[go: up one dir, main page]

WO1986000813A1 - Compositions pharmaceutiques renfermant des gels - Google Patents

Compositions pharmaceutiques renfermant des gels Download PDF

Info

Publication number
WO1986000813A1
WO1986000813A1 PCT/DE1985/000237 DE8500237W WO8600813A1 WO 1986000813 A1 WO1986000813 A1 WO 1986000813A1 DE 8500237 W DE8500237 W DE 8500237W WO 8600813 A1 WO8600813 A1 WO 8600813A1
Authority
WO
WIPO (PCT)
Prior art keywords
active ingredient
prostaglandin
pluronic
agents
agent
Prior art date
Application number
PCT/DE1985/000237
Other languages
German (de)
English (en)
Inventor
Bernhard Better
Evelyn Grosse
Ingfried Zimmermann
Johannes-Wilhelm Tack
Original Assignee
Schering Aktiengesellschaft
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 Aktiengesellschaft filed Critical Schering Aktiengesellschaft
Publication of WO1986000813A1 publication Critical patent/WO1986000813A1/fr
Priority to DK111686A priority Critical patent/DK111686A/da

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.
PCT/DE1985/000237 1984-07-27 1985-07-18 Compositions pharmaceutiques renfermant des gels WO1986000813A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
DK111686A DK111686A (da) 1984-07-27 1986-03-11 Gelholdige farmaceutiske praeparater

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19843428264 DE3428264A1 (de) 1984-07-27 1984-07-27 Gelhaltige pharmazeutische zubereitungen
DEP3428264.5 1984-07-27

Publications (1)

Publication Number Publication Date
WO1986000813A1 true WO1986000813A1 (fr) 1986-02-13

Family

ID=6242046

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DE1985/000237 WO1986000813A1 (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)

Cited By (9)

* 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
EP0455396A1 (fr) * 1990-05-01 1991-11-06 MDV Technologies, Inc. Compositions de gel aqueux et leur utilisation
WO1994028872A1 (fr) * 1993-06-04 1994-12-22 Warner-Lambert Company Medication sans alcool contre les rhumes et pour les sinus
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
WO2000028955A1 (fr) * 1998-11-12 2000-05-25 Minnesota Mining And Manufacturing Company Composition de blanchiment dentaire
US6312667B1 (en) 1998-11-12 2001-11-06 3M Innovative Properties Company Methods of etching hard tissue in the oral environment
WO2003037276A1 (fr) * 2001-11-01 2003-05-08 3M Innovative Properties Company Distribution d'un hydrogel sous forme de brouillard fin
US6669927B2 (en) 1998-11-12 2003-12-30 3M Innovative Properties Company Dental compositions

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2909876B2 (ja) * 1994-01-24 1999-06-23 恭弘 小川 造影剤
RU2741710C1 (ru) * 2018-07-12 2021-01-28 Елена Валентиновна Аршинцева Термический способ стерилизации жидких лекарственных средств, содержащих в своем составе полоксамер

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LU68215A1 (fr) * 1972-08-11 1974-02-21
US3867521A (en) * 1970-08-26 1975-02-18 Scherer Corp R P Method for absorption of drugs
DE2708152A1 (de) * 1976-02-26 1977-09-08 Flow Pharma Inc Pharmazeutisches traegermaterial und dessen verwendung
GB1516653A (en) * 1974-08-09 1978-07-05 West Laboratories Inc Poloxamer-iodine gel
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
EP0012926A1 (fr) * 1978-12-19 1980-07-09 Byk Gulden Lomberg Chemische Fabrik GmbH Solutions d'agents de contraste pour rayons X
GB2041220A (en) * 1979-01-29 1980-09-10 Perstorp Ab Medical preparations containing prostaglandins
US4365516A (en) * 1978-01-06 1982-12-28 Rockwell International Corporation Ultrasonic couplant gel compositions and method for employing same

Patent Citations (9)

* 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
LU68215A1 (fr) * 1972-08-11 1974-02-21
GB1516653A (en) * 1974-08-09 1978-07-05 West Laboratories Inc Poloxamer-iodine gel
DE2708152A1 (de) * 1976-02-26 1977-09-08 Flow Pharma Inc Pharmazeutisches traegermaterial und dessen verwendung
FR2400903A1 (fr) * 1976-02-26 1979-03-23 Krezanoski Joseph Vehicules pharmaceutiques liquides, transparents, miscibles a l'eau et compositions se gelifiant a la temperature du corps pour l'apport de produits pharmaceutiques a des membranes muqueuses
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
EP0012926A1 (fr) * 1978-12-19 1980-07-09 Byk Gulden Lomberg Chemische Fabrik GmbH Solutions d'agents de contraste pour rayons X
GB2041220A (en) * 1979-01-29 1980-09-10 Perstorp Ab Medical preparations containing prostaglandins

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, Vol. 77, No. 26, 25 December 1972, Columbus, Ohio (US) I.R. SCHMOLKA: "Artificial Skin. 1. Preparation and Properties of Pluronic F-127 Gels for Treatment of Burns" see pages 265-266, Abstract 168578h. & J. Biomed. Mater. Res. 1972, 6 (6) 571-82 (Eng.) *
CHEMICAL ABSTRACTS, Vol. 95, No. 10, August 1981, Columbus, Ohio (US) CHEN-CHOW et al.: "In Vitro Release of Lidocaine from Pluronic F-127 Gels" see page 401, Abstract 49300y & Int. J. Pharm. 1981, 8 (2), 89-99 (Eng.) *

Cited By (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
EP0455396A1 (fr) * 1990-05-01 1991-11-06 MDV Technologies, Inc. Compositions de gel aqueux et leur utilisation
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
WO2000028955A1 (fr) * 1998-11-12 2000-05-25 Minnesota Mining And Manufacturing Company Composition de blanchiment dentaire
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
US6669927B2 (en) 1998-11-12 2003-12-30 3M Innovative Properties Company Dental compositions
USRE42024E1 (en) 1998-11-12 2011-01-11 3M Innovative Properties Company Dental compositions
WO2003037276A1 (fr) * 2001-11-01 2003-05-08 3M Innovative Properties Company Distribution d'un hydrogel sous forme de brouillard fin
US6620405B2 (en) 2001-11-01 2003-09-16 3M Innovative Properties Company Delivery of hydrogel compositions as a fine mist

Also Published As

Publication number Publication date
ES545616A0 (es) 1987-06-01
AU4672385A (en) 1986-02-25
DK111686D0 (da) 1986-03-11
DK111686A (da) 1986-03-11
IL75921A0 (en) 1985-12-31
ES8705763A1 (es) 1987-06-01
EP0227656A1 (fr) 1987-07-08
JPS61502817A (ja) 1986-12-04
DE3428264A1 (de) 1986-03-06

Similar Documents

Publication Publication Date Title
DE69524152T2 (de) Sterile Gelzusammensetzung zur Wundbehandlung
US2155658A (en) Surgical and medical preparations
DE2727913C2 (fr)
DE69006760T2 (de) Spritzgel-Packung, Verwendung und Darstellung derselben.
DE60103894T2 (de) Sprühfähige Wundversorgungszusammensetzungen
DE2708152A1 (de) Pharmazeutisches traegermaterial und dessen verwendung
DE69728783T2 (de) Verbesserte arzneimittel
WO1986000813A1 (fr) Compositions pharmaceutiques renfermant des gels
EP0334083B1 (fr) Composition lyophilisée à base de ifosfamide-mesna et procédé pour sa préparation
DE68903814T2 (de) Etoposid-loesungen.
DE3536560A1 (de) Augentropfen enthaltend bromokryptin
DE69904727T2 (de) Injizierbares arzneimittel auf basis eines pharmazeutisch verträglichen salzes von clopidogrel bzw. von ticlopidin
DE3123823C2 (de) Spermientötendes Mittel
AT397460B (de) Verfahren zur herstellung eines pharmazeutischen trockenpräparates enthaltend ein diclofenac-salz
EP0277462B1 (fr) Procèdè de fabrication de solutions nasales contenant de la calcitonine synthètique humaine.
DE69106727T2 (de) Kosmetikum oder arzneimittel in form eines steifen gels, insbesondere zur einarbeitung von einschlüssen.
EP0366888A1 (fr) Préparation pharmaceutique pour le traitement des inflammations des membranes muqueuses nasales
DE69232409T2 (de) Ungepufferte, vorgemischte ranitidin-formulierung
DE19912436A1 (de) Ibuprofen-Lösung
DE3787274T2 (de) Pharmazeutische Präparate, die eine wässerige Lösung eines Pyranoquinolins enthalten.
EP0436015B1 (fr) Preparation pharmaceutique pour administration rectale
EP0119156B1 (fr) Composition pharmaceutique contenant des prostaglandines et sa préparation
DE68912947T2 (de) Ein lösliches ibopamin-salz enthaltende augenarzneizubereitung.
DE2607849C3 (de) Gelatisierte Zubereitung enthaltend Glykole und Verfahren zur Herstellung der Zubereitung
DE2723936A1 (de) Ophthalmische loesung fuer die glaucom-behandlung

Legal Events

Date Code Title Description
AK Designated states

Designated state(s): AU DK HU JP SU US

AL Designated countries for regional patents

Designated state(s): AT BE CH DE FR GB IT LU NL SE

WWE Wipo information: entry into national phase

Ref document number: 1985903649

Country of ref document: EP

WWP Wipo information: published in national office

Ref document number: 1985903649

Country of ref document: EP

WWW Wipo information: withdrawn in national office

Ref document number: 1985903649

Country of ref document: EP