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DE10008948A1 - L-Ascorbic acid formulation, containing isotonic saline as carrier providing transport through cell membranes, useful e.g. as antibacterial or antiviral agent, bronchodilator, vasodilator and radical scavenger - Google Patents

L-Ascorbic acid formulation, containing isotonic saline as carrier providing transport through cell membranes, useful e.g. as antibacterial or antiviral agent, bronchodilator, vasodilator and radical scavenger

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Publication number
DE10008948A1
DE10008948A1 DE10008948A DE10008948A DE10008948A1 DE 10008948 A1 DE10008948 A1 DE 10008948A1 DE 10008948 A DE10008948 A DE 10008948A DE 10008948 A DE10008948 A DE 10008948A DE 10008948 A1 DE10008948 A1 DE 10008948A1
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Prior art keywords
ascorbic acid
isotonic saline
antibacterial
bronchodilator
acid
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DE10008948A
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German (de)
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Peter Kohler
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    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (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)
  • Inorganic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

A synthetic L-ascorbic acid (LAA) formulation (I) contains isotonic saline (0.9 % sodium chloride solution) as carrier to transport LAA through cell membranes into animal cells. ACTIVITY : Antibacterial; virucidal; immunostimulant; vasotropic; antiinflammatory; antiasthmatic; antiallergic; hepatotropic; bronchodilator. MECHANISM OF ACTION : Hormone activation; mediation in intracellular protein synthesis by hormones and enzyme; activation of complement system (especially C3b); increasing IgG, IgG, IgM, nitrogen monoxide (NO) and inducible nitrogen monoxide synthase (iNOS) level increasing agent; cyclic adenosine monophosphate (cAMP) activator; superoxide dismutase-like radical scavenger; carnitine synthesis regulation.

Description

L-Ascorbinsäure und NaCl als Hormon Aktivator u. InfektionskillerL-ascorbic acid and NaCl as a hormone activator u. Infection killer

Der wasserlösliche Wirkstoff L-Ascorbinsäure mit NaCl als Carrier erreicht sublingual über die Mundschleimhaut hämatogen den Pulmonalkreislauf (Umgehung des first pass effects)!The water-soluble active ingredient L-ascorbic acid with NaCl as a carrier reached sublingually through the oral mucosa hematogenous the pulmonary circulation (bypassing the first pass effect)!

Hierdurch wird der second messen er cAMP aktiviert, z. B. aus durch Monooxygenasen entstandenes (Nor)-Adrenalin, ACTH u. a. first mes­ senger.This activates the second measure cAMP, e.g. B. from through Monooxygenases (nor) adrenaline, ACTH and the like. a. first mes senger.

Sowie eGMP durch NO-Synthase über DAG (Diacylglycerol), Calmodulin unter Beteiligung von Ca2+ u. a.As well as eGMP by NO synthase via DAG (diacylglycerol), calmodulin with the participation of Ca2 + and others

Hieraus resultiert eine Dilatation der Bronchien und Gefässe. Schnelle Wirkung (Sofortwirkung 30-60 sek.).This results in dilation of the bronchi and vessels. Fast action (immediate action 30-60 sec.).

Antibakterielle und Antivirale Wirkung durch Aktivierung des Komplementsystems, insbesonders C3b, Anstieg von IgA, IgG, IgM, sowie Anstieg von NO, unter anderem durch iNOS.Antibacterial and antiviral effects by activating the Complement system, especially C3b, increase in IgA, IgG, IgM, and an increase in NO, among other things due to iNOS.

Langsame Wirkung (ein bis sieben Tage)Slow effect (one to seven days)

Als Radikalfänger bei sublingualer (Pulmonalkreislauf) und/oder oraler Anwendung mit Verstoffwechslung in der Leber, als Immunmodulator zur Zellentgiftung, als Sauerstoff-Ozon- Radikalkiller mit SOD - Super Oxyd Dismutase ähnlicher Wirkung.As a radical scavenger in sublingual (pulmonary circulation) and / or oral use with metabolism in the liver, as an immunomodulator for cell poisoning, as an oxygen-ozone Radical killer with SOD - super oxide dismutase-like effect.

L-Ascorbinsäure ist an der Biosynthese von Carnitin beteiligt, wichtig für die Muskelfunktion bei Poliomyelitis und Post-Polio-Syndrom.
Wirkstoff/Carrier: L-Ascorbinsäure (weisses Pulver),
NaCl-Natriumchlorid 0,9%ige isotonische Kochsalzlösung
Mischung: ca. 0,6-1 g L-Ascorbinsäure auf 50 ml NaCl.
Anwendung/Dosierung: von obiger Lösung einige Sprühstösse sublingual (wie bei Nitro);
und/oder: Oral zur systemischen Applikation.
Als Nasenspray.
Als Halsspray.
Wirkung: Nach ca. 60 sek. (Sofortwirkung) Dilatation der Bronchien mit Schleimlösung.
Ausheilung von Infekten des Hals-Nasen- Rachen-Raumes und des Bronchialsystems.
Nebenwirkungen: Cortison bei Übersteuerung (feedback) durch zu stark erhöhtes NO (iNOS-Expression)
Oxalsteinbildung bei Disposition möglich.
Schilddrüsen-Hormon-Stimmulation durch Tyrosin-Thyroxin, cAMP, IP3, DAG mögl.
Schwitzen (selten) durch intra-interzelluläre Ca2+-Wellen, IP3 L-ascorbic acid is involved in the biosynthesis of carnitine, important for muscle function in poliomyelitis and post-polio syndrome.
Active ingredient / carrier: L-ascorbic acid (white powder),
NaCl sodium chloride 0.9% isotonic saline
Mixture: approx. 0.6-1 g L-ascorbic acid to 50 ml NaCl.
Application / dosage: a few sprays of the above solution sublingually (as with Nitro);
and / or: Oral for systemic application.
As a nasal spray.
As a throat spray.
Effect: after approx. 60 sec. (Immediate effect) Bronchial dilation with mucous solution.
Healing of infections of the ear, nose and throat and the bronchial system.
Side effects: cortisone in case of oversteer (feedback) due to excessive NO (iNOS expression)
Oxal stone formation possible with disposition.
Thyroid hormone stimulation by tyrosine thyroxine, cAMP, IP3, DAG possible
Sweating (rare) due to intra-intercellular Ca2 + waves, IP3

Einige Wirkungen von L-Ascorbinsäure und NaClSome effects of L-ascorbic acid and NaCl

  • 1. Dilatation der Bronchien: Bei Bronchitis, Asthma Bronchiale und Gefäße sublingual und/oder oral.1. Bronchial dilation: For bronchitis, bronchial asthma and vessels sublingually and / or orally.
  • 2. Infektabwehr: Bei akut eitriger oder chron. Bronchitis mit und ohne Asthma Bronchiale nach drei bis sieben Tagen kuriert.
    Bei akuter Rhinitis oder allergi­ scher, Laryngitis acuta, Laryngotracheitis, nach Stunden bis Tagen kuriert.    2. Defense against infections: In acute purulent or chronic. Bronchitis with and without bronchial asthma cured after three to seven days.
    In acute rhinitis or allergic, laryngitis acuta, laryngotracheitis, cured after hours to days.
  • 3. Entgiftung: Cofaktor bei der Entgiftung toxischer Metaboliten (freie Radikale, Sauerstoff-Radikale) z. B. bei Reperfusion-SOD- ähnliche Wirkung.
    Leberentgiftung    3. Detoxification: Cofactor in the detoxification of toxic metabolites (free radicals, oxygen radicals) z. B. in reperfusion SOD-like effect.
    Liver detoxification
  • 4. Carnitin-Synthese: Beteiligt an der Carnitin-Synthese, wichtig für die Muskelfunktion bei Poliomyelitis und Post-Polio- Syndrom.4. Carnitine synthesis: involved in the synthesis of carnitine, important for muscle function in poliomyelitis and post-polio Syndrome.
L-Ascorbinsäure - biochemische Wirkungen und LiteraturL-ascorbic acid - biochemical effects and literature (1) Dilatation der Bronchien und Gefäße(1) Dilation of the bronchi and vessels

Biochemie Löffler, 6. Auflage, S. 512;
Bayer Vitamine, Hippokrates Verlag, S. 243;
Pharma Wellhöner, S. 42-43;
Bässler Vitamin Lexikon, S. 196-197;
Physiologie Thews, S. 61 u. 530;
Römpp Chemie Lexikon, S. 4948;
Wörterbuch der Medizin, S. 2172;
Friedrich Vitamine U u. S-Verlag, S. 633;
Münchner Med. Wochenschrift 134 Nr. 48, S. 55-56;
Laborjournal 10/98, S. 21;
Biochemie-Atlas, Michal, Spektrum Verlag, S. 228.Biochemie Löffler, 6th edition, p. 512;
Bayer Vitamine, Hippokrates Verlag, p. 243;
Pharma Wellhöner, pp. 42-43;
Bässler Vitamin Lexikon, pp. 196-197;
Physiologie Thews, p. 61 u. 530;
Römpp Chemie Lexikon, p. 4948;
Dictionary of Medicine, p. 2172;
Friedrich Vitamins U u. S-Verlag, p. 633;
Munich Med. Wochenschrift 134 No. 48, pp. 55-56;
Labor Journal 10/98, p. 21;
Biochemie-Atlas, Michal, Spektrum Verlag, p. 228.

(2) Infekt-Immunabwehr(2) Infectious Defense

Friedrich Vitamine, U u. S-Verlag, S. 628-631;
Bässler Vitamin Lexikon, S. 206;
Biochemie Karlson, Thieme Verlag 14. Aufl., S. 511-512, 459;
Biochemie Styer, Spektrum Verl., S. 395;
Roche med. Lexikon 4. Auflage, S. 933-934 u. 1240;
Pneumologie Ferlinz, Thieme Verl., S. 272;
Bisalski Vitamine Thieme Verl., S. 134-135 u. 360;
Immunologie Thieme 4. Auflage, S. 150;
Apotheken Umschau A4/99, S. 20.Friedrich Vitamine, U u. S-Verlag, pp. 628-631;
Bässler Vitamin Lexikon, p. 206;
Biochemie Karlson, Thieme Verlag 14th ed., Pp. 511-512, 459;
Biochemie Styer, Spektrum Verl., P. 395;
Roche med. Lexicon 4th edition, pp. 933-934 u. 1240;
Pneumology Ferlinz, Thieme Verl., P. 272;
Bisalski Vitamins Thieme Verl., Pp. 134-135 u. 360;
Immunologie Thieme 4th edition, p. 150;
Apotheken Umschau A4 / 99, p. 20.

(3) Radikalfänger (SOD), Leberentgiftung(3) radical scavenger (SOD), liver detoxification

Bässler Vitamin Lexikon, S. 195, 262;
Biesalski Vitamine, Thieme, S. 134;
Forth Pharma 6. Auflage, S. 594, 596;
Internet: kurz und fündig, S. 18;
medizin report Nr. 4/1999, S. 20-21;
Römpp Chemie Lexikon, S. 4394.Bässler Vitamin Lexikon, p. 195, 262;
Biesalski Vitamine, Thieme, p. 134;
Forth Pharma 6th edition, pp. 594, 596;
Internet: in a nutshell, p. 18;
medicine report No. 4/1999, pp. 20-21;
Römpp Chemie Lexikon, p. 4394.

(4) Energie/Muskel(4) energy / muscle

Biesalski Vitamine, Thieme Verlag, S. 134;
Bayer Vitamine, Hippokrates, S. 244;
Römpp Chemie Lexikon, S. 4948;
Apotheken Umschau A3/99, S. 52-53.Biesalski Vitamine, Thieme Verlag, p. 134;
Bayer Vitamine, Hippocrates, p. 244;
Römpp Chemie Lexikon, p. 4948;
Apotheken Umschau A3 / 99, pp. 52-53.

(5) Nebenwirkungen(5) side effects

Pneumologie, Nr. 6/1998;
Laborjournal, 8/99;
Römpp Chemie Lexikon 9. Aufl., S. 4781. Pneumology, No. 6/1998;
Laboratory Journal, 8/99;
Römpp Chemie Lexikon 9th ed., P. 4781.

Beschreibungdescription

L-Ascorbinsäure mit NaCl als Carrier dringt durch die Zell­ membran (erste Wirkung) ins Zellinnere ein (zweite Wirkung) und verändert (beeinflusst) dort durch Hormon- und Enzym- Regulation die Proteinsynthese.L-ascorbic acid with NaCl as a carrier penetrates the cell membrane (first effect) into the cell interior (second effect) and changes (influenced) there by hormone and enzyme Regulation of protein synthesis.

Dies bewirkt eine Gefäss- und Bronchien Dilatation und hat antiphlogistische Wirkung.This causes dilation and vascular and bronchial tubes has anti-inflammatory effects.

Dies geschieht durch Aktivierung von cAMP, cGMP und NO, Stickstoffmonoxyd sowie durch den Anstieg des Komplement­ systems und IgA, IgG, und IgM.This is done by activating cAMP, cGMP and NO, Nitric oxide and the increase in complement systems and IgA, IgG, and IgM.

Anwendungapplication

L-Ascorbinsäure und NaCl soll sublingual und/oder oral sustituiert werden je nach der gewünschten Wirkung, Lungenkreislauf (Umgehung des first pass effects) oder Verstoffwechslung in der Leber.L-ascorbic acid and NaCl are said to be sublingual and / or oral depending on the desired effect, Pulmonary circulation (bypassing the first pass effect) or Metabolism in the liver.

Eine Toleranzentwicklung konnte nach bisher zweijähriger Anwendung nicht festgestellt werden.A tolerance development could take place after two years Application cannot be determined.

Mit dieser Methode müsste es den Gelehrten der zuständigen Forschungsbereiche möglich sein, die vielen bisher nicht sich bewiesenen biologischen Funktionen von L-Ascorbinsäure in Vitro und in Vivo zu testen. With this method it should be the scholar of the responsible Research areas may be possible that many have not so far proven biological functions of L-ascorbic acid to be tested in Vitro and in Vivo.  

NebenwirkungenSide effects

Um unkontroliertes Zellwachstum bei Anwendung von L-Ascorbinsäure und NaCl (Aktivierung der Wachstumsfaktoren EGF, IGF I u. II, DAG-Diacylglycerol, Inositol-tris-phosphat und Ca2+) zu verhindern ist die Anwendung von NaCl und Retinol zur Zelldifferenzierung ratsam.In order to prevent uncontrolled cell growth when using L-ascorbic acid and NaCl (activation of the growth factors EGF, IGF I and II, DAG-diacylglycerol, inositol-tris-phosphate and Ca2 + ), the use of NaCl and retinol for cell differentiation is advisable.

Aktenzeichen P 44 00 716.7 vom 12.01.1994Case number P 44 00 716.7 from January 12, 1994

Beim Auftreten starker Rasselgeäusche nach Substitution von L-Ascorbinsäure und NaCl ist die Anwendung von DL-a-Tocopherolacetat und NaCl - Aktenzeichen 197 08 668.3 vom 03.01.1997 als fettlösliches Antiphlogistikum angebracht.When strong rattling occurs after substitution of L-ascorbic acid and NaCl is the use of DL-a-tocopherol acetate and NaCl file number 197 08 668.3 from January 3rd, 1997 as fat soluble Anti-inflammatory drug attached.

Um einem möglichen Anstieg von Thromboxan und einer Thrombozyten- Aggregation durch L-Ascorbinsäure und NaCl vorzubeugen ist ebenfalls NaCl und Tocopherol anzuwenden.To prevent a possible increase in thromboxane and platelet Prevent aggregation by L-ascorbic acid and NaCl also use NaCl and tocopherol.

Als Alternative ist ASS (Aspirin) möglich - Kontraindikationen wie Allergien, Magenulcera, Cortison usw. sind zu beachten!As an alternative, ASA (aspirin) is possible - contraindications such as allergies, gastric ulcers, cortisone, etc. must be considered!

Literatur zur ZelldifferenzierungLiterature on cell differentiation

Biologie für Mediziner, Thieme Verlag, 2. Aufl., Seite 351-352;
Biochemie Karlson dto. Verlag, 14. Aufl., Seite 546;
Biochemie stryer Spektrum Verlag, 4. Aufl., Seite 371-373;
Biochemie Löffler Springer Verlag, 6. Aufl., Seite 1092-1093.Biology for medical professionals, Thieme Verlag, 2nd ed., Pages 351-352;
Biochemie Karlson dto. Verlag, 14th ed., Page 546;
Biochemie stryer Spektrum Verlag, 4th ed., Pages 371-373;
Biochemistry Löffler Springer Verlag, 6th ed., Page 1092-1093.

Claims (1)

1. Diese leiten sich her aus dem synthetischen Wirkstoff L-Ascorbinsäure (weisses Pulver, siehe Formel unten) welche durch die isotonische Kochsalzlösung NaCl 0,9% als Transporteur (Carrier) durch die Zellmembran in die tierische Zelle getragen wird.
Die beschriebene Wirkung wird dadurch an der Zellmembran und/oder im Zellinnern erreicht.
Formel Friedrich Vitamine
Strukturformeln von L-Ascorbinsäure (a), Dehydro-L-ascorbinsäure (b), Semidehydro-L-ascorbin­ säure (Ascorbylradial) (c) und L-Threonsäure (d).
Chemie
Synthese
Es wurden zwar viele Verfahren beschrieben, die "klassische Reichsteinsynthese" (1934) ist jedoch immer noch die ergiebigste und ist bis heute die Grundlage der industriellen Produktion. Die wichtigsten Schritte sind: katalytische Druckhy­ drierung von D-Glucose zu D-Sorbit; Oxidation von D-Sorbit zu L-Sorbose mittels Acetobacter suboxidans in der Submerskultur; Herstellung von Diaceton-L-sorbose und deren Oxidation mit Per­ manganat in alkalischer Lösung zur Carbonsäu­ re; hydrolytische Abspaltung von Aceton unter Bildung von 2-Oxo-L-gulonsäure; Enolisierung zu Ascorbinsäure (Abb. 13-2). Zur Herstellung von 1 kg Ascorbinsäure sind 2 bis 4 kg Glucose erforderlich. Heute werden Tausende Jahres­ tonnen Ascorbinsäure produziert. Ihre Verwen­ dung ist sehr vielseitig. Etwa 60-70% der weltwei­ ten Vitamin-C-Produktion werden dem Sektor Lebensmittelindustrie zugeführt.1. These are derived from the synthetic active ingredient L-ascorbic acid (white powder, see formula below) which is carried through the cell membrane into the animal cell by the isotonic saline solution NaCl 0.9% as a carrier.
The effect described is achieved on the cell membrane and / or inside the cell.
Formula Friedrich Vitamins
Structural formulas of L-ascorbic acid (a), dehydro-L-ascorbic acid (b), semidehydro-L-ascorbic acid (Ascorbyl radial) (c) and L-threonic acid (d).
chemistry
synthesis
Although many processes have been described, "classic Reichstein synthesis" (1934) is still the most productive and is the basis of industrial production to this day. The most important steps are: catalytic pressure hydrogenation from D-glucose to D-sorbitol; Oxidation of D-sorbitol to L-sorbose using Acetobacter suboxidans in the submerged culture; Production of diacetone-L-sorbose and its oxidation with per manganate in alkaline solution to carboxylic acid; hydrolytic cleavage of acetone to form 2-oxo-L-gulonic acid; Enolization to ascorbic acid ( Fig. 13-2). 2 to 4 kg of glucose are required to produce 1 kg of ascorbic acid. Today, thousands of tons of ascorbic acid are produced every year. Their use is very versatile. Around 60-70% of global vitamin C production is supplied to the food industry sector.
DE10008948A 2000-02-25 2000-02-25 L-Ascorbic acid formulation, containing isotonic saline as carrier providing transport through cell membranes, useful e.g. as antibacterial or antiviral agent, bronchodilator, vasodilator and radical scavenger Withdrawn DE10008948A1 (en)

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US9138452B2 (en) 2008-04-10 2015-09-22 U.S. Nutraceuticals, LLC Plant derived seed extract rich in essential fatty acids derived from Perilla seed: composition of matter, manufacturing process and use
US9414620B2 (en) 2008-04-10 2016-08-16 U.S. Nutraceuticals, LLC Perilla seed composition
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US9532965B2 (en) 2008-04-10 2017-01-03 U.S. Nutraceuticals, LLC Plant derived seed extract rich in essentially fatty acids derived from Salvia hispanica L. seed: composition of matter, manufacturing process and use
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US9770047B2 (en) 2008-04-10 2017-09-26 U.S. Nutraceuticals, LLC Perilla seed composition

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