Physiologically active substance-containing granular composition and method of producing the same

A technology for physiologically active substances and compositions, which is applied to the field of granular compositions containing physiologically active substances and their preparation, can solve the problems of limited use, poor thermal stability, cumbersome drying steps, etc., and achieves improvement in low recovery rate and good operability. , good water solubility

Inactive Publication Date: 2009-09-16
KANEKA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method has the advantage of fewer steps, but its low recovery is a big problem
In addition, sometimes the powder obtained by the spray drying method has poor fluidity or is prone to static electricity, and it is difficult to use it directly at this time, and further granulation steps are necessary
[0005] In addition, the spray freezing method (spray cooler, Patent Document 3), which is one of the preparation methods of the oxidized coenzyme Q10 powder preparation, has the advantage of good recyclability compared with the spray drying method, but the following problems can be cited: The granulation steps and drying steps at extremely low temperature are cumbersome; excipient ingredients are limited to gelatin; poor thermal stability, etc.
Furthermore, the present situation is that in order to perform the spray freezing method or the spray drying method, specific expensive equipment is required, which is unreasonable from the viewpoint of cost.
[0006] So far, water-soluble powder of oxidized coenzyme Q10 and its production method have been developed, but most of its uses are limited, and most of them are used for tablets or food.

Method used

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  • Physiologically active substance-containing granular composition and method of producing the same
  • Physiologically active substance-containing granular composition and method of producing the same
  • Physiologically active substance-containing granular composition and method of producing the same

Examples

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preparation example Construction

[0121] In the preparation method of the present invention, the emulsified particle size of the oily component (A) containing physiologically active substances in the above-mentioned oil-in-water emulsion composition is preferably in the range of 0.01 to 50 μm, more preferably in the range of 0.01 to 20 μm, most preferably in the range of 0.01 ~10μm range. When the average particle diameter of the oily component (A) in an oil-in-water emulsion composition exceeds 50 micrometers, the oral absorbability of the obtained granular composition may fall. On the contrary, when the average particle size of the oily component (A) in the oil-in-water emulsion composition is less than 0.01 μm, it is often difficult to maintain the stability of the emulsion droplets during the preparation process. By controlling the particle size of the emulsified liquid droplets in this step, the domain particle size in the obtained granular composition can be controlled.

[0122] The emulsified particle ...

Embodiment 1

[0157] At 60°C, make 6g gum arabic ( Naturels; EFICACIA-M) was dissolved in 24 g of distilled water to obtain an aqueous solution of a water-soluble excipient. Separately, 4 g of oxidized coenzyme Q10 (manufactured by Kaneka Co., Ltd.; Kaneka Coenzyme Q10) was dissolved at 60°C in an oily component (A) which was added to a water-soluble vehicle solution at 60°C. It emulsified at 10000 rpm x 6 minutes, and obtained the oil-in-water type emulsion composition. The emulsified particle size of oxidized coenzyme Q10 in the oil-in-water emulsion composition is about 1 μm. 34g of the obtained oil-in-water emulsified composition was added to the oily component (B) preheated to 100°C while stirring to prepare an oil-in-water-in-oil (O / W / O) emulsion, the oily component ( B) Consists of 60 g of MCT (Acter M-2 manufactured by Riken Vitamin Co., Ltd.) and 12 g of surfactant (triglyceryl pentaoleate: SY-GlysterPO-3S manufactured by Sakamoto Pharmaceutical Co., Ltd., HLB3.0). In addition...

Embodiment 2

[0161] The amount of gum arabic was changed to 4g, and the amount of oxidized coenzyme Q10 was changed to 6g. Except that, the same method as described in Example 1 was used to obtain a granular composition containing oxidized coenzyme Q10. The average particle diameter of the obtained granular composition was 662 μm, the sphericity was 0.94, and the average particle diameter of the oxidized coenzyme Q10 region was 1845 nm.

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Abstract

The present invention provides a particulate composition wherein an oil component (A) comprising a water-insoluble bioactive substance is poly-dispersed while forming a domain in a matrix comprising of a water-soluble excipient based on a water-soluble polymer, and wherein the sphericity of the particulate composition is not less than 0.9 and a method of producing the same. The particulate composition simultaneously has excellent water solubility, workability, tabletability and heat-resistance. It also provides a food, food with nutrient function claims, food for specified health uses, nutritional supplement, nutritional product, animal drug, drink, feed, pet food, cosmetic, pharmaceutical product, therapeutic drug, prophylactic drug and the like, which contain the particulate composition.

Description

technical field [0001] The present invention relates to a granular composition containing physiologically active substances and a preparation method thereof. Specifically, the present invention relates to a granular composition containing a physiologically active substance and a preparation method thereof. The granular composition containing a physiologically active substance has both powder properties that are easy to handle and high oral absorbability. Background technique [0002] When the physiologically active substance is poorly water-soluble or fat-soluble, it is difficult to process it into a tablet or directly add it to foods such as beverages, and in many cases, the absorbability when ingested orally is low. For example, it is known that coenzyme Q10 is a fat-soluble crystalline powder having a melting point of about 48° C., and has very low absorbability when taken orally because it is poorly soluble in water. [0003] Coenzyme Q10 is a physiological component th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/10A61K9/20A61K31/07A61K31/122A61K31/203A61K31/355A61K31/59A61K36/48A61K47/02A61K47/14A61K47/22A61K47/24A61K47/26A61K47/32A61K47/36A61K47/38A61K47/42A61P3/02A61P9/04A61P39/06A61P43/00
CPCA61K31/355A61K31/202A61K31/122A61K31/59A61K36/484A61K9/113A61K9/2054A61K31/07A61K31/201A61K9/205A61K31/20A61P3/02A61P39/06A61P43/00A61P9/04A61P9/10
Inventor 柳乐洋三池原俊则植田贵志赤尾信介
Owner KANEKA CORP
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