Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules
Reexamination Certificate
2000-06-01
2003-03-11
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Capsules
C424S451000, C424S455000, C424S456000, C424S489000, C424S490000, C424S491000, C424S492000
Reexamination Certificate
active
06531150
ABSTRACT:
TECHNICAL FIELD
The present invention relates to an encapsulated unsaturated fatty acid substance. Particularly, the present invention relates to an encapsulated unsaturated fatty acid substance which is enteric and does not deteriorate with time, and a method for producing the encapsulated unsaturated fatty acid substance.
BACKGROUND ART
There have been used water-soluble capsules which encapsulate an oily liquid component and the like in a gelatin containing layer, because they can keep the content isolated from surroundings so as to protect the content, or to eliminate bad odor generating from the content.
Recently, it has been found that an unsaturated fatty acid or its derivative, such as eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA) and the like, has an effect on prevention and cure of hyperlipidemia, and one wishes to take it orally. Since the effective unsaturated fatty acid or derivative thereof has strong odor and it is difficult for us to directly take it, it has been served in a form of a capsule encapsulating it by the gelatin containing layer.
It is known, however, that the capsule encapsulating unsaturated fatty acid or derivative thereof decreases its water-solubility of the gelatin layer as time goes and at last results in insoluble with water. That is believed to cause by a reaction of the unsaturated fatty acid or derivative thereof with gelatin.
In order to prevent the capsule layer containing gelatin from insolubilizing due to the unsaturated fatty acid or derivative thereof, there is proposed a method wherein citric acid is added to gelatin to form a capsule coating layer (as disclosed in Japanese Paten Kokai Publication Sho 59 (1984)-39834), a method wherein a pH of gelatin is adjusted to no more than 5 to form a capsule coating layer (as disclosed in Japanese Paten Kokai Publication Sho 64 (1989)-38019), or the Japanese Paten Kokai Publication Hei 7 (1995)-69861 proposes a method wherein acid or its salt is formulated into a gelatin containing layer to form a capsule containing higher fatty acid or fats, in order to prevent the reaction between gelatin and the content of the capsule.
According to the methods as disclosed in the above-mentioned publications, insolubilization of the gelatin layer is inhibited, but another disadvantage may occur. For example, a part of gelatin layer (particularly, a surface of the layer exposed to air) is brittle and then turns its color to brown to deteriorate the capsule, because gelatin as a film-forming component for the capsule layer is reacted with citric acid or the acid component to be added. In producing the capsule, acid adversely affects and prevents gelatin from gelling to prolong its production period of time. As a result, efficiency of production is poor.
DISCLOSURE OF INVENTION
Accordingly, an object of the present invention is to provide a capsule encapsulating an unsaturated fatty acid or derivative thereof as a content in a gelatin layer, having disadvantages as mentioned above (for example, brittleness, browning and poor efficiency of production of the capsule).
The present invention relates to encapsulated unsaturated fatty acid substance comprising an unsaturated fatty acid or a derivative thereof (
11
) as a content and a coating layer (
10
) mainly containing gelatin, encapsulating the content (
11
), wherein a water-soluble gel layer (
12
) containing an acid or an acid salt thereof is present between the coating layer (
10
) and the content (
11
).
The present invention further provides a method for producing the encapsulated unsaturated fatty acid substance, comprising simultaneously extruding three components from three nozzles into a cooling solution, wherein the first component is an unsaturated fatty acid or a derivative thereof (
4
) and is extruded from the first nozzle (
1
), the second component is an acid or an acid salt thereof (
5
) and is extruded from the second nozzle (
2
), the third component is a capsule coating material mainly containing gelatin (
6
) and is extruded from the third nozzle (
3
), and the first nozzle (
1
), second nozzle (
2
) and third nozzle (
3
) are arranged concentrically and their diameters gradually increase in a numerical order.
BEST MODE FOR CARRYING OUT THE INVENTION
The present invention will explain briefly as follows.
Capsule
FIG. 1
schematically shows a cross-sectional view of a capsule (
20
) of the present invention, encapsulating an unsaturated fatty acid or derivative thereof as a content (
11
) with a coating layer (
10
) mainly containing gelatin. In
FIG. 1
, number “
10
” indicates the coating layer, “
11
” indicates the content and “
12
” indicates a water-soluble gel layer containing acid or acid salt thereof.
Coating Layer
A material for forming the coating layer (
10
) of the capsule (
20
) according to the present invention generally formed from gelatin, and if desired, another material such as a protein except gelatin, or a polysaccharide (for example, albumin, pectin, guaran gum, carrageenan, agar and the like) may be contained. When the material for forming the coating layer contains protein or polysaccharide, it may be contained in an amount of 100 parts by weight to one part by weight, preferably 67 parts by weight to one part by weight, based on 100 parts by weight of gelatin being its base material.
The coating layer (
10
) may contain an additive, for example an enteric material, a plasticizer, a preservative and a colorant and the like, in addition to gelatin and the materials mentioned above.
A suitable example of the enteric material used in the present invention is pectin, alginic acid, cellulose such as carboxyl methylcellulose, celluloseacetate phthalate, and the like, Eudragit® which is one of an acrylic copolymer, and the like, but these are not limitative examples. Preferred is pectin as the enteric material. The addition of the enteric material into the material for forming the coating layer (
10
) makes the capsule (
20
) is enteric and therefore the capsule does not dissolve in stomach when oral administration of it. As the result, so-called “returned odor” (that is, pleasant odor or fishy-smelling odor returned from a stomach to an oral cavity generated from fish oil and the like present in the content of the capsules by the dissolution of the capsule in stomach would disappear, and therefore, the product quality increases.
The plasticizer may include polyhydric alcohols, such as sorbitol, glycerin, polyethylene glycol and the like. In the present invention, examples of the suitable preservative and colorant are known in the art and include benzoic acid, para-oxybenzoate, caramel colorant, gardenia colorant, carotene colorant, tar colorant and the like.
A total amount of the additives may be two parts by weight to 98 parts by weight, based on 100 parts by weight of gelatin in the coating layer. Particularly, the enteric material may be contained in an amount of two parts by weight to 98 parts by weight, based on 100 parts by weight of gelatin.
In order to inhibit oxygen-permeability of the capsule of the present invention, sucrose may be contained in the coating layer, in addition to the film-forming material and additives. When sucrose is not contained in the coating layer, oxygen may permeate through the water-soluble gel layer (
12
) to reach the content and oxidize the unsaturated fatty acid and derivative thereof (
11
) during a long storage period of time. Oxidized unsaturated fatty acid and derivative thereof increase peroxide value (POV) and deteriorate product quality. Sucrose efficiently inhibits the disadvantage. Sucrose may be contained in an amount of one part by weight to 100 parts by weight based on 100 parts by weight of gelatin.
Water-soluble Gel Layer
The capsule (
20
) of the present invention contains the water-soluble gel layer (
12
) between the coating layer (
10
) and the content (
12
). An example of a material used for forming the water-soluble gel layer (
12
) includes protein or polysaccharide as a film-forming material which has been hitherto used for production of the capsule
Higuchi Junko
Kamaguchi Ryosei
Kozaki Toshio
Sunohara Hideki
Yoshikado Masatomo
Merchant & Gould P.C.
Morishita Jintan Co., Ltd.
Page Thurman K.
Tran S.
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