JP2007117181A - Soft capsule - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a soft capsule using a wrapping material of little disintegration delay, excellent temperature resistance and stable quality using a raw material not derived from animal. <P>SOLUTION: As the wrapping material of the capsule, hydroxypropyl cellulose and/or hydroxypropyl methylcellulose is used. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to a soft capsule, and more particularly to a soft capsule manufactured using two encapsulating film sheets.

  One type of capsule is a so-called soft capsule, most of which uses gelatin as an encapsulant (capsule), and its typical production method is liquid, pasty, powdery, etc. This is a method in which a product is encapsulated with an encapsulating material that is increased in plasticity by adding a polyhydric alcohol such as glycerin or sorbitol to gelatin, and then molded into a certain shape under heat.

  That is, the contents are filled between two encapsulating film sheets, and the two encapsulating film sheets are melt bonded by pressing and heating, and are cut and dried.

  However, gelatin, which is conventionally used as an encapsulating material, is manufactured from animals such as cattle, pigs, birds, and fish, and its essence is a protein. There is a drawback that it is necessary to remove the sex protein molecule and it is difficult to remove it. In addition, since conventional capsule encapsulating materials such as gelatin are mainly thermoreversible gels (rosset gels), they are easily affected by temperature, and can be deformed under temperature changes during product distribution and storage conditions at high temperatures. There were defects such as elution of the contents.

  In addition, this gelatin used as a soft capsule encapsulating material is entangled with complex actions based on heat, light, colorants (eg caramel), natural (animal) derived materials, etc. It is a material whose solubility is gradually reduced, and as a result, it tends to cause a collapse delay. In fact, for example, blueberries, garlic, minerals, ascorbic acid and the like often cause a delayed decay.

  Recently, plant-derived pullulan is sometimes used as an encapsulating material for hard capsules, but the quality retention performance of the contents of hard capsules is greatly reduced compared to conventional gelatin and the like. For this reason, pullulan has never been used as a material for soft capsules.

  The problem to be solved by the present invention is to solve the above-mentioned drawbacks of conventional soft capsules, more specifically, using raw materials not derived from animals, having little decay delay, and having excellent temperature resistance and It is to develop a new soft capsule using a stable quality encapsulant.

  This problem is solved with respect to soft capsules by using an encapsulant made of hydroxypropylcellulose and / or hydroxypropylmethylcellulose.

  The encapsulating material used in the present invention is hydroxypropyl cellulose (hereinafter referred to as HPC) and / or hydroxypropyl methylcellulose (hereinafter referred to as HPMC).

  Hydroxypropyl cellulose is a high molecular weight material with surface activity and has excellent functions as an edible film forming agent, coating agent, protective colloid agent, foam stabilizer, emulsion stabilizer (oil-in-water type), dispersant, thickener, etc. Have When the aqueous solution is heated, the viscosity increases and gels, but when it is cooled, it returns to the original solution state. However, this hydroxypropyl cellulose has never been used as an encapsulating material for soft capsules.

Hydroxypropyl methylcellulose (hereinafter referred to as HPMC) used in the present invention is a compound represented by [C ₆ H ₇ O ₂ (OH) _X (COH 3) _Y (OCH) ₂ CHOHCH ₃ ) _Z ] _n The substituted structure has a molecular weight of 162.14, a molecular weight of about 180 at a substitution degree of 1.19, about 210 at a substitution degree of 2.37, a molecular weight of 13,000 at an n of about 70, and a molecular weight of about 200 at an n of about 1000. , 000.

  This hydroxypropyl methylcellulose (HPMC) is a mixed ether of methyl and hydroxypropyl cellulose and is prepared by reacting cellulose fibers with caustic soda, methyl chloride, propylene oxide.

  In Japan, it is listed in the second part of the Japanese Pharmacopoeia (listed from the 10th revision (announced in April 1981)), tablet, granule coating agent, binder, syrup suspension stabilizer. , Used as a thickener for poultices, water retention agent and cartilage. However, this HPMC has never been used as an encapsulating material for soft capsules.

  The present inventor has recognized that it is extremely important to develop a new encapsulating material other than the conventional gelatin in order to eliminate the difficulty of the encapsulating material of the conventional soft capsule, and many years of research As a result, the inventors have found that this HPC and / or HPMC can be a very excellent soft capsule encapsulating material, and have completed the present invention.

  In the present invention, as described above, the case where HPC and HPMC are used alone or in combination is included, but particularly when HPC and HPMC are used in a specific ratio, the synergistic action is caused. Thus, the oxygen barrier property of the obtained soft capsule is remarkably improved. In this case, the ratio (% by weight) of HPC: HPMC is 95.0: 5.0 to 99.9: 0.1 or 5.0: 95 to 0.1: 99.9, preferably 99.0: 1. 0-99.9: 0.1 or 1.0: 99.0-0.1: 99.9. Outside this range, synergy is not expected.

  In the present invention, an organic acid can be further added as a third component to HPC and / or HPMC. By adding this third component, the acid resistance is remarkably improved.

  Typical examples of the organic acid in this case include citric acid, malic acid, fumaric acid, tartaric acid, ascorbic acid and the like. The amount used is usually 0.1 to 3.0 with respect to 100 parts by weight of HPC and / or HPMC.

  In the present invention, the method itself for producing a soft capsule using an encapsulating material may be performed using a conventional method, and a representative example thereof is a method using a conventional rotary capsule filling machine. It can be illustrated.

  In the present invention, other gelling agents and additives can be added to the encapsulating material as required, for example, pearlizing agents such as gelatin, seaweed extract, agar, pigment, fish phosphorus foil, various vitamins, etc. Etc. can be illustrated.

  In the present invention, HPC and / or HPMC is used as a capsule material to form a capsule, and various components can be widely used as the capsule contents at this time. Royal jelly, garlic extract, minerals, ascorbic acid, etc. can also be used.

  The encapsulating material of the present invention is not derived from animals or plants, is less prone to decay delay, can be produced industrially stably, and therefore has no difficulty with conventional gelatin, There is no difficulty in storage conditions under temperature changes or high temperatures, and an extremely excellent capsule can be provided.

  Hereinafter, the present invention will be described in detail with reference to examples. However, in the following examples,% indicates% by weight.

HPC ... 30%
Glycerin 9%
Water ... 61%
Soybean oil containing 50% blueberry extract powder in a capsule film produced according to a conventional method while heating and mixing the above ingredients at a predetermined ratio, degassing, applying to a rotary capsule filling machine, spreading and drying. Was filled into a soft capsule with an internal volume of 300 mg. The capsules were stored under conditions of 40 ° C. and RH 75%, and the change in disintegration time was measured using water as a solvent, and the results shown in Table 1 were obtained.

Comparative Example 1

  In Example 1 above, the components used were the following components, and all other components were treated in the same manner as Example 1. The change in disintegration time at this time was measured in the same manner, and is also shown in Table 1 below.

Gelatin 45%
Glycerin 5%
Water: 50%

  In Example 1 above, the components used were the following components, and all other components were treated in the same manner as Example 1. The change in the decay time at this time was measured in the same manner. The result was 12.0 min at filling and 11.4 min after 3 months.

HPMC ... 25%
Sorbitol ... 5%
Water ... 70%

  In Example 1 above, garlic extract powder was used in place of the blueberry extract powder, and everything else was processed in the same manner as Example 1. Further, at this time, the disintegration time was measured, and it was 13.0 min at filling and 12.8 min after 2 months.

HPC ... 20%
Water ... 80%
The above two components are heated and mixed homogeneously, degassed and spread while drying with a spreader attached to a rotary capsule filling machine, and commercially available DHA oil (containing 46% as DHA) is obtained by a conventional method. Filled to make a soft capsule with an inner volume of 250 mg, stored under the conditions of 40 ° C. and RH 75%, and measured the peroxide value (meq / kg) of the filling over time. Obtained.

  In Example 4, instead of HPC 20% and water 80%, HPMC 20% and water 80% were used, and everything else was processed in the same manner as in Example 4 to obtain capsules. The results of measuring the peroxide value (meq / kg) of this product in the same manner are also shown in Table 2.

  In Example 4 above, the components used were the following components, and everything else was treated in the same manner as in Example 4 and the peroxide value (meq / kg) was measured in the same manner. The results are shown in Table 2 below.

HPC ... 19.5%
HPMC ... 0.5%
Water: 80.0%

HPMC ... 19.5%
HPC: 0.5%
Water: 80.0%

HPC 22.5%
Glycerin ... 2.0%
Citric acid: 0.5%
Water ... 75.0%
The above four components were heated and mixed, degassed, spread on a rotary capsule filling machine, spread and dried, and then filled with commercially available grape seed oil by a conventional method to produce a soft capsule having an internal volume of 270 mg. The capsule was subjected to a disintegration test using water, artificial gastric fluid (PH1.2) and artificial intestinal fluid (PH6.8), and the results shown in Table 3 were obtained.

  In Example 8 above, citric acid was not used and glycerin was adjusted to 2.5%, and the others were all treated in the same manner as in Example 8, and the disintegration test was conducted in the same manner. The results are also shown in Table 3.

  In Example 8 above, the components shown below were used, and everything else was processed in the same manner as Example 8 to produce soft capsules. The disintegration test of this thing was similarly implemented. The measurement results are shown in Table 4.

HPMC 22.0%
Sorbitol ... 2.0%
Apple cider vinegar ... 1.0%
Water ... 75.0%

  In Example 10 above, malic acid was not used and the water content was 76.0%, and everything else was processed in the same manner as in Example 10 to prepare soft capsules. This was subjected to the same disintegration test. The results are also shown in Table 4.

Claims (3)

  A soft capsule comprising at least one of hydroxypropylcellulose and hydroxypropylmethylcellulose as an encapsulating material for a soft capsule.   The ratio (% by weight) when the hydroxypropylcellulose and hydroxypropylmethylcellulose are used in combination is 95: 5 to 99.9: 0.1 or 5:95 to 0.1: 99.9. Item 2. A soft capsule according to Item 1. The soft capsule according to claim 1 or 2, further comprising an organic acid as a third component in the encapsulating material.