Self-emulsifying pellets prepared by wet granulation in high-shear mixer: influence of formulation variables and preliminary study on the in vitro absorption

Franceschinis, Erica; Voinovich, Dario; Grassi, Mario; Perissutti, Beatrice; Filipović-Grčić, Jelena; Martinac, Anita; Meriani-Merlo, Francesco

doi:10.1016/j.ijpharm.2004.07.046

Cited by 62 publications

(27 citation statements)

References 13 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Microcrystalline cellulose and lactose were added into liquid SMEDDS as solid carriers to produce self-emulsifying pellets by wet granulation. 12) Solid SMEDDS granules were prepared by spray-drying method with colloidal silica or dextran as solid carriers. 13) Polyvinyl alcohol or hydroxypropyl-β-cyclodextrantrin were used as carriers to form a solid SMEDDS microcapsule.…”

mentioning

confidence: 99%

Enhanced Oral Bioavailability of Pueraria Flavones by a Novel Solid Self-microemulsifying Drug Delivery System (SMEDDS) Dropping Pills

Guan

Zhang

Shi-lin

et al. 2016

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

To improve bioavailability of pueraria flavones (PF), a self-microemulsifying drug delivery system (SMEDDS) dropping pills composed of PF, Crodamol GTCC, Maisine 35-1, Cremophor RH 40, 1,2-propylene glycol and polyethylene glycol 6000 (PEG6000) was developed. Particle size, zeta potential, morphology and in vitro drug release were investigated, respectively. Pharmacokinetics, bioavailability of PF-SMEDDS dropping pills and commercial Yufengningxin dropping pills were also evaluated and compared in rats. Puerarin treated as the representative component of PF was analyzed. Dynamic light scattering showed the ability of PF-SMEDDS dropping pills to form a nanoemulsion droplet size in aqueous media. The type of media showed no significant effects on the release rate of PF. PF-SMEDDS dropping pills were able to improve the in vitro release rate of PF, and the in vitro release of these dropping pills was significantly faster than that of Yufengningxin dropping pills. There was a dramatic difference between the mean value of t 1/2, peak concentration (C max ), the area of concentration-time curve from 0 to 6 h (AUC 0-6 h ) of PF-SMEDDS dropping pills and that of commercial Yufengningxin dropping pills. A pharmacokinetic study showed that the bioavailability of PF was greatly enhanced by PF-SMEDDS dropping pills. The value of C max and relative bioavailability of PF-SMEDDS dropping pills were dramatically improved by an average of 1.69-and 2.36-fold compared with that of Yufengningxin dropping pills after gavage administration, respectively. It was concluded that bioavailability of PF was greatly improved and that PF-SMEDDS dropping pills might be an encouraging strategy to enhance the oral bioavailability of PF.Key words self-microemulsion; pueraria flavone (PF); dropping pill; release in vitro; relative bioavailability Radix Puerariae, the dried root of the leguminous plant pueraria lobata (WILLD.) OHWI, is a traditional Chinese herb medicine. Pueraria flavones (PF), major active ingredients extract from pueraria, are mixtures of several active ingredients that include puerarin, daidzin, daidzein, puerarin-7-xyloside and so on. Puerarin is the most abundant and major active ingredient. PF were found effective clinically to treat a variety of cardiovascular diseases, 1) including coronary heart disease, angina pectoris and hypertension. It was also effective in treating arrhythmia, migraines, sudden deafness and menopause, etc. 2,3)However, the effectiveness of PF as cardiovascular disease remedy is restricted by its poor solubility, short elimination half-life and rapid first-pass metabolism after oral administration. Only 15.91% of PF are absorbed from the gastrointestinal tract after oral administration.4) The commercial formulations of PF include dropping pills, tablets and injection. Only 3.95% of puerarin in Yufengningxin tablets is absorbed compared with puerarin injection. 5) Yufengningxin dropping pills are a formulation of PF obtained from pueraria lobata and are marketed in China. In order to improve the bioa...

show abstract

mentioning

confidence: 99%

Enhanced Oral Bioavailability of Pueraria Flavones by a Novel Solid Self-microemulsifying Drug Delivery System (SMEDDS) Dropping Pills

Guan

Zhang

Shi-lin

et al. 2016

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

show abstract

“…The authors suggest that the properties of surfactants need to be considered when selecting them for the formulation of SE pellets. Franceschinis et al (2005) developed a new method for preparing self-emulsifying pellets by wet granulation consisting of a binder solution containing an oil (mono and diglycerides), polysorbate 80 and nimesulide as a model drug. The oil surfactant mixture was added to water to obtain binder solution.…”

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.

View full text Add to dashboard Cite

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.

show abstract

“…This method of administration some shortcomings especially in the manufacturing process, leading to high production costs. 7 Moreover, these dosage forms may be inconvenient to use in addition to incompatibility problems with the soft gelatin shells.…”

Section: Introductionmentioning

confidence: 99%

Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication

Sallam¹,

Bosca²

2015

IJN

View full text Add to dashboard Cite

In this study, an optimized nanodispersible oral dosage form (containing a lactate ester) was developed for cilostazol (CZL). CZL is a phosphodiesterase inhibitor used for intermittent claudication. We aimed to improve the dissolution rate and absorption of CZL giving it a better chance of oral bioavailability, and to evaluate its stability on storage. Suitable compositions of nanoemulsion preconcentrate formulations were screened via solubility and compatibility tests. Response surface methodology and a desirability approach were applied to optimize preconcentrates containing minimum amount of surfactant mixture, maximum amount of lipid, and possessing the smallest globule size, with the highest emulsification and dissolution rates and minimum risk of drug precipitation. As part of the optimization process, the main effect, interaction effects and quadratic effects of amounts of lipid, and surfactant/co-surfactant ratio on % transmittance, globule size, emulsification time, drug precipitation, and drug release were investigated. The optimized formulation consisting of 28.9% butyl lactate, 28.9% Capryol ® , 27.82% Solubilisant Gamma ® 2429, and 14.18% Transcutol ® possessing a globule size of 60 nm was mixed with Aerosil ® 200. This gave uniform free flowing granules, which were characterized for surface and powder properties. The self-nanoemulsifying granules (SNEGs) filled into hard gelatin capsules showed two- and threefold increase in CZL released compared with conventional tablet and pure drug, respectively. The amount of drug permeated using non-everted sac technique from the SNEGs was twofold higher than that permeated from the tablet suspension. The shelf life was 526 days at 25°C. Our study illustrated that the developed SNEGs, with bioenhancing ingredients, held great potential as a superior alternative to traditional oral formulations of CZL.

show abstract

Self-emulsifying pellets prepared by wet granulation in high-shear mixer: influence of formulation variables and preliminary study on the in vitro absorption

Cited by 62 publications

References 13 publications

Enhanced Oral Bioavailability of Pueraria Flavones by a Novel Solid Self-microemulsifying Drug Delivery System (SMEDDS) Dropping Pills

Enhanced Oral Bioavailability of Pueraria Flavones by a Novel Solid Self-microemulsifying Drug Delivery System (SMEDDS) Dropping Pills

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

Optimization, ex vivo permeation, and stability study of lipid nanocarrier loaded gelatin capsules for treatment of intermittent claudication

Contact Info

Product

Resources

About