JPS6115831A - Rapidly disintegrable hard gelatin capsule - Google Patents

Abstract

PURPOSE:The titled hard capsule, obtained by incorporating gelatin with sodium hydrogencarbonate in a specific proportion, having constant rapid disintegrating property in the stomach, slightly affected by change with time, and easily preparable at a low cost. CONSTITUTION:A rapidly disintegrable hard gelatin capsule obtained by incorporating gelatin with 1-20wt%, particularly 5-10wt% sodium hydrogencarbonate. The above-mentioned capsule is prepared according to the conventional method, but a gelatin solution, to which the sodium hydrogencarbonate is added, must be adjusted to neutral - alkaline, e.g. 7.5-8.9pH. The temperature in operation is preferably kept at 40-45 deg.C. The capsule is decomposed under acidic conditions in the stomach by evolving gaseous carbon dioxide, which is capable of disintegrating the above-mentioned capsule rapidly and surely.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to hard gelatin capsules, and more particularly to hard gelatin capsules having a constant rapid disintegration property. As used herein, the term "capsule" refers to a capsule membrane that contains contents such as medicine, and when it contains contents, it is called a capsule.

l! Latin hard capsules are mainly used to make astringent or irritating drugs easier to take internally, and with some exceptions such as enteric-coated capsules, they disintegrate quickly in the stomach. However, it is desirable to release the contents into the stomach.

However, the quality of gelatin, which is the basis of hard capsules, varies depending on the raw material and the type of gelatin, and therefore, capsules manufactured from gelatin have a high RFD Ia.
14 is not constant. Furthermore, during long-term storage, U-latin capsules undergo changes in eaves time due to various reasons, resulting in a decrease in disintegration. It is not uncommon for this to become a clinical problem.

LIJL order Therefore, conventionally, jelly strength A3 and viscosity are constant (1 or less, using gelatin as a raw material, or using t!Latin as a protein, adding proteolytic enzymes to C Labun, etc.) 1), methods have been proposed to promote the disintegration of force J leeches. However, the disintegration properties of capsules manufactured by these methods are not necessarily constant, and the change in R over time It is not possible to completely avoid the effects. First, these manufacturing methods have the disadvantage of high production costs, and are not completely satisfactory. Therefore, they are more practical and faster. Tagawa, a disintegrating hard capsule, is still desired.

[111] In view of the above-mentioned circumstances, the present inventor has created a gelatin hard capsule that rapidly disintegrates in the stomach, has a constant disintegrating property, and is difficult to be affected by changes over time. And low□
As a result of intensive research with the aim of developing a cost-effective manufacturing method, we found that if hard capsules were manufactured by blending sodium bicarbonate, which has traditionally been frequently used in the food and pharmaceutical fields, with gelatin, this sodium bicarbonate The present inventors have discovered that the 1-latin hard capsule is decomposed by generating carbon dioxide gas under acidic conditions in the stomach, and that the generated gas quickly and reliably disintegrates the 1-latin hard capsule, leading to the completion of the present invention.

That is, the present invention provides a hard gelatin capsule made by blending sodium bicarbonate with gelatin.

The blending ratio of sodium bicarbonate in the gelatin hard capsule of the present invention can be 1 to 20% by weight relative to gelatin. When used in excess of this range, sodium bicarbonate precipitates during the drying of the capsules, and not only does the film, which should be transparent, become translucent, but it also fails to maintain sufficient strength. On the other hand, if it is less than 1%,
There is a possibility that rapid disintegration properties may not be obtained. Therefore, it is appropriate to select from within the above range, and a particularly preferred blending ratio is 5 to 10% by weight ω.

In order to produce the hard gelatin capsules of the present invention, an appropriate amount of carbonated water and sodium chloride may be added to and dissolved in a gelatin solution prepared according to a general recipe, and then molded in a conventional manner. However, it is necessary to pay attention to the following points. Sodium bicarbonate decomposes below 17.5 and generates carbon dioxide gas, so the gelatin solution to which sodium bicarbonate is added should be adjusted to neutral or weakly alkaline, for example IIH 7.5 to 8.9. is necessary.

In general, since sodium hydrogen carbonate decomposes and foams when heated in an aqueous solution state, it is necessary to maintain the temperature during operation at 40° C. or lower.

Generally, it is preferable to maintain the gelatin solution at a temperature of 40 to 45° C. in consideration of temperature for smooth molding operations.

Under the conditions described above, a gelatin solution containing sodium bicarbonate is prepared, coloring agents, fragrances, etc. are added as desired, and the capsule is formed into capsules of any size using ordinary capsule manufacturing equipment. A hard gelatin capsule of the invention can be obtained. Although the hard capsules of the present invention can be manufactured using gelatin raw materials for ordinary capsule manufacturing, sufficient rapid disintegration properties can be obtained; however, if necessary, they may be treated with low-viscosity gelatin or succinic acid. It can also be produced using gelatin treated with gelatin, single gelatin treated with alkali, or a mixture of two or more of these gelatin. In such cases, even more rapid disintegration properties can be expected.

[Bile 11 The Relatin hard capsule of the present invention contains sodium bicarbonate, so when taken, the sodium bicarbonate quickly decomposes under acidic conditions in the stomach, and the carbon dioxide gas generated at this time easily decomposes. Collapse and cover. Since this collapse of the capsule is caused by the generation of carbon dioxide gas, it is less affected by the properties of the raw material gelatin or by insolubilization due to changes in the capsule over time. Therefore, constant and reliable rapid disintegration can be achieved. Furthermore, the hard capsules of the present invention can be easily produced by simply adding sodium bicarbonate to a gelatin solution, and therefore are low cost, suitable for industrialization, and extremely practical.

The present invention will be explained in detail by giving examples below.

Example 1 7 ko of gelatin to 14 ko of distilled water! 60 minutes while stirring.
℃ to completely dissolve. To this solution was added 975 ml of titanium oxide aqueous dispersion (21.8% by weight), and then l
) H was adjusted to about 8.0.

To this gelatin solution, 350 g of sodium hydrogen carbonate (concentration of 5% by weight relative to gelatin, 1.5% by weight in gelatin solution) was added as an aqueous solution, and the viscosity was appropriately adjusted, followed by defoaming treatment by a conventional method. Obtained like this #:! The Latin solution was charged into a capsule manufacturing device and molded into a size 10 capsule.

-〇- The dissolution time and disintegration time of the capsules of the present invention were measured according to the test method described in the 10th edition of the Japanese Pharmacopoeia (1981). Capsules prepared in the same manner without the addition of sodium bicarbonate served as a control. The results are shown in Table 1 below. The dissolution time was expressed as the average value of five sample capsules, and the disintegration time was expressed as the average value of six sample capsules.

(Left below) Hard gelatin capsules were obtained in the same manner as in Example 1, except that 10% by weight of sodium hydrogen carbonate was added to the gelatin.

This hard capsule showed the same shortening effect on dissolution time and disintegration time as the capsule obtained in Example 1.

Claims (1)

[Claims] 1-20% by weight of sodium bicarbonate based on gelatin
Rapidly disintegrating gelatin hard capsules containing the following ratio: