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WO2006108595A1 - Utilisation de sporopollenine et/ou de ses derives en tant que constituant d'agents pharmaceutiques, de produits medicaux et de complements alimentaires - Google Patents

Utilisation de sporopollenine et/ou de ses derives en tant que constituant d'agents pharmaceutiques, de produits medicaux et de complements alimentaires Download PDF

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Publication number
WO2006108595A1
WO2006108595A1 PCT/EP2006/003257 EP2006003257W WO2006108595A1 WO 2006108595 A1 WO2006108595 A1 WO 2006108595A1 EP 2006003257 W EP2006003257 W EP 2006003257W WO 2006108595 A1 WO2006108595 A1 WO 2006108595A1
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WO
WIPO (PCT)
Prior art keywords
sporopollenin
medicaments
use according
derivatives
tablet
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/EP2006/003257
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German (de)
English (en)
Inventor
Andreas Maack
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.)
MAACK INES
Original Assignee
MAACK INES
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 MAACK INES filed Critical MAACK INES
Publication of WO2006108595A1 publication Critical patent/WO2006108595A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23LFOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • A23L33/105Plant extracts, their artificial duplicates or their derivatives
    • 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
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/3533,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355Tocopherols, e.g. vitamin E
    • 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
    • A61K31/375Ascorbic acid, i.e. vitamin C; Salts thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/04Sulfur, selenium or tellurium; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/06Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00Medicinal preparations containing inorganic active ingredients
    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/30Zinc; Compounds thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes

Definitions

  • the present invention relates to the use of sporopollenin and / or their derivatives as a constituent of food supplements, medical products or of medicaments for the treatment of poisonings caused by agents which are selected from the group of chemotherapeutic agents, radiotherapeutic agents, heavy metals, dioxins and polychlorinated biphenyls .
  • EP-A-1, 503,772 JP2004503025 (Dr. Andreas Maack) describes a sporopollenin-containing composition which, as a solution or as a solid form for cosmetic, pharmaceutical purposes such as poisoning in general and for the treatment of microbial diseases, as a chelating agent and can be used as a dietary supplement.
  • WO 05/000280 A2 (Dr. Mackenzie et al) relates to a pharmaceutical or dietary preparation which contains an effective amount of an active ingredient which is applied to the carrier sporopollenin.
  • a sporopollenin is understood, for example, according to Römpp - Lexikon Naturstoffe, 1997, page 604, keyword: sporopollenin, a polyterpene found in pollen (pollen), which may arise from oxidative polymerization of carotenoids and their esters. Sporopollenin can still be found in small amounts in spores and pollen from plants, such as ferns, club moss, pollen, but also as a component of special types of algae. It is commercially available from Bärlappspore through Polysciences Europe GmbH, Eppelheim, DE or from Chlorella algae through RTC GmbH, Norsehl, DE. It has surprisingly been found that sporopollenin and / or its derivatives can be used as a constituent of food supplements, medical products or medicaments for the treatment of special poisoning / side effects.
  • chemotherapeutic agents antineoplastic agents
  • radiotherapeutic agents heavy metals
  • dioxins dioxins
  • the present invention thus relates to the use of sporopollenin and / or their derivatives as a constituent of dietary supplements, medicinal products or of medicaments for the treatment of poisonings which are caused by agents which are selected from the group of chemotherapeutics, radiotherapeutics, heavy metals, dioxins and polychlorinated Biphenyls.
  • Poisoning in the sense of the present invention also means the alleviation of side effects which have been caused by chemotherapy and radiotherapy agents.
  • the treatment of the poisoning can be carried out prophylactically, for example when dealing with heavy metals, dioxins and perchlorinated biphenyls and before / during and / or after the start of radio- and chemotherapy as well as following poisoning therapeutically in the form of food supplements or drugs.
  • the radiotherapeutic agents are in particular radiopharmaceuticals and / or substances such as uranium, radium, technetium, etc. that expose them to ionizing radiation.
  • Antineoplastics such as those in Kleemann-Engel - Pharmaceutical substances, version 4.0, on CD-ROM, Stuttgart / New York: 2001 by Georg Thieme Verlag under the same name, are particularly suitable as chemotherapeutic agents whose damage / side effects are to be reduced can be found.
  • Examples of common cancer treatment agents such as cytostatics are:
  • Radiotherapeutics within the meaning of the present invention, the damage / side effects of which are to be reduced, are to be understood as contrast agents and the use of ionizing radiation during / before and / or after cancer therapies.
  • Heavy metals within the meaning of the present invention means both the corresponding elements, for example dusts, and their compounds, for example soluble compounds, the elements having a density of more than 5 g / cm 3 .
  • Examples include: arsenic, lead, cadmium, chromium, mercury, zinc, thallium, nickel, molybdenum, manganese and radioactive heavy metals such as uranium, radium, technetium and their compounds.
  • dioxins the damage of which is to be reduced, are taken to mean double-unsaturated six-membered ring systems with two oxygen atoms in the ring.
  • Römpp Chemie Lexikon Editor: Falbe, Reglitz] 9th edition 1989, keyword Dioxin, p. 996 f.
  • PCB Polychlorinated biphenyls
  • the medicaments are administered orally, in particular as capsules or tablets over the body cavities, in particular as Suppositories, capsules or tablets or as a liquid pharmaceutical form, in particular as a nasal spray or for inhalation.
  • the orally administered medicaments are an optionally gastric juice-resistant capsule, a coated or optionally gastric juice-resistant tablet, a tablet with a delayed release of active ingredient or a tablet for use in the oral cavity.
  • the medicaments are administered parenterally, in particular as infusion or injection preparations.
  • infusion or injection preparations We refer to Schöffling op. Cit., Pages 362 - 377.
  • the aforementioned medicinal products are used both as human medicinal products and as veterinary medicinal products.
  • the sporopollenin used according to the invention and its derivatives together with further auxiliaries and additives, for example selenium and / or zinc and / or magnesium, vitamin C, vitamin E, carotenes (preferably beta-carotene and its derivatives) and / or unsaturated fatty acids and / or other drugs.
  • auxiliaries and additives for example selenium and / or zinc and / or magnesium, vitamin C, vitamin E, carotenes (preferably beta-carotene and its derivatives) and / or unsaturated fatty acids and / or other drugs.
  • the sporopollenin derivatives are an amino, thiol, carboxylic acid, amino acid, polyol or halogen-functionalized sporopollenin and the soluble and parenteral administration forms are sporopollenin, in particular dissolved by means of an emulsifier.
  • the preparation of such derivatives is explained in more detail in WO 2005/000280 A1 and there in exemplary embodiments 9-15 and the corresponding general description.
  • the sporopollenin and / or their derivatives of the aforementioned type are used for the production and as a component of medicinal products or medical products of a radio protective agent / detoxifying agent (antidote) against poisoning by heavy metals / dioxins / PCBs.
  • a radio protective agent means an agent which protects the body cells from the damaging effects of ionizing radiation and / or cytostatics.
  • This component to be used in addition to sporopollenin is, for example, 2 - [(3-aminopropyl) amino] ethanethiol dihydrogenphosphate (ester), also known as Amifostine, Ethiophos, Gammaphos, commercially available as Ethylol, used as a radio protector for cis-platinum damage.
  • radio protector 9-methoxy-7 H-furo [3,2-g] [1] benzopyran-7-one, also known as methoxsalen, ammoidin, methoxypsoralen, methoxysalen; Xanthotoxin, which is used commercially as meladinin.
  • radio protector 6- (tri fluoromethoxy) -2-benzothiazolamine also known as riluzole.
  • Example 1 Use of sporopollenin in a gelatin capsule:
  • a gelatin capsule with a filling volume of 0.5 ml (capsule size 1) was filled with a mixture of 150 mg sporopollenin and 10 mg of the filler (mannitol, milk sugar, cellulose powder).
  • Example 2 Sporopollenin as a suppository:
  • a base was prepared and melted by triturating 1 g of sporopollenin with 9 g of a hard fat with a high hydroxyl number (Stadimol® from Stada Arzneistoff AG, Bad Vibel, mixture of mono-, di- and triglycerides of saturated fatty acids, HZ: 40-50).
  • the mass was poured out with stirring at 40 0 C in the individual cannulas, the suppositories allowed to solidify and the G confuseschwarte removed.
  • Example 3 Solution for injection with sporopollenin
  • An injection solution was prepared from 0.1 g Sporopollenin, 2 g of Brij 35 emulsifier P (Laureth-23) was prepared and 20.1 g of water, after the components at 121 0 C for at least 15 minutes at 2 a heat sterilization have been subjected bar.
  • Example 4 Food supplements after intoxication by heavy metals and / or dioxins
  • a gelatin capsule with a filling volume of 0.68 ml (capsule size 0) was filled with a mixture of 250 mg sporopollenin and 30 mg of the filler (mannitol, milk sugar, cellulose powder).

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Botany (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Mycology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Toxicology (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Biotechnology (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Microbiology (AREA)
  • Medical Informatics (AREA)
  • Nutrition Science (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne l'utilisation de sporopollénine et/ou de ses dérivés en tant que constituant d'agents pharmaceutiques ou de produits médicaux pour réaliser le traitement thérapeutique et/ou prophylactique, et/ou de compléments alimentaires pour prévenir des effets secondaires et/ou des intoxications lié(e)s à des agents radioactifs et/ou des agents cytotoxiques et/ou des métaux lourds, des dioxines et/ou des biphényles polychlorés.
PCT/EP2006/003257 2005-04-11 2006-04-10 Utilisation de sporopollenine et/ou de ses derives en tant que constituant d'agents pharmaceutiques, de produits medicaux et de complements alimentaires Ceased WO2006108595A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102005016714.4 2005-04-11
DE102005016714A DE102005016714A1 (de) 2005-04-11 2005-04-11 Verwendung von Sporopollenin und/oder deren Derivaten als Bestandteil von Arzneimitteln, Medizinalprodukten und Nahrungsergänzungsmitteln

Publications (1)

Publication Number Publication Date
WO2006108595A1 true WO2006108595A1 (fr) 2006-10-19

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Family Applications (1)

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PCT/EP2006/003257 Ceased WO2006108595A1 (fr) 2005-04-11 2006-04-10 Utilisation de sporopollenine et/ou de ses derives en tant que constituant d'agents pharmaceutiques, de produits medicaux et de complements alimentaires

Country Status (2)

Country Link
DE (1) DE102005016714A1 (fr)
WO (1) WO2006108595A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8784851B2 (en) 2005-07-28 2014-07-22 University Of Hull Topical formulations containing sporopollenin
US8828464B2 (en) 2008-07-09 2014-09-09 University Of Hull Whitened exine shells

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003094942A1 (fr) * 2002-05-13 2003-11-20 Maack, Ines Composition soluble contenant de la sporopollenine et utilisation de ladite composition
WO2004083401A2 (fr) * 2003-03-18 2004-09-30 Timothy Nicholas Ray Chlorelle a membrane cellulaire fragmentee et son procede de preparation
WO2005000280A2 (fr) * 2003-06-27 2005-01-06 University Of Hull Forme posologique

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003094942A1 (fr) * 2002-05-13 2003-11-20 Maack, Ines Composition soluble contenant de la sporopollenine et utilisation de ladite composition
WO2004083401A2 (fr) * 2003-03-18 2004-09-30 Timothy Nicholas Ray Chlorelle a membrane cellulaire fragmentee et son procede de preparation
WO2005000280A2 (fr) * 2003-06-27 2005-01-06 University Of Hull Forme posologique

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE BIOSIS [online] BIOSCIENCES INFORMATION SERVICE, PHILADELPHIA, PA, US; 1984, PORE R S: "DE TOXIFICATION OF CHLORDECONE POISONED RATS WITH CHLORELLA AND CHLORELLA DERIVED SPOROPOLLENIN", XP002387756, Database accession no. PREV198478039773 *
DRUG AND CHEMICAL TOXICOLOGY AN INTERNATIONAL JOURNAL FOR RAPID COMMUNICATION, vol. 7, no. 1, 1984, pages 57 - 72, ISSN: 0148-0545 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8784851B2 (en) 2005-07-28 2014-07-22 University Of Hull Topical formulations containing sporopollenin
US8828464B2 (en) 2008-07-09 2014-09-09 University Of Hull Whitened exine shells

Also Published As

Publication number Publication date
DE102005016714A1 (de) 2006-10-12

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