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Microparticulate systems for the oral administration of biologically active substances

A technology for biologically active substances and microparticles, which is applied in the field of microparticle systems for oral administration of biologically active substances, and can solve problems such as low bioavailability

Inactive Publication Date: 2009-02-11
UNIV DELGI STUDI DI MILANO +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Said factors lead to partial or total degradation of the nutraceuticals added to the feed, resulting in low bioavailability of the substance once administered to the animal

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Preparation of Microparticle System Containing 6% α-Tocopherol

[0073] Emulsion A: Equal amounts of poloxamer (0.4% w / v BSAF, Ludwigshafen, Germany) and sodium lauryl sulfate (0.4% w / v Sigma-Aldrich, Milan, Italy) were dissolved in distilled water at room temperature middle. Alpha-tocopherol (1.6% w / v, Sigma-Aldrich, Milan, Italy) was added to the resulting solution under constant stirring to provide a stable and homogeneous emulsion.

[0074] Solution B: A 2% aqueous solution of low viscosity sodium alginate (250 cps, 2% solution, 25° C.) (Sigma-Aldrich, Milan, Italy) was prepared at room temperature.

[0075] Solution C: polymethacrylate (Eudragit , , Pharma, GmbH, Darmstadt, Germany) in a 20% w / v solution in phosphate buffer at pH 7.5.

[0076] Solution C was added to solution B at a volume ratio of 1:2 under continuous stirring, and then added to emulsion A at a volume ratio of 3:1 under continuous stirring.

[0077] The percentage composition of the obtained ...

Embodiment 2

[0088] Preparation of Microparticle System Containing 22% α-Tocopherol

[0089] Emulsion A:

[0090] Poloxamer 407 (2% w / v BSAF, Ludwigshafen, Germany) and sodium lauryl sulfate (2% w / v Sigma-Aldrich, Milan, Italy) were dissolved at room temperature under constant magnetic stirring at 100 rpm in distilled water. [alpha]-Tocopherol (8% w / v, Sigma-Aldrich, Milan, Italy) was added to the solution with turbine stirring (Ultra Turrax) for 15 minutes: a stable emulsion was obtained.

[0091] Solution B:

[0092] Low viscosity sodium alginate (250 cp, 2% solution, 25° C.) was prepared at a concentration of 2% w / v under constant magnetic stirring at 100 rpm at room temperature (alginic acid, sodium salt, low viscosity, Sigma-Aldrich, Milan, Italy) in water solution.

[0093] Solution C:

[0094] Polymethacrylate (Eudragit Pharma, GmbH, Darmstadt, Germany) 20% w / v solution in phosphate buffer pH 7.5.

[0095] Solution C was added to solution B at a volume ratio of 1:2 under c...

Embodiment 3

[0109] Preparation of microparticle system containing 6% rutin

[0110] Suspension A:

[0111] Poloxamer 407 (0.4% w / v BSAF, Ludwigshafen, Germany) and sodium lauryl sulfate (0.4% w / v Sigma-Aldrich, Milan, Italy) were dissolved at room temperature under constant magnetic stirring at 100 rpm in distilled water. Rutin (1.6% w / v, Sigma-Aldrich, Milan, Italy) was added to the solution with turbine stirring (Ultra Turrax) for 15 minutes: a stable suspension was obtained.

[0112] Solution B:

[0113] Low viscosity sodium alginate (250 cp, 2% solution, 25° C.) was prepared at a concentration of 2% w / v under constant magnetic stirring at 100 rpm at room temperature (alginic acid, sodium salt, low viscosity, Sigma-Aldrich, Milan, Italy) in water solution.

[0114] Solution C:

[0115] Polymethacrylate (Eudragit Pharma, GmbH, Darmstadt, Germany) 20% w / v solution in phosphate buffer pH 7.5.

[0116] Add solution C to solution B at a volume ratio of 1:2 under constant magnetic ...

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Abstract

The present invention relates to gastroresistant and enterosoluble microparticulate systems for the encapsulation of biologically active substances selected from: flavonoids, vitamins, antioxidants, immunostimulants, starchy and non-starchy polysaccharides, probiotics, prebiotics, intestinal trophism regulators, oligoelements, enzymes and bioactive peptides. Such microparticulate systems allow the administration of the aforementioned nutraceutic substances to animals such as porcines, bovines, caprines, ovines, equids, canids, felines, camelids, lagomorphs, rodents, fowl, and other mammals, including humans, fish and crustaceans, increasing the bioavailability.

Description

technical field [0001] The present invention relates to microparticle systems for oral administration of biologically active substances such as nutraceuticals and their corresponding preparation methods. Background technique [0002] "Functional food" is defined as a food or its ingredients that have a positive effect on one or more specific bodily functions, which go beyond a purely nutritional effect, leading to an improvement in the state of health or well-being and / or prophylaxis and treatment disease. Products with defined chemical structures present in functional foods as natural ingredients are defined as "nutraceuticals". [0003] Functional foods or nutraceuticals (including foods when they are concentrated) have potential health benefits if they are taken in effective doses and made bioavailable to produce their biological activity . [0004] The use of nutraceuticals and functional foods is already common in the population, but due to the effective reduction of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16
CPCA61K9/1652A23K1/146A23K1/009A61K9/1635A23K1/18A23K1/1643A23K1/1603A61K9/1617A23K1/1758A23K1/1631A23K10/18A23K10/37A23K20/147A23K20/163A23K20/174A23K20/30A23K50/00Y02P60/87
Inventor 丹尼尔·维戈马西莫·福斯蒂妮萨拉·斯科卡埃尔奥诺拉·穆纳里玛丽亚·路易莎·托雷厄鲍多·科特弗朗西斯科·德斯蒙里塔·帕特齐亚·阿昆诺玛丽亚·罗萨里亚·劳罗
Owner UNIV DELGI STUDI DI MILANO
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