AT366573B - METHOD FOR PRODUCING A PHARMACEUTICAL PREPARATION - Google Patents

METHOD FOR PRODUCING A PHARMACEUTICAL PREPARATION

Info

Publication number
AT366573B
AT366573B AT0221080A AT221080A AT366573B AT 366573 B AT366573 B AT 366573B AT 0221080 A AT0221080 A AT 0221080A AT 221080 A AT221080 A AT 221080A AT 366573 B AT366573 B AT 366573B
Authority
AT
Austria
Prior art keywords
sep
producing
pharmaceutical preparation
polyethylene glycol
ester
Prior art date
Application number
AT0221080A
Other languages
German (de)
Other versions
ATA221080A (en
Inventor
H Ludwig Dr Schlager
Original Assignee
Gerot Pharmazeutika
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 Gerot Pharmazeutika filed Critical Gerot Pharmazeutika
Priority to AT0221080A priority Critical patent/AT366573B/en
Priority to SE8004383A priority patent/SE445422B/en
Priority to NO801759A priority patent/NO153951C/en
Priority to FR8013490A priority patent/FR2459658A1/en
Priority to FI801988A priority patent/FI72428C/en
Priority to DE19803023109 priority patent/DE3023109A1/en
Priority to GB8020457A priority patent/GB2052980B/en
Publication of ATA221080A publication Critical patent/ATA221080A/en
Application granted granted Critical
Publication of AT366573B publication Critical patent/AT366573B/en
Priority to US06/594,060 priority patent/US4913901A/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/04Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/366Lactones having six-membered rings, e.g. delta-lactones
    • A61K31/37Coumarins, e.g. psoralen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A61K8/498Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Description

  

   <Desc/Clms Page number 1> 
 



   Die Erfindung betrifft ein Verfahren zur Herstellung einer oral applizierbaren und stabilen Lösung, welche den zur Photochemotherapie der Psoriasis verwendbaren Wirkstoff Methoxsalen   (8-Methoxy-furo - 3', 2 !   : 6,   7"j-cumarin)   mit der Formel 
 EMI1.1 
 
 EMI1.2 
 

 <Desc/Clms Page number 2> 

 Beispiel 3 : 
 EMI2.1 
 
<tb> 
<tb> 0, <SEP> 34 <SEP> g <SEP> Methoxsalen
<tb> 6, <SEP> 50 <SEP> g <SEP> Polyäthylenglykol <SEP> 300
<tb> 1, <SEP> 80 <SEP> g <SEP> Partialestergemisch <SEP> von <SEP> Ca <SEP> -C'2- <SEP> Fettsäuren <SEP> mit <SEP> oxyäthyliertem <SEP> Glycerin
<tb> 1, <SEP> 06 <SEP> g <SEP> Benzylalkohol
<tb> 0, <SEP> 92 <SEP> g <SEP> Glycerinformal*)
<tb> 0, <SEP> 16 <SEP> g <SEP> Aromastoff <SEP> 
<tb> 
 Beispiel 4 :

   
 EMI2.2 
 
<tb> 
<tb> 0, <SEP> 42 <SEP> g <SEP> Methoxsalen
<tb> 4, <SEP> 80 <SEP> g <SEP> Glycerinformal*)
<tb> 2, <SEP> 20 <SEP> g <SEP> Glycofurol**)
<tb> 1, <SEP> 84 <SEP> g <SEP> Pfefferminzöl <SEP> 
<tb> 1, <SEP> 56 <SEP> g <SEP> Partialestergemisch <SEP> hydrierter <SEP> Ricinusölfettsäuren <SEP> mit <SEP> oxyäthyliertem <SEP> Glycerin
<tb> 
 Beispiel 5 : 
 EMI2.3 
 
<tb> 
<tb> 0, <SEP> 43 <SEP> g <SEP> Methoxsalen
<tb> 5, <SEP> 00 <SEP> g <SEP> Glycerinformal*)
<tb> 2, <SEP> 32 <SEP> g <SEP> Polyäthylenglykol <SEP> 300
<tb> 2, <SEP> 06 <SEP> g <SEP> Partial <SEP> estergemisch <SEP> von <SEP> Ricinusölfettsäuren <SEP> mit <SEP> oxyäthyliertem <SEP> Glycerin
<tb> 1, <SEP> 34 <SEP> g <SEP> Dimethylsulfoxyd
<tb> 0, <SEP> 16 <SEP> g <SEP> Aromastoff <SEP> 
<tb> 
 
Beispiel 6 :

   Man löst 10 g pulverisiertes Methoxsalen durch Rühren in einer Mischung von 365 g Polyäthylenglykol 400,50 g Dimethylacetamid, 50 g Glycerin und 40 g Glycerintriacetat auf, verdünnt mit 30 g Wasser, rührt gut durch und füllt jeweils 0, 5 ml der erhaltenen Lösung mittels einer Dosiervorrichtung in Kapseln ab. Diese enthalten dann 10 mg Wirkstoff/Kapsel. 



   *) Glycerinformal stellt ein Gemisch aus 4-Hydroxymethyl-1, 3-dioxolan und   5-Hydroxy-1, 3-dioxan   dar. 



    **) Glycofurole   sind Polyäthylenglykoläther des Tetrahydrofurfurylalkohols (H. Janistyn, Handbuch der Kosmetika und Riechstoffe, 3. Auflage, 1. Band, pp. 443,444). 



   PATENTANSPRÜCHE : 
1. Verfahren zur Herstellung einer pharmazeutischen Zubereitung zur oralen Verabreichung, gegebenenfalls in. Form von Kapseln, welche den Wirkstoff 8-Methoxy-furo-   [ 3', 2'   :   6,   -cumarin und gewünschtenfalls pharmazeutisch verwendbare Geschmackskorrigentien, Antioxydantien und/oder Konservierungsmittel enthält, dadurch gekennzeichnet, dass man eine stabile Lösung des Wirkstoffes herstellt, wobei als Lösungsmittel ein pharmazeutisch verwendbares ätherisches Öl, ein Ester oder Partialester einer C2- bis C30-Fettsäure mit einem zwei-bis achtwertigen Alkohol oder mit Polyglycerin, ein 3 bis 6 C-Atome enthaltendes Dialkylamid oder das Dimethylsulfoxyd bzw.

   Mischungen dieser Lösungsmittel untereinander und gegebenenfalls in Kombination mit Polyäthylen-   glykol (en) bzw.   dessen (deren) Ester oder Äther,   l, 3-Dioxolan-Derivat (en), Alkylenglykol (en),   Wasser und/oder Alkoholen eingesetzt werden.



   <Desc / Clms Page number 1>
 



   The invention relates to a method for producing an orally administrable and stable solution which contains the active ingredient methoxsalen (8-methoxy-furo-3 ', 2!: 6, 7 "j-coumarin) with the formula which can be used for photochemotherapy of psoriasis
 EMI1.1
 
 EMI1.2
 

 <Desc / Clms Page number 2>

 Example 3:
 EMI2.1
 
<tb>
<tb> 0, <SEP> 34 <SEP> g <SEP> methoxsalen
<tb> 6, <SEP> 50 <SEP> g <SEP> polyethylene glycol <SEP> 300
<tb> 1, <SEP> 80 <SEP> g <SEP> partial ester mixture <SEP> of <SEP> Ca <SEP> -C'2- <SEP> fatty acids <SEP> with <SEP> oxyethylated <SEP> glycerol
<tb> 1, <SEP> 06 <SEP> g <SEP> benzyl alcohol
<tb> 0, <SEP> 92 <SEP> g <SEP> glycerin formal *)
<tb> 0, <SEP> 16 <SEP> g <SEP> flavor <SEP>
<tb>
 Example 4:

   
 EMI2.2
 
<tb>
<tb> 0, <SEP> 42 <SEP> g <SEP> methoxsalen
<tb> 4, <SEP> 80 <SEP> g <SEP> glycerin formal *)
<tb> 2, <SEP> 20 <SEP> g <SEP> glycofurol **)
<tb> 1, <SEP> 84 <SEP> g <SEP> peppermint oil <SEP>
<tb> 1, <SEP> 56 <SEP> g <SEP> partial ester mixture <SEP> hydrogenated <SEP> castor oil fatty acids <SEP> with <SEP> oxyethylated <SEP> glycerol
<tb>
 Example 5:
 EMI2.3
 
<tb>
<tb> 0, <SEP> 43 <SEP> g <SEP> methoxsalen
<tb> 5, <SEP> 00 <SEP> g <SEP> glycerin formal *)
<tb> 2, <SEP> 32 <SEP> g <SEP> polyethylene glycol <SEP> 300
<tb> 2, <SEP> 06 <SEP> g <SEP> Partial <SEP> ester mixture <SEP> of <SEP> castor oil fatty acids <SEP> with <SEP> oxyethylated <SEP> glycerol
<tb> 1, <SEP> 34 <SEP> g <SEP> dimethyl sulfoxide
<tb> 0, <SEP> 16 <SEP> g <SEP> flavor <SEP>
<tb>
 
Example 6:

   10 g of pulverized methoxsalen are dissolved by stirring in a mixture of 365 g of polyethylene glycol, 400.50 g of dimethylacetamide, 50 g of glycerol and 40 g of glycerol triacetate, diluted with 30 g of water, stirred well and filled with 0.5 ml of the solution obtained a dosing device in capsules. These then contain 10 mg of active ingredient / capsule.



   *) Glycerin formal is a mixture of 4-hydroxymethyl-1, 3-dioxolane and 5-hydroxy-1, 3-dioxane.



    **) Glycofurols are polyethylene glycol ethers of tetrahydrofurfuryl alcohol (H. Janistyn, Handbook of Cosmetics and Fragrances, 3rd edition, 1st volume, pp. 443,444).



   PATENT CLAIMS:
1. A process for the preparation of a pharmaceutical preparation for oral administration, optionally in the form of capsules which contain the active ingredient 8-methoxy-furo- [3 ', 2': 6, -coumarin and, if desired, pharmaceutically usable taste correctives, antioxidants and / or preservatives contains, characterized in that a stable solution of the active ingredient is prepared, the solvent used being a pharmaceutically usable essential oil, an ester or partial ester of a C2 to C30 fatty acid with a dihydric or octane alcohol or with polyglycerol, a 3 to 6 C. Dialkylamide containing atoms or the dimethyl sulfoxide or

   Mixtures of these solvents with one another and optionally in combination with polyethylene glycol (s) or their (their) ester or ether, 1,3-dioxolane derivative (s), alkylene glycol (s), water and / or alcohols are used.

 

Claims (1)

2. Verfahren nach Anspruch l, dadurch gekennzeichnet, dass ein Partialester einer C2 - bis C],-Fettsäure mit einem zwei- bis achtwertigen Alkohol, der seinerseits an den unveresterten OH-Gruppen mit Polyäthylenglykol veräthert ist, eingesetzt wird. <Desc/Clms Page number 3>  2. The method according to claim l, characterized in that a partial ester of a C2 - to C], - fatty acid with a two to eight-valent alcohol, which in turn is etherified on the unesterified OH groups with polyethylene glycol, is used.  <Desc / Clms Page number 3>   3. Verfahren nach Anspruch 1, dadurch gekennzeichnet, dass als Ester oder Partialester ein solcher eingesetzt wird, dessen Fettsäurerest ungesättigt ist und/oder eine OH-Gruppe enthält.  3. The method according to claim 1, characterized in that the ester or partial ester used is one whose fatty acid residue is unsaturated and / or contains an OH group.
AT0221080A 1979-06-25 1980-04-24 METHOD FOR PRODUCING A PHARMACEUTICAL PREPARATION AT366573B (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
AT0221080A AT366573B (en) 1980-04-24 1980-04-24 METHOD FOR PRODUCING A PHARMACEUTICAL PREPARATION
SE8004383A SE445422B (en) 1979-06-25 1980-06-12 PHARMACEUTICAL PREPARATION FOR ORAL ADMINISTRATION CONTAINING 8-METOXY-FURO- / 3 ', 2': 6,7 / -CUMARIN
NO801759A NO153951C (en) 1979-06-25 1980-06-13 PROCEDURE FOR THE PREPARATION OF A PHARMACEUTICAL PREPARATION CONTAINING 8-METOXY-FURO- (3 [, 2 [: 6,7) -CUMARIN.
FR8013490A FR2459658A1 (en) 1979-06-25 1980-06-18 PROCESS FOR THE PREPARATION OF AN ORAL-ADMINISTRATIVE METHOXSALEN-BASED PHARMACEUTICAL COMPOSITION
FI801988A FI72428C (en) 1979-06-25 1980-06-19 FRAMSTAELLNINGSFOERFARANDE FOER ETT STABILT, FARMACEUTISKT 8-METOXIFURO- (3 ', 2': 6,7) -COUMIN PREPARATION.
DE19803023109 DE3023109A1 (en) 1979-06-25 1980-06-20 METHOXAL SALES PREPARATION FOR ORAL ADMINISTRATION
GB8020457A GB2052980B (en) 1979-06-25 1980-06-23 Pharmaceutical composition for oral administration comprising methoxsalen
US06/594,060 US4913901A (en) 1979-06-25 1984-03-28 Pharmaceutical composition for oral administration and process for the use thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
AT0221080A AT366573B (en) 1980-04-24 1980-04-24 METHOD FOR PRODUCING A PHARMACEUTICAL PREPARATION

Publications (2)

Publication Number Publication Date
ATA221080A ATA221080A (en) 1981-09-15
AT366573B true AT366573B (en) 1982-04-26

Family

ID=3530055

Family Applications (1)

Application Number Title Priority Date Filing Date
AT0221080A AT366573B (en) 1979-06-25 1980-04-24 METHOD FOR PRODUCING A PHARMACEUTICAL PREPARATION

Country Status (1)

Country Link
AT (1) AT366573B (en)

Also Published As

Publication number Publication date
ATA221080A (en) 1981-09-15

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UEP Publication of translation of european patent specification