DE629662C - Process for the production of a concentrated, durable, aqueous theophylline solution - Google Patents

Process for the production of a concentrated, durable, aqueous theophylline solution

Info

Publication number
DE629662C
DE629662C DEE43783D DEE0043783D DE629662C DE 629662 C DE629662 C DE 629662C DE E43783 D DEE43783 D DE E43783D DE E0043783 D DEE0043783 D DE E0043783D DE 629662 C DE629662 C DE 629662C
Authority
DE
Germany
Prior art keywords
concentrated
durable
theophylline
solution
production
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
DEE43783D
Other languages
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to DEE43783D priority Critical patent/DE629662C/en
Application granted granted Critical
Publication of DE629662C publication Critical patent/DE629662C/en
Expired legal-status Critical Current

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
    • 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
    • A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
    • 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
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones

Description

Verfahren zur Herstellung einer konzentrierten, haltbaren, wäßrigen Theophyllinlösung Die therapeutische Verwendbarkeit von Theophyllin zu Injektionszwecken ist dadurch stark eingeschränkt, daß dieser Stoff in kaltem Wasser nur sehr wenig (etwa zu 0,5010) löslich ist. Den bekannten wasserlöslichen Theophyllinverbindungen haften gewisse Nachteile an. Teils reagieren sie stark alkalisch und verursachen daher bei intramuskulärer Injektion unangenehme Schmerzen, teils sind sie nicht in der üblichen Weise durch Erhitzen ohne Zersetzung sterilisierbar.Process for the preparation of a concentrated, durable, aqueous theophylline solution The therapeutic usability of theophylline for injection purposes is severely limited by the fact that this substance is only very sparingly soluble (about 0.5010) in cold water. The known water-soluble theophylline compounds have certain disadvantages. Sometimes they have a strong alkaline reaction and therefore cause unpleasant pain when injected intramuscularly, sometimes they cannot be sterilized in the usual way by heating without decomposition.

Es ist ferner bekannt, in Wasser schwer lösliche Stoffe durch Zusatz von Lösungsvermittlern besser löslich zu machen, insbesondere ist schon vorgeschlagen worden, Coffein-Natriumbenzoat als Lösungshilfsmittel zur Herstellung konzentrierter Theophyllinlösungen .zu verwenden. Eine so hergestellte Lösung enthält neben etwa io Theophyllin etwa 30010 Coffein-Natriumbenzoat.It is also known that substances that are sparingly soluble in water can be made more soluble by adding solubilizers; in particular, it has already been proposed to use caffeine sodium benzoate as a dissolving aid for the preparation of concentrated theophylline solutions. A solution prepared in this way contains, in addition to about 10 o theophylline, about 30,010 caffeine sodium benzoate.

Durch das Verfahren der vorliegenden Erfindung gelingt es nun, konzentrierte Lösungen von Theophyllin mit geringeren Mengen von festen Lösungsvermittlern herzustellen, was für die Verwendbarkeit der Lösungen für Injektionszwecke von Bedeutung ist.By the method of the present invention it is now possible to concentrate Prepare solutions of theophylline with smaller amounts of solid solubilizers, which is important for the usability of the solutions for injection purposes.

Es wurde gefunden, daß die Herstellung einer wäßrigen; hochkonzentrierten, hitzebeständigen und haltbaren Theophyllinlösung dadurch möglich wird, daß man Theophyllin, Coffein und p-Aminobenzoyldiäthylaminoäthanolhydrochlorid in einem Molekularverhältnis von 2:1:1 in Wasser, gegebenenfalls in der Wärme, löst. Diese Mischung enthält also etwa 45 % Theophyllin, 3 10/0 p-Aminobenzoyldiäthylaminoäthanolhydrochlorid und 2¢ 0/p Coffein. Wird die Gesamtmenge der festen Stoffe im Verhältnis i : i o in Wasser gelöst, so beträgt die Konzentration der Lösung an Theophyllin etwa 4,5%; die Löslichkeit des letzteren ist also verzehnfacht. Die Lösung reagiert neutral und ist ohne Zersetzung sterilisierbar. Dampft man die Lösung im Vakuum zur Trockne ein, so erhält man eine weiße Masse, die in Wasser wieder im gleichen Verhältnis löslich ist.It has been found that the preparation of an aqueous; highly concentrated, heat-resistant and durable theophylline solution is made possible by dissolving theophylline, caffeine and p-aminobenzoyldiethylaminoethanol hydrochloride in a molecular ratio of 2: 1: 1 in water, optionally in the heat. This mixture thus contains about 45% theophylline, 3 1 0/0 p-aminobenzoyl diethylaminoethanol hydrochloride and 2 0 / p caffeine. If the total amount of solids is dissolved in water in the ratio i: io, the concentration of theophylline in the solution is about 4.5%; the solubility of the latter is thus tenfold. The solution reacts neutrally and can be sterilized without decomposition. If the solution is evaporated to dryness in a vacuum, a white mass is obtained which is soluble in water in the same proportion.

Claims (1)

PATENTANSPRUCH: Verfahren zur Herstellung einer konzentrierten, haltbaren, wäßrigen Theophyllinlösung, dadurch gekennzeichnet, daß Theophyllin, Coffein und p-Aminobenzoyldiäthylaminoäthanolhydrochlorid in einem Molekularverhältnis von etwa 2:1:1 in Wasser gelöst werden. Claim: Process for the preparation of a concentrated, durable, aqueous theophylline solution, characterized in that theophylline, caffeine and p-aminobenzoyl diethylaminoethanol hydrochloride are dissolved in water in a molecular ratio of about 2: 1: 1.
DEE43783D 1933-01-11 1933-01-11 Process for the production of a concentrated, durable, aqueous theophylline solution Expired DE629662C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
DEE43783D DE629662C (en) 1933-01-11 1933-01-11 Process for the production of a concentrated, durable, aqueous theophylline solution

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DEE43783D DE629662C (en) 1933-01-11 1933-01-11 Process for the production of a concentrated, durable, aqueous theophylline solution

Publications (1)

Publication Number Publication Date
DE629662C true DE629662C (en) 1936-05-08

Family

ID=7079609

Family Applications (1)

Application Number Title Priority Date Filing Date
DEE43783D Expired DE629662C (en) 1933-01-11 1933-01-11 Process for the production of a concentrated, durable, aqueous theophylline solution

Country Status (1)

Country Link
DE (1) DE629662C (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2519450A (en) * 1949-01-11 1950-08-22 Chattanooga Medicine Co Theophylline-monoaminobenzoic acid-alkali metal hydroxide reaction product
DE944518C (en) * 1950-08-20 1956-06-14 Byk Gulden Lomberg Chem Fab Process for the preparation of solutions of xanthines substituted in the 1,3-position

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2519450A (en) * 1949-01-11 1950-08-22 Chattanooga Medicine Co Theophylline-monoaminobenzoic acid-alkali metal hydroxide reaction product
DE944518C (en) * 1950-08-20 1956-06-14 Byk Gulden Lomberg Chem Fab Process for the preparation of solutions of xanthines substituted in the 1,3-position

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