharmacy Devi Ahilya Vishwavidhylaya, 452020 Indore, India 
b Dr. Dayaram Patel Pharmacy College, SardarBaug, Station Road, 394601 Bardoli, Gujarat, India 
c School of Pharmacy and Technology Management, SVKM'S NMIMS, Green Pharma Industrial Park, TSIIC, Jadcherla, 509301 Hyderabad, India 

Corresponding author. School of Pharmacy and Technology Management, SVKM'S NMIMS, Green Industrial Park, TSIIC, Jadcherla, 509301 Hyderabad, India.School of Pharmacy and Technology Management, SVKM'S NMIMS, Green Industrial Park, TSIIC, JadcherlaHyderabad509301India

Graphical abstract




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Highlights

Fenofibrate (FNF), an anti-hyperlipidemic agent, suffers from poor water solubility.
Vitamin E TPGS) shown efficacy as molecular biomaterial to enhance bioavailability.
Fast dissolving tablets of FNF were prepared using Vit E TGPS mediated solid dispersion approach.
The dissolution rate of FNF from fast dissolving tablets developed by Vitamin E TPGS mediated solid dispersion was further tested.
The obtained data were kept into different in vitro kinetic models, including zero and first order, Higuchi and Hixon-Crowell model.
The investigation present an industrially applicable solution to develop novel fast dissolving tablets.

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Summary

Objective

Fenofibrate (FNF), an anti-hyperlipidemic agent, suffers from poor water solubility (0.000707mg/ml) and belongs to class II drug as per BCS, shows a slow dissolution rate. The current investigation aimed to fabricate a fast-dissolving tablet of FNF (not available in the commercial market) using solid dispersion technique employing Vitamin E-D-α-Tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) as molecular biomaterial to enhance dissolution rate and reduce the time required to reach the systemic circulation.

Materials and methods

Firstly, carrier material was selected based on the release study via preparing solid dispersion using the melting method, and prepared solid dispersion was characterized. Secondly, fast-dissolving tablets from solid dispersion were fabricated using the direct compression tool and characterized for X-ray diffraction (XRD) pattern, friability, hardness, content uniformity, weight variation and in vitro disintegration test.

Results

The X-ray diffraction study confirmed the successful formation of solid dispersion using vitamin E TPGS by analyzing the change in physical state. The fabricated solid dispersion exhibited higher drug content than a physical mixture of FNF. An excipient interference study was also performed in methanol and 0.75% w/v sodium lauryl sulphate. It revealed no significant alterations in the absorption peak of FNF as analyzed using UV spectroscopy at 287nm. In addition, water absorption ratio phase solubility and wetting time were also assessed. In -vitro release of FNF from developed tablets was found significantly higher (93.23%±3.11; p<0.001) as compared to prepared compressed tablet of pure FNF (12.21±2.34%). The dissolution rate was also determined, and data were then kept to various kinetic models such as zero-order chemical kinetic, first-order chemical kinetic, Hixon-Crowell and Higuchi chemical kinetic.

Conclusion

A complete and sequential in vitro and physicochemical characterization of developed formulation was carried out to set-up improved and effective treatment for high blood cholesterol.

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Résumé

Objectif

Le fénofibrate (FNF), un agent anti-hyperlipidémique, souffre d'une faible solubilité dans l'eau (0,000707 mg/ml) et appartient à la classe II des médicaments selon BCS, montre une vitesse de dissolution lente. L'enquête actuelle visait à fabriquer un comprimé de FNF à dissolution rapide (non disponible sur le marché commercial) en utilisant une technique de dispersion solide utilisant du succinate de polyéthylèneglycol 1000 de vitamine E-D-α-tocophéryl (vitamine E TPGS) comme biomatériau moléculaire pour améliorer le taux de dissolution et réduire le temps nécessaire pour atteindre la circulation systémique.

Matériels et méthodes

Tout d'abord, le matériau de support a été sélectionné sur la base de l'étude de libération via la préparation d'une dispersion solide à l'aide de la méthode de fusion, et la dispersion solide préparée a été caractérisée. Deuxièmement, des comprimés à dissolution rapide à partir d'une dispersion solide ont été fabriqués à l'aide de l'outil de compression directe et caractérisés pour le motif de diffraction des rayons X (XRD), la friabilité, la dureté, l'uniformité du contenu, la variation de poids et le test de désintégration in vitro.

Résultats

L'étude de diffraction des rayons X a confirmé la formation réussie d'une dispersion solide à l'aide de vitamine E TPGS en analysant le changement d'état physique. La dispersion solide fabriquée présentait une teneur en médicament plus élevée qu'un mélange physique de FNF. Une étude d'interférence des excipients a également été réalisée dans du méthanol et du laurylsulfate de sodium à 0,75 % p/v. Il n'a révélé aucune altération significative du pic d'absorption du FNF tel qu'analysé par spectroscopie UV à 287 nm. De plus, la solubilité de la phase du rapport d'absorption d'eau et le temps de mouillage ont également été évalués. La libération in vitro de FNF à partir de comprimés développés a été trouvée significativement plus élevée (93,23 % ± 3,11 ; p < 0,001) par rapport au comprimé compressé préparé de FNF pur (12,21 ± 2,34 %). Le taux de dissolution a également été déterminé, et les données ont ensuite été conservées dans divers modèles cinétiques tels que la cinétique chimique d'ordre zéro, la cinétique chimique de premier ordre, la cinétique chimique Hixon-Crowell et Higuchi.

Conclusion

Une caractérisation in vitro et physico-chimique complète et séquentielle de la formulation développée a été réalisée pour mettre en place un traitement amélioré et efficace de l'hypercholestérolémie.

Il testo completo di questo articolo è disponibile in PDF.

Keywords : Solid dispersion, X-ray diffraction, Dissolution test, Vitamin E TPGS, Fast Dissolving Tablets, Bioavailability, Drug kinetics


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Vol 81 - N° 2

P. 284-299 - Marzo 2023 Ritorno al numero
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