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WO1995017199A1 - Nouveaux melanges therapeutiques de glucides pour attenuer les troubles du sommeil - Google Patents

Nouveaux melanges therapeutiques de glucides pour attenuer les troubles du sommeil Download PDF

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Publication number
WO1995017199A1
WO1995017199A1 PCT/US1994/014734 US9414734W WO9517199A1 WO 1995017199 A1 WO1995017199 A1 WO 1995017199A1 US 9414734 W US9414734 W US 9414734W WO 9517199 A1 WO9517199 A1 WO 9517199A1
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WO
WIPO (PCT)
Prior art keywords
dextrose
galactose
acid
composition
ratio
Prior art date
Application number
PCT/US1994/014734
Other languages
English (en)
Inventor
Judith J. Wurtman
Jeff L. Shear
Alvin Kershman
Original Assignee
Walden Laboratories, Inc.
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 Walden Laboratories, Inc. filed Critical Walden Laboratories, Inc.
Publication of WO1995017199A1 publication Critical patent/WO1995017199A1/fr

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Classifications

    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7004—Monosaccharides having only carbon, hydrogen and oxygen atoms

Definitions

  • the present invention generally relates to novel therapeutic compositions comprising carbohydrate blends, to processes for preparing such carbohydrate blends and to methods of using the foregoing for general use as a sleep aid and relaxant and for assistance with sleep difficulties and disorders.
  • the invention is related to a carbohydrate blend that aids in relaxation and drowsiness, using the body's natural digestive process. Unlike pharmaceuticals, it does so without side effects or risk of dependency, and unlike natural remedies is proven effective in clinical tests.
  • the present invention is directed generally to novel therapeutic compositions comprising carbohydrate blends, to methods of using same for the general use as a sleep aid and relaxant and for assistance with sleep difficulties and disorders, and to processes for preparing said carbohydrate blends.
  • the present invention is directed to therapeutic compositions comprising novel blends of carbohydrates, such as but not limited to dextrose, galactose, and mixtures thereof.
  • said therapeutic compositions include carbohydrate blends comprising novel mixtures of dextrose and galactose, in ratios of about 10:1 to 1:1 respectively.
  • compositions comprising carbohydrate blends of dextrose and galactose in ratios of about 6:1 to 1:1.
  • a composition comprising a carbohydrate blend of dextrose and galactose in a ratio of about 5:1.
  • said carbohydrate blends are in the form of a solution comprising dextrose, galactose and water. More preferably, the solution comprises about 5 mL of water to 1 gram of carbohydrate. More preferably, the solution further comprises an acidulant to maintain a therapeutically effective pH. Such acidulants include but are not limited to adipic acid, citric acid, fumaric acid, lactic acid, succinic acid, tartaric acid, ascorbic acid, acetic acid, and malic acid. Preferred are solutions with a pH of less than 5.
  • a solution comprising 60g total carbohydrate comprised of 50g dextrose and lOg galactose, 280 mL water and malic acid to maintain the solution at a pH of 2.
  • Another embodiment of the invention is directed to methods of using said therapeutic compositions, effective as inducers of drowsiness for the general use as a sleep aid and relaxant and for assistance with sleep difficulties and disorders comprising administering such novel compositions to subjects in need of said treatment.
  • a further embodiment of the invention is a process for the production of novel carbohydrate blends for use in said therapeutic composition.
  • Said process comprises the steps of hydrolysing lactose, crystallizing the products, drying the products and adjusting the ratio of dextrose to galactose by adding anhydrous dextrose. More preferred is the process wherein the hydrolysing step comprises acid or lactase enzymatic hydrolysis. Also more preferred is the process wherein the crystallization step comprises selectively and separately crystallizing the products dextrose and galactose or crystallizing both dextrose and galactose together.
  • the present invention is generally directed to pharmaceutical compositions comprising a carbohydrate blend, preferably in the form of a solution, for general use as a sleep aid and relaxant and for assistance with sleep difficulties and disorders.
  • carbohydrate blend refers to a mixture of carbohydrates including but not limited to dextrose, galactose, and mixtures thereof.
  • the carbohydrate blend is dextrose and galactose in ratios of 10:1 to 1:1. More preferably the ratio of dextrose to galactose is from about 6:1 to 1:1. Specifically preferred is the ratio 5:1 dextrose to galactose.
  • solution refers to mixtures of carbohydrate blends of dextrose and galactose in water.
  • water includes distilled, deionized or tap water.
  • dextrose as used herein and in the claims reflects to glucose or polymers thereof.
  • Preferred is a solution further comprising an acidulant to maintain a therapeutically effective pH.
  • acidulant as used herein, includes acids which can maintain the pH of the solution at less than 5.
  • Such acids include but are not limited to adipic acid, citric acid, fumaric acid, lactic acid, succinic acid, tartaric acid, ascorbic acid, acetic acid, and malic acid. Preferred is the acidulant malic acid.
  • the phrase "therapeutically effective" as used herein and in the claims refers to that amount of carbohydrate blend necessary to administer to a subject to induce the desired effect of drowsiness.
  • the therapeutic compositions of this invention can be administered as general use as a sleep aid and relaxant and for assistance with sleep -difficulties and disorders by any means that produces contact of the active agent with the agent's site of action in the body of a mammal. They can be administered by any conventional means available for use in conjunction with therapeutic agents. They can be administered alone, but generally administered with a carrier selected on the basis of the chosen route of administration and standard therapeutic practice.
  • Dosage forms contain from about 20g - lOOg of active ingredient per unit. In these therapeutic compositions the active ingredient will ordinarily be present in an amount of about 0.5-95% by weight based on the total weight of the composition.
  • the active ingredient can be administered orally in solid dosage forms, such as capsules, tablets, and powders if taken together with a suitable amount of water, or in liquid dosage forms, such as elixirs, syrups, and suspensions. It can also be administered parenterally, in sterile liquid dosage forms.
  • Gelatin capsules contain the active ingredient and other powdered carriers, such as cellulose derivatives, magnesium stearate, stearic acid, and the like. Similar diluents can be used to make compressed tablets. Both tablets and capsules can be manufactured as sustained release products to provide for continuous release of medication over a period of hours. Compressed tablets can be sugar coated or film coated to mask any unpleasant taste and protect the tablet from the atmosphere, or enteric coated for selective disintegration in the gastrointestinal tract.
  • powdered carriers such as cellulose derivatives, magnesium stearate, stearic acid, and the like. Similar diluents can be used to make compressed tablets. Both tablets and capsules can be manufactured as sustained release products to provide for continuous release of medication over a period of hours. Compressed tablets can be sugar coated or film coated to mask any unpleasant taste and protect the tablet from the atmosphere, or enteric coated for selective disintegration in the gastrointestinal tract.
  • colorings and flavorings can be employed in any dosage form to improve the taste of the therapeutic composition to increase patient acceptance, and to make it more palatable.
  • Such flavorings can include but are not limited to artificial or real: chocolate, vanilla, strawberry, coffee, banana, orange, etc.
  • water, a suitable oil, saline, and glycols such as propylene glycol or polyethylene glycols are suitable carriers for parenteral solutions.
  • Solutions for parenteral administration preferably contain a suitable stabilizing agents, and if necessary, buffer substances.
  • Anti-oxidizing agents such as sodium bisulfite, sodium sulfite, or ascorbic acid, either alone or combined, are suitable stabilizing agents.
  • citric acid and its salts and sodium EDTA are described in Remington's Pharmaceutical Sciences. Mack Publishing Company, a standard reference text in this field.
  • compositions can also be prepared in the form of a food-stuff.
  • a food-stuff Such forms include, but are not limited to: a cold or hot liquid or powdered beverage, soup, pudding, wafer, a snack bar, cookies, cakes, breakfast cereal form, frozen hard or soft dessert format, fruit roll-up, gummy confection, pasta form, chewable tablets, solid food or confection bars, or other snack, etc.
  • Another embodiment is the process for the preparation of carbohydrate blends comprising dextrose and galactose.
  • Lactose is comprised of 50% dextrose and 50% galactose.
  • lactose In order to obtain a pure form of either of the carbohydrates, lactose must be broken down into its integral parts.
  • galactose is only available when lactose is digested.
  • protein and fats which may interfere with the ability of galactose and dextrose to induce drowsiness or function as a night time sleep aid. Therefore, it is preferred that specific methods be employed to obtain the monosaccharide in the purest form available.
  • Lactose was acid hydrolyzed and in a selective crystallization process galactose was crystallized separate from dextrose and dried. Dry galactose was then mixed with dry anhydrous dextrose in the proper proportion with additional flavors and acidulant.
  • Lactose was acid hydrolyzed into dextrose and galactose with both sugars crystallized out together. The mix was then dried, resulting in a 50/50 blend of dextrose to galactose. To the 50/50 blend was added additional dextrose to meet the appropriate ratio required when rehydrated for consumption plus flavor and acidulants.
  • Lactose in solution was treated with the enzyme lactase, which resulted in the hydrolysis of lactose into dextrose and galactose.
  • the mixture was then dried, forming crystals of galactose and dextrose at a ratio of 50/50, or the material was concentrated. Crystallized and then dried.
  • the 50/50 blend was then mixed with additional dextrose and acidulants so that when rehydrated, will result in the proper ratio for treatment.
  • Another reason for following the prescribed methods set out in Examples 1-3 above is that many individuals cannot digest lactose. Therefore, it is necessary to provide galactose and dextrose already in solution and without the presence of other interfering factors such as protein and fat. In this preferred embodiment, the benefit of sleep inducement is optimized.
  • EXAMPLE 4 In a controlled double-blind study with 8 subjects, all subjects fell asleep after taking the product, while none fell asleep after taking control products or placebo. None of the subjects knew that the product could help them sleep. A composition was made containing 50g dextrose, lOg galactose, 280 mL water, and sufficient malic acid to maintain the pH of the solution pH of 2.
  • composition of the present invention was administered to subjects each week for a period of four weeks. All subjects receiving said composition of the present invention fell into a deep sleep, whereas control compositions had no effect. The results show that compositions comprising a carbohydrate blend of the present invention are effective at inducing drowsiness, thereby are useful as therapeutic agents to aid in sleep disorders.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention se rapporte à de nouvelles compositions thérapeutiques comprenant des mélanges de glucides, à des procédés de préparatin de ces mélanges de glucides et à des procédés d'utilisation de ceux-ci pour qu'ils puissent servir d'une façon générale comme médicament favorisant le sommeil et comme relaxant, et pour aider à surmonter les difficultés et les troubles du sommeil.
PCT/US1994/014734 1993-12-22 1994-12-21 Nouveaux melanges therapeutiques de glucides pour attenuer les troubles du sommeil WO1995017199A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US168,493 1988-03-15
US16849393A 1993-12-22 1993-12-22

Publications (1)

Publication Number Publication Date
WO1995017199A1 true WO1995017199A1 (fr) 1995-06-29

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1994/014734 WO1995017199A1 (fr) 1993-12-22 1994-12-21 Nouveaux melanges therapeutiques de glucides pour attenuer les troubles du sommeil

Country Status (1)

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WO (1) WO1995017199A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013174882A1 (fr) * 2012-05-23 2013-11-28 Ruhlmann Juergen Composition destinée au traitement d'un trouble du rythme circadien
WO2015136030A1 (fr) * 2014-03-13 2015-09-17 Ruhlmann Jürgen Composition pour une utilisation dans le traitement de la fatigue, des troubles de la concentration, des symptômes de sevrage, des maux de tête et des refroidissements, en particulier de la dégradation des performances, de la déprime et de la fatigue

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2681858A (en) * 1950-11-30 1954-06-22 Nat Dairy Res Lab Inc Conversion of lactose to glucose and galactose
US2826502A (en) * 1955-04-28 1958-03-11 Nat Dairy Prod Corp Conversion of lactose to glucose and galactose with a minimum production of oligosaccharides
US3981773A (en) * 1973-07-20 1976-09-21 Agence Nationale De Valorisation De La Recherche (Anvar) Process for the preparation of galactose and beverages based on galactose from solutions containing lactose
US4229440A (en) * 1978-11-27 1980-10-21 Fujiya Confectionery Company Limited Pharmaceutical composition containing the polysaccharide KGF-C as active ingredient
US4511590A (en) * 1981-09-17 1985-04-16 Caldwell Marion J Low-lactose, low-galactose imitation milk product

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2681858A (en) * 1950-11-30 1954-06-22 Nat Dairy Res Lab Inc Conversion of lactose to glucose and galactose
US2826502A (en) * 1955-04-28 1958-03-11 Nat Dairy Prod Corp Conversion of lactose to glucose and galactose with a minimum production of oligosaccharides
US3981773A (en) * 1973-07-20 1976-09-21 Agence Nationale De Valorisation De La Recherche (Anvar) Process for the preparation of galactose and beverages based on galactose from solutions containing lactose
US4229440A (en) * 1978-11-27 1980-10-21 Fujiya Confectionery Company Limited Pharmaceutical composition containing the polysaccharide KGF-C as active ingredient
US4511590A (en) * 1981-09-17 1985-04-16 Caldwell Marion J Low-lactose, low-galactose imitation milk product

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JOURNAL OF NUTRITION, Volume 116, issued 1986, KWAN et al., "Effects of a Low Carbohydrate Isoenergetic Diet on Sleep Behavior and Pulmonary Functions in Healthy Female Adult Humans", pages 2393-2402. *
PEDIATRICS, Volume 90, issued 1992, OBERLANDER et al., "Shortterm Effects of Feed Composition on Sleep and Crying in Newborns", pages 733-740. *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013174882A1 (fr) * 2012-05-23 2013-11-28 Ruhlmann Juergen Composition destinée au traitement d'un trouble du rythme circadien
WO2015136030A1 (fr) * 2014-03-13 2015-09-17 Ruhlmann Jürgen Composition pour une utilisation dans le traitement de la fatigue, des troubles de la concentration, des symptômes de sevrage, des maux de tête et des refroidissements, en particulier de la dégradation des performances, de la déprime et de la fatigue
DE102014103443A1 (de) 2014-03-13 2015-09-17 Jürgen Ruhlmann Komposition zur Verwendung zur Behandlung von Müdigkeit, Konzentrationsschwäche, Entzugserscheinungen, Kopfschmerzen und Erkältungskrankheiten, insbesondere Leistungsabfall, Kater und Müdigkeit

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