JP2000336028A - Capsule preparation - Google Patents

Abstract

PROBLEM TO BE SOLVED: To improve an attachment-preventing performance simply and surely without accompanying inconveniences in such as an appearance, a disintegrating property, a molding property, etc. in a capsule preparation. SOLUTION: This capsule preparation is obtained by blending a solid or liquid hydrophobic material at a normal temperature into its membrane composition. Especially, as the hydrophobic material, a material selected from a group consisting of a vegetable wax, an animal wax, a mineral-based wax, a petroleum wax, an oil and fat, a fatty acid ester, an alkylglycerylether, a hydrogenated oil, a fatty acid and lecithin, is blended by <=5.0 pt.wt. based on 100 pts.wt. gelatin.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to pharmaceuticals, cosmetics,
The present invention relates to capsules such as soft capsules used for health foods, general foods, quasi-drugs, and the like.

[0002]

2. Description of the Related Art Conventionally, capsules containing gelatin or the like as a film component have had a problem of mutual adhesion between capsules and adhesion to a container after a production process and after a product is completed. Conventional techniques for preventing the adhesion of capsules include forming an anti-adhesion coating layer such as carnauba wax on the coating surface as described in JP-A-56-156212, or JP-A-2-22221. In some cases, an anti-adhesion component such as calcium is added to the film component described in the official gazette.

[0003]

However, in the prior art in which the coating surface of the capsule is coated with an anti-adhesion coating layer, the manufacturing process of the capsule is inevitably increased, which leads to an increase in cost or a seam on the surface of the coating. The capsules having the disadvantages such as poor appearance such as non-uniform coating at the seam portion, and peeling of the coating layer over time have disadvantages. Further, in the case of a soft capsule having irregularities such as a so-called "self-cut type", it is difficult to uniformly coat the anti-adhesion coating layer on the film surface.

In the prior art in which an anti-adhesion component is blended with a film component of a capsule, it is necessary to use a large amount of the anti-adhesion component with respect to the film base (gelatin), resulting in poor appearance and disintegration time. , And new inconveniences such as deterioration of moldability at the time of production occur.

[0005] An object of the present invention is to simply and surely improve the anti-adhesion performance of capsules without causing disadvantages such as appearance, disintegration, and moldability.

[0006]

According to the first aspect of the present invention, a solid or liquid hydrophobic substance at room temperature or a mixture thereof is blended with a film component of a capsule.

According to a second aspect of the present invention, in the first aspect of the present invention, the hydrophobic substance is a liquid when a coating liquid is prepared.

According to a third aspect of the present invention, in the first or second aspect, the hydrophobic substance which is solid at room temperature is a vegetable wax, an animal wax, a mineral wax, or a petroleum wax. , Oils and fats, fatty acid esters, alkyl glyceryl ethers, hardened oils, fatty acids, and lecithin.

Plant wax is a plant-derived wax.
Wax existing on the surface of plant leaves, seeds, fruits, etc. or as a storage substance can be obtained by heating with water or extracting with a solvent.

[0010] Animal wax is an animal-derived wax,
For example, beeswax obtained from beehives, lanolin obtained by separation and extraction from wool, and the like are listed.

[0011] Mineral waxes are waxes derived from minerals, that is, non-living substances that occur naturally.

The petroleum-based wax is included in the category of mineral-based wax, and is a wax obtained through petroleum fractionation and purification.

[0013] Fats and oils are triesters of fatty acids and glycerin, and are included in all kinds of animals and plants in nature. The fats and oils in claim 3 refer to those which are solid at normal temperature.

Fatty acid esters are substances obtained by dehydrating one or two molecules of a fatty acid and an alcohol.

Alkyl glyceryl ether is a substance contained in shark and cod liver oil and the like.

Hardened oils are those obtained by subjecting various fats and oils to hydrogenation treatment to saturate some or all of the unsaturated bonds (such as double bonds) of the fats and oils to increase the melting point. Depending on the degree of hydrogenation, hardened oils of various melting points can be produced from one type of fat or oil.

Fatty acids are defined as having one carboxy group (—COOH).
It is a single chain compound that is obtained by, for example, hydrolyzing various fats and oils.

Lecithin is a phospholipid widely present in various animal and vegetable oils, and is obtained by further extracting and purifying from total lipids extracted from tissues. Representative examples are soy lecithin and egg yolk lecithin. The lecithin in claim 3 refers to those which are solid at room temperature.

The present invention described in claim 4 is the first to third aspects of the present invention.
In the present invention according to any one of the above, the hydrophobic substance which is liquid at normal temperature is a substance selected from the group consisting of vegetable oils, hydrocarbons, and lecithin.

[0020] Vegetable oil refers to a vegetable triglyceride which is liquid at room temperature among plant triglycerides produced from plant seeds, fruits, nuclei, germs and the like. As a general chemical structure, it is known that it is a triglyceride of various (mainly, medium chain [C number is 8 to 12]) fatty acids.

Typical examples of hydrocarbons include liquid paraffin (including light and low-viscosity ones).

The lecithin according to the fourth aspect is a liquid at room temperature (including a paste).

The present invention described in claim 5 provides the invention according to claims 1-4.
In the present invention according to any one of the above, the hydrophobic substance is not more than 5.0 parts by weight based on 100 parts by weight of gelatin.

[0024]

According to the first, third and fourth aspects of the present invention, the following effects are obtained. Of the hydrophobic substances uniformly dispersed in the coating, fine hydrophobic substance particles exposed on the coating surface coat the coating surface, and the coating layer of the hydrophobic substance prevents adhesion. The capsules rub against each other in a manufacturing process such as drying of the capsules, so that the formation of the coating layer of the hydrophobic substance is further improved.

Since the above-mentioned anti-adhesion coating layer is not provided by coating, the cost is increased due to an increase in the number of manufacturing steps, the appearance is poor such as the unevenness of the formation of the coating layer at the seam portion of the coating surface, and the coating layer is deteriorated with time. No inconvenience such as peeling occurs.

The amount of the hydrophobic substance relative to the film base (eg, gelatin or succinated gelatin) is, for example, 1% by weight.
The required adhesion preventing performance can be ensured while using a small amount as described below. Therefore, even if a hydrophobic substance is blended, the basic film performance (appearance, disintegration,
It does not adversely affect moldability.

It has been found that the above-mentioned effects are not limited to the hydrophobic substance which is a solid at room temperature, but it can be surprisingly obtained similarly with a hydrophobic substance which is a liquid at room temperature. Further, both a solid at room temperature and a liquid at room temperature can be mixed.

According to the second aspect of the invention, the following effects are obtained. By making the hydrophobic substance a liquid at the time of preparing the coating liquid, the dispersibility of the hydrophobic substance in the coating can be made more uniform, and the above-described adhesion prevention performance can be further improved. During the preparation of the coating liquid, the liquid hydrophobic substance reduces the viscosity of the coating liquid and promotes defoaming for improving the appearance of the capsule,
It also contributes to shortening the defoaming time.

According to the fifth aspect of the invention, the following effects are obtained. When the hydrophobic substance is 5.0 parts by weight or less based on 100 parts by weight of gelatin for both hydrophobic substances at room temperature and liquid at room temperature, the film must have an appearance free from clouding (turbidity). And is suitable for use.

[0030]

DESCRIPTION OF THE PREFERRED EMBODIMENTS First Embodiment (Tables 1 to 1)
1) The film of the capsule (especially soft capsule) according to the present invention is composed of (A) a film base, and (B) a hydrophobic substance, (C) and other compounds.

(A) Film Base Gelatin or succinated gelatin can be used as the film base.

(B) Hydrophobic substance (Tables 1 and 2) A hydrophobic substance which is solid at normal temperature is used. This hydrophobic substance is preferably liquid at the time of preparing the coating liquid.

Examples of the hydrophobic substance include plant waxes, animal waxes, and mineral waxes shown in Table 1.
Petroleum waxes, fats and oils, fatty acid esters described in Table 2,
A substance selected from the group consisting of alkyl glyceryl ethers, hardened oils, fatty acids, and lecithin can be used.

The hydrophobic substances used in the present invention are not limited to those shown in Tables 1 and 2, but may be other than those shown in Tables 1 and 2, for example, tallow fatty acid triglyceride and hardened palm fatty acid as solid fats and oils at normal temperature. Triglycerides, hardened tallow fatty acid triglycerides, hardened palm oil can be used as hardened oil, and glycerin fatty acid esters, polyglycerin fatty acid esters, sorbitan fatty acid esters, propylene glycol fatty acid esters, and sucrose fatty acid esters can also be used.

[0035]

[Table 1]

[0036]

[Table 2]

(C) Other Compounds As other compounds, the following can be compounded. Other gelling agents Agar, carrageenan, alginates, gellan gum, etc.

Plasticizer glycerin, sorbitol, polyethylene glycol,
Propylene glycol, etc.

Colorants Titanium oxide, various tar pigments, various natural pigments, iron sesquioxide, caramel, natural calcium agent, etc.

Preservatives Various esters of paraoxybenzoic acid (methyl, ethyl,
Propyl, butyl, etc.), sorbic acid and its salts

Flavoring agents, flavoring agents Various flavors, cherry, lemon, orange, strawberry, vanilla, cocoa, etc., various sweeteners such as saccharin, sodium saccharin, stevia, sugars, etc.

(Test 1) (Tables 3 and 4) For each of Examples A to F of the present invention and Comparative Example 1, coating films were prepared according to the formulation shown in Table 3. That is, Examples A to F of the present invention
Is 100 parts by weight of gelatin and 30 parts by weight of glycerin,
0.5 parts by weight of beeswax, beeswax, candelilla wax, carnauba wax, lanolin wax, and synchro wax were blended as the normal temperature solid hydrophobic substance of the present invention.
0 parts by weight, glycerin only 30 parts by weight,
In this case, the hydrophobic substance of the present invention was not blended.

[0043]

[Table 3]

Samples obtained by cutting the film sheets of Examples A to F and Comparative Example 1 into strips each measuring 1 cm × 4 cm were placed in glass bottles, each of which was sealed with a resin cap. After storing this bottle in a constant temperature and humidity chamber at 40 ° C and 75% RH for 1 week,
Table 4 was obtained by evaluating the ease of peeling between the sheets. In the evaluation of Table 4, the ease of peeling of each sheet of the invention examples A to F was compared with the ease of peeling of the sheet of Comparative Example 1, and those that were more easily peeled were marked as +, and the larger the number of +, the more easily the sheet was peeled. Indicates that

According to Table 4, in Examples A to F of the present invention,
High adhesion prevention performance can be obtained.

[0046]

[Table 4]

(Test 2) (Tables 5 to 7) In each of Examples G, H and I of the present invention and Comparative Example 2, a coating liquid was prepared according to the formulation shown in Table 5, and a rotary soft capsule manufacturing apparatus (die roll) was prepared. : Drop type) to produce soft capsules containing 280 mg of vegetable oil. That is, Examples G, H, and I of the present invention were composed of 100 parts by weight of gelatin and 20 parts of glycerin.
Parts by weight, D-sorbitol 70% liquid 10 parts by weight, caramel 1.
Comparative Example 2 was prepared by blending 0.5 parts by weight of lanolin wax, candelilla wax, and beeswax as the normal-temperature solid hydrophobic substance of the present invention with respect to 5 parts by weight.
Is 100 parts by weight of gelatin, 20 parts by weight of glycerin, 10 parts by weight of a 70% solution of D-sorbitol, and 1.5 parts by weight of caramel, and does not contain the hydrophobic substance of the present invention.

[0048]

[Table 5]

The soft capsules of Examples G, H and I of the present invention and Comparative Example 2 were placed in bottles as specimens, and after opening the storage condition (temperature, humidity and time) shown in Table 6, the bottles were opened. Is placed upside down on a desk, and then the drop height is gradually increased from 1 cm to 10 cm. At each stage when the soft capsule drops, the soft capsule drops without adhering to the inner wall of the bottle. Table 6 shows the cumulative number of drops.

[0050]

[Table 6]

Further, the soft capsules of Examples G, H, and I of the present invention and Comparative Example 2 were placed in bottles as specimens, and after the storage conditions (temperature and time) in Table 7 were passed in a sealed state with a metal cap, Place the bottle upside down on the desk, then drop the height 1
Table 7 shows the cumulative number of the soft capsules that dropped without being attached to the inner wall of the bottle at each stage when the soft capsules were gradually dropped from 10 cm to 10 cm.

[0052]

[Table 7]

According to Tables 6 and 7, Examples G, H and I of the present invention were obtained.
In this case, high adhesion prevention performance can be obtained.

(Test 3) (Tables 8 to 10) In the present invention, for each of A ′ to F ′ and A ″ to F ″,
Film sheets were prepared according to the formulations shown in Tables 8 and 9. Inventive Examples A 'to F' were compared with Inventive Examples A to F (0.5 parts by weight of hydrophobic substance) prepared in Test 1 by adding 100 parts by weight of gelatin to those hydrophobic substances. And 5.0 parts by weight. The present invention examples A "to F" differ from the present invention examples A to F in that the blending amount of the hydrophobic substance is 10 parts by weight with respect to 100 parts by weight of gelatin.

[0055]

[Table 8]

[0056]

[Table 9]

The anti-adhesion properties of the inventive examples A ′ to F ′ and A ″ to F ″ were evaluated under the same test conditions as in the test 1 for the inventive examples A to F, and Table 10 was obtained.
Table 10 also shows the results of Table 4 obtained in Test 1 for Invention Examples A to F.

According to Table 10, it was confirmed that even when the blending amount of the hydrophobic substance was increased in the film sheet using the hydrophobic substance which was a solid at room temperature, there was almost no difference in the adhesion preventing effect.

[0059]

[Table 10]

(Test 4) (Table 11) With respect to the present invention examples A to F prepared in test 1, and the present invention examples A 'to F' and A "to F" prepared in test 3, the appearance was evaluated. Table 11 was obtained.

According to Table 11, it was recognized that, when the amount of the hydrophobic substance was increased in the film sheet using the hydrophobic substance which was a solid at room temperature, there was a problem in appearance. Specifically, 0.5% for 100 parts by weight of gelatin (common to each material)
There were no problems with the appearance in parts by weight, and there were some problems with 5.0 parts by weight, but within the allowable range, and 10 parts by weight were poor.
The film becomes cloudy (turbid) if the amount of the hydrophobic substance to be blended is large.
Is caused. Therefore, as a preferable range that can be used from the aspect of appearance, the blending amount of the hydrophobic substance is 5.0 parts by weight or less based on 100 parts by weight of gelatin.

[0062]

[Table 11]

(Second Embodiment) (Tables 12 to 16) The capsule (particularly soft capsule) according to the present invention is composed of (A) a film base, (B) a hydrophobic substance, (C) other Are blended.

(A) Film base As the film base, gelatin or succinated gelatin can be used.

(B) Hydrophobic substance (Table 12) A hydrophobic substance which is liquid at normal temperature is used. It is preferable that the hydrophobic substance is liquid even when the coating liquid is prepared.

As the hydrophobic substance, for example, substances selected from the group consisting of vegetable oils, hydrocarbons, and lecithin shown in Table 12 can be used.

[0067]

[Table 12]

(C) Other Compounds As other compounds, the following can be compounded. Other gelling agents Agar, carrageenan, alginates, gellan gum, etc.

Plasticizer glycerin, sorbitol, polyethylene glycol,
Propylene glycol, etc.

Colorant Titanium oxide, various tar dyes, various natural dyes, iron sesquioxide, caramel, natural calcium agent, etc.

Preservatives Various esters of paraoxybenzoic acid (methyl, ethyl,
Propyl, butyl, etc.), sorbic acid and its salts

Flavoring agents, flavoring agents Various flavors, cherry, lemon, orange, strawberry, vanilla, cocoa, etc., various sweeteners such as saccharin, sodium saccharin, stevia, sugars, etc.

(Test 5) (Tables 13 to 15) Coating sheets were prepared according to the formulations shown in Table 13 for Examples 1 to 3 of the present invention. That is, in Examples of the present invention, 0.5 parts by weight, 5.0 parts by weight, and 10 parts by weight of coconard MT (trade name) as hydrophobic substances of a room temperature liquid of the present invention were added to 100 parts by weight of gelatin and 30 parts by weight of glycerin, respectively. It is blended.

[0074]

[Table 13]

In addition, coating sheets were prepared according to the formulations shown in Table 14 for Examples 1 to 3 of the present invention. That is, the present invention examples are
100 parts by weight of gelatin and 30 parts by weight of glycerin, each 0.5 parts by weight as a hydrophobic substance of a room temperature liquid of the present invention,
It contains 5.0 parts by weight and 10 parts by weight of light liquid paraffin.

[0076]

[Table 14]

Under the same test conditions as in Test 1 for Inventive Examples A to F, the anti-adhesion performance was evaluated for Inventive Example 1 to give Table 15.

According to Table 15, it was recognized that even when the amount of the hydrophobic substance was increased in the film sheet using the hydrophobic substance at room temperature, there was almost no difference in the adhesion preventing effect.

[0079]

[Table 15]

(Test 6) (Table 16) The appearance of each of Examples 1 to 3 of the present invention was evaluated.
Table 16 was obtained. According to Table 16, it was recognized that when the blending amount of the hydrophobic substance was increased in the film sheet using the hydrophobic substance at room temperature, a problem occurred in the appearance. Specifically, for 100 parts by weight of gelatin (common to each material)
At 0.5 parts by weight, there was no problem in appearance, and at 5.0 parts by weight, there was some problem, but within the allowable range, and at 10 parts by weight, it was poor. This is because when the amount of the hydrophobic substance to be blended is large, the film becomes cloudy (turbidity). Therefore, as a preferable range that can be used from the viewpoint of appearance, the blending amount of the hydrophobic substance is 5.0 parts by weight or less based on 100 parts by weight of gelatin.

[0081]

[Table 16]

[0082]

As described above, according to the present invention, it is possible to easily and surely improve the anti-adhesion performance of the capsule without any disadvantages such as appearance, disintegration and moldability.

Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat II (reference) A61K 7/00 A61K 7/00 J C 47/08 47/08 47/12 47/12 47/14 47/14 47 / 24 47/24 47/42 47/42 47/44 47/44

Claims (5)

[Claims] 1. A capsule prepared by blending a solid or liquid hydrophobic substance at room temperature or a mixture thereof with a film component of the capsule. 2. The capsule according to claim 1, wherein the hydrophobic substance is a liquid at the time of preparing a coating liquid. 3. The hydrophobic substance which is solid at room temperature is selected from the group consisting of vegetable wax, animal wax, mineral wax, petroleum wax, oil and fat, fatty acid ester, alkyl glyceryl ether, hardened oil, fatty acid and lecithin. The capsule according to claim 1 or 2, which is a substance to be prepared. 4. The hydrophobic substance which is liquid at normal temperature is a vegetable oil,
The capsule according to any one of claims 1 to 3, which is a substance selected from the group consisting of hydrocarbons and lecithin. 5. The capsule according to claim 1, wherein the amount of the hydrophobic substance is 5.0 parts by weight or less based on 100 parts by weight of gelatin.