JP2003073262A - Inclusion coating agent for solid preparation, the resultant solid preparation, method for producing the same, and foods - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an inclusion coating agent for solid preparations which are hopeful of applications to e.g. pharmaceuticals, supplements, foods, confectionery, to provide such solid preparations, to provide a method for producing one of the preparations, and to provide foods as such preparations. SOLUTION: This method for producing one of the solid preparations comprises spraying a medicinal component with 1-40 wt.% of a reducing sparingly digestible dextrin in the form of an aqueous solution followed by drying to effect including the medicinal component into powder or granules, or tablets by compression, or capsules by encapsulation.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an inclusion coating agent for solid preparations, solid preparations, a method for producing the same, and foods, which are expected to be used in, for example, pharmaceuticals, health supplements, foods, confectionery and the like. Regarding

[0002]

2. Description of the Related Art Conventionally, when granulating powder raw materials,
It has been carried out using sugar such as starch, gelatin, sucrose, or lactose, natural rubber, and microcrystalline cellulose as a binder. These binders play the role of a glue for fixing the powders to each other during preparation of the preparation and food granules, facilitating the manufacture of granules, and further facilitating the manufacture of tablets and capsules using the granules. But,
With the granules, tablets, and capsules produced with these binders, effects other than the above-mentioned granulation action cannot be expected. Further, in ingestion, a predetermined amount of the medicinal component is taken into the body at a time, so that the side effect of the medicinal component is reduced and the efficacy is maintained, the absorption rate in the body is controlled and the medicinal component is Various techniques have been proposed in which a material that delays the release rate is used as a foreskin material. For example, Japanese Patent Application Laid-Open No. 5-310598 discloses a technique of controlling the release of a medicinal component with polyglycerin fatty acid ester. Further, Japanese Patent Laid-Open No. 5-221854 discloses that
A technique for controlling drug efficacy with hydroxypropylmethyl cellulose is disclosed in Japanese Patent Publication No. 8-52061, which is a technique for prolonging drug efficacy with an excipient containing a heteropolysaccharide gum and a cationic cross-linking agent, JP-A-6-206833. The official gazette discloses a technique of delaying the drug effect by using hemicellulose and an auxiliary agent as an outer coat or a sugar coating agent.

[0003]

As described above, many absorption (release) inhibitors have been proposed and disclosed in the past, but the concept is to maintain the efficacy of the medicinal components at once. It is common in that it avoids a transient high blood concentration that occurs when a large amount of a medicinal component is consumed (absorbed in the living body). That is, when the absorption rate is high and a high blood concentration is produced, the blood concentration is rapidly lowered, and the drug efficacy period is short. However, in order to maintain a predetermined blood concentration, it is necessary to increase the amount of the medicinal component to be taken. According to the studies by the present inventors, the above-mentioned various materials can achieve a predetermined purpose of suppressing the absorption rate of the medicinal component in vivo and maintaining the efficacy to some extent, but only a part of the medicinal component. Was absorbed, and most of the remaining medicinal components were decomposed and excreted without being absorbed in the living body. Therefore, the present inventors aim to propose a technique capable of improving the absorption rate in vivo and the penetration rate into blood, and enabling high blood concentration and long-term blood concentration maintenance. To do.

[0004]

The present invention has been proposed in view of the above, and proposes an inclusion coating agent for a solid preparation, which is characterized by comprising a reduced indigestible dextrin. Further, the present invention is 1 to 40% by weight with respect to the medicinal component.
Also included is a solid preparation which is characterized in that it is incorporated or coated with the reduced indigestible dextrin of (1) to form a powder or granules, or it is compressed into tablets or capsules. suggest. Further, the present invention provides
1 to 40% by weight of the reduced indigestible dextrin with respect to the medicinal component is sprayed or kneaded in the form of an aqueous solution and dried to obtain a powder or granules, or a tablet or a tablet thereof. We also propose a method for producing a solid preparation characterized by being filled in a capsule. In addition, the present invention, 1 to 40% by weight of water-soluble dietary fiber is added to the medicinal component to be included or coated to form a powder or granules, which is used as a food material in health foods and confectionery raw materials. Food products characterized by being mixed are also proposed.

[0005]

BEST MODE FOR CARRYING OUT THE INVENTION As the medicinal ingredient used in the present invention, a pharmaceutical agent or a health supplement ingredient can be used.
Generally, a water-soluble solid (powder) is used, but it may be oil-soluble, liquid, or gel.

The reduced indigestible dextrin used in the present invention improves the absorption rate of the medicinal component in the body and the penetration rate into the blood, has a high blood concentration, and maintains the blood concentration for a long time. The amount of the reduced indigestible dextrin added to the medicinal component is 1 to 40% by weight as described above,
If it is less than 1% by weight, the above-mentioned predetermined effect cannot be obtained. On the other hand, when it is more than 40% by weight, no further increase in the effect is observed and the compounding amount of the medicinal component is limited, which is not preferable.

Further, when a surfactant such as glycerin fatty acid ester or sucrose fatty acid ester is used together with the above-mentioned indigestible dextrin, the in vivo absorption rate and blood are higher than in the case where only the indigestible dextrin is used. The permeation rate into the blood is higher, the blood concentration is higher, and the blood concentration is maintained for a longer period of time. The amount of the surfactant added to the medicinal component is 1 to 20% by weight, but 1% by weight
If it is less, the above-described predetermined effect cannot be obtained.
On the other hand, if it is more than 20% by weight, no further increase in the effect is observed and the compounding amount of the medicinal component is limited, which is not preferable.

In the present invention, 1 to 4 are added to the medicinal component.
By spraying or kneading 0% by weight of a reduced indigestible dextrin in the state of an aqueous solution and drying it, the absorption rate of the medicinal component in the body and the penetration rate into the blood are improved, resulting in high blood concentration and long-term concentration. It is possible to maintain the blood concentration of. It is possible to maintain high blood concentration and long-term blood concentration,
This means that the amount of the medicinally active ingredient that is wastedly decomposed and discharged is suppressed, and that it is more efficiently absorbed into the living body. Further, the above-mentioned effect is compared with the case of the same amount of only the medicinal component which does not use reductive indigestible dextrin, and in order to suppress unnecessary high blood concentration, the amount itself is reduced. Can be adjusted. That is, in the present invention, since the medicinal component is absorbed very efficiently in the living body, compared to the case of only the medicinal component that does not use the conventional reductive indigestible dextrin even if the amount of the expensive medicinal component used is greatly reduced. The same or higher effect can be expected.
The obtained product may be in the form of powder or granules, or it may be tableted into tablets or filled in capsules, but the capacity and cost can be reduced.

[0009]

The present invention will be described in more detail by the following examples, but the present invention is not limited to these examples. Prior to the examples, the test method used in each example will be described.

[Experimental Group and Samples, Preparation Thereof] Samples of groups 1 to 5 were prepared with the material compositions shown below.

Group 1 sample: Vitamin C ························································································································· Vitamin C powder A reducing or indigestible dextrin is added in the form of an aqueous solution or an alcohol-containing aqueous solution, and then kneaded and then dried or spray-dried to obtain a powder or granular solid preparation in which vitamin C is incorporated or coated with the reduced indigestible dextrin. It was

Group 2 sample; Vitamin C: 92% by weight Reduction indigestible dextrin: 5% by weight Glycerin fatty acid ester: 3% by weight 5% by weight The reduction resistant indigestible dextrin and the glycerin fatty acid ester were included or coated in the same manner as the preparation of the above-mentioned Group 1 sample except that a mixture of the reduced resistant digestive dextrin and 3% by weight of glycerin fatty acid ester was used. A powdery or granular solid preparation was obtained.

Sample of Group 3; Vitamin C ····· 80% by weight reduced indigestible dextrin ··· 20% by weight Except that 20% by weight of reduced indigestible dextrin was used. In the same manner as in the preparation of the sample of the first group, a powdery or granular solid preparation in which vitamin C was incorporated or coated with reducing indigestible dextrin was obtained.

4 group sample: Vitamin C ······ 77% by weight reduction indigestible dextrin ··· 20% by weight Glycerin fatty acid ester ··· 3% by weight 20% by weight Vitamin C was ingested or coated with reduction-resistant digestive dextrin and glycerin fatty acid ester in exactly the same manner as in the preparation of the above-mentioned Group 1 samples except that a mixture of reduction-resistant digestive dextrin and 3% by weight of glycerin fatty acid ester was used. A powdery or granular solid preparation was obtained.

Group 5 sample: Vitamin C: 100% by weight Vitamin C alone was used as a sample (sample without inclusion coating agent).

[Method of Administering Animal Group and Sample] 1 to 5
For each group of samples, 6 male rats were used for each group before experiment 1
Preliminary breeding for a week was performed. During this preliminary breeding period, water and feed were freely ingested and the animals were bred in a 12-hour day / night cycle. In addition, the feed during the preliminary breeding period and the experiment period was a normal breeding feed. The samples in each group were administered by oral sonde within the same time after suspending an amount corresponding to 100 mg / kg of vitamin C in a fixed amount of purified water.

[Measurement of Vitamin C Concentration in Blood] Immediately before administration of the sample, 1 hour, 2 hours, 3 hours, 6 hours after administration,
Blood was collected after 9 hours, 12 hours, and 24 hours, and the vitamin C concentration in blood was measured.

[Experimental Results] The vitamin C concentration in blood at each time is shown in Table 1, and the transition thereof is shown in FIG.

[Table 1] The pharmacokinetic parameters are shown in Table 2.

[Table 2]

From Tables 1 and 2 and FIG. 1, the absorption of vitamin C in rats of the groups 1 to 4 produced according to the present invention is significantly higher than that of the vitamin C alone, which is the sample of group 5. It was confirmed that the concentration was improved and that the high concentration was maintained continuously. In particular, the 2nd group sample and the 4th group sample in which reduction resistant indigestible dextrin and glycerin fatty acid ester were used in combination showed higher absorbability than the 1st group sample and the 3rd group sample using only the reduction resistant indigestible dextrin, and moreover, in the blood. It was confirmed that the vitamin C concentration can be maintained at a high level. Although such an effect tends to be enhanced depending on the amount of only the reduced resistant digestive dextrin sprayed, the results were further enhanced by further spraying the glycerin fatty acid ester. This concentration was about 14 in the 1st group compared with the 5th group in the pharmacokinetic parameter AUC.
It increased to 0%, and about 17 when the number of groups increased to 3
It had increased to 0%. In addition, in the case of the 2 groups, it increased further, showing a pharmacokinetics of more than double that of about 210%,
There is almost no change in group 4 compared to group 2. From these results, it became clear that in the present invention, in the formulation of spraying only the indigestible dextrin on the medicinal component, the function is sufficiently exerted in the range of 5 to 20% by weight. Further, preferably, a more preferable action is observed in a preparation produced by further spraying about 3% of glycerin fatty acid ester at the same time.

[0020]

INDUSTRIAL APPLICABILITY As described above, according to the present invention, 1 to 40% by weight of reductive indigestible dextrin is sprayed in the form of an aqueous solution to the medicinal component and dried to include or coat the medicinal component. The absorption rate in vivo and the penetration rate into blood are improved, and high blood concentration and long-term blood concentration can be maintained. Therefore, in the present invention, the medicinal ingredient is extremely efficiently absorbed in the living body, and even if the amount of the expensive medicinal ingredient used is greatly reduced, it is equivalent to the case where only the medicinal ingredient not using the conventional reductive indigestible dextrin is used. Alternatively, a higher effect can be expected. Further, the obtained product may be in the form of powder or granules, or may be tableted by compressing it, or may be in the state of being filled in a capsule, but the capacity and cost can be reduced in any form. be able to.

[Brief description of drawings]

FIG. 1 is a graph showing changes in blood vitamin C concentration after administration of various samples of solid preparations in Examples of the present invention.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61K 47/14 A61K 47/14 47/36 47/36 B01J 2/00 B01J 2/00 B 2/04 2 / 04 2/22 2/22 // A61K 31/375 A61K 31/375 (72) Inventor Nobuhide Kaizu 2-10-17 Aketsumi, Setagaya-ku, Tokyo F-term (reference) 4B018 LE02 MD10 MD25 MD36 MF08 4B035 LC06 LE01 LG10 LG17 LG18 LK09 LP36 4C076 AA38 AA41 AA55 AA67 AA94 BB01 CC24 DD47F EE38H FF21 FF32 FF43 GG09 GG12 4C086 AA01 BA18 MA02 MA03 MA05 MA34 MA35 MA37 MA38 MA41 NA10 NA12 ZC28 4G004 BA00 EA00 EA00

Claims (6)

[Claims] 1. An inclusion coating agent for a solid preparation, which comprises a reduced indigestible dextrin. 2. The inclusion coating agent for a solid preparation according to claim 1, which contains a surfactant together with the reduced indigestible dextrin. 3. A medicinal ingredient is added with 1 to 40% by weight of a reduced indigestible dextrin, and is included or coated to obtain a powder or granules, or a tablet is obtained by compressing it. A solid preparation characterized by being filled in a capsule. 4. A reduction indigestible dextrin together with 1-2.
The solid preparation according to claim 3, wherein 0% by weight of a surfactant is added. 5. A 1-40% by weight reducing indigestible dextrin based on the medicinal component is sprayed or kneaded in the form of an aqueous solution and dried to give a powder or granules, or a tablet obtained by tableting the same. A method for producing a solid preparation, which is characterized in that it is filled into a capsule or a capsule. 6. A 1-40% by weight reduction-resistant indigestible dextrin is added to a medicinal component to be included or coated to form a powder or granules, which is used as a food material in health foods and confectionery raw materials. Foods characterized by being mixed.