JPH05124960A - Sodium valproate preparation - Google Patents
Sodium valproate preparationInfo
- Publication number
- JPH05124960A JPH05124960A JP28608791A JP28608791A JPH05124960A JP H05124960 A JPH05124960 A JP H05124960A JP 28608791 A JP28608791 A JP 28608791A JP 28608791 A JP28608791 A JP 28608791A JP H05124960 A JPH05124960 A JP H05124960A
- Authority
- JP
- Japan
- Prior art keywords
- sodium valproate
- aluminum silicate
- synthetic aluminum
- water
- calcium salt
- 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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【０００１】[0001]
【産業上の利用分野】本発明は、長期間保存しても潮解
することなく安定で、流動性に優れたバルプロ酸ナトリ
ウム製剤に関する。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a sodium valproate preparation which is stable without deliquescence even after long-term storage and has excellent fluidity.
【０００２】[0002]
【従来の技術】バルプロ酸ナトリウムは抗てんかん剤と
して臨床において広く使用されている。しかし、バルプ
ロ酸ナトリウムは強い吸湿性の結晶であるため、これを
製剤化するにあたっては、湿度に対する工夫がなされな
ければならない。BACKGROUND OF THE INVENTION Sodium valproate is widely used clinically as an antiepileptic agent. However, since sodium valproate is a highly hygroscopic crystal, it is necessary to take measures against humidity when formulating it.
【０００３】従来、この防湿法としては、錠剤の場合に
は、フィルムコーティング、糖衣等を施す方法が行われ
ているが、これも散剤、細粒剤、顆粒剤の場合には困難
であった。Conventionally, as the moisture-proof method, in the case of tablets, a method of applying film coating, sugar coating, etc. has been carried out, but this is also difficult in the case of powders, fine granules and granules. ..
【０００４】しかるところ、近年、バルプロ酸ナトリウ
ムに保水能に富む合成ケイ酸アルミニウムを配合すれ
ば、この潮解性がほぼ完全に阻止されることが報告され
た（特開昭６１−１８６３１３号）。しかし、バルプロ
酸ナトリウムに合成ケイ酸アルミニウムを配合すると、
その潮解性は防止できるが、吸湿とともにウイスカーが
発生、成長し、粒剤が凝集し、流動性や他剤との配合性
が著しく損なわれるという問題があった。従って、特開
昭６１−１８６３１３号の発明では、これに更に、ワッ
クス類、高級脂肪酸類、硬化油類又はデンプン誘導体を
配合してウイスカーの発生を阻止する方法がとられてい
る。In recent years, however, it has been reported that this deliquescent property is almost completely prevented by blending sodium valproate with a synthetic aluminum silicate having a high water-retaining ability (Japanese Patent Laid-Open No. 61-186313). However, when synthetic aluminum silicate is mixed with sodium valproate,
Although the deliquescent property can be prevented, there is a problem that whiskers are generated and grow with moisture absorption, and the granules agglomerate, so that the fluidity and the mixability with other agents are significantly impaired. Therefore, in the invention of JP-A-61-186313, a method of preventing the generation of whiskers by further incorporating waxes, higher fatty acids, hydrogenated oils or starch derivatives into the composition is adopted.
【０００５】[0005]
【発明が解決しようとする課題】しかしながら、この方
法も、無用なワックス類等を配合しなければならないと
いう欠点があり、バルプロ酸ナトリウムの有利な防湿法
が望まれていた。However, this method also has the drawback that unnecessary waxes and the like must be blended, and an advantageous method for preventing moisture from sodium valproate has been desired.
【０００６】[0006]
【課題を解決するための手段】斯かる実情において、本
発明者は鋭意研究を行った結果、水溶性カルシウム塩で
処理した合成ケイ酸ナトリウムを使用すれば、ウイスカ
ーの発生が全く見られないことを見出し、本発明を完成
した。Under such circumstances, the inventors of the present invention have conducted diligent research, and as a result, when synthetic sodium silicate treated with a water-soluble calcium salt was used, generation of whiskers was not observed at all. Then, the present invention was completed.
【０００７】すなわち、本発明は、バルプロ酸ナトリウ
ム及び水溶性カルシウム塩で処理した合成ケイ酸アルミ
ニウムを含有するバルプロ酸ナトリウム製剤を提供する
ものである。[0007] That is, the present invention provides a sodium valproate preparation containing sodium valproate and a synthetic aluminum silicate treated with a water-soluble calcium salt.
【０００８】本発明において、合成ケイ酸アルミニウム
を処理する水溶性カルシウム塩としては、例えば塩化カ
ルシウム、硝酸カルシウム、酢酸カルシウム等が挙げら
れる。これらのカルシウム塩で合成ケイ酸アルミニウム
を処理する方法としては、カルシウム塩の水溶液、好ま
しくは０．１〜１Ｍ濃度の水溶液を調製し、これに合成
ケイ酸アルミニウムを浸漬処理するか、あるいは合成ケ
イ酸アルミニウムを充填したカラムに上記のカルシウム
塩水溶液を流して処理する方法などが挙げられる。In the present invention, examples of the water-soluble calcium salt for treating synthetic aluminum silicate include calcium chloride, calcium nitrate, calcium acetate and the like. As a method for treating the synthetic aluminum silicate with these calcium salts, an aqueous solution of the calcium salt, preferably an aqueous solution having a concentration of 0.1 to 1 M, is prepared, and the synthetic aluminum silicate is immersed in the aqueous solution, or the synthetic silica is treated. Examples include a method in which the above-described calcium salt aqueous solution is flown through a column packed with aluminum acid salt to perform treatment.
【０００９】バルプロ酸ナトリウムと上記合成ケイ酸ア
ルミニウムの配合割合は、重量比で、１０〜８０：２０
〜９０が好ましい。本発明の製剤中には、上記の必須成
分のほかに、通常使用される任意成分を配合することが
できる。The compounding ratio of sodium valproate and the above synthetic aluminum silicate is 10 to 80:20 by weight.
~ 90 is preferred. In the preparation of the present invention, in addition to the above-mentioned essential components, any commonly used component can be added.
【００１０】[0010]
【作用】本発明の製剤におけるウイスカーの発生防止機
序の詳細は必ずしも明らかでないが、次の如くであると
推測される。すなわち、合成ケイ酸アルミニウムは酸強
度の強い固体酸であるため、これをバルプロ酸ナトリウ
ムと混合すると、バルプロ酸ナトリウムのＮａがイオン
交換されてバルプロ酸に変化し、その過程でウイスカー
が発生する。しかるところ、本発明の合成ケイ酸アルミ
ニウムはＣａイオンで置換されているので、最早バルプ
ロ酸ナトリウムをバルプロ酸に変化させることがなく、
ウイスカーが発生しないものと推測される。The mechanism of preventing whiskers from occurring in the preparation of the present invention is not clear, but it is presumed to be as follows. That is, since synthetic aluminum silicate is a solid acid having a strong acid strength, when this is mixed with sodium valproate, Na of sodium valproate is ion-exchanged to change to valproic acid, and whiskers are generated in the process. However, since the synthetic aluminum silicate of the present invention is substituted with Ca ions, it no longer changes sodium valproate into valproic acid,
It is assumed that whiskers do not occur.
【００１１】[0011]
【発明の効果】本発明のバルプロ酸ナトリウム製剤は、
長期間保存しても潮解することがなく安定で、流動性に
優れているとともに、ウイスカーの発生もない優れたも
のである。The sodium valproate preparation of the present invention is
It is stable without deliquescence even after long-term storage, has excellent fluidity, and does not generate whiskers.
【００１２】[0012]
【実施例】次に実施例を挙げて説明する。EXAMPLES Next, examples will be described.
【００１３】実施例１ （１）合成ケイ酸アルミニウム２５ｇを水約２００〜３
００mlに懸濁し、吸引濾過を行った。濾過後、０．１Ｍ
ＣａＣｌ2 １ｌ又は１Ｍ ＣａＣｌ2 １ｌを漏斗
に注ぎ、吸引濾過を行った。濾過後、水約２００〜３０
０mlで洗浄した。４０℃で一昼夜乾燥後、３２メッシュ
で篩過して、試料とした。 （２）バルプロ酸ナトリウム４ｇと試料４ｇを乳鉢で混
合し、エタノール４mlを加え、練合した。シャーレに移
し、４０℃で一昼夜乾燥した。乾燥後、３２メッシュで
篩過して、散剤を得た。 （３）上で得た散剤を、室温、５０％RHの条件下に１週
間放置し、ウイスカーの発生を走査型電子顕微鏡で観察
した。その結果、無処理合成ケイ酸アルミニウムの場合
にはウイスカーの発生がみられたが、０．１Ｍ及び１Ｍ
ＣａＣｌ2 処理合成ケイ酸アルミニウムの場合には全
くウイスカーの発生は認められなかった。Example 1 (1) 25 g of synthetic aluminum silicate was added to about 200 to 3 of water.
It was suspended in 00 ml and suction-filtered. After filtration, 0.1M
1 liter of CaCl 2 or 1 liter of 1M CaCl 2 was poured into the funnel and suction filtered. After filtration, water about 200-30
Wash with 0 ml. After drying at 40 ° C. for 24 hours, it was sieved with 32 mesh to obtain a sample. (2) 4 g of sodium valproate and 4 g of the sample were mixed in a mortar, and 4 ml of ethanol was added and kneaded. The mixture was transferred to a petri dish and dried at 40 ° C for one day. After drying, it was sieved with 32 mesh to obtain a powder. (3) The powder obtained above was allowed to stand for 1 week under conditions of room temperature and 50% RH, and the generation of whiskers was observed with a scanning electron microscope. As a result, whiskers were generated in the case of untreated synthetic aluminum silicate, but 0.1M and 1M
No generation of whiskers was observed in the case of CaCl 2 -treated synthetic aluminum silicate.
Claims (2)
ウム塩で処理した合成ケイ酸アルミニウムを含有するバ
ルプロ酸ナトリウム製剤。1. A sodium valproate formulation containing synthetic aluminum silicate treated with sodium valproate and a water-soluble calcium salt.
溶液である請求項１記載のバルプロ酸ナトリウム製剤。2. The sodium valproate preparation according to claim 1, wherein the water-soluble calcium salt is an aqueous solution of calcium chloride.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP28608791A JPH05124960A (en) | 1991-10-31 | 1991-10-31 | Sodium valproate preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP28608791A JPH05124960A (en) | 1991-10-31 | 1991-10-31 | Sodium valproate preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH05124960A true JPH05124960A (en) | 1993-05-21 |
Family
ID=17699774
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP28608791A Pending JPH05124960A (en) | 1991-10-31 | 1991-10-31 | Sodium valproate preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH05124960A (en) |
-
1991
- 1991-10-31 JP JP28608791A patent/JPH05124960A/en active Pending
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