EP0227656A1 - Compositions pharmaceutiques renfermant des gels - Google Patents

Compositions pharmaceutiques renfermant des gels

Info

Publication number
EP0227656A1
EP0227656A1 EP85903649A EP85903649A EP0227656A1 EP 0227656 A1 EP0227656 A1 EP 0227656A1 EP 85903649 A EP85903649 A EP 85903649A EP 85903649 A EP85903649 A EP 85903649A EP 0227656 A1 EP0227656 A1 EP 0227656A1
Authority
EP
European Patent Office
Prior art keywords
active ingredient
prostaglandin
pluronic
agents
agent
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Withdrawn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
EP85903649A
Other languages
German (de)
English (en)
Inventor
Bernhard Better
Evelyn Grosse
Ingfried Zimmermann
Johannes-Wilhelm Tack
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.)
Bayer Pharma AG
Original Assignee
Schering AG
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 Schering AG filed Critical Schering AG
Publication of EP0227656A1 publication Critical patent/EP0227656A1/fr
Withdrawn legal-status Critical Current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
    • A61K9/0034—Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers

Definitions

  • the invention relates to new gel formulations for therapeutic and diagnostic purposes and to a method for producing these formulations.
  • DE-OS 30 01 454 discloses lyophilisate formulations of hydroxyl-containing films with prostaglandins, which are converted into ready-to-use viscous solutions before use. The disadvantage of these formulations is that they form lumps which complicate the release of the active ingredient or prevent it.
  • DE-OS 33 07 816 describes lyophilisates of alkali polyacrylates which are mixed with aqueous solutions of prostaglandins. Although the active ingredient is released better from this formulation, the partially inhomogeneous incorporation of the active ingredient into such gels with a consistently high viscosity and above all the applicability of these gels by the user remains unsatisfactory.
  • the invention was based on the object of developing gel formulations for active ingredients with limited stability which are to be used in body cavities or on body surfaces.
  • CA 1072-413 (Derwent Publication No. 18422C / 11) specifies the possible uses of polyoxyethylene-polyoxypropylene block copolymers as carriers for pharmaceuticals for therapeutic or prophylactic use on the body surface or in body cavities.
  • the weight percentage of gel fractions is given as 15-50%.
  • the preferred range emerges from the exemplary embodiment with 30% by weight: 20% Pluronic F 127 and 10% Pluronic L 44 in aqueous solution.
  • Pluronic F-127 preparations can only be found for ophthalmic practice (DE-OS 27 03 152). It has now been found that for the therapeutic and diagnostic use of Pluronic F-127 gel formulations in body cavities or on body areas, the proportion of 18 to 19 percent by weight of Pluronic F-127 proves to be particularly advantageous in these formulations.
  • the invention also relates to a method for producing Pluronic F-127 gel formulations for therapeutic and diagnostic use.
  • Aqueous Pluronic F-127 solutions with a Pluronic F-127 content of 18-19 percent by weight are easily movable liquids with low viscosity at low and high temperatures and only form medium viscosity (20-50 ° C) highly viscous gels.
  • This reversible sol-gel process allows the dissolved active ingredient to be easily incorporated homogeneously into a cooled Pluronic F-127 solution and drawn into a suitable application system (e.g. syringe with catheter tube).
  • a highly viscous gel forms at the application site during and immediately after application.
  • Figure 1 shows the temperature-dependent viscosity behavior of Pluronic F-127 solutions with different proportions of Pluronic F-127. It can be seen from this figure that an optimal viscosity for the body temperature range is achieved with solutions whose Pluronic F-127 content is between 13 and 19 percent by weight. A 20% Pluronic F-127 solution has to be cooled lower than a 13-19% solution in order to dissolve the active ingredient.
  • Figure 2 in which the percentage of Pluronic F-127 was plotted against temperature, also shows why the 18-19% range is a particularly preferred range for galenical preparations.
  • Pluronic F-127 formulations of the present invention have the advantage over the gels based on cellulose derivatives which have hitherto been customary in that the active ingredient in the cool state has no particular properties. Cooling can be incorporated, that Pluronic F-127 can be sterilized without changing its gel behavior and that the polymer in Pluronic F-127 solutions has short-term stability. All Pluronic F-127 formulations are easy to apply when cool and guarantee intensive fogging of the mucous membrane before they heat up and form gel. Pluronic F-127 is a good gel-forming agent that is compatible with the mucous membrane, is toxicologically harmless and is absorbed by the body after some time.
  • the invention relates both to gel formulations with prostaglandins, steroid hormones, antifungals and antibiotics for theraneutic purposes and to gel formulations with X-ray contrast agents, ultrasound contrast agents and NMR contrast agents for diagnostic purposes.
  • the invention also relates to a method for producing gel formulations with the substances mentioned above.
  • the gel formulations according to the invention contain the
  • Active ingredient in the therapeutically or diagnostically effective dose which is well known for the active ingredients under consideration. If necessary, known and customary auxiliaries are added to the new formulations in galenics.
  • Pluronic F-127 are completely dissolved in 6.4g water (for injections) at a temperature of around 15 ° C.
  • the solution cooled to 10 ° C., is filtered through a membrane filter with a pore size of 1.2 ⁇ m, filled into 10 ml vials and sterilized in an autoclave at 120 ° C. for 20 minutes.
  • the Pluronic F-127 solutions are stored at temperatures below 8 ° C.
  • the contents of an ampoule containing 100 pg of the active ingredient 16-phenoxyprostaglandin-E 2 -methanesulfonamide with 2.0 ml of water are taken up and added to the vial with the cooled Pluronic F-127 solution. After briefly shaking, a clear, homogeneous solution is formed which gels at temperatures above 18 ° C.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)

Abstract

On décrit des compositions pharmaceutiques ou des produits de diagnostic renfermant du Pluronic F-127 qui contiennent une quantité thérapeutique ou diagnostique active du principe actif et 18 à 19% pds de Pluronic F-127, formateur de gel ainsi qu'un procédé de préparation de ces produits.
EP85903649A 1984-07-27 1985-07-18 Compositions pharmaceutiques renfermant des gels Withdrawn EP0227656A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE3428264 1984-07-27
DE19843428264 DE3428264A1 (de) 1984-07-27 1984-07-27 Gelhaltige pharmazeutische zubereitungen

Publications (1)

Publication Number Publication Date
EP0227656A1 true EP0227656A1 (fr) 1987-07-08

Family

ID=6242046

Family Applications (1)

Application Number Title Priority Date Filing Date
EP85903649A Withdrawn EP0227656A1 (fr) 1984-07-27 1985-07-18 Compositions pharmaceutiques renfermant des gels

Country Status (8)

Country Link
EP (1) EP0227656A1 (fr)
JP (1) JPS61502817A (fr)
AU (1) AU4672385A (fr)
DE (1) DE3428264A1 (fr)
DK (1) DK111686A (fr)
ES (1) ES8705763A1 (fr)
IL (1) IL75921A0 (fr)
WO (1) WO1986000813A1 (fr)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0386960A3 (fr) * 1989-03-07 1991-10-23 American Cyanamid Company Compositions pharmaceutiques utilisables comme véhicules de délivrance d'un médicament et/ou comme pansements pour blessures
JP2926749B2 (ja) * 1989-04-25 1999-07-28 吉富製薬株式会社 プロスタグランジン含有液状組成物
CA2040460C (fr) * 1990-05-01 1997-06-10 Tacey X. Viegas Distribution de medicaments au moyen de gels thermoreversibles
US5593683A (en) * 1990-05-01 1997-01-14 Mdv Technologies, Inc. Method of making thermoreversible polyoxyalkylene gels
US5948387A (en) * 1990-06-01 1999-09-07 Imarx Pharmaceutical Corp. Contrast media for ultrasonic imaging
WO1994028872A1 (fr) * 1993-06-04 1994-12-22 Warner-Lambert Company Medication sans alcool contre les rhumes et pour les sinus
JP2909876B2 (ja) * 1994-01-24 1999-06-23 恭弘 小川 造影剤
US6669927B2 (en) 1998-11-12 2003-12-30 3M Innovative Properties Company Dental compositions
US6312666B1 (en) 1998-11-12 2001-11-06 3M Innovative Properties Company Methods of whitening teeth
US6312667B1 (en) 1998-11-12 2001-11-06 3M Innovative Properties Company Methods of etching hard tissue in the oral environment
US6620405B2 (en) * 2001-11-01 2003-09-16 3M Innovative Properties Company Delivery of hydrogel compositions as a fine mist
EP3790597A4 (fr) * 2018-07-12 2022-03-09 Arshintseva, Elena Valentinovna Procédé thermique de stérilisation de poloxamère comprenant des médicaments liquides

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3867521A (en) * 1970-08-26 1975-02-18 Scherer Corp R P Method for absorption of drugs
US3852210A (en) * 1972-08-11 1974-12-03 Flow Pharma Inc Stable liquid detergent concentrates containing active oxygen
CA1051776A (fr) * 1974-08-09 1979-04-03 Murray W. Winicov Gel de poloxamer-iode
US4100271A (en) * 1976-02-26 1978-07-11 Cooper Laboratories, Inc. Clear, water-miscible, liquid pharmaceutical vehicles and compositions which gel at body temperature for drug delivery to mucous membranes
CA1072413A (fr) * 1976-07-13 1980-02-26 West Laboratories Systemes de gel de type poloxamer, a temperature de gelification superieure a la temperature ambiante
US4365516A (en) * 1978-01-06 1982-12-28 Rockwell International Corporation Ultrasonic couplant gel compositions and method for employing same
DE2966768D1 (en) * 1978-12-19 1984-04-12 Byk Gulden Lomberg Chem Fab Solutions of x-ray contrast agents
SE431821B (sv) * 1979-01-29 1984-03-05 Perstorp Ab Lagringsstabilt, prostaglandininnehallande medicinskt preparat

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO8600813A1 *

Also Published As

Publication number Publication date
IL75921A0 (en) 1985-12-31
DK111686D0 (da) 1986-03-11
ES545616A0 (es) 1987-06-01
AU4672385A (en) 1986-02-25
JPS61502817A (ja) 1986-12-04
DK111686A (da) 1986-03-11
WO1986000813A1 (fr) 1986-02-13
DE3428264A1 (de) 1986-03-06
ES8705763A1 (es) 1987-06-01

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Legal Events

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PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

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Effective date: 19870123

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RIN1 Information on inventor provided before grant (corrected)

Inventor name: GROSSE, EVELYN

Inventor name: TACK, JOHANNES-WILHELM

Inventor name: ZIMMERMANN, INGFRIED

Inventor name: BETTER, BERNHARD

17Q First examination report despatched

Effective date: 19890529

STAA Information on the status of an ep patent application or granted ep patent

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18D Application deemed to be withdrawn

Effective date: 19891010

RIN1 Information on inventor provided before grant (corrected)

Inventor name: BETTER, BERNHARD

Inventor name: GROSSE, EVELYN

Inventor name: ZIMMERMANN, INGFRIED

Inventor name: TACK, JOHANNES-WILHELM