CH221459A - Process for the preparation of a solvent for theophylline. - Google Patents

Process for the preparation of a solvent for theophylline.

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Publication number
CH221459A
CH221459A CH221459DA CH221459A CH 221459 A CH221459 A CH 221459A CH 221459D A CH221459D A CH 221459DA CH 221459 A CH221459 A CH 221459A
Authority
CH
Switzerland
Prior art keywords
sep
theophylline
solvent
preparation
solutions
Prior art date
Application number
Other languages
German (de)
Inventor
Aktiengesellschaft Che Homburg
Original Assignee
Chemiewerk Homburg Aktiengesel
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 Chemiewerk Homburg Aktiengesel filed Critical Chemiewerk Homburg Aktiengesel
Publication of CH221459A publication Critical patent/CH221459A/en

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Description

  

      Terfahren    zur Herstellung eines     Lösungsmittels    für     Theophyllin.       Die Erfindung bezieht sich auf die Her  stellung eines     Lösunps        mittels    für     Theophyllin.     



       Theophyllin    wird in der Therapie zu  zahlreichen Zwecken verwendet. Dieser Ver  wendung sind aber durch .die Schwerlöslich  keit des     Theophyllins    in Wasser     .Seliran-          ken    gesetzt.  



  Es sind bereits verschiedene Verfahren  bekannt, um das     schwerlösliche        Theophyllin     in     wässrige    Lösungen überzuführen. Hierbei  hat man als     Lösungsvermittler        hauptsächlich     verschiedene Amine angewendet, und     zwarPi-          pera.zin        (deutsche        Patentschriften    Nr.     21.18'76,     217620 und 224981), primäre oder sekundäre       aliphatische    Diamine, insbesondere Äthylen  diamin (deutsche Patentschrift Nr.

   238695),       Diäthaeolamin    (deutsche     Patentschrift    Nr.       583054    der     An.melderin)    und schliesslich  auch wasserunlösliche Amine wie     ss-Phenyl-          isopropylamin    oder seine Derivate mit     ephe-          drinartiger    Wirkung (-deutsche Patentschrif  ten Nr. 690488 und<B>69139</B> der     Anmnelderin).       Die     nach    :

  diesen zahlreichen     Vorschlägen     erhaltenen Lösungen entsprechen zwar zahl  reichen Wünschen, haben aber den     Nachteil,     ziemlich stark alkalisch zu sein.     Es    ist für       Injektionszwecke        wünschenswert,    Lösungen       des        Theophyllins    zu erhalten, die einen mög  lichst neutralen oder gegebenenfalls schwach  sauren     pH-Wert    aufweisen.  



  Es wurde nun     befunden,    dass man ein  Lösungsmittel für das     Theophyllin,        das',der-          artige        Theophyllinlösungen    ergibt, dadurch       herstellen    kann, dass man 'Salze zur Lösungs  vermittlung geeigneter Amine mit     ss-Resor-          cylsäure    mit Wasser vermischt.  



  In Ausübung der     Erfindung    kann man  sowohl Salze der an sich     wasserlöslichen     Amine, z. B. des     Äthylendiamins    oder     Diätha-          nolamins,    verwenden als auch Salze an sich       wmseriinlöslicher    oder     achwerlöslicher    Amine,  z.

   B. des     ss-Phenylisopropylamins    oder seiner  Derivate mit     ephedrinartiger    Wirkung, wie       Ephedri:n    selbst oder synthetisches, racemi-    
EMI0002.0001     
  
    sches <SEP> Epliedrin <SEP> (Phenylmethylaniinopi@opa  nol) <SEP> zur <SEP> Anwendun-- <SEP> bringen. <SEP> In <SEP> allen <SEP> Fällen
<tb>  bekommt <SEP> man <SEP> Lösungsmittel <SEP> für <SEP> Theophyl  lin, <SEP> die <SEP> konzentrierte. <SEP> mit <SEP> MTasser <SEP> klar <SEP> ver  dünnbare <SEP> Lösungen <SEP> ergeben, <SEP> die <SEP> schwaeh  sa.uer <SEP> bezw. <SEP> neutral <SEP> reagieren.
<tb>  



  )Will <SEP> man <SEP> die <SEP> Lösungen <SEP> auf <SEP> bestimmte
<tb>  ganz <SEP> genaue <SEP> PH-Werte <SEP> einstellen, <SEP> so <SEP> ist <SEP> dies
<tb>  dadurch <SEP> möglich, <SEP> da.ss <SEP> man <SEP> neben <SEP> dein <SEP> re.sor  cylsa.uren <SEP> Salz <SEP> eine <SEP> geringe <SEP> llen.ge <SEP> an <SEP> freier
<tb>  Re.sorcvlsäure <SEP> einerseits <SEP> oder <SEP> an <SEP> freien <SEP> Ami  nen <SEP> anderseits <SEP> verwendet.

              Beispiele:     1. 58,5     g        ss-resoreylsaures        Epliedrin    wer  den mit     destilliertem        Wasser    zu     WI    I ein' Lö  sung     vermischt.    In dieser Lösung     können     17     g        Theophyllin    gelöst werden.  
EMI0002.0013     
  
    ?. <SEP> fi-1,,8 <SEP> gf <SEP> ss-i@esorcyl:saiireh <SEP> Diäthanolamin
<tb>  werden <SEP> ad <SEP> 100 <SEP> ein' <SEP> iii <SEP> Wasser <SEP> gelöst. <SEP> In <SEP> die  ser <SEP> Lüsuiig <SEP> können <SEP> 1(>> <SEP> g <SEP> Theophyllin <SEP> gelöst
<tb>  werden.
<tb>  



  Die <SEP> pH-Werte <SEP> der <SEP> nach <SEP> diesen <SEP> Beispielen
<tb>  erhaltenen <SEP> Lösungen <SEP> bewegen <SEP> siele <SEP> zwischen
<tb>  -5-7,4.



      Method of making a solvent for theophylline. The invention relates to the Her position of a solution means for theophylline.



       Theophylline is used in therapy for a variety of purposes. This use is, however, due to the poor solubility of theophylline in water. Selirands.



  Various methods are already known for converting the sparingly soluble theophylline into aqueous solutions. Here, different amines have mainly been used as solubilizers, namely pipera.zin (German patent specifications 21.18'76, 217620 and 224981), primary or secondary aliphatic diamines, in particular ethylene diamine (German patent specification No.

   238695), diethaeolamine (German patent specification No. 583054 by the applicant) and finally also water-insoluble amines such as β-phenylisopropylamine or its derivatives with an ephe- drine-like effect (-German patent specifications No. 690488 and <B> 69139 </ B > the applicant). The after    :

  The solutions obtained from these numerous proposals, while satisfying numerous wishes, have the disadvantage of being rather strongly alkaline. For injection purposes, it is desirable to obtain solutions of theophylline which have a pH that is as neutral as possible, or possibly weakly acidic.



  It has now been found that a solvent for theophylline, which gives such theophylline solutions, can be produced by mixing salts with ß-resorcylic acid with water to mediate the solution of suitable amines.



  In the practice of the invention, both salts of the water-soluble amines, eg. B. of ethylenediamine or diethanolamine, use as well as salts per se insoluble or slightly soluble amines, z.

   B. of ss-phenylisopropylamine or its derivatives with ephedrine-like effects, such as ephedri: n itself or synthetic, racemi-
EMI0002.0001
  
    sches <SEP> Epliedrin <SEP> (Phenylmethylaniinopi @ opa nol) <SEP> for <SEP> application - <SEP>. <SEP> In <SEP> all <SEP> cases
<tb> you get <SEP> one <SEP> solvent <SEP> for <SEP> theophylline, <SEP> the <SEP> concentrated. <SEP> with <SEP> MTasser <SEP> clear <SEP> dilutable <SEP> solutions <SEP> result, <SEP> the <SEP> black sa.uer <SEP> resp. <SEP> react neutrally <SEP>.
<tb>



  ) If <SEP> one <SEP> wants to determine the <SEP> solutions <SEP> on <SEP>
<tb> completely <SEP> set exact <SEP> PH values <SEP>, <SEP> so <SEP> is <SEP> this
<tb> thereby <SEP> possible, <SEP> da.ss <SEP> man <SEP> next to <SEP> your <SEP> re.sor cylsa.uren <SEP> salt <SEP> a <SEP> low <SEP > llen.ge <SEP> to <SEP> freer
<tb> Re.sorcvläure <SEP> on the one hand <SEP> or <SEP> on <SEP> free <SEP> amines <SEP> on the other hand <SEP> used.

              Examples: 1. 58.5 g of ss-resoreyl acid epliedrin are mixed with distilled water to form a solution. 17 g of theophylline can be dissolved in this solution.
EMI0002.0013
  
    ?. <SEP> fi-1,, 8 <SEP> gf <SEP> ss-i @ esorcyl: saiireh <SEP> diethanolamine
<tb> <SEP> ad <SEP> 100 <SEP> a '<SEP> iii <SEP> water <SEP> are dissolved. <SEP> In <SEP> these <SEP> Lüsuiig <SEP> can <SEP> 1 (>> <SEP> g <SEP> theophylline <SEP> dissolved
<tb> be.
<tb>



  The <SEP> pH values <SEP> of the <SEP> according to <SEP> these <SEP> examples
<tb> received <SEP> solutions <SEP> move <SEP> and <SEP> between
<tb> -5-7.4.

 

Claims (1)

PATENTANSPRUCH: Verfahren zur Herstellung eines Lösun bs- mit.iels für Theophyllin, dadurch ; ekenn- zcichnel, dass man Salze zur Lösungsvermitt lung geeigneter Amine mit ss-ssesoreylsäure mit Wasser vermiseht. PATENT CLAIM: Process for the preparation of a solution for theophylline, thereby; It is noted that salts for solubilizing suitable amines with ß-ssesoreyl acid are mixed with water.
CH221459D 1940-05-25 1941-05-09 Process for the preparation of a solvent for theophylline. CH221459A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE221459X 1940-05-25

Publications (1)

Publication Number Publication Date
CH221459A true CH221459A (en) 1942-05-31

Family

ID=5840124

Family Applications (1)

Application Number Title Priority Date Filing Date
CH221459D CH221459A (en) 1940-05-25 1941-05-09 Process for the preparation of a solvent for theophylline.

Country Status (1)

Country Link
CH (1) CH221459A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE917564C (en) * 1951-09-26 1954-09-06 Kali Chemie Ag Process for the production of permanent aqueous solutions of khellin
DE948184C (en) * 1953-01-31 1956-08-30 Hoechst Ag Process for the production of aqueous solutions of steroid hormones

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE917564C (en) * 1951-09-26 1954-09-06 Kali Chemie Ag Process for the production of permanent aqueous solutions of khellin
DE948184C (en) * 1953-01-31 1956-08-30 Hoechst Ag Process for the production of aqueous solutions of steroid hormones

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