JPS603364B2 - Pharmaceutical composition for injection - Google Patents
Pharmaceutical composition for injectionInfo
- Publication number
- JPS603364B2 JPS603364B2 JP10704880A JP10704880A JPS603364B2 JP S603364 B2 JPS603364 B2 JP S603364B2 JP 10704880 A JP10704880 A JP 10704880A JP 10704880 A JP10704880 A JP 10704880A JP S603364 B2 JPS603364 B2 JP S603364B2
- Authority
- JP
- Japan
- Prior art keywords
- injection
- pharmaceutical composition
- dimethyl sulfoxide
- neocyanine
- present
- 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.)
- Expired
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 6
- 238000002347 injection Methods 0.000 title description 7
- 239000007924 injection Substances 0.000 title description 7
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims description 24
- 230000000694 effects Effects 0.000 description 6
- 239000000203 mixture Substances 0.000 description 6
- 239000000243 solution Substances 0.000 description 6
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 5
- 239000003708 ampul Substances 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 208000002193 Pain Diseases 0.000 description 4
- 239000012153 distilled water Substances 0.000 description 4
- 206010037844 rash Diseases 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 4
- 208000010201 Exanthema Diseases 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 3
- 201000005884 exanthem Diseases 0.000 description 3
- 238000011160 research Methods 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- CEJANLKHJMMNQB-UHFFFAOYSA-M cryptocyanin Chemical compound [I-].C12=CC=CC=C2N(CC)C=CC1=CC=CC1=CC=[N+](CC)C2=CC=CC=C12 CEJANLKHJMMNQB-UHFFFAOYSA-M 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 235000019441 ethanol Nutrition 0.000 description 2
- 231100000636 lethal dose Toxicity 0.000 description 2
- 208000004296 neuralgia Diseases 0.000 description 2
- 230000028327 secretion Effects 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 238000005303 weighing Methods 0.000 description 2
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 description 1
- 208000001034 Frostbite Diseases 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 208000000112 Myalgia Diseases 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 208000037114 Symptom Flare Up Diseases 0.000 description 1
- 238000009395 breeding Methods 0.000 description 1
- 230000001488 breeding effect Effects 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 229910052802 copper Inorganic materials 0.000 description 1
- 239000010949 copper Substances 0.000 description 1
- 239000013078 crystal Substances 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- 239000012895 dilution Substances 0.000 description 1
- 238000010790 dilution Methods 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 239000012155 injection solvent Substances 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 230000007659 motor function Effects 0.000 description 1
- 208000013465 muscle pain Diseases 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000010079 rubber tapping Methods 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 230000002269 spontaneous effect Effects 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- ANRHNWWPFJCPAZ-UHFFFAOYSA-M thionine Chemical compound [Cl-].C1=CC(N)=CC2=[S+]C3=CC(N)=CC=C3N=C21 ANRHNWWPFJCPAZ-UHFFFAOYSA-M 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【発明の詳細な説明】
本発明は、神経痛、リュウマチ、振動病等の治療に箸効
を奏する新規な注射用医薬組成物に関するものである。DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a novel pharmaceutical composition for injection that is effective in treating neuralgia, rheumatism, vibration disease, and the like.
さら詳しくいえば、本発明は、感光色素ネオシアニンと
して知られている１，１′，１″ートリエチルー１１−
（４′−キノリル）一４，４″‐ペンタメチンキノシア
ニンジョージド（以下ネオシアニンという）を有効成分
とした注射用医薬組成物に関するものである。ネオシア
ニンは、構造式
で示される、融点２８１〜３℃（分解）をもつ、極めて
鎚溶性の銅赤色結晶であり、エタノールにはわずかに溶
けて淡緑色溶液となる。More specifically, the present invention relates to 1,1',1'' triethyl-11-
This invention relates to an injectable pharmaceutical composition containing (4'-quinolyl)-4,4''-pentamethinequinocyanine georgeide (hereinafter referred to as neocyanine) as an active ingredient.Neocyanine has a melting point of 281 to It is a very soluble copper red crystal with a temperature of 3°C (decomposition) and is slightly soluble in ethanol to form a pale green solution.
これまで、このネオシアニン７０〜７２重量％とクリプ
トシアニン（１，１′ージエチルー４，４′ートリメチ
ンキノシアニンョージド）２８〜３の重量％から成るシ
アニン色素複合体を、炭酸水素ナトリウムと混合して蒸
留水に溶かし、凍傷、神経痛、リュウマチの治療に用い
ることは知られていた。Until now, a cyanine dye complex consisting of 70 to 72% by weight of this neocyanine and 28 to 3% by weight of cryptocyanin (1,1'-diethyl-4,4'-trimethine quinocyaninogenide) was prepared with sodium bicarbonate. It was known to be mixed and dissolved in distilled water and used to treat frostbite, neuralgia, and rheumatism.
しかしながら、この色素複合体は組成が一定せず効果が
不安定であり、また難潟性であるため注射薬として投与
した場合、治療に十分な量を与えることが困難であると
いう欠点があった。本発明者らは、このような欠点を克
服し、安定した薬理効果を示し、かつ注射薬として十分
な量を投与しうるネオシアニン含有医薬組成物を開発す
るために、鋭意研究を重ねた結果、ネオシアニンはクリ
プトシアニンと複合させず、純粋な形で使用した場合に
おいても良好な治療効果を奏しうろこと及びこれはジメ
チルスルホキシド‘こよく溶解し、しかもこの溶液は水
とよく混和しうろことを見出し、この知見に基づいて本
発明をなすに至つた。However, this pigment complex has an inconsistent composition, unstable effects, and is difficult to maintain, so when administered as an injection, it is difficult to administer a sufficient amount for treatment. . The present inventors have conducted extensive research in order to overcome these drawbacks, exhibit stable pharmacological effects, and develop a neocyanine-containing pharmaceutical composition that can be administered in sufficient amounts as an injection drug. It was discovered that neocyanin has a good therapeutic effect even when used in its pure form without being complexed with cryptocyanin, and that it dissolves well in dimethyl sulfoxide, and that this solution is also miscible with water. Based on this knowledge, the present invention was accomplished.
すなわち、本発明は、前記綾造式（１）で示されるネオ
シアニンを、ジメチルスルホキシドに溶解して成る注射
用医薬組成物を提供するものである。That is, the present invention provides an injectable pharmaceutical composition prepared by dissolving neocyanine represented by Ayazo formula (1) in dimethyl sulfoxide.
本発明において溶剤として用いるジメチルスルホキシド
は、通常注射剤溶剤として１回の投与に使用される程度
の量例えば０．５〜２の‘では、人体に対し全く副作用
を示さず、安全に使用しうろことが認められている。Dimethyl sulfoxide used as a solvent in the present invention does not exhibit any side effects on the human body in the amount normally used for one administration as an injection solvent, for example, 0.5 to 2. It is recognized that
本発明組成物は、有効成分であるネオシアニンを、この
溶剤中に濃度０．０５〜１．０％（Ｗ／Ｖ）になるよう
な割合で溶解することによって調製される。本発明組成
物には、一般の注射剤に慣用されている添加剤を所望に
応じて添加することができる。The composition of the present invention is prepared by dissolving neocyanine, which is an active ingredient, in this solvent at a concentration of 0.05 to 1.0% (W/V). Additives commonly used in general injections can be added to the composition of the present invention as desired.
このような添加剤としては、例えば安定剤、溶解補助剤
、緩衝剤、保存剤、難癖化剤などがある。このようにし
て調製された本発明組成物、ガラスアンプルに１〜２の
‘程度の量で詰めて、製品化される。Examples of such additives include stabilizers, solubilizers, buffers, preservatives, and addictive agents. The thus-prepared composition of the present invention is packed into a glass ampoule in an amount of about 1 to 2 cm to produce a product.
使用に際しては、この組成物をそのまま、もしくは同量
の蒸留水で希釈し、疹通個所に注射器をを用いて投与さ
れる。本発明組成物の成人一日当りの投与量としては、
ネオシアシニン基準で、１〜５の９が適当であり、必要
に応じて２〜５回に分狂することができる。In use, this composition is administered as is or diluted with the same amount of distilled water and administered to the rash using a syringe. The daily dosage for adults of the composition of the present invention is as follows:
Based on neocyacinin, a ratio of 9 on a scale of 1 to 5 is appropriate, and can be increased to 2 to 5 times as needed.
本発明によると、従来注射による投薬が困難であったネ
オシアニンを、治療に必要な量だけ任意に投薬しうるの
で、治療効果を向上しうる上に、アンプルとして広く供
給しうるので、容易に利用できるという利点がある。According to the present invention, neocyanine, which has conventionally been difficult to administer by injection, can be administered arbitrarily in the amount required for treatment, improving the therapeutic effect. In addition, it can be widely supplied as an ampoule, making it easy to use. It has the advantage of being possible.
次に実施例により本発明をさらに詳細に説明する。Next, the present invention will be explained in more detail with reference to Examples.
参考例
ジメチルスルホキシドの毒性を試験するために、次の動
物実験を行った。Reference Example The following animal experiment was conducted to test the toxicity of dimethyl sulfoxide.
体重１５〜２５夕のマウス１０匹（おす５匹、めす５匹
）と、体重１７０〜２３０夕のラット１０匹（おす５匹
、めす５匹）を１グループとし、各グループごとに異な
る量のジメチルスルホキシド（同仁薬化学研究所製、試
薬特級）を投与したのち、温度２２犯、湿度５５％に保
った飼育室内で標準飼料を用いて７日間飼育し、生存状
況を観察した。One group consisted of 10 mice (5 males, 5 females) weighing 15-25 mm and 10 rats (5 males, 5 females) weighing 170-230 mm, and each group received a different amount of After administering dimethyl sulfoxide (manufactured by Dojin Pharmaceutical Research Institute, reagent special grade), the animals were raised for 7 days using standard feed in a breeding room maintained at 22°C temperature and 55% humidity, and their survival status was observed.
前記のジメチルスルホキシドの投与は、これを０．９％
食塩水で、１０の【／ｋ９になるように希釈したものを
それぞれの動物の尾に静脈注射することによって行った
。The administration of dimethyl sulfoxide mentioned above is 0.9%
Dilutions of 10/k9 in saline were performed by intravenous injection into the tail of each animal.
このようにして、平均致死量を求めたところジメチルス
ルホキシドに基づくＬＤ別‘ま６．９泌／ｋ９であった
。In this way, the average lethal dose was determined and was found to be 6.9 secretions/k9 based on dimethyl sulfoxide.
また、比較のために、全く同様にしてエチルアルコール
の平均致死量を求めたところＬはｏは２．８泌／ｋ９で
あった。For comparison, the average lethal dose of ethyl alcohol was determined in exactly the same manner and was found to be 2.8 secretions/k9 for L and o.
このことから、ジメチルスルホキシド‘ま叢性が著しく
低いことが分る。This shows that dimethyl sulfoxide's plexus is extremely low.
実施例 １
ジメチルスルホキシド（同仁薬化学研究所製、試薬特級
）に、ネオシアニン（イーストマンコダック社製、純度
１００％）を加え、６０ｑｏでかきまぜながら溶解させ
、前者１の‘中に後者１奴を含有する溶液を調製する。Example 1 Neocyanine (manufactured by Eastman Kodak Co., Ltd., purity 100%) was added to dimethyl sulfoxide (manufactured by Dojin Pharmaceutical Research Institute, reagent special grade), dissolved while stirring at 60 qo, and 1 part of the latter was added to 1 part of the former. Prepare a solution containing:
この溶液を室温まで冷却し、ろ過して固形物を除いたの
ち、１の‘ずつアルプルに充んし、溶融閉封し、さらに
常法に従って滅菌処理する。このようにしてアンプル入
注射剤を調製した。実施例 ２
実施例１で得たアンプルを開封し、ネオシアニンのジメ
チルスルホキシド溶液を取り出し、蒸留水１の‘で希釈
したのち、注射器を用いて、種々の症状を示す１０人の
患者の疹痛個所に投与した。This solution is cooled to room temperature, filtered to remove solid matter, filled in 1/2 inch portions into an Alpul, melted and sealed, and further sterilized according to a conventional method. In this way, an ampoule injection was prepared. Example 2 Open the ampoule obtained in Example 1, take out the dimethyl sulfoxide solution of neocyanine, dilute it with 1 part of distilled water, and use a syringe to inject the sore spots of 10 patients showing various symptoms. was administered.
ネオシアニンの投薬量は３の９／日でこれを３回に分注
した。このようにして治療した１０日後の効果を第１表
に示す。表中の記号は次の意味をもつ。The dosage of neocyanine was 3:9/day, which was divided into three doses. The effects after 10 days of treatment in this manner are shown in Table 1. The symbols in the table have the following meanings.
十十十 箸効
十十 有効
十 やや有効
士 判定不能又は不変
症状悪化副作用
実施例 ３
実施例１で得たアンプルを開封し、ネオシアニンのジメ
チルスルホキシド溶液を取り出し、蒸留水１のとで希釈
したのち注射器を用いて、身体各部の筋肉の自発痛、運
動痛等の症状を示す１０人の振動病患者の疾痛個所に数
回にわたって投与した。110 Chopstick effect 10 Effective 10 Effective 10 Somewhat effective person Undeterminable or unchangeable symptom worsening side effect Example 3 Open the ampoule obtained in Example 1, take out the dimethyl sulfoxide solution of neocyanine, dilute it with 1 part of distilled water, and then Using a syringe, the drug was administered several times to the affected areas of 10 patients with vibration disease who exhibited symptoms such as spontaneous muscle pain and exercise pain in various parts of the body.
このようにして治療した後の効果を第２表に示す。第２
表
１）疹痛の改善度は投与終了後疹痛の自覚症状の改善の
割合を示す。The effects after treatment in this manner are shown in Table 2. Second
Table 1) Degree of improvement in rash pain indicates the rate of improvement in subjective symptoms of rash pain after completion of administration.
２）持続日数は、疹痛の自覚症状改善の持続日数を示す
。2) The number of days of duration indicates the number of days that the subjective symptoms of eruption pain continue to improve.
３）握力及びタッピングは、末梢運動機能の回復度を示
す指標として測定したものである。3) Grip strength and tapping were measured as indicators of the degree of recovery of peripheral motor function.
Claims (1)
−キノリル）−４，４″−ペンタメチンキノシアニンジ
ヨージドを、ジメチルスルホキシドに溶解して成る注射
用医薬組成物。[Claims] 1 1,1',1''-triethyl-11-(4'
An injectable pharmaceutical composition prepared by dissolving quinolyl)-4,4''-pentamethine quinocyanine diiodide in dimethyl sulfoxide.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10704880A JPS603364B2 (en) | 1980-08-04 | 1980-08-04 | Pharmaceutical composition for injection |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10704880A JPS603364B2 (en) | 1980-08-04 | 1980-08-04 | Pharmaceutical composition for injection |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5731609A JPS5731609A (en) | 1982-02-20 |
| JPS603364B2 true JPS603364B2 (en) | 1985-01-28 |
Family
ID=14449188
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP10704880A Expired JPS603364B2 (en) | 1980-08-04 | 1980-08-04 | Pharmaceutical composition for injection |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS603364B2 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002078669A1 (en) * | 2001-03-30 | 2002-10-10 | Takeda Chemical Industries, Ltd. | Medicinal solutions |
-
1980
- 1980-08-04 JP JP10704880A patent/JPS603364B2/en not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| JPS5731609A (en) | 1982-02-20 |
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