JPS59144741A - Calcium hopantenate composition - Google Patents
Calcium hopantenate compositionInfo
- Publication number
- JPS59144741A JPS59144741A JP1809183A JP1809183A JPS59144741A JP S59144741 A JPS59144741 A JP S59144741A JP 1809183 A JP1809183 A JP 1809183A JP 1809183 A JP1809183 A JP 1809183A JP S59144741 A JPS59144741 A JP S59144741A
- Authority
- JP
- Japan
- Prior art keywords
- calcium
- cyclodextrin
- calcium hopantenate
- hopantenate
- composition
- Prior art date
- 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.)
- Pending
Links
Landscapes
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
【発明の詳細な説明】
本発明はホバンテン酸カルシウムにβ−サイクロデキス
トリンをモル比にて１ ： ０．１〜２の範囲で配合し
てなるホバンテン酸カルシウム組成物に関する。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a calcium fobantenate composition comprising calcium fobantenate and β-cyclodextrin in a molar ratio of 1:0.1 to 2.
ホパンテン酸カルシウムはブドウ糖の脳内への取り込み
を増加させ、また脳内のブドウ糖代謝を促進させる薬理
作用を有し、注意力低下、言語障害、意欲低下の緩解、
軽度精神発育遅滞、脳炎後遺症、脳性麻痺等の治療薬と
して用いられている。その用法、用量は通常粉末状のま
ま経口的に投与され、１日量として７才以上では１．５
，９．６〜３才では１ｇ、３才未満は０５〜１ｇとされ
ており、比較的長期に亘り継続的に服用される。Calcium hopantenate has pharmacological effects that increase the uptake of glucose into the brain and promote glucose metabolism in the brain.
It is used as a treatment for mild mental retardation, sequelae of encephalitis, cerebral palsy, etc. Its usage and dosage is usually administered orally in powder form, and the daily dose is 1.5
, 9.6 to 3 years of age is 1 g, and those under 3 years of age are 0.5 to 1 g, and are taken continuously over a relatively long period of time.
しかし、このホパンテン酸カルシウムは苦味があり、ま
たその形態が粉末状の原末のままであることも相俟って
、服用し難いのが難点であり、その改善が望まれていた
。However, this calcium hopanthenate has a bitter taste and is difficult to take due to the fact that it is in the form of a powdered bulk powder, and there has been a desire to improve this problem.
一般に経口的に投与される粉末状薬剤の服用を容易にす
る方法としては錠剤にしたり、カプセルに詰める方法或
いは甘味剤と共に濃厚液（シロップ）とする方法等が知
られており、これらの方法では苦味がマスクされる効果
もあり好都合である。ただ、ホパンテン酸カルシウムの
場合には１回当りの服用量が比較的多いため、錠剤やカ
プセル剤よりは液剤の方が飲み易い、特に、粉末状で保
存し服用時に水等に溶解又は懸濁して用いる所謂ドライ
シロップ剤は薬剤の包装、流通経費の低減、保存時の安
定性の維持等の観点から好適である。しかし、ホバンテ
ン酸カルシウムは水に対する溶解量の点では問題ないが
、溶解速度が遅い欠点がある。溶解時に温湯を用いるか
加熱すれば溶解時間は可成り短縮するが煩雑であること
は免れかい。In general, there are known ways to make it easier to take powdered drugs that are orally administered, such as making them into tablets, filling them in capsules, or making them into a concentrated liquid (syrup) with a sweetener. It also has the effect of masking bitterness, which is convenient. However, in the case of calcium hopanthenate, the dose per dose is relatively large, so liquid preparations are easier to swallow than tablets or capsules, especially when stored in powder form and dissolved or suspended in water etc. before taking. The so-called dry syrup used for drug packaging is suitable from the viewpoints of reducing drug packaging, distribution costs, and maintaining stability during storage. However, although calcium fobantenate has no problem in terms of the amount of dissolution in water, it has the disadvantage of slow dissolution rate. If hot water or heating is used during dissolution, the dissolution time can be considerably shortened, but it is not complicated.
本発明者らは種々検討を重ねた結果、ホバンテン酸カル
シウムにβ−サイクロデキストリンをモル比にてに０１
〜２の範囲で配合した組成物がホバンテン酸カルシウム
の持つ苦味が消失し、しかも、水に対する溶解速度が速
く々す、粉末剤としてその！Ｉま服用するにしても或い
はドライシロップ剤として水に溶解して服用するにして
も甚だ好都合であることを見い出し本発明を完成するに
至った。As a result of various studies, the present inventors found that the molar ratio of β-cyclodextrin to calcium fobantenate was 0.1
A composition formulated in the range of ~2 eliminates the bitter taste of calcium fobantenate, and has a high dissolution rate in water, making it a powder! The present inventors have discovered that it is extremely convenient to take the drug either directly or dissolved in water as a dry syrup, leading to the completion of the present invention.
以下、本発明のホバンテン酸カルシウム組成物の組成と
効果について、苦味試験及び溶解速度試験の結果を示し
更に具体的に説明する。Hereinafter, the composition and effects of the calcium fobantenate composition of the present invention will be explained in more detail by showing the results of a bitterness test and a dissolution rate test.
１）苦味試験
ホパンテン酸カルシウム粉末及びこれにβ−サイクロデ
キストリンを所定の割合に混合した粉末を、それぞれホ
パンテン酸カルシウムの濃度として１．００ｍ９／ｍＡ
になるように水に溶解し、パネラ−による感応テストを
行い以下の４段階の基準により苦味を評価した。1) Bitterness test Calcium hopantenate powder and powder mixed with β-cyclodextrin at a predetermined ratio were each tested at a concentration of 1.00 m9/mA as calcium hopantenate powder.
It was dissolved in water so as to give the desired bitterness, and a sensitivity test was conducted by a panel to evaluate the bitterness according to the following 4-level criteria.
◎：苦味を全く感じない ○：苦味を殆んど感じない。◎: No bitterness at all ○: Almost no bitterness felt.
△：苦味が若干残る
×：苦味を明瞭に感じる
２）＃解試験
ホバンテン酸カルシウム粉末及びこれにβ−サイクロデ
キストリンを所定の割合に混合した粉末を、それぞれ０
．２．９採り水１ ｍｌに加えて室温で攪拌し、その時
の状態を観察ｌ〜て以下の４段階の基準で溶解性を判定
した。△: Some bitterness remains ×: Bitterness is clearly felt 2) #Answer test Calcium fobantenate powder and powder mixed with β-cyclodextrin at a predetermined ratio were each mixed with 0
．． 2.9 was added to 1 ml of sampled water and stirred at room temperature, the state at that time was observed and the solubility was determined according to the following 4-level criteria.
◎ ５分間り、内で全て溶解した
０ ５乃至１５分間で全て溶解した
△ １５乃至３（）分間で全て溶解したＸ ３０分以
上でも不溶分が残存したこれらの結果を以下に示す。◎ All dissolved within 5 minutes 0 All dissolved within 5 to 15 minutes △ All dissolved within 15 to 3 minutes X Insoluble matter remained even after 30 minutes These results are shown below.
１：ＯＸ Ｘ
１２：］ Ｘ Ｘ１０： １
△ △８： １
０ ０
４：１ ０ ０
２： １ ◎ ○１５： １
◎ ◎１ ：１
◎ ◎１ ：１５ ◎
０１ ：２ ◎ △上記か
らも明らか々如く、本発明の組成物に於いてホパンテン
酸カルシウムとβ−サイクロデキストリンの組成は、モ
ル比にて１：０．１〜２の範囲が好適であり、更に実用
的な観点から特に好捷しくけ０．２〜１．５の範囲が適
当である。1:OXX12:]XX10:1
△ △8: 1
0 0 4:1 0 0 2: 1 ◎ ○15: 1
◎ ◎1:1
◎ ◎1:15 ◎
01 :2 ◎ △As is clear from the above, the composition of calcium hopanthenate and β-cyclodextrin in the composition of the present invention is preferably in a molar ratio of 1:0.1 to 2. Furthermore, from a practical point of view, a range of 0.2 to 1.5 is particularly suitable.
本発明のホバンテン酸カルシウムは通常、上記範囲のβ
−サイクロデキストリンと混合し、これに少量の水を加
えて充分に混練した後、乾燥する方法等により調製され
る。The calcium fobantenate of the present invention typically has a β within the above range.
- Prepared by mixing with cyclodextrin, adding a small amount of water, thoroughly kneading, and drying.
以下に具体的な調製法について実施例を示す。Examples of specific preparation methods are shown below.
１）ホパンテン酸カルシウム０．９ｇとβ−サイクロデ
キス） ＩＪン２ｇに水３ｍｌを加えて室温で３０分激
しく攪拌し、約５０°Ｃ，３０ｚｉＨｇで減圧乾燥して
ホパンテン酸カルシウム：β−ザイクロデキストリンの
モル比１：１の製剤を得た。1) Calcium hopanthenate (0.9 g and β-cyclodextrin) Add 3 ml of water to 2 g of IJ, stir vigorously at room temperature for 30 minutes, and dry under reduced pressure at approximately 50°C and 30 ziHg to prepare calcium hopanthenate: β-cyclodextrin. A formulation with a molar ratio of 1:1 was obtained.
２）ホパンテン酸カルシウム１３６ｇとβ−サイクロデ
キストリン２ｇに水４鮮を加えて室温で３０分激しく攪
拌し約５０°Ｃ，３０ｍｍＨｇで減圧乾燥してホパンテ
ン酸カルシウム：β−サイクロデキストリンのモル比１
．５ ： １の製剤を得た。2) Add 4 fresh water to 136 g of calcium hopanthenate and 2 g of β-cyclodextrin, stir vigorously at room temperature for 30 minutes, and dry under reduced pressure at approximately 50°C and 30 mmHg to obtain a calcium hopanthenate:β-cyclodextrin molar ratio of 1.
．． A 5:1 formulation was obtained.
３）ホバンテン酸カルシウム０．９．９とβ−サイクロ
デキストリン１ｇに水２ｍｌを加えて室温で３０分激し
く攪拌し約５０°０．３０ｍｍＨｇで減圧乾燥してホバ
ンテン酸カルシウム：β−サイクロデキストリンのモル
比２：１の製剤を得た。3) Add 2 ml of water to 0.9.9 g of calcium fobantenate and 1 g of β-cyclodextrin, stir vigorously at room temperature for 30 minutes, and dry under reduced pressure at about 50° and 0.30 mmHg to obtain the mole of calcium fobantenate: β-cyclodextrin. A formulation with a ratio of 2:1 was obtained.
４）ホパンテン酸カルシウム１．８９とβ−サイクロデ
キストリン１ｇに水３ｍｌを加えて室温で３０分激しく
攪拌し約５０°Ｃ，３０＋＋ｍＨｇで減圧乾燥してホバ
ンテン酸カルシウム：β−サイクロデキストリンのモル
比４：１の製剤を得た。4) Add 3 ml of water to 1.89 calcium hopantenate and 1 g of β-cyclodextrin, stir vigorously at room temperature for 30 minutes, and dry under reduced pressure at about 50°C and 30++ mHg to obtain a calcium hopantenate: β-cyclodextrin molar ratio of 4. :1 formulation was obtained.
５）ホパンテン酸カルシウム１．８．９とβ−サイクロ
デキストリン０．５９に水３ｍｌを加えて室温で３０分
激しく攪拌し約５０ ’Ｃ％ ３０ ｍｕ Ｈｇで減圧
乾燥してホバンテン酸カルシウム：β−サイクロデキス
トリンのモル比８：１の製剤を得た。5) Add 3 ml of water to 1.8.9 ml of calcium hopantenate and 0.59 ml of β-cyclodextrin, stir vigorously at room temperature for 30 minutes, and dry under reduced pressure at approximately 50'C% 30 mu Hg to obtain calcium hopantenate: β- A formulation with a molar ratio of cyclodextrin of 8:1 was obtained.
得られた組成物は粉状であるが、これは前述の通り苦味
が無いため飲み易く、壕だ溶解速度も改善されているの
でその″！、マ粉剤、顆粒剤又はドライシロップ剤とし
て服用される。勿論、必要に応じて更に錠剤、カプセル
剤等に加工しても良い。The resulting composition is in powder form, but as mentioned above, it is easy to drink because it has no bitter taste, and its dissolution rate is improved, so it can be taken as a powder, granules, or dry syrup. Of course, it may be further processed into tablets, capsules, etc., if necessary.
特許出願人 昭和電工株式会社 代理人 菊地精−Patent applicant: Showa Denko Co., Ltd. Agent Sei Kikuchi
Claims (1)
ンをモル比にて１ ： ０．１〜２の範囲で配合してな
るホバ／テン酸カルシウム組成物。Calcium hopantenate with β-cyclodextrin) IJ
1. A calcium thenate composition comprising calcium thenate in a molar ratio of 1:0.1 to 2.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1809183A JPS59144741A (en) | 1983-02-08 | 1983-02-08 | Calcium hopantenate composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1809183A JPS59144741A (en) | 1983-02-08 | 1983-02-08 | Calcium hopantenate composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS59144741A true JPS59144741A (en) | 1984-08-18 |
Family
ID=11961962
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP1809183A Pending JPS59144741A (en) | 1983-02-08 | 1983-02-08 | Calcium hopantenate composition |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS59144741A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61268621A (en) * | 1985-05-21 | 1986-11-28 | Sankyo Co Ltd | Syrup pharmaceutical |
| JP2007152020A (en) * | 2005-12-08 | 2007-06-21 | Olympus Corp | Endoscope apparatus |
| EA011243B1 (en) * | 2008-04-09 | 2009-02-27 | Михаил Константинович Кузьмич | Composition having nootropic properties and method for preparing thereof |
| US8279273B2 (en) | 2006-01-27 | 2012-10-02 | Olympus Corporation | Endoscope apparatus |
-
1983
- 1983-02-08 JP JP1809183A patent/JPS59144741A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS61268621A (en) * | 1985-05-21 | 1986-11-28 | Sankyo Co Ltd | Syrup pharmaceutical |
| JP2007152020A (en) * | 2005-12-08 | 2007-06-21 | Olympus Corp | Endoscope apparatus |
| US8194380B2 (en) | 2005-12-08 | 2012-06-05 | Olympus Corporation | Endoscope apparatus |
| US8279273B2 (en) | 2006-01-27 | 2012-10-02 | Olympus Corporation | Endoscope apparatus |
| EA011243B1 (en) * | 2008-04-09 | 2009-02-27 | Михаил Константинович Кузьмич | Composition having nootropic properties and method for preparing thereof |
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