JP3585306B2 - Antiseptic / antifungal agent - Google Patents
Antiseptic / antifungal agent Download PDFInfo
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- JP3585306B2 JP3585306B2 JP00449796A JP449796A JP3585306B2 JP 3585306 B2 JP3585306 B2 JP 3585306B2 JP 00449796 A JP00449796 A JP 00449796A JP 449796 A JP449796 A JP 449796A JP 3585306 B2 JP3585306 B2 JP 3585306B2
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- Prior art keywords
- nicotinamide
- capsule
- fatty acid
- antiseptic
- present
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- Medicinal Preparation (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Description
【０００１】
【産業上の利用分野】
本発明はニコチン酸アミド及びショ糖脂肪酸エステルを含むカプセルに関する。
【０００２】
【従来技術】
食品、医薬品等の保存性を高めるため、防腐防黴の手段を講じることが必要であり、その手段の一つとして防腐防黴剤を添加することが広く行われている。従来、防腐防黴剤としてパラオキシ安息香酸エチル、パラオキシ安息香酸プロピル、ソルビン酸等が使用されてきた。しかし、近年添加物の安全性に関する懸念から天然添加物が注目され、防腐剤の分野においても種々検討されている。同時に、既存のものであっても、防腐防黴効果を有するものを探索する努力も続けられている。例えば、特開平６−１０５６７３号公報にはニコチン酸を有効成分とする食品用制菌剤が開示され、また、特開昭５１−３２７３５号公報にはグリシン及びシスチンにさらにアスコルビン酸及び／又はニコチン酸を添加することを特徴とする食品の保存法が開示されている。一方、ショ糖脂肪酸エステルも抗菌作用を有することが知られている（防菌防黴、第５巻（No.7）１頁〜１３頁（１９７７年））。
【０００３】
【発明が解決しようとする課題】
上記の既存の化合物の防腐防黴効果は充分なものではない。また、特開昭５１−３２７３５号公報にはニコチン酸アミドには抗菌作用がないと記載されており、また、防菌防黴第５巻には、多くの既存物質の抗菌効果が記載されているが、特定の組み合わせにより、防菌防黴効果が相乗的に増加されることに関する記述はほとんどない。本発明者は、既存化合物の防腐防黴効果を鋭意検討した結果、意外にもニコチン酸アミド及びショ糖脂肪酸エステルを組み合わせることにより、効果が顕著に増強されることを見出し本発明を完成させた。
【０００４】
【課題を解決するための手段】
本発明は、ニコチン酸アミド及びショ糖脂肪酸エステルを含有する内服用カプセルである。
【０００５】
本発明における防腐防黴とは、医薬品や食品が腐敗することを妨げ若しくは遅延し、またカビが生育することを妨げることである。ことに医薬品、健康食品等に用いられるカプセル剤は保存条件によってはカビが生育しやすいため、カプセル皮膜に防腐防黴の手段を講じることが必須であり、本発明が特に有効である。
【０００６】
本発明におけるニコチン酸アミドの使用量は、医薬品カプセルの皮膜に配合する場合は１カプセル当たり0.1〜5mg、好ましくは0.5〜5mgである。カプセル皮膜は、皮膜の組成が多様であり、また水分量がカプセルごとに大きく異なるため、本発明にかかる防腐防黴剤の有効範囲をカプセル重量に対する比率で正確に表現することは困難であるが、おおよそゼラチン１重量部に対し、ニコチン酸アミドが0.001〜0.05重量部であり、好ましくは0.005〜0.05重量部である。また、本発明にかかるニコチン酸アミドを食品の保存剤として使用する場合には、通常、食品１重量部に対して0.001〜0.05重量部であり、好ましくは0.005〜0.05重量部である。
【０００７】
この有効量は、ニコチン酸アミドが有する、末梢循環障害改善作用等の作用よりはるかに少ない量であり、本発明における効果は従来知られていた作用とは全く別の予測できない作用である。本発明におけるニコチン酸アミドの防腐防黴効果は、ショ糖脂肪酸エステルを加えることによりさらに増強される。その増強の程度は、防腐防黴効果が既に知られているショ糖脂肪酸エステルをニコチン酸アミドに加えたことにより期待される単なる相加効果よりはるかに大きなものである。
【０００８】
ショ糖脂肪酸エステルに期待されるニコチン酸アミドの増強作用は、ニコチン酸アミド１重量部に対し、ショ糖脂肪酸エステル0.01〜20重量部好ましくは0.1〜10重量部を添加することにより達成される。ニコチン酸アミド及びショ糖脂肪酸エステルの混合物としての使用量は、医薬品カプセルの皮膜に配合する場合は１カプセル当たり0.1〜5mg好ましくは0.5〜5mgである。前述のように、本発明にかかる防腐防黴剤の有効範囲をカプセルに対する比率で正確に表現することは困難であるが、おおよそゼラチン１重量部に対し、ニコチン酸アミド及びショ糖脂肪酸エステルの混合物として0.001〜0.05重量部好ましくは0.005〜0.05重量部である。
【０００９】
ショ糖脂肪酸エステルはショ糖にエステル結合する脂肪酸により多くの種類があるが、本発明においては炭素数６から１８の飽和若しくは不飽和の脂肪酸が好ましく、炭素数８から１２の飽和若しくは不飽和の脂肪酸が好ましい。また、モノエステル、ジエステル又はそれらの異性体によっては特に限定されず、いずれも用いることができる。
【００１０】
本発明にかかる防腐防黴剤の使用方法は、例えばカプセル皮膜の場合、ゼラチン、グリセリン、色素等の皮膜成分に、本発明にかかるニコチン酸アミド及びショ糖脂肪酸エステルを混合し、水を加えて加温溶解後、成型して得ることができる。ショ糖脂肪酸エステルが水に溶解しにくい場合は、エタノール等に溶解して加えるとよい。
【００１１】
【実施例】
次に本発明を実施例を挙げて具体的に説明するが、本発明はこれらに限定されるものではない。
【００１２】
比較例１
表１に示す組成にてゼラチン、濃グリセリン及びニコチン酸アミドを精製水に加温溶解させた。このゼラチン液に、あらかじめ水に分散させた色素等を加え、皮膜液とした。皮膜液は60℃のサービスタンクにて保温した。ソフトカプセル用の内容液はd-α-トコフェロールと中鎖脂肪酸グリセリンエステルの混合物を用いた。内容液と皮膜液を用いカプセルマシンにてソフトカプセルを得た。
【００１３】
実施例１
比較例１におけるニコチン酸アミドの代わりに、ショ糖脂肪酸エステル（SE-M-1695、三菱化学フーズ）及びニコチン酸アミドを用い、同様に操作してソフトカプセルを得た。
【００１５】
対照例１
比較例１においてニコチン酸アミドを用いずに、他は同様に操作してソフトカプセルを得た。
【００１６】
比較例２
比較例１におけるニコチン酸アミドの代わりにショ糖脂肪酸エステル（SE-M-1695、三菱化学フーズ）を用い、同様に操作してソフトカプセルを得た。
【００１７】
【効果】
本発明にかかる防腐防黴剤の効果を以下に示す。
試験方法 Aspergillus niger ATCC5088及びAspergillus sp.を供試菌株とし、グルコースペプトン（BBL社製）に寒天（Difco社）を15％添加したグルコースペプトン寒天培地に植菌後、25℃の培養器中で２週間、胞子が十分着生するまで培養した（前培養）。前培養にて胞子を十分着生させた供試菌株からリン酸緩衝生理食塩液（pH7.2）を用いて1.0×107個/mlの胞子懸濁液を調製した。実施例１、比較例１〜２及び対照例１で得たソフトカプセル３０カプセルに胞子懸濁液0.25mlをカプセル表面に均一になるように塗布した。その後、カプセルを７カプセルずつに分け、25℃において相対湿度75％、86％、91％、100％のデシケータに保存した。保存後、経時的にカビの生育を肉眼及び顕微鏡を用いて観察した。結果を表２〜４に示した。
【００１８】
表よりニコチン酸アミド及びショ糖脂肪酸エステルを併用すると効果が顕著に増強することが明らかである。
【図面の簡単な説明】
【図１】図１はハンバーグ中の微生物増殖に伴う発熱を測定したバイオサーモアナライザーによるチャートである。[0001]
[Industrial applications]
The present invention relates to capsules containing nicotinamide and sucrose fatty acid esters.
[0002]
[Prior art]
In order to enhance the preservability of foods, pharmaceuticals and the like, it is necessary to take preservative and antifungal means. As one of the means, the addition of antiseptic and antifungal agents is widely used. Conventionally, as a preservative / antifungal agent, ethyl paraoxybenzoate, propyl paraoxybenzoate, sorbic acid and the like have been used. However, in recent years, natural additives have attracted attention due to concerns about the safety of the additives, and various studies have been made in the field of preservatives. At the same time, efforts have been made to search for existing ones having an antiseptic and antifungal effect. For example, JP-A-6-105673 discloses a bacteriostatic agent for foods containing nicotinic acid as an active ingredient, and JP-A-51-32735 discloses glycine and cystine as well as ascorbic acid and / or nicotine. A method for preserving food, characterized by adding an acid, is disclosed. On the other hand, sucrose fatty acid esters are also known to have an antibacterial action (antibacterial and fungicide, Vol. 5, No. 7, pages 1 to 13 (1977)).
[0003]
[Problems to be solved by the invention]
The preservative and fungicidal effects of the above existing compounds are not sufficient. Japanese Patent Application Laid-Open No. 51-32735 discloses that nicotinamide has no antibacterial effect, and the antibacterial and antifungal volume 5 describes antibacterial effects of many existing substances. However, there is almost no description that a specific combination synergistically increases the fungicidal and fungicidal effect. The present inventors have intensively studied the antiseptic and fungicidal effects of existing compounds, and surprisingly found that the effect is significantly enhanced by combining nicotinamide and sucrose fatty acid ester, and completed the present invention. .
[0004]
[Means for Solving the Problems]
The present invention is an internal capsule containing nicotinamide and sucrose fatty acid ester.
[0005]
The antiseptic and antifungal in the present invention refers to preventing or delaying the decay of pharmaceuticals and foods and preventing the growth of mold. In particular, since the capsules used for pharmaceuticals, health foods and the like tend to grow mold depending on the storage conditions, it is essential to take preservative and fungicide measures on the capsule film, and the present invention is particularly effective.
[0006]
The nicotinamide used in the present invention is used in an amount of 0.1 to 5 mg, preferably 0.5 to 5 mg per capsule when incorporated into the capsule of a pharmaceutical capsule. Capsule coatings have a variety of coating compositions, and the amount of water varies greatly from capsule to capsule. Therefore, it is difficult to accurately express the effective range of the antiseptic / antifungal agent according to the present invention in proportion to the weight of the capsule. The nicotinamide is used in an amount of 0.001 to 0.05 part by weight, preferably 0.005 to 0.05 part by weight, based on 1 part by weight of gelatin. When the nicotinamide according to the present invention is used as a food preservative, it is usually 0.001 to 0.05 part by weight, preferably 0.005 to 0.05 part by weight, per part by weight of the food.
[0007]
This effective amount is much smaller than the effects of nicotinamide, such as the effects of improving peripheral circulatory disorders, and the effects of the present invention are completely different and unpredictable from the conventionally known effects. The preservative / antifungal effect of nicotinamide in the present invention is further enhanced by adding a sucrose fatty acid ester. The extent of the enhancement is much greater than the mere additive effect expected from adding sucrose fatty acid esters, whose preservative and antifungal effects are already known, to nicotinamide.
[0008]
The expected effect of succinic fatty acid ester on nicotinamide is achieved by adding 0.01 to 20 parts by weight, preferably 0.1 to 10 parts by weight, of sucrose fatty acid ester to 1 part by weight of nicotinamide. The amount of nicotinamide and sucrose fatty acid ester used as a mixture is 0.1 to 5 mg, preferably 0.5 to 5 mg per capsule when incorporated into the capsule of a pharmaceutical capsule. As described above, it is difficult to accurately express the effective range of the antiseptic / fungicide according to the present invention in terms of the ratio to the capsule. However, a mixture of nicotinamide and sucrose fatty acid ester is preferably used in an amount of about 1 part by weight of gelatin. 0.001 to 0.05 part by weight, preferably 0.005 to 0.05 part by weight.
[0009]
There are many types of sucrose fatty acid esters among fatty acids ester-linked to sucrose. In the present invention, saturated or unsaturated fatty acids having 6 to 18 carbon atoms are preferable, and saturated or unsaturated fatty acids having 8 to 12 carbon atoms are preferable. Fatty acids are preferred. There is no particular limitation on the monoester, diester or their isomers, and any of them can be used.
[0010]
The method of using the antiseptic / antifungal agent according to the present invention is, for example, in the case of a capsule film, mixing a nicotinamide and a sucrose fatty acid ester according to the present invention with film components such as gelatin, glycerin and pigment, and adding water. It can be obtained by molding after heating and melting. When the sucrose fatty acid ester is difficult to dissolve in water, it may be dissolved in ethanol or the like and added.
[0011]
【Example】
Next, the present invention will be specifically described with reference to examples, but the present invention is not limited thereto.
[0012]
Comparative Example 1
Gelatin, concentrated glycerin and nicotinamide having the compositions shown in Table 1 were dissolved in purified water by heating. To this gelatin solution, a pigment or the like previously dispersed in water was added to form a coating solution. The coating liquid was kept warm in a 60 ° C. service tank. As the content liquid for the soft capsule, a mixture of d-α-tocopherol and a medium-chain fatty acid glycerin ester was used. Soft capsules were obtained with a capsule machine using the content liquid and the coating liquid.
[0013]
Example 1
A sucrose fatty acid ester (SE-M-1695, Mitsubishi Chemical Foods) and nicotinamide were used in place of nicotinamide in Comparative Example 1, and soft capsules were obtained in the same manner.
[0015]
Comparative Example 1
A soft capsule was obtained in the same manner as in Comparative Example 1 , except that nicotinamide was not used.
[0016]
Comparative Example 2
A sucrose fatty acid ester (SE-M-1695, Mitsubishi Chemical Foods) was used in place of nicotinamide in Comparative Example 1, and a soft capsule was obtained in the same manner.
[0017]
【effect】
The effects of the antiseptic / antifungal agent of the present invention are shown below.
Test method Aspergillus niger ATCC5088 and Aspergillus sp. Were used as test strains, and inoculated on glucose peptone (BBL) supplemented with glucose peptone agar medium containing 15% agar (Difco), and then incubated in a 25 ° C incubator. The cells were cultured for a week until spores had sufficiently set (preculture). A 1.0 × 10 7 spore / ml spore suspension was prepared from a test strain on which spores had sufficiently grown in the preculture using phosphate buffered saline (pH 7.2). To 30 capsules of the soft capsules obtained in Example 1, Comparative Examples 1 and 2 and Control Example 1 , 0.25 ml of the spore suspension was uniformly applied on the capsule surface. Thereafter, the capsules were divided into 7 capsules and stored at 25 ° C. in desiccators at 75%, 86%, 91% and 100% relative humidity. After storage, the growth of the mold was observed over time using the naked eye and a microscope. The results are shown in Tables 2 to 4.
[0018]
It is clear from the table that the effect is significantly enhanced when nicotinamide and sucrose fatty acid ester are used in combination.
[Brief description of the drawings]
BRIEF DESCRIPTION OF DRAWINGS FIG. 1 is a chart obtained by measuring a heat generated by a microorganism growing in a hamburger, using a biothermometer.
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP00449796A JP3585306B2 (en) | 1996-01-16 | 1996-01-16 | Antiseptic / antifungal agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP00449796A JP3585306B2 (en) | 1996-01-16 | 1996-01-16 | Antiseptic / antifungal agent |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH09194306A JPH09194306A (en) | 1997-07-29 |
| JP3585306B2 true JP3585306B2 (en) | 2004-11-04 |
Family
ID=11585713
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP00449796A Expired - Fee Related JP3585306B2 (en) | 1996-01-16 | 1996-01-16 | Antiseptic / antifungal agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3585306B2 (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2274236T3 (en) * | 2002-06-20 | 2007-05-16 | Astion Dermatology A/S | NOVEDOUS COMPLEXES OF ESTERES OF FATTY ACIDS OF POLYHYDROXIALCANS AND NACINAMIDE. |
| JP2013094095A (en) * | 2011-10-31 | 2013-05-20 | Victory Japan Kk | Soft drink and method of manufacturing the same |
| JP5986416B2 (en) * | 2012-04-11 | 2016-09-06 | 花王株式会社 | Skin preparation |
-
1996
- 1996-01-16 JP JP00449796A patent/JP3585306B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JPH09194306A (en) | 1997-07-29 |
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