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WO2009056114A2 - Utilisation de poudres de polyéthylène-glycol et compositions contenant ces poudres - Google Patents

Utilisation de poudres de polyéthylène-glycol et compositions contenant ces poudres Download PDF

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Publication number
WO2009056114A2
WO2009056114A2 PCT/DE2008/001756 DE2008001756W WO2009056114A2 WO 2009056114 A2 WO2009056114 A2 WO 2009056114A2 DE 2008001756 W DE2008001756 W DE 2008001756W WO 2009056114 A2 WO2009056114 A2 WO 2009056114A2
Authority
WO
WIPO (PCT)
Prior art keywords
polyethylene glycol
particles
distribution
powder
particle size
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.)
Ceased
Application number
PCT/DE2008/001756
Other languages
German (de)
English (en)
Other versions
WO2009056114A3 (fr
Inventor
Michael Brock
Thorsten Kamp
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.)
Sasol Germany GmbH
Original Assignee
Sasol Germany GmbH
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 Sasol Germany GmbH filed Critical Sasol Germany GmbH
Publication of WO2009056114A2 publication Critical patent/WO2009056114A2/fr
Publication of WO2009056114A3 publication Critical patent/WO2009056114A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L71/00—Compositions of polyethers obtained by reactions forming an ether link in the main chain; Compositions of derivatives of such polymers
    • C08L71/02—Polyalkylene oxides
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L2203/00—Applications
    • C08L2203/02—Applications for biomedical use

Definitions

  • the invention relates to the use of polyethylene glycol powders of spherical polyethylene glycol particles having a narrow particle size distribution and compositions containing them. '
  • Polyethylene glycols with high molecular weights at 2O 0 C and atmospheric pressure are solid substances and are known in various dosage forms. They are available as a flowable melt as well as in block form, as a flake, mahde or spray powder.
  • Disadvantage of the flowable melt is that they can be obtained only in heatable tanker and thus in large quantities. For the storage of the melt heatable storage containers are still necessary.
  • Disadvantage of the block-shaped polyethylene glycols is that they must be melted time consuming before processing. The same applies to the flaky polyethylene glycols.
  • Polyethylene glycols as grinding powder are characterized by lack of flowability and thus by a high tendency of clumping. This can lead to the capacity being reduced to end products during processing by blockages of inlets or outlets or conveying means, e.g. Screw conveyors or pneumatic conveyors, is severely limited. Furthermore, grinding powders have only a low bulk density, whereby high storage capacities are necessary. Furthermore, polyethylene glycol grinding powders have a broad particle size distribution. Polyethylene glycol grinding powders have a strong tendency to interfere with solvent blending such as e.g. Water, to clump or float on the surface, so that the release time is greatly prolonged.
  • solvent blending such as e.g. Water
  • polyethylene glycol spray powders represent an advance in terms of improved dissolution behavior compared to the grinding powders, they still tend to form clumps during processing.
  • the particle size distribution is still very broad and the particles tend to agglomerate.
  • the bulk density of polyethylene glycol spray powders is low. High bulk density, good flowability, a narrow particle size distribution and a short dissolution time of polyethylene glycol powders in water are essential prerequisites for a very wide variety of applications and are still not fully met by the commercially available polyethylene glycol powders.
  • Object of the present invention is to provide a solid polyethylene glycol powder for this necessitating applications that is characterized by a high flowability and thus a low tendency to clumping, high bulk density, a narrow particle size distribution and short dissolution time in water.
  • the polyethylene glycol powder is characterized by an average molecular weight (number average) of 1500 to 20,000 g / mol, in particular 3350 to 4000 g / mol, a particle size of 100-1000 microns (determined by sieve analysis according to DGK H-II 2), in particular 200 to 400 .mu.m, wherein at least 90%, more preferably at least 95% of the particles have a size within a distribution of ⁇ 100 .mu.m and the particles almost exclusively, in particular exclusively, have a spherical shape.
  • the powder furthermore preferably has a monomodal particle size distribution, wherein at least 90%, in particular at least 95%, of the particles have a size within a distribution of ⁇ 100 ⁇ m, in particular ⁇ 50 ⁇ m, about the maximum of the particle size distribution.
  • the polyethylene glycol powder is obtainable, for example, by a process for producing spherical or spherical particles from liquids by dripping.
  • a casting liquid is supplied in this case in the form of a melt with pressure to a nozzle head.
  • the liquid jets emerging from the nozzle are constricted into individual segments and divided.
  • the surface tension pulls the liquid thread together. This leads to a rupture of the liquid jet and the formation of thread cylinders, which in turn transform into drops by the surface tension.
  • the generated drops are cured by cooling.
  • the balls must be solidified in their spherical shape, otherwise caused by the air resistance drops.
  • the hardening section can be designed as a cooling tower or drying tower, for example during the dripping of a melt.
  • the polyethylene glycol powder preferably has in each case independently of one another the following properties: an average molecular weight, in particular from 3350 to 4000 g / mol, at least 90%, preferably at least 95%, of the particles have a size within 200 to 400 ⁇ m, a dissolution time in 20 ° C warm water of not more than 30 seconds at a concentration of 10 g to 100 ml (experimental procedure see example), a bulk density of at least 670 g / l and / or a angle of repose cot ⁇ > 1.85 (determined according to DIN ISO 4324).
  • polyethylene glycol powders solid at room temperature can be used in selected applications with particular and unexpected benefits.
  • solid polyethylene glycols e.g. used in combination with liquid polyethylene glycols, as ointment bases or suppository masses (suppositories).
  • tabletting excipients as an aid in coating and coating of tablets, in handwashing pastes, soaps and syndet pieces, tableted denture cleaners, detergents, dishwashing agents, in the rubber industry, as intermediates in the production of polyurethanes, in the ceramics industry, in the Production of grinding compounds, in metalworking, in the paper and printing industry.
  • One of the suitable uses according to the invention is the use of the polyethylene glycol powders as or in laxatives. These bind a certain amount of fluid that comes from the solution with which they are taken. They are not absorbed by the body. As a result, the supplied amount of liquid passes unhindered to the rectum, where the evacuation reflex is triggered by stretching the intestinal wall mechanically.
  • the polyethylene glycols can be used for chronic constipation and for intestinal flushing, for example, several liters of a solution are drunk or administered via a gastric lavage. Salt losses can be prevented by addition of electrolyte in physiological concentration.
  • Polyethylene glycol powders for use as laxatives contain, in addition to at least about 85% by weight polyethylene glycol powder, other ingredients, e.g. up to a total of 15% by weight of electrolytes, sweetening, flavoring and coloring agents.
  • the constituents used are predominantly solids, preferably pulverulent components, which are processed by simple mixing to give the powdered laxatives.
  • the laxatives are preferably available in small packages such as sachets wherein the pouch contents are dissolved in water prior to use by adding the entire contents of the pouch to the water with stirring.
  • the polyethylene glycol powders represent by far the largest proportion by weight of the laxative, the properties of the laxative in the production, storage and dissolving behavior in water are decisively determined by the polyethylene glycol and the morphology of the powder.
  • a trouble-free production of the laxative which essentially includes the transport to the mixer, the mixing process and the filling process in the bag, is only possible if the polyethylene glycol powder is not prone to clumping, so is sufficiently free-flowing.
  • the bulk density of the laxative and thus the polyethylene glycol powder is as high as possible.
  • the particle size distribution of the polyethylene glycol powder is as narrow as possible to prevent separations into large and small particles during production and storage of the laxative.
  • the laxative and thus the polyethylene glycol powder, quickly dissolves in water and does not form lumps or floating on the water surface during preparation.
  • the requirement profile mentioned above for polyethylene glycols is only insufficiently satisfied by spray powder for the abovementioned reasons.
  • the polyethylene glycol powders can be used in several areas of gastroenterology, wherein the substance is used inter alia for the purification of the intestine, especially before a colonoscopy. For the purposes of the present application, these are also laxatives.
  • the polyethylene glycol powders can be used in the following cosmetic preparations: creams and lotions, perfumes, deodorants, insect repellents, lipsticks, toothpastes, hair care products, tooth cleansing tablets and bath additives.
  • polyethylene glycol grinding powders and spray powders have a broad particle size distribution.
  • Table 1 is intended to demonstrate this by way of example with reference to polyethylene glycol powders having an average molecular weight of 3350 g / mol.
  • the particle size distribution was determined by sieve analysis by means of a Retsch screening machine based on DGF H-II 2. While the particle size distribution of the commercially available grinding and spraying powders varies over a range of ⁇ 63 to> 630 ⁇ m, the powder according to the invention has a very narrow particle size of 200 to 400 ⁇ m.
  • Table 2 gives an overview of the dissolution time of a marketable polyethylene glycol grinding powder and marketable polyethylene glycol spray powders A and B in comparison to a polyethylene glycol powder according to the invention in water.
  • the average molecular weight of all 4 products is 3350 g / mol.
  • the release time was determined as follows:
  • Table 2 shows that the polyethylene glycol powder according to the invention is significantly faster soluble in water, as the marketable ground powder and the common spray powders.
  • the clumping tendency of polyethylene glycol powders correlates with its rideability.
  • the flowability of powders is determined by determining the angle of repose according to DIN ISO 4324 and stated in cot ⁇ . The larger cot ⁇ , the better the flowability and the lower the lumping tendency. 5
  • the tester according to Dr. med. Pfrengle be used on the basis of DIN ISO 4324. There, the angle of repose of the powder trickling out of a funnel (with stirring) is measured.
  • Table 3 gives an overview of the determined angle of repose of a commercially available polyethylene glycol grinding powder and of the commercially available polyethylene glycol spray powders A and B in comparison with a polyethylene glycol powder used according to the invention.
  • the average molecular weight of all 4 products is 3350 g / mol.
  • the flowability of the inventive polyethylene glycol powder is significantly better than that of the marketable grinding powder and the common spray powder. 0

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Polymers & Plastics (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Preparation (AREA)
  • Cosmetics (AREA)
  • Detergent Compositions (AREA)

Abstract

L'invention concerne l'utilisation de poudres de polyéthylène-glycol composées de particules sphériques de polyéthylène-glycol à répartition granulométrique étroite, et des compositions contenant ces poudres.
PCT/DE2008/001756 2007-11-02 2008-10-31 Utilisation de poudres de polyéthylène-glycol et compositions contenant ces poudres Ceased WO2009056114A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102007052870A DE102007052870A1 (de) 2007-11-02 2007-11-02 Verwendung von Polyethylenglykol-Pulvern und Zusammensetzungen enthaltend diese
DE102007052870.3 2007-11-02

Publications (2)

Publication Number Publication Date
WO2009056114A2 true WO2009056114A2 (fr) 2009-05-07
WO2009056114A3 WO2009056114A3 (fr) 2009-07-09

Family

ID=40445580

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DE2008/001756 Ceased WO2009056114A2 (fr) 2007-11-02 2008-10-31 Utilisation de poudres de polyéthylène-glycol et compositions contenant ces poudres

Country Status (2)

Country Link
DE (1) DE102007052870A1 (fr)
WO (1) WO2009056114A2 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8999313B2 (en) 2012-09-11 2015-04-07 Norgine Bv Compositions
US9592252B2 (en) 2011-03-11 2017-03-14 Norgine Bv Colonoscopy—preparation
CN107567481A (zh) * 2015-02-16 2018-01-09 科莱恩国际有限公司 装饰材料、尤其是人造雪及其制备方法
WO2018222773A3 (fr) * 2017-05-30 2019-02-07 Chan Eugene Y Substrats peptidiques fluorogènes pour mesures de facteur xa en solution et en phase solide

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0816061B2 (ja) * 1988-07-13 1996-02-21 森下ルセル株式会社 腸管洗浄液用組成物と腸管洗浄液
DE19617924A1 (de) 1996-05-05 1997-11-13 Brace Gmbh Chemie Plastics Dat Verfahren und Vorrichtung zur Schwingungsanregung von flüssigen Medien bei der Herstellung von sphärischen Granulaten
US6461546B1 (en) * 1998-08-03 2002-10-08 Ut-Battelle Apparatus for and method of producing monodisperse submicron polymer powders from solution
JP4655349B2 (ja) * 2000-10-18 2011-03-23 日油株式会社 経口医薬用ポリエチレングリコールおよびその製造方法
JP5041642B2 (ja) * 2001-08-30 2012-10-03 日本製薬株式会社 経口腸管洗浄液用組成物及び経口腸管洗浄液用充填製剤
WO2004089343A1 (fr) * 2003-04-09 2004-10-21 Ranbaxy Laboratories Limited Comprimes hydrosolubles
DE102004006670A1 (de) * 2004-02-11 2005-09-01 Clariant Gmbh Festes pulverförmiges Polyethylenglykol mit bimodaler Korngrößenverteilung, dessen Herstellung und dessen Verwendung
CN101036668A (zh) * 2007-02-15 2007-09-19 刘宇 含有聚乙二醇4000的颗粒剂

Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10646512B2 (en) 2011-03-11 2020-05-12 Norgine Bv Colonoscopy - preparation
US11529368B2 (en) 2011-03-11 2022-12-20 Norgine Bv Colonoscopy—preparation
US9592252B2 (en) 2011-03-11 2017-03-14 Norgine Bv Colonoscopy—preparation
US10792306B2 (en) 2011-03-11 2020-10-06 Norgine Bv Colonoscopy—preparation
US10780112B2 (en) 2011-03-11 2020-09-22 Norgine Bv Colonoscopy-preparation
US9707297B2 (en) 2012-09-11 2017-07-18 Norgine Bv Compositions
US10016504B2 (en) 2012-09-11 2018-07-10 Norgine Bv Compositions
US8999313B2 (en) 2012-09-11 2015-04-07 Norgine Bv Compositions
US10918723B2 (en) 2012-09-11 2021-02-16 Norgine Bv Colon cleansing compositions and methods of use
US9326969B2 (en) 2012-09-11 2016-05-03 Norgine Bv Compositions
US12083179B2 (en) 2012-09-11 2024-09-10 Norgine Bv Colon cleansing compositions and method of use
US20180244968A1 (en) * 2015-02-16 2018-08-30 Clariant International Ltd. Decorative Material, Particularly Artificial Snow, And A Method For Producing Same
CN107567481B (zh) * 2015-02-16 2019-09-10 科莱恩国际有限公司 装饰材料、尤其是人造雪及其制备方法
CN107567481A (zh) * 2015-02-16 2018-01-09 科莱恩国际有限公司 装饰材料、尤其是人造雪及其制备方法
WO2018222773A3 (fr) * 2017-05-30 2019-02-07 Chan Eugene Y Substrats peptidiques fluorogènes pour mesures de facteur xa en solution et en phase solide

Also Published As

Publication number Publication date
DE102007052870A1 (de) 2009-05-07
WO2009056114A3 (fr) 2009-07-09

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