JPS59172417A - Soft capsule containing riboflavin butyrate - Google Patents

Abstract

PURPOSE:To obtain the titled transparent soft capsule stable to light and having beautiful appearance, by coating a drug containing riboflavin butyrate useful as a remedy for arteriosclerosis and a tocopherol compound with a film-forming agent containing a specific pigment. CONSTITUTION:A drug containing riboflavin butyrate and a tocopherol compound is coated with a film-forming agent containing a pigment capable of absorbing the light of 300-500nm, preferably 400-500nm in wavelength (e.g. Food Yellow 5, Food Yellow 4, beta-carotene, etc.). Food Yellow 5 is especially suitable as the pigment. The addition of the pigment of the film-forming agent enables to avoid the decomposition of riboflavin butyrate simultaneously to the melanization caused by the photo-reduction reaction of riboflavin butyrate with tocopherol. The tocopherol is effective to mitigate the disorder of the peripheral blood flow.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to transparent soft capsules containing riboflavin butyrate and tocopherols as active ingredients. ' Riboflavin butyrate is known to have excellent effects on the prevention and treatment of arteriosclerosis, and is used in powder form as tablets, granules, or powders, or dissolved in oil as soft capsules. ing. The present inventors prepared soft capsules by mixing riboflavin butyrate with tocopherols for the purpose of slowing down peripheral blood circulation disorder. I learned that items stored under scattered light exhibit a blackening phenomenon and lose their commercial value.'17-
9 The present inventors have conducted various studies to solve these drawbacks, and as a result, have completed the present invention.

That is, the drug containing the present invention's acetic acid ester and tocopherols was applied at a wavelength of 300 to 550 nm.
This is a transparent soft capsule containing riboflavin butyrate encapsulated with a film-forming agent containing a pigment that absorbs light.

According to the findings of the present inventors, the aforementioned blackening phenomenon occurs as a result of the photoreduction reaction of riboflavin butyrate ester with tocopherols. Furthermore, it has been revealed that riboflavin butyrate is decomposed in oil by peroxides derived from linoleic acid, etc. in oil.

Therefore, the present inventors added 300 to 550 nm, preferably 400 nm, to the film forming agent as a means to simultaneously avoid these blackening phenomena and the decomposition of riboflavic acid butyester.
It has been found that by containing a dye that absorbs light of ~500 nm, transparent soft capsules that are stable against p1 light and have a beautiful appearance can be obtained.

First, in order to produce the soft capsules of the present invention, riboflavin butyrate and tocopherols are mixed and dissolved in oil to obtain an oil liquid for filling soft capsules.

Soft capsules can be prepared by filling this filling oil liquid between, for example, two belt-shaped film-forming agents and pressing the film-forming agent from both sides with a mold. As a method for preparing soft capsules, an automatic rotary set, a semi-automatic Colton method, a manual flat plate method, etc. can be adopted. The shape of the soft capsule can also be variously spherical or elliptical.

Examples of the oils used in the present invention include wheat germ oil, rice oil, safflower oil, soybean oil, rapeseed oil, corn oil, peanut oil, mono-, di- and triesters of fatty acids having 4 to 18 carbon atoms, or mixtures thereof. Can be mentioned. Additionally, additives such as sweeteners and flavoring agents can be added as appropriate.

Examples of film-forming agents for soft capsules include gelatin, but in order to prevent atmospheric moisture from migrating into the soft capsules, sorbitol is added in an amount of 10 to 30%, preferably 15 to 25%, based on gelatin. It is preferable to use it in the range of %. The amount of the pigment added is 0.4 to 1% based on the weight of the film.

In the present invention, the ratio of riboflavin butyrate to tocopherols is preferably 4 to 20 times that of riboflavin butyrate. Tocopherol used/”#4!: L, Tetj: a-α-tocopherol, dJ-α-tocopherol, acetic acid d-α
-tocopherol, natural tocopherol (CMTO), and the like.

In addition, examples of pigments that absorb light at 600 to 500 r+m include Food Yellow No. 5, Food Yellow No. 4, gardenia (crocin), β-carotene, safflower yellow, and curcumin, among which Food Yellow No. 5 is particularly good. These dyes are used after being uniformly dispersed in a film forming agent.

Next, in order to concretely illustrate the history of the present invention, examples will be given and explained.

Example 1 All of the components shown in Table 1 below were dissolved by heating to obtain a uniform oil solution for filling capsules. Further, each component shown in Table 2 was mixed and dissolved by heating to prepare a film forming agent.

Soft capsules were manufactured using the above-mentioned filling oil and film-forming agent using an automatic rotary type filling machine.

The obtained soft capsules were placed on a sunny day under direct sunlight (0,
0459θrg/rust 2·min) for 7 days, and changes in appearance were observed. The test results are shown in Table 6.

Table 2 Soft Capsule Film Forming Agent Prescription Example 2 Each component shown in Table 4 below was heated to obtain a uniform oil solution for filling capsules. Further, each component shown in Table 5 was mixed and dissolved to prepare a film forming agent.

Soft capsules were manufactured using the above-mentioned filling oil and film forming agent using an automatic rotary capsule filling machine.

The obtained soft capsules were stored under direct sunlight for 7 days in a sunny mortar, and changes in appearance were observed. The test results are shown in Table 6.

Table 4 Oil liquid formulation for soft capsule filling Table 5 Soft capsule film forming agent formulation

Claims (1)

[Claims] A soft capsule containing riboflavin butyrate, characterized in that a drug containing riboflavin butyrate and tocopherols is encapsulated with a film-forming agent containing a pigment that absorbs light in the wavelength range of 600 to 550 nm.