CH229981A - Process for the preparation of a solution containing strychnine oxide. - Google Patents
Process for the preparation of a solution containing strychnine oxide.Info
- Publication number
- CH229981A CH229981A CH229981DA CH229981A CH 229981 A CH229981 A CH 229981A CH 229981D A CH229981D A CH 229981DA CH 229981 A CH229981 A CH 229981A
- Authority
- CH
- Switzerland
- Prior art keywords
- strychnine
- oxide
- oil
- preparation
- solution containing
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
Landscapes
- Health & Medical Sciences (AREA)
- Dermatology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
Verfahren zur Herstellung einer strychninoxydhaltigen Lösung;.
Wird Strychnin in Öl gelöst, so tritt bei Injektion die bekannte Depotwirkung ein, die zur Folge hat, dass nicht nur die Wirkungsdauer des St. rychnins verlängert wird, sondern auch infolge langsamerer Resorption die Giftwirkung verringert wird. Versuche haben ergeben, dass die Toxizität bei Öllösung gegenüber der wässrigen Lösung etwa auf den fünften Teil zurückgeht.
Es wurde nun gefunden, dass durch Erhitzen einer Lösung von Strychnin in Peroxyde enthaltenden öligen Lösungsmitteln, wie fetten Ölen oder freien Fettsäuren, gegebenenfalls gelöst in fetten Ölen, eine überraschende weitere Entgiftung unter völliger Erhaltung der therapeutischen Wirkung erzielt wird, welche die toxische Dosis weiter auf das Doppelte oder Mehrfache der nicht erhitzten Öllösung steigert.
Diese Entgiftung beruht, wie gefunden wurde, auf der Umwandlung von Strychnin in Strychninoxyd vermöge der in den fetten Ölen und Fettsäuren vorhandenen Peroxyde und hat den grossen Vorteil, dass von dem neuen Produkt unbedenklich Dosen injiziert werden können, welche bei gewöhnlichen Lösungen leicht zu Krampferscheinungen führten. Ferner kann bei der Möglichkeit erhöhter Strychnindosen mit dem neuen Produkt eine länger dauernde Depotwirkung und gleichzeitig eine noch stärkere ilAreislaufwir- kung erzielt werden.
Als erfindungsgemässes Lösungsmittel kommt insbesondere Weizenkeimöl in Frage, welches den Vorteil bietet, dass durch die Injektion dem Patienten gleichzeitig Vitamine zugeführt werden.
Beispiele:
1. 2 g Strychninbase werden mit 200 cm3 Weizenkeimöl auf dem siedenden Wasserbad zur Lösung gebracht und anschliessend im Brutschrank 70 Stunden auf 700 erwärmt.
Die Lösung bleibt auch nach dem Erkalten klar.
2. 1 g Strychnin wird mit 3 g Ölsäure auf dem Wasserbad verschmolzen und mit 200 cm3 Sesamöl verdünnt, wobei klare Lösung eintritt. An Stelle von Sesamöl kann auch Olivenöl, Maisöl oder entsäuertes Weizenkeimöl zur Verdünnung verwendet werden. Anschliessend wird die Lösung 70 Stunden auf 700 erwärmt. Die Lösung bleibt auch nach dem Erkalten klar.
Process for the preparation of a solution containing strychnine oxide ;.
If strychnine is dissolved in oil, the well-known depot effect occurs upon injection, which means that not only the duration of the effect of the St. rychnine is extended, but also that the poisonous effect is reduced as a result of slower absorption. Tests have shown that the toxicity of an oil solution compared to the aqueous solution is about a fifth.
It has now been found that by heating a solution of strychnine in peroxides containing oily solvents, such as fatty oils or free fatty acids, optionally dissolved in fatty oils, a surprising further detoxification is achieved with complete retention of the therapeutic effect, which further increases the toxic dose increases twice or more times the unheated oil solution.
This detoxification is based, as has been found, on the conversion of strychnine into strychnine oxide by means of the peroxides present in the fatty oils and fatty acids and has the great advantage that doses of the new product can be safely injected, which easily lead to symptoms of cramps in common solutions . Furthermore, with the possibility of increased strychnine doses, the new product can achieve a longer-lasting depot effect and at the same time an even stronger circulatory effect.
Wheat germ oil, in particular, comes into consideration as the solvent according to the invention, which offers the advantage that vitamins are simultaneously supplied to the patient through the injection.
Examples:
1. 2 g of strychnine base are dissolved in 200 cm3 of wheat germ oil on a boiling water bath and then heated to 700 for 70 hours in an incubator.
The solution remains clear even after cooling.
2. 1 g strychnine is fused with 3 g oleic acid in a water bath and diluted with 200 cm3 sesame oil, whereby a clear solution occurs. Instead of sesame oil, olive oil, corn oil or deacidified wheat germ oil can also be used for dilution. The solution is then heated to 700 for 70 hours. The solution remains clear even after cooling.
Claims (1)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE229981X | 1939-02-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CH229981A true CH229981A (en) | 1943-11-30 |
Family
ID=5868122
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CH229981D CH229981A (en) | 1939-02-08 | 1941-10-28 | Process for the preparation of a solution containing strychnine oxide. |
Country Status (1)
| Country | Link |
|---|---|
| CH (1) | CH229981A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1015808B (en) * | 1953-07-21 | 1957-09-19 | Donau Pharmazie G M B H | Process for the production of new N-oxydstrychnine or N-oxyd-brucic acid esters of amino alcohols |
| EP0132105A2 (en) * | 1983-07-13 | 1985-01-23 | Yamanouchi Pharmaceutical Co. Ltd. | Oily composition of aclarubicin or hydrochloride thereof |
-
1941
- 1941-10-28 CH CH229981D patent/CH229981A/en unknown
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1015808B (en) * | 1953-07-21 | 1957-09-19 | Donau Pharmazie G M B H | Process for the production of new N-oxydstrychnine or N-oxyd-brucic acid esters of amino alcohols |
| EP0132105A2 (en) * | 1983-07-13 | 1985-01-23 | Yamanouchi Pharmaceutical Co. Ltd. | Oily composition of aclarubicin or hydrochloride thereof |
| EP0132105A3 (en) * | 1983-07-13 | 1986-08-27 | Yamanouchi Pharmaceutical Co. Ltd. | Oily composition of aclarubicin or hydrochloride thereof |
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