DE10103262A1 - Suppository containing oxybutynin, useful for treatment of incontinence, avoids side effects and allows an increase in dose - Google Patents

Suppository containing oxybutynin, useful for treatment of incontinence, avoids side effects and allows an increase in dose

Info

Publication number
DE10103262A1
DE10103262A1 DE2001103262 DE10103262A DE10103262A1 DE 10103262 A1 DE10103262 A1 DE 10103262A1 DE 2001103262 DE2001103262 DE 2001103262 DE 10103262 A DE10103262 A DE 10103262A DE 10103262 A1 DE10103262 A1 DE 10103262A1
Authority
DE
Germany
Prior art keywords
oxybutynin
suppository
active ingredient
side effects
incontinence
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.)
Withdrawn
Application number
DE2001103262
Other languages
German (de)
Inventor
Axel Schmidt-Dossi
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 DE2001103262 priority Critical patent/DE10103262A1/en
Publication of DE10103262A1 publication Critical patent/DE10103262A1/en
Withdrawn legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate

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  • Health & Medical Sciences (AREA)
  • Emergency Medicine (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)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Pharmaceutical composition (C1)for functional bladder disorders is a suppository containing at least 7.5 mg of oxybutynin (I), especially as the hydrochloride. ACTIVITY : Uropathic. No suitable biological data given. MECHANISM OF ACTION : None given in the source material.

Description

Die Erfindung betrifft ein Arzneimittel gegen Blasenfunktionsstörung mit dem Wirkstoff Oxybutynin.The invention relates to a medicament against Bladder dysfunction with the active ingredient oxybutynin.

Es ist allgemein bekannt, daß der Wirkstoff Oxybutynin- Hydrochlorid bei Blasenfunktionsstörung erfolgreich eingesetzt werden kann. So wird in der US-A-6,124,355 eine Therapie gegen Inkontinenz beschrieben, bei welcher dem Patient der Wirkstoff in unterschiedlichen Dosierungen oral in Form von Tabletten verabreicht wird. Es hat sich allerdings gezeigt, daß bei höheren Oxybutynin-Konzentrationen bei einer oralen Darreichungsform unerwünschte und unangenehme Nebeneffekte auftreten.It is well known that the active ingredient oxybutynin Hydrochloride successful in bladder dysfunction can be used. For example, US-A-6,124,355 described a therapy for incontinence in which the patient the active ingredient in different Dosages are administered orally in the form of tablets. However, it has been shown that at higher Oxybutynin concentrations in an oral Dosage form undesirable and unpleasant Side effects occur.

Der Erfindung liegt die Aufgabe zugrunde, ein Arzneimittel mit dem Wirkstoff Oxybutynin bereitzustellen, das auch mit höheren Dosierungen im wesentlichen ohne unangenehme Nebeneffekte verabreicht werden kann.The invention is based on the object Medicines with the active ingredient oxybutynin to provide that even with higher doses in administered essentially without unpleasant side effects can be.

Die Aufgabe wird gemäß der Erfindung dadurch gelöst, daß das Arzneimittel als Suppositorium ausgebildet ist, das wenigstens 7,5 mg Oxybutynin, insbesondere Oxybutynin- Hydrochlorid enthält. Vorzugsweise sind in dem Suppositorium 7,5 bis 15 mg, insbesondere 10 mg Wirkstoff enthalten. Es hat sich herausgestellt, daß ein solches Arzneimittel trotz der hohen Dosierung von Oxybutynin gut verträglich ist. Unerwartete Nebenwirkungen wurden nicht erkannt. The object is achieved according to the invention in that the drug is designed as a suppository, the at least 7.5 mg oxybutynin, especially oxybutynin Contains hydrochloride. Preferably in the Suppository 7.5 to 15 mg, in particular 10 mg of active ingredient contain. It has been found that such Medicines good despite the high dosage of oxybutynin is tolerated. There were no unexpected side effects recognized.  

Das Suppositorium kann einen üblichen Hilfs- beziehungsweise Trägerstoff aufweisen, der bei Körpertemperatur schmilzt und den Wirkstoff freigibt. Es können beispielsweise Kakaobutter oder eine Glyceringelatine eingesetzt werden.The suppository can be a usual auxiliary or have a carrier which at Body temperature melts and releases the active ingredient. It can, for example, cocoa butter or a Glycerol gelatin can be used.

Gemäß einer bevorzugten Ausführungsform der Erfindung enthält das Suppositorium als Hilfsstoff eine modifizierte ungesättigte Pflanzenfettsäure als Hartfett, einen Füllstoff und den Wirkstoff. Es kann beispielsweise vorgesehen werden, daß das Suppositorium 175 bis 225 mg, insbesondere 190 bis 210 mg Füllstoff, 1.500 bis 2.500 mg, insbesondere 1.800 bis 1.900 mg Hartfett und den Wirkstoff enthält. Der Füllstoff kann Lactose-Monohydrat sein, das auch als Resorbtionsverbesserer dient.According to a preferred embodiment of the invention contains the suppository as an adjuvant modified unsaturated vegetable fatty acid as hard fat, a filler and the active ingredient. For example, it can that the suppository be 175 to 225 mg, in particular 190 to 210 mg of filler, 1,500 to 2,500 mg, in particular 1,800 to 1,900 mg of hard fat and the Contains active ingredient. The filler can be lactose monohydrate be, which also serves as a resorption enhancer.

Die Erfindung wird im folgenden anhand eines Ausführungsbeispiels näher erläutert. Für ein Suppositorium werden 10 mg Wirkstoff Oxybutynin- Hydrochlorid gemäß Pharmacopoea Europaea NT 99 (Ph. Eur. NT 99) mit etwa 200 mg Lactose-Monohydrat und etwa 1890 mg Hartfett (beispielsweise Witepsol® H15) unter Wärmeeinwirkung vermischt und in der gewünschten Suppositoriums-Hülse abgekühlt. Es entsteht ein Suppositorium mit einem Gewicht von etwa 2,1 g mit der gewünschten Dosierung von Oxybutynin.The invention is based on a Embodiment explained in more detail. For a Suppository 10 mg of active ingredient oxybutynin Hydrochloride according to Pharmacopoea Europaea NT 99 (Ph.Eur. NT 99) with about 200 mg lactose monohydrate and about 1890 mg Hard fat (e.g. Witepsol® H15) under Heat mixed and in the desired Suppository sleeve cooled. It arises Suppository weighing about 2.1 g with the desired dosage of oxybutynin.

Claims (5)

1. Arzneimittel gegen Blasenfunktionsstörung mit dem Wirkstoff Oxybutynin, dadurch gekennzeichnet, daß das Arzneimittel als Suppositorium ausgebildet ist, das wenigstens 7,5 mg Oxybutynin, insbesondere Oxybutynin- Hydrochlorid enthält.1. drug against bladder dysfunction with the active ingredient oxybutynin, characterized in that the drug is designed as a suppository which contains at least 7.5 mg oxybutynin, in particular oxybutynin hydrochloride. 2. Arzneimittel nach Anspruch 1, dadurch gekennzeichnet, daß das Suppositorium 7,5 bis 15 mg, insbesondere 10 mg Wirkstoff enthält.2. Medicament according to claim 1, characterized in that the suppository 7.5 to 15 mg, especially 10 mg Contains active ingredient. 3. Arzneimittel nach Anspruch 1 oder 2, dadurch gekennzeichnet, daß das Suppositorium ein Hartfett, einen Füllstoff und den Wirkstoff enthält.3. Medicament according to claim 1 or 2, characterized characterized in that the suppository is a hard fat, a Contains filler and the active ingredient. 4. Arzneimittel nach einem der Ansprüche 1 bis 3, dadurch gekennzeichnet, daß das Suppositorium 175 bis 225 mg, insbesondere 190 bis 210 mg Füllstoff, 1.500 bis 2.500 mg, insbesondere 1.800 bis 1.900 mg Hartfett und den Wirkstoff enthält.4. Medicament according to one of claims 1 to 3, characterized characterized in that the suppository 175 to 225 mg, in particular 190 to 210 mg of filler, 1,500 to 2,500 mg, in particular 1,800 to 1,900 mg of hard fat and the Contains active ingredient. 5. Arzneimittel nach einem der Ansprüche 1 bis 4, dadurch gekennzeichnet, daß der Füllstoff Lactose-Monohydrat ist.5. Medicament according to one of claims 1 to 4, characterized characterized in that the filler is lactose monohydrate.
DE2001103262 2001-01-25 2001-01-25 Suppository containing oxybutynin, useful for treatment of incontinence, avoids side effects and allows an increase in dose Withdrawn DE10103262A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
DE2001103262 DE10103262A1 (en) 2001-01-25 2001-01-25 Suppository containing oxybutynin, useful for treatment of incontinence, avoids side effects and allows an increase in dose

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE2001103262 DE10103262A1 (en) 2001-01-25 2001-01-25 Suppository containing oxybutynin, useful for treatment of incontinence, avoids side effects and allows an increase in dose

Publications (1)

Publication Number Publication Date
DE10103262A1 true DE10103262A1 (en) 2002-08-01

Family

ID=7671681

Family Applications (1)

Application Number Title Priority Date Filing Date
DE2001103262 Withdrawn DE10103262A1 (en) 2001-01-25 2001-01-25 Suppository containing oxybutynin, useful for treatment of incontinence, avoids side effects and allows an increase in dose

Country Status (1)

Country Link
DE (1) DE10103262A1 (en)

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5532278A (en) * 1995-01-31 1996-07-02 Sepracor, Inc. Methods and compositions for treating urinary incontinence using optically pure (S)-oxybutynin
WO1996023492A1 (en) * 1995-01-31 1996-08-08 Sepracor, Inc. Treating urinary incontinence using (s)-oxybutynin and (s)-desethyloxybutynin
DE19622902A1 (en) * 1995-06-07 1996-12-12 Alza Corp Skin permeation increasing compositions comprising glycerol monolaurate and lauryl acetate
WO1998000126A1 (en) * 1996-06-28 1998-01-08 Sepracor, Inc. Treating urinary incontinence using (s)-oxybutynin and (s)-desethyloxybutynin
WO1998011888A1 (en) * 1996-09-19 1998-03-26 American Home Products Corporation Method of treating urinary incontinence
US6123961A (en) * 1996-09-25 2000-09-26 Bridge Pharma, Inc. Treating urinary incontinence with (R)-desethyloxybutynin and (R)-oxybutynin
WO2000071108A2 (en) * 1999-05-20 2000-11-30 Sepracor Inc. Methods for treatment of asthma using s-oxybutynin
WO2001017480A2 (en) * 1999-09-09 2001-03-15 Androsolutions, Inc. Methods and compositions for preventing and treating urinary tract disorders

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5532278A (en) * 1995-01-31 1996-07-02 Sepracor, Inc. Methods and compositions for treating urinary incontinence using optically pure (S)-oxybutynin
WO1996023492A1 (en) * 1995-01-31 1996-08-08 Sepracor, Inc. Treating urinary incontinence using (s)-oxybutynin and (s)-desethyloxybutynin
DE19622902A1 (en) * 1995-06-07 1996-12-12 Alza Corp Skin permeation increasing compositions comprising glycerol monolaurate and lauryl acetate
WO1998000126A1 (en) * 1996-06-28 1998-01-08 Sepracor, Inc. Treating urinary incontinence using (s)-oxybutynin and (s)-desethyloxybutynin
WO1998011888A1 (en) * 1996-09-19 1998-03-26 American Home Products Corporation Method of treating urinary incontinence
US6123961A (en) * 1996-09-25 2000-09-26 Bridge Pharma, Inc. Treating urinary incontinence with (R)-desethyloxybutynin and (R)-oxybutynin
WO2000071108A2 (en) * 1999-05-20 2000-11-30 Sepracor Inc. Methods for treatment of asthma using s-oxybutynin
WO2001017480A2 (en) * 1999-09-09 2001-03-15 Androsolutions, Inc. Methods and compositions for preventing and treating urinary tract disorders

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