DE725923C - Process for the production of concentrated solutions of organic medicinal products which are poorly soluble or insoluble in water - Google Patents

Process for the production of concentrated solutions of organic medicinal products which are poorly soluble or insoluble in water

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Publication number
DE725923C
DE725923C DEU12901D DEU0012901D DE725923C DE 725923 C DE725923 C DE 725923C DE U12901 D DEU12901 D DE U12901D DE U0012901 D DEU0012901 D DE U0012901D DE 725923 C DE725923 C DE 725923C
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DE
Germany
Prior art keywords
weight
parts
water
production
insoluble
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
Application number
DEU12901D
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German (de)
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
CHEM FAB SCHUERHOLZ
Original Assignee
CHEM FAB SCHUERHOLZ
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by CHEM FAB SCHUERHOLZ filed Critical CHEM FAB SCHUERHOLZ
Priority to DEU12901D priority Critical patent/DE725923C/en
Application granted granted Critical
Publication of DE725923C publication Critical patent/DE725923C/en
Expired legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (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 konzentrierter Lösungen von in Wasser schwer- oder unlöslichen organischen Arzneistoffen Es ist bekannt, Urethane als Lösungsvermittler für schwer lösliche Arzneimittel zu verwenden. Die mit wäßrigen Urethanlösungen erhältlichen Konzentrationen sind aber unzureichend, so daß versucht wurde, diese durch. anderweitige Zusätze zu erhöhen. Aber auch die mit solchen Hilfsmitteln erhaltenen Konzentrationen gehen praktisch nicht über /o hinaus.Process for the production of concentrated solutions of or insoluble organic drugs It is known to use urethanes as solubilizers to be used for poorly soluble drugs. Those with aqueous urethane solutions available concentrations are inadequate, so that this was tried by. to increase other additives. But also those obtained with such aids Concentrations practically do not exceed / o.

Es wurde nun gefunden, daß man mit Hilfe von Alkoholen oder deren Estern das Lösungsvermögen von Urethanen in einem AIaße erhöhen kann, das keinesfalls zu erwarten mar. So gelingt es, Barbitursäureabkömmlinge und viele andere Arzneimittel zu 15 °/n und mehr in haltbare Lösungen zu überführen. It has now been found that with the help of alcohols or their Esters can increase the dissolving power of urethanes to an extent that by no means expected mar. This is how it succeeds in making barbituric acid derivatives and many other drugs to convert 15% and more into durable solutions.

Während es sich bei den bisher zusätzlich verwendeten Lösungsvermittlern um mehr oder minder differente Substanzen handelt, z. T. um solche mit starker pharmakologischer Eigenwirkung, ist bei vorliegendem Verfahren keine wesentliche Beeinflussung der in Lösung gebrachten Arzneimittel vorhanden, zumal meist nur geringe Mengen des als Zusatz benötigten Alkohols bzw. Esters erforderlich sind. While it is the case with the solubilizers additionally used so far more or less different substances are involved, e.g. T. to those with strong pharmacological Intrinsic effect, is not a significant influence on the present method Drugs brought into solution are present, especially since usually only small amounts of the alcohol or ester required as an additive are required.

Die erfindungsgemäße Zusammenstellung der LöSungsvermittler besitzt praktisch keine vsvirl;ung und ermöglicht die Herstellung von Lösungen von hoher Konzentration, welche selbst bei Temperaturen, die wesentlich unterhalb der Zimmertemperatur, z. B. bei 13 0 C, liegen, haltbar sind, und zwar auf unbegrenzte Zeitdauer. The composition according to the invention of the solubilizer has practically no vsvirl; ung and enables the preparation of solutions of high Concentration, which even at temperatures that are significantly below room temperature, z. B. at 13 0 C, are durable, and for an unlimited period of time.

Beispiel I I8 Gewichtsteile Diäthylbarbitursäure, 62 Gewichtsteile Äthylurethan, 10 Gewichtsteile Äthylalkohol und 10 Gewichtsteile ÄVasser geben eine haltbare Lösung. Example I 18 parts by weight of diethyl barbituric acid, 62 parts by weight Ethyl urethane, 10 parts by weight of ethyl alcohol and 10 parts by weight of water give a durable solution.

Beispiel 2 25 Gewichtsteile Phenyläthylbarbitursäure, 57 Gewichtsteile Äthylurethan, 7 Gewichtsteile Wasser und 1 1 Gewichtsteile Glykol geben eine klare, haltbare und sterilisierbare Lösung. Example 2 25 parts by weight of phenylethylbarbituric acid, 57 parts by weight Ethyl urethane, 7 parts by weight of water and 1 1 parts by weight of glycol give a clear, durable and sterilizable solution.

Beispiel 3 20 Gewichtsteile Diäthylbarbitursäure, 60 Gewichtsteile Äthylurethan. 7 Gewichtsteile Wasser und I3 Gewichtsteile Essigsäureäthylester geben eine klare und haltbare Lösung. Example 3 20 parts by weight of diethyl barbituric acid, 60 parts by weight Ethyl urethane. Add 7 parts by weight of water and 13 parts by weight of ethyl acetate a clear and durable solution.

Ebenso verhalten sich: Beispiel 4 20 Gewichtsteile fliäthylbarbitursäure, 64 Gewichtsteile Äthylurethan, 8 Gewichtsteile Wasser und 8 Gewichtsteile Amylenhydrat. The same applies: Example 4 20 parts by weight of fliethylbarbituric acid, 64 parts by weight of ethyl urethane, 8 parts by weight of water and 8 parts by weight of amylene hydrate.

Beispiel 5 30 Gewichtsteile Chinin (Base), 50 Gewichtsteile Äthylurethan, 10 Gewichtsteile Wasser und Io Gewichtsteile Amylenhydrat. Example 5 30 parts by weight of quinine (base), 50 parts by weight of ethyl urethane, 10 parts by weight of water and 10 parts by weight of amylene hydrate.

Beispiel 6 25 Gewichtsteile Chinin (Base), So Gewichtsteile Athylurethan, 10 Gewichtsteile Wasser und 15 Gewichtsteile Glykol. Example 6 25 parts by weight of quinine (base), so parts by weight of ethyl urethane, 10 parts by weight of water and 15 parts by weight of glycol.

Beispiel 7 30 Gewichtsteile Kampher, 50 Gewichtsteile Äthylurethan, IO Gewichtsteile Wasser und IO Gewichtsteile Glykol. Example 7 30 parts by weight of camphor, 50 parts by weight of ethyl urethane, 10 parts by weight of water and 10 parts by weight of glycol.

Claims (1)

PATENTANSPRUCH: Verfahren zur Herstellung konzentrierter, haltbarer, tropf- bzw. injizierbarer Lösungen von in Wasser schwer oder unlöslichen organischen Arzneistoffen unter Verwendung von Lösungsvermittlern, dadurch gekennzeichnet, daß eine Mischung von Urethanen mit Wasser und wasserlöslichen Alkoholen oder deren wasserlöslichen Estern als Lösungsmittel verwendet wird. PATENT CLAIM: Process for the production of concentrated, durable, Drip or injectable solutions of sparingly or insoluble organic solutions in water Medicinal substances using solubilizers, characterized in that a mixture of urethanes with water and water-soluble alcohols or their water-soluble esters is used as a solvent. Ergänzungsblatt atent Patentschrift 72 mit Supplementary sheet atent patent specification 72 with
DEU12901D 1935-03-08 1935-03-08 Process for the production of concentrated solutions of organic medicinal products which are poorly soluble or insoluble in water Expired DE725923C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
DEU12901D DE725923C (en) 1935-03-08 1935-03-08 Process for the production of concentrated solutions of organic medicinal products which are poorly soluble or insoluble in water

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DEU12901D DE725923C (en) 1935-03-08 1935-03-08 Process for the production of concentrated solutions of organic medicinal products which are poorly soluble or insoluble in water

Publications (1)

Publication Number Publication Date
DE725923C true DE725923C (en) 1943-11-30

Family

ID=7568138

Family Applications (1)

Application Number Title Priority Date Filing Date
DEU12901D Expired DE725923C (en) 1935-03-08 1935-03-08 Process for the production of concentrated solutions of organic medicinal products which are poorly soluble or insoluble in water

Country Status (1)

Country Link
DE (1) DE725923C (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE954724C (en) * 1953-04-09 1956-12-20 Dr Siegfried Fischl Process for increasing the water solubility of lipophilic therapeutic substances

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE954724C (en) * 1953-04-09 1956-12-20 Dr Siegfried Fischl Process for increasing the water solubility of lipophilic therapeutic substances

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