Preparation and characterization of a self-emulsifying pellet formulation

Abdalla, Ahmed M. E.; Mäder, Karsten

doi:10.1016/j.ejpb.2006.11.015

Cited by 94 publications

(50 citation statements)

References 17 publications

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“…The drum was rotated at 25 rpm for 4 min. Loss of pellet weight with respect to the initial value was then calculated as the percentage friability (21).…”

Section: Size and Friability Of The Thc-sefdds Pelletsmentioning

confidence: 99%

Controlled Release of Oral Tetrahydrocurcumin from a Novel Self-Emulsifying Floating Drug Delivery System (SEFDDS)

et al. 2010

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Abstract. The objectives of this study were to develop and evaluate a novel self-emulsifying floating drug delivery system (SEFDDS) that resulted in improved solubility, dissolution, and controlled release of the poorly water-soluble tetrahydrocurcumin (THC). The formulations of liquid self-emulsifying drug delivery system (SEDDS; mixtures of Labrasol, Cremophor EL, Capryol 90, Labrafac PG) were optimized by solubility assay and pseudo-ternary phase diagram analysis. The liquid SEDDS was mixed with adsorbent (silicon dioxide), glyceryl behenate, pregelatinized starch, sodium starch glycolate, and microcrystalline cellulose and transformed into pellets by the extrusion/spheronization technique. The resulting pellets with 22% liquid SEDDS had a uniform size and good self-emulsification property. The microemulsions in aqueous media of different self-emulsifying floating pellet formulations were in a particle size range of 25.9-32.5 nm. Use of different weight proportions of glyceryl behenate and sodium starch glycolate in pellet formulations had different effects on the floating abilities and in vitro drug release. The optimum formulation (F2) had a floating efficiency of 93% at 6 h and provided a controlled release of THC over an 8-h period. The release rate and extent of release of THC liquid SEDDS (80% within 2 h) and self-emulsifying floating pellet formulation (80% within 8 h) were significantly higher than that of unformulated THC (only 30% within 8 h). The pellet formulation was stable under intermediate and accelerated storage conditions for up to 6 months. Controlled release from this novel SEFDDS can be a useful alternative for the strategic development of oral solid lipid-based formulations.

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“…The drum was rotated at 25 rpm for 4 min. Loss of pellet weight with respect to the initial value was then calculated as the percentage friability (21).…”

Section: Size and Friability Of The Thc-sefdds Pelletsmentioning

confidence: 99%

Controlled Release of Oral Tetrahydrocurcumin from a Novel Self-Emulsifying Floating Drug Delivery System (SEFDDS)

et al. 2010

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“…The incorporation of the self-microemulsifying mixture into a solid dosage form is desirable, but challenging, because selfmicroemulsifying properties are harder to achieve with solid materials [7] . Therefore, it is necessary to determine whether or not the tablet that is composed of a self-microemulsifying mixture and solid materials can self-microemulsify when it contacts water or SGF.…”

Section: Self-microemulsifying Studymentioning

confidence: 99%

“…Furthermore, incompatibility problems with the capsule shell are common [7] . Recently, with the development of new materials and a novel preparation process, there is growing interest in the study of solid selfNovel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test microemulsifying drug delivery systems (S-SMEDDS) [5,[7][8][9][10][11][12][13][14] . Compared with the traditional SMEDDS, S-SMEDDS can increase stability, extend storage time, reduce gastrointestinal irritation, and improve patient compliance.…”

Section: Introductionmentioning

confidence: 99%

Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test

2011

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Aim: To develop a novel gastroretentive drug delivery system based on a self-microemulsifying (SME) lipid mixture for improving the oral absorption of the immunosuppressant tacrolimus. Methods: Liquid SME mixture, composed of Cremophor RH40 and monocaprylin glycerate, was blended with polyethylene oxide, chitosan, polyvinylpyrrolidone and mannitol, and then transformed into tablets via granulation, with ethanol as the wetting agent. The tablets were characterized in respect of swelling, bioadhesive and SME properties. In vitro dissolution was conducted using an HCl buffer at pH 1.2. Oral bioavailability of the tablets was examined in fasted beagle dogs. Results: The tablet could expand to 13.5 mm in diameter and 15 mm in thickness during the initial 20 min of contact with the HCl buffer at pH 1.2. The bioadhesive strength was as high as 0.98±0.06 N/cm 2 . The SME gastroretentive sustained-release tablets preserved the SME capability of the liquid SME formations under transmission electron microscope. The drug-release curve was fit to the zero-order release model, which was helpful in reducing fluctuations in blood concentration. Compared with the commercially available capsules of tacrolimus, the relative bioavailability of the SME gastroretentive sustained-release tablets was 553.4%±353.8%. Conclusion: SME gastroretentive sustained-release tablets can enhance the oral bioavailability of tacrolimus with poor solubility and a narrow absorption window.

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“…Plasma drug concentration was significantly higher when the drug was orally administered from self-emulsifying pellets and self-emulsifying solution when compared to aqueous suspension at the same dose. Abdalla and Mader (2007) prepared three selfemulsifying pellet formulations by melting cithrol GMS (mono and diglycerides) and solutol HS 15. To this molten blend, the drug (diazepam) and dry microcrystalline cellulose (MCC) were added to obtain a suitable mass for extrusion.…”

Section: Self-emulsifying Pellets (Se Pellets)mentioning

confidence: 99%

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

Wadhwa¹,

Nair²,

Kumria³

2011

Braz. J. Pharm. Sci.

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Self-emulsifying therapeutic system (SETs) provide an effective and intelligent solution to the various issues related to the formulation of hydrophobic drugs with limited solubility in gastrointestinal fluid. Although the potential utility of SETs is well known, only in recent years has a mechanistic understanding of the impact of these systems on drug disposition emerged. These in situ emulsion-forming systems have a high stability when incorporated in various dosage forms. SETs are being looked upon as systems which can overcome the problems associated with delivery of poorly water soluble drugs. An in-depth knowledge about lipids and surfactants that can contribute to these systems, criterion for their selection and the proportion in which they can be used, represent some crucial factors determining the in vivo performance of these systems. This article presents a comprehensive account of various types of self-emulsifying formulations with emphasis on their composition and examples of currently marketed preparations.Uniterms: Lipid based formulations. Self-emulsifying therapeutic system. Self-emulsification.O sistema terapêutico auto-emulsionante (SETs) fornece solução eficaz e inteligente para os vários problemas relativos à formulação de fármacos hidrofóbicos com solubilidade limitada no fluido gastrintestinal. Embora a utilidade potencial dos SETs seja bem conhecida, só recentemente se compreendeu, mecanisticamente,o impacto desses sistemas na disposição de fármacos. Estes sistemas de formação de emulsão in situ têm alta estabilidade, quando incorporados em várias formas de dosagem. Os SETs têm sido considerados como sistemas que podem resolver problemas associados à liberação de fármacos pouco solúveis em água. O conhecimento profundo dos lipídios e tensoativos que podem ser utilizados para estes sistemas e o critério para a sua seleção e proporção na qual eles são utilizados são alguns dos fatores cruciais que determinam o desempenho do sistema in vivo. Este artigo apresenta o relato abrangente de vários tipos de formulações auto-emulsificantes, com ênfase em sua composição e exemplos das preparações que são correntemente comercializadas.Unitermos: Formulações baseadas em lipídio. Sistema terapêutico auto-emulsificante. Autoemulsificação.

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Preparation and characterization of a self-emulsifying pellet formulation

Cited by 94 publications

References 17 publications

Controlled Release of Oral Tetrahydrocurcumin from a Novel Self-Emulsifying Floating Drug Delivery System (SEFDDS)

Controlled Release of Oral Tetrahydrocurcumin from a Novel Self-Emulsifying Floating Drug Delivery System (SEFDDS)

Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

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