JP2003192578A - Soft capsule - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To prevent occurrence of liquid leakage and crack with passage of time and delay of disintegration time in a soft capsule containing hydrophilic powder of a concentrate obtained from a natural product in the content solution and using gelatin as a film. <P>SOLUTION: In this soft capsule using gelatin as the film, the content solution comprises 20-50% hydrophilic powder of the concentrate obtained from the natural product and 0.1-30% polyglycerol-condensed ricinolate (having 2-10 glycerol unit and 2-10 ricinolic acid unit). <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention TECHNICAL FIELD OF THE INVENTION

The present invention relates to a soft capsule containing gelatin as a film, which is used in foods, pharmaceuticals, cosmetics, etc., which contains a hydrophilic powder of a concentrate obtained from a natural product and polyglycerol condensed ricinoleic acid ester as a content liquid. .

[Prior art]

Soft capsules are generally capsule preparations containing a fat and oil-soluble component as a content liquid and gelatin as a film.
Widely used in the fields of food, pharmaceuticals, cosmetics, etc.
This is because soft capsules can easily mix a certain amount of ingredients,
This is because the content components can be kept stable. Recently, a method of filling a content liquid in which a hydrophilic powder is dispersed in an oil phase with a surfactant, a stabilizer, etc. has been developed, and the versatility of soft capsules is further increasing.

[Problems to be Solved by the Invention]

However, when the content of the hydrophilic powder increases, the hydrophilic powder adheres to the joint portion of the gelatin film during filling of the content liquid to make the joint portion brittle, and the content liquid leaks due to temperature change, aging, etc. There is a problem. Although there is a method of thickening the gelatin film to deal with such a problem, there is a serious drawback that the disintegration time of the soft capsule is significantly delayed.

Further, generally, the hydrophilic powder of a concentrate obtained from a natural product contains aldehydes, ketose, oxides and the like. Therefore, if a soft capsule is filled with the content liquid containing the hydrophilic powder, the gelatin becomes insoluble due to the reaction of the lysine residue of gelatin with aldehydes or ketose, or the aldehyde formation due to the oxidation of the lysine residue, resulting in disintegration of the soft capsule. There is a problem that time is delayed with time. When the disintegration time is delayed, there arises a problem that the capsule is not dissolved in the digestive system and the contents of the capsule are not absorbed by the human body.

To address such a problem, Japanese Patent Laid-Open No. 8-245
No. 372 discloses a soft capsule in which a film contains acid-treated gelatin, a reducing agent, etc., and JP-A No. 2000-44465 discloses a soft capsule in which a film contains chemically modified gelatin and polyglucose. Although the disintegration time can be prevented from being delayed with time, the disintegration itself is poor from the beginning, and a fundamental solution has not yet been reached.

In view of such circumstances, as a result of intensive investigations by the present inventors, even if a large amount of hydrophilic powder of a concentrate obtained from a natural product is mixed in the content liquid of the soft capsule, a predetermined polyglycerin condensation is obtained. It has been found that the inclusion of ricinoleic acid ester can prevent the liquid leakage of the soft capsule with time, the delay of the disintegration time, and the like, and completed the present invention.

[Means for Solving the Problems]

That is, according to the present invention, when 20 to 50% of a hydrophilic powder of a concentrate obtained from a natural product is mixed in the content liquid, polyglycerin condensed ricinoleic acid ester (glycerin units 2 to 10 and ricinoleic acid unit) is added. 2-10)
It is a soft capsule containing gelatin as a film which prevents leakage of liquid over time, delay of disintegration time, etc. by containing 0.1 to 30% of.

The hydrophilic powder of the concentrate obtained from the natural product according to the present invention means a hydrophilic powder obtained by concentrating the extract of the natural product, squeezed juice, or the natural product itself. For example, as the hydrophilic powder of the extract concentrate, ginseng, eleuthero,
Agaricus, Ganoderma lucidum, Phellinus linteus, Gymnema, Aloe, Turmeric, Ginkgo biloba, Mulberry leaf, Herbal medicine such as bear bamboo, soybean,
Grains such as rice and wheat, tea such as green tea, oolong tea, black tea, vegetables such as carrots, pumpkin, spinach, cabbage, fruits such as blueberries, grapes, oranges, apples, mandarins, lemons, milk, goat milk, sheep milk, etc. Milk, sardines, bonito, oysters, seafood such as squid, meat such as chicken, pork and beef, propolis,
Examples include powders obtained by concentrating an extract solution of cold water such as royal jelly, hot water, alcohol, hydrous alcohol and the like. Examples of the hydrophilic powder of the squeezed concentrate include powders obtained by squeezing the above-mentioned crude drugs, vegetables, fruits and the like. Further, as the hydrophilic powder of the concentrate of the natural product itself, the above-mentioned crude drug, grain,
Examples thereof include powders obtained by drying, concentrating and crushing tea, vegetables, fruits, milk, seafood, meat, propolis, royal jelly and the like. As the hydrophilic powder of the concentrate obtained from these natural products, those subjected to treatment such as enzyme, hydrolysis, and purification as necessary can be used. Further, the hydrophilic powder of the concentrate obtained from a natural product can be used alone or in combination of two or more kinds.

The particle size of the powder is not particularly limited, but 60 mesh or less is preferable, 80 mesh or less is more preferable, and 100 mesh or less is more preferable. The water content of the powder is preferably 7% or less, more preferably 5% or less.

The polyglycerin condensed ricinoleic acid ester is usually a condensed ricinoleic acid obtained by dehydration-condensing glycerin and polyglycerin obtained by adding a catalyst to castor oil fatty acid and heating to 180 to 210 ° C. under a nitrogen gas stream. Is obtained by esterification at 180 to 210 ° C. under a nitrogen gas stream. Polyglycerin condensed ricinoleic acid ester is widely used in foods, pharmaceuticals, cosmetics and the like, and commercially available products can be used. The polyglycerin condensed ricinoleic acid ester of the present invention has 2 glycerin units.
-10, and those having a ricinoleic acid unit of 2 to 10 are used.
More preferably, the glycerin unit is 4 to 6 and the ricinoleic acid unit is 4 to 6. Incidentally, JP-A-9-1639
No. 63 has 1 glycerin unit in the content liquid which is an emulsion.
Although soft capsules using an ester of polyglycerin and polyhydroxycarboxylic acid of No. 15 to 15 are disclosed, the present invention improves the stability and hot water solubility of the emulsion, and the soft capsule according to the present invention. It does not suggest a capsule.

A soft capsule having a gelatin coating containing a hydrophilic powder of a concentrate obtained from a natural product and a polyglycerin condensed ricinoleic acid ester in the content liquid of the present invention can be further prepared by adding lecithin to the content liquid. The effect can be enhanced. Lecithin is a phospholipid containing phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol and the like obtained from soybean, egg yolk and the like. Lecithin is a natural zwitterionic surfactant, which is widely used in foods, pharmaceuticals, cosmetics, etc., and commercially available products can be used. Soy lecithin as lecithin,
In addition to egg yolk lecithin, powdered lecithin obtained by degreasing and concentrating these with acetone, fractionated lecithin obtained by fractionation and concentration with ethanol, enzymatically hydrolyzed enzymatically decomposed lecithin, and the like may be mentioned. These may be used alone or in combination of two or more kinds. Can be used.

The content of the hydrophilic powder of the concentrate obtained from the natural product according to the present invention in the content liquid is 20 to 50%. The content of polyglycerin condensed ricinoleic acid ester is 0.1 to 30%, more preferably 0.1 to 10%. When lecithin is added, it is recommended to add 0.1-5%.

As the content liquid of the soft capsule of the present invention, perilla oil, rice germ oil, wheat germ oil, soybean oil, rapeseed oil, corn oil, safflower oil, sesame oil, cottonseed oil, palm oil and other vegetable oils, fish oils, Animal fats and oils such as squid oil, whale oil, beef tallow, lard,
Hydrocarbons such as squalane and paraffin, waxes such as beeswax, rice bran wax and carnauba wax, nutritional enhancers such as vitamins, minerals and amino acids, surfactants such as glycerin fatty acid ester and sucrose fatty acid ester, vitamin E, hydroxytoluene, hydroxy Antioxidants such as anisole, those used in foods such as higher alcohols, pharmaceuticals, cosmetics and the like can be appropriately mixed.

The gelatin film according to the present invention is based on a mixture of gelatin with a plasticizer such as glycerin or sorbit. The type and blending ratio of gelatin and plasticizer are appropriately selected in consideration of the size and shape of the intended soft capsule. If necessary, additives such as dyes can be added. As the gelatin, those used in foods, pharmaceuticals, cosmetics and the like such as alkali-treated gelatin, acid-treated gelatin, enzyme-treated gelatin and chemically modified gelatin can be appropriately selected and used.

The content liquid according to the present invention may be prepared by a general method. For example, oil and fat, polyglycerin condensed ricinoleic acid ester, wax and the like are heated and dissolved at 60 to 80 ° C and cooled to 30 to 50 ° C. To this, add hydrophilic powder of concentrate obtained from natural product, lecithin, antioxidant, etc. and mix evenly with a high-speed stirrer such as homomixer, and then grind with a grinder such as Mycoloider and sieve. Then, defoaming is performed under reduced pressure to obtain a content liquid.

The soft capsules may be molded by a general method such as a rotary method, a flat plate method or a double nozzle method, but the effect of the present invention is exerted particularly in the soft capsules by the rotary method or the flat plate method. For molding soft capsules by the rotary method, for example, a rotary capsule molding machine equipped with a metering pump for feeding the content liquid, a roller for feeding the gelatin sheet, a punching die, etc. is used to fill the content liquid, press-bond the gelatin sheet and form the capsule. Simultaneous molding. Then, the film moisture is dried by a rotary drum dryer until the water content in the film is 10% or less, to obtain soft capsules.

【Example】

Next, typical examples will be given to explain the present invention in detail, but the present invention is not limited thereto. The compounding amounts shown in the examples are% by weight.

Example 1 <Prescription> Blending amount (%) 1. Perilla oil 51.0 2. Polyglycerin condensed ricinoleic acid ester 3.0 (glycerin unit 6, ricinoleic acid unit 5.5) 3. Beeswax 12.0 4. Vitamin E 3.0 5. Soy lecithin 1.0 6. Powder of hot water extract of Ganoderma lucidum (particle size 80 mesh or less, water content 4.5%) 30.0 <Production method> Components 1 to 3 are heated and melted at 70 ° C. and cooled to 40 ° C., and then components 4 to 6 Add homomixer (20
(00 rpm) for 30 minutes, crushed with Mycoloider, and sieved with 83 mesh (opening 180 μm). Further, what was defoamed under a reduced pressure of 720 mmHg was used as a content liquid. The coating solution used is 100 parts of gelatin, 35 parts of glycerin and 80 parts of purified water heated and dissolved, and the content solution is filled with a rotary capsule molding machine to form a film. It was dried to 7% to obtain an elliptical soft capsule having a total weight of 550 mg and a content liquid amount of 360 mg.

A soft capsule obtained by replacing the glycerin unit or the ricinoleic acid unit of the polyglycerin-condensed ricinoleic acid ester (glycerin unit 6 and ricinoleic acid unit 5.5) of Example 1 with the polymerized unit of Table 1 was used as an Example. 2 to 4 and Comparative Examples 1 to 3.

[0020]

[Table 1]

Soft capsules obtained by adjusting the total amount of polyglycerin condensed ricinoleic acid ester of Example 1 as shown in Table 2 and adjusting the total amount with perilla oil were designated as Examples 5 to 7 and Comparative Example 4. .

[0022]

[Table 2]

Comparative Example 5 was a soft capsule obtained by replacing the polyglycerin condensed ricinoleic acid ester with a glycerin monofatty acid ester of Table 3 or a polyglycerin fatty acid ester whose fatty acid is a fatty acid other than condensed ricinoleic acid.
It was set to 10.

[0024]

[Table 3]

Example 8 Example 8 was the same as Example 1 except that soybean lecithin was replaced with perilla oil.

Example 9 <Prescription> Compounding amount (%) 1. Rice germ oil 50.0 2. Polyglycerin condensed ricinoleic acid ester 2.0 (glycerin unit 6, ricinoleic acid unit 5.5) 3. Beeswax 4.5 4. Vitamin E 3.0 5. Soy lecithin 0.5 6. Powder of hydroalcoholic extract of blueberry juice 40.0 (particle size 80 mesh or less, water content 3.4%) <Production method> Components 1 to 3 are heated and dissolved at 70 ° C and cooled to 40 ° C, and then components 4 to 6 are prepared. Add homomixer (20
After mixing at 00 rpm) for 30 minutes, it is crushed with Mycoloider and sieved with 83 mesh (opening 180 μm). Further, what was defoamed under a reduced pressure of 720 mmHg was used as a content liquid. The coating solution is 100 parts of gelatin and 3 glycerin.
Using 5 parts and 80 parts of purified water heated and dissolved, the content liquid was filled with a rotary capsule molding machine to mold and dried with a rotary drum dryer until the film moisture became 8%, An elliptical soft capsule having a weight of 550 mg and a content liquid amount of 360 mg was obtained.

Example 10 <Prescription> Compounding amount (%) 1. Corn oil 53.0 2. Polyglycerin condensed ricinoleic acid ester 1.5 (glycerin unit 6, ricinoleic acid unit 5.5) 3. Beeswax 7.0 4. Vitamin E 3.0 5. Soy lecithin 0.5 6. Powder of hot water extract of Agaricus 35.0 (particle size 80 mesh or less, water content 4.3%) <Production method> Components 1 to 3 were heated and dissolved at 70 ° C and cooled to 40 ° C, and then components 4 to 6 were added. Add the homomixer (20
After mixing at 00 rpm) for 30 minutes, it is crushed with Mycoloider and sieved with 83 mesh (opening 180 μm). Further, what was defoamed under a reduced pressure of 720 mmHg was used as a content liquid. The coating solution is 100 parts of gelatin and 3 glycerin.
Using 5 parts and 80 parts of purified water heated and dissolved, the content liquid was filled with a rotary capsule molding machine and molded, and dried with a rotary drum dryer until the film moisture became 7%, Oval soft capsules having a weight of 480 mg and a content liquid amount of 250 mg were obtained.

【The invention's effect】

The effects of the present invention will be described in detail in the following experimental examples. 1000 soft capsules of each of Examples 1 to 8 and Comparative Examples 1 to 10 were placed in a glass closed container, and
The liquid leakage, cracking and disintegration time of the soft capsules after storage for 2 months at ℃ were observed. Liquid leakage and cracks were visually observed, and the disintegration time was determined by the disintegration test method of the Japanese Pharmacopoeia (test liquid: purified water, n = 6,
It was performed according to (using an auxiliary board).

Table 4 shows the number of liquid leaks and cracks generated over time and the disintegration time. In each of the soft capsules of Examples 1 to 8 according to the present invention, liquid leakage and cracking with time do not occur, and delay of disintegration time is prevented. In particular, in Examples in which polyglycerin condensed ricinoleic acid ester having 4 to 6 glycerin units and 4 to 6 ricinoleic acid units and soybean lecithin were used in combination, an excellent effect of preventing delay of disintegration time was obtained. On the other hand, it can be seen that soft capsules using other surfactants cause liquid leakage or cracking over time, and the disintegration time is delayed. In Table 4, E represents hydrophilic powder of a concentrate obtained from a natural product, R represents polyglycerin condensed ricinoleic acid ester, and D represents soybean lecithin.

[0030]

[Table 4]

From the above results, 20 to 50% of hydrophilic powder of the concentrate obtained from the natural product in the content liquid, polyglycerin condensed ricinoleic acid ester (glycerin unit 2 to 10)
And a gelatin-coated soft capsule characterized by containing 0.1 to 30% of ricinoleic acid units 2 to 10) does not cause liquid leakage or cracking over time, and is unlikely to delay disintegration time. Proved. Further, it has been clarified that a more excellent effect can be obtained by adding lecithin to the composition in an amount of 0.1 to 5%.

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Claims (3)

[Claims] 1. A content liquid containing 20 to 50% hydrophilic powder of a concentrate obtained from a natural product and 0.1% polyglycerin condensed ricinoleic acid ester (glycerin units 2 to 10 and ricinoleic acid units 2 to 10). A soft capsule containing gelatin as a coating, characterized in that the soft capsule contains -30%. 2. The soft capsule according to claim 1, wherein the content liquid contains 0.1 to 5% of lecithin. 3. A polyglycerin condensed ricinoleic acid ester having 4 to 6 glycerin units and 4 to 6 ricinoleic acid units.
6. The soft capsule according to claim 1 or 2, which is 6.