JPH0222221A - Capsule having improved lubricating property and disintegrating property - Google Patents

Abstract

PURPOSE:To obtain capsules having excellent adhesion preventing effects, lubricating properties and disintegrating properties by blending gelatin with a calcium salt or a natural calcium agent consisting essentially of the calcium salt. CONSTITUTION:Gelatin is blended with >=10wt.%, preferably 40-60wt.% calcium salt such as calcium carbonate, calcium hydrogenphosphate, calcium lactate, calcium gluconate or a natural calcium agent such as eggshell, bovine bone powder or shell consisting essentially of the calcium salt to give capsules having excellent lubricating properties. When calcium carbonate is used as the calcium salt, calcium carbonate evolves a carbon dioxide gas under an acidic condition in the stomach and soft capsules of gelatin are rapidly and surely destroyed.

Description

DETAILED DESCRIPTION OF THE INVENTION (Field of Industrial Application) The present invention primarily relates to a capsule having a capsule coating that improves its sliding properties and disintegration properties.
In the present invention, a capsule refers to a type of airtight container formed by a capsule film containing gelatin, glycerin, water, etc. as the main ingredients, and a capsule is a container in which the contents such as pharmaceuticals, foods, or cosmetics are placed inside the capsule. It means a filled solid agent.

(Prior Art) Generally, in order to have good quality as a capsule, it is necessary for the capsule film to maintain a constant water content.

However, in reality, the moisture content of capsules, especially soft capsules, tends to vary greatly depending on environmental conditions. In particular, under conditions of high humidity and temperature, the capsule film becomes wet and softens, and the slipperiness of the capsule itself is affected. This has the disadvantage that it is difficult to carry out packaging and filling of capsules smoothly.

In addition, the capsules have other drawbacks, such as being adhesively bonded to each other and not being able to be removed when ingested, or softening and deforming, resulting in a loss of commercial value in terms of appearance.

Furthermore, with some exceptions such as enteric-coated capsules, capsules are desired to disintegrate quickly in the stomach and release the contents.

However, gelatin, which is the base material of the capsule film, undergoes various changes over time during long-term storage, which may lead to a decrease in its disintegrability.

To this end, conventional methods have been to use gelatin as a raw material whose jelly strength and viscosity are below a certain value, or to take advantage of the fact that gelatin is a protein9, to mix specific amino acids into gelatin as proteolytic enzymes or disintegration aids. Although methods have been proposed for promoting the disintegration properties of capsules, they have not always been satisfactory.

Additionally, as a known technique, Japanese Patent Application Laid-Open No. 15831/1983 can be mentioned, which improves the disintegration property by blending sodium hydrogen carbonate into gelatin, but the temperature condition during production is maintained at 406C or less. The drawback was that it needed to be done.

(Technical Problem) The present invention was made in view of the shortcomings of the prior art, and its technical problem is to propose a capsule that improves and promotes the sliding properties and disintegration properties of the capsule film.

(Technical Means) In order to solve the above technical problem, the present invention is configured as follows.

First, about 10% of gelatin is mixed with a calcium salt such as calcium carbonate, calcium hydrogen phosphate, calcium lactate, or calcium glyconate, or a natural calcium agent such as eggshell, beef bone meal, or seashell containing said calcium salt as a main component. % or more to increase the slipperiness of the capsule.

Preferably, the blending ratio is 40 to 60% by weight.

Second, among the above-mentioned calcium salts, a carbonate or a natural calcium carbonate agent containing the calcium carbonate as the main component is blended at a ratio of about 10% by weight or more to gelatin to increase the slipperiness and disintegration of the capsule. It is.

Preferably, the blending ratio is 40 to 60% by weight.

It is well known that if the amount of glycerin added to gelatin is increased, soft capsules will be obtained, and if the amount added is small, hard capsules will be obtained.

In FIG. 1, reference numeral 1 denotes a capsule body, which is a type of sealed container formed into various shapes, for example, an oval shape, by a capsule film 2 whose main components are gelatin, glycerin, water, etc. In reality, the capsule body 1 does not exist independently, but a capsule filled with the contents exists.

3 is a calcium salt such as calcium carbonate, calcium hydrogen phosphate, calcium lactate, calcium glyconate, etc., which is blended in an appropriate amount in the capsule skin WIz.

In other words, it is blended in a proportion of about 10% by weight or more based on gelatin.

Preferably, the blending ratio is 40 to 60% by weight.

4 is a natural calcium agent such as eggshell, beef bone meal, seashell, etc. The calcium salt 3 mentioned above is the main component, and a mixture of the natural calcium salt is blended into the capsule film 2 in an appropriate amount.

In other words, it is blended in a proportion of about 10% by weight or more based on gelatin.

Preferably, the blending ratio is 40 to 60% by weight.

The contents 5 are medicines, health foods, etc., and are in the form of powder, fruit, liquid, slurry, etc.

6 is a capsule, which is a solid preparation in which the contents 5 are filled into a capsule body 1 made of gelatin as a base.

(Effect) (a) In the invention described in claim 1, calcium salt,
Addition of a natural calcium agent resulted in a significant anti-adhesion effect and improved sliding properties.

In addition, the thickness of the capsule film became thicker, and the influence of air oxidation was reduced.

Furthermore, in the case of natural calcium preparations, there are no legal restrictions on the amount used, so calcium is safe.

(b) In the invention set forth in claim 2, the capsule contains calcium carbonate that generates carbon dioxide gas under acidic conditions in the stomach;
Soft gelatin capsules are quickly and reliably disintegrated.

(Example 1) (1) Compounding ratio of capsule film Gelatin, concentrated glycerin, and various types of calcium forming the capsule film were mixed in the proportions shown in Table 1, such as specimens N00l and N10, and used as samples.

Note that the eggshell calcium agent has calcium carbonate as its main component.

Part 1 table Mixed by

The gelatin solution thus obtained was placed in a soft capsule manufacturing apparatus (not shown), filled with contents 5, and oval 5-shaped capsules 6 were molded in a conventional manner.

In addition, the filling liquid as the above-mentioned content 5 is a fluid, < rough-in is used, the filling amount is 250 mg, and the skin (2) before drying is used.
About the manufacturing method of capsules.

After mixing and stirring gelatin and concentrated glycerin prepared at the mixing ratio shown in Table 1 at a temperature of 60'C until completely dissolved,
(3) Adhesion test method and result conditions (a) Oval 5 type capsule 6 was used as a dry sample, 6
Take 5 samples of 10 samples from each sample, place them randomly in a No. 6 glass sample bottle 7, and keep the bottle mouth open at a constant temperature and humidity of 30'C2 relative humidity (RH) 100%. When stored in the tank for 24 hours, the 6'♀ glass sample bottle 7 was taken out, returned to room temperature, and then the following test was performed.

Condition (b) In the above condition (a), the temperature is 40'''C2 relative humidity (
RH) when changed to 60%.

Below are test 1 for condition (a) and condition (b). Two types of test 2 were conducted.

(Test 1) As shown in Figures 2 and 3, 6 capsules and 1
I knocked down the glass sample bottle 7 contained in j on the desk 8.

Table 2 shows the numerical values (cumulative numerical values) of the capsules 6 that fell from the inner wall of the glass sample bottle 7 at that time.

(Test 2) As shown in FIG. 4, the glass sample bottle 7 was dropped from the desk 8 at heights h=L cm, 3 cm, and 5 cm.

The numerical values (cumulative numerical values) of the capsules 6 that fell from the inner wall of the glass sample bottle 7 at that time are also shown in Table 2.

Table 2 Condition 30''c, RH 100% This value indicates the cumulative number.

All 10 capsules 6 stored under condition (b), that is, a temperature of 40'C and a relative humidity of 60%, fell from the inner wall when the glass sample bottle 7 was only knocked down on the desk 8.

(4) Detailed consideration of the adhesion test results It was found that capsules containing calcium in the capsule film 2 had lower adhesion and greater sliding properties than capsules containing no calcium.

(5) Disintegration test method and results A disintegration test was conducted in artificial gastric fluid at a temperature of 37@C based on the disintegration test method (known) of the Japanese Pharmacopoeia Law.

The results are shown in Table 3.

Incidentally, n=6 means that six capsules of the same type were used and each was subjected to one round test.

Table 3: n=6.

It was about 4 minutes away in terms of destruction time.

(6) Consideration of disintegration test results It was found that capsules containing calcium carbonate in the capsule film 2 had faster disintegration than capsules containing no calcium carbonate.

(7) Method and results for measuring the thickness of the capsule film After the capsule was dried, the center of the capsule of the specimen was cut, and the thickness of the cross section was measured using an Il microscope.

The results are shown in Table 4.

Table 4: n=5 A lucium agent was included, and test tsuba 0 had a calcium-free surface, but according to the measurement results of the film thickness, the film with calcium was approximately 0.08 mm thicker.

(8) Discussion based on the results of film thickness measurement It was found that the film thickness of capsules containing calcium in the capsule film 2 was thicker than that of capsules containing no calcium.

Therefore, it is less affected by air oxidation and has excellent storage stability over time.

(Example 2) Hard capsules were molded by a dipping method using an aqueous gelatin solution to which an eggshell calcium agent was added at a blending ratio of 20% by weight to gelatin.

This capsule was subjected to the same tests as the soft capsule obtained in Example 1, and as a result, improvements in slipping properties, disintegration properties, and increase in film thickness were observed. (Data attachment omitted)

[Brief explanation of the drawing]

Figure 1 is an enlarged perspective view of the main parts of the product of the present invention, Figures 2 to 4
The figure is a front view of the product of the present invention being tested for adhesion. 1... Capsule body 2. Φe capsule membrane 6...
capsules

Claims (2)

[Claims] (1) Capsules with improved gliding properties that contain calcium salts or natural calcium agents containing calcium salts as the main ingredient, such as eggshells, beef bone meal, shells, etc., at a ratio of about 10% by weight or more to gelatin. (2) Calcium carbonate among calcium salts or natural calcium agents such as eggshells and seashells containing calcium carbonate as a main component are blended at a ratio of about 10% by weight or more to gelatin to improve sliding and disintegration properties. improved capsule