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
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
• • 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
  • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P13/00—Drugs for disorders of the urinary system
  • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
  • A61P3/02—Nutrients, e.g. vitamins, minerals
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
  • A61P3/06—Antihyperlipidemics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P3/00—Drugs for disorders of the metabolism
  • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

• L-carnitine More generally, the physiological and pharmacological properties of L-carnitine have been the subject of the following recent publications:
• L-lysine or its organic acid salts or inorganic, exerts a potentiating or synergistic effect vis-à-vis the biological effects of L-carnitine.
• the present invention relates more particularly to new pharmaceutical and / or dietetic compositions characterized in that they contain as a single ingredient active L-carnitine, in combination with L-lysine or one of its organic or inorganic acid salts.
• compositions according to the invention exert favorable effects at the level of the nitrogenous hydrocarbon or electrolytic metabolism of various tissues, and, consequently, at the level of the functions of these in different physiological or pathological situations, in particular when these are accompanied by disturbances of muscle functions (hypoexcitability, hypocontractility).
• compositions will therefore find application in particular in the treatment of undernutrition states (post-operative, post-infection, post-trauma, post-chemotherapy, chronic respiratory failure, the elderly, the newborn), prediabetes or diabetics, hyperlipemia or in the treatment of heart disease (angina, heart failure), liver failure, cirrhosis.
• undernutrition states post-operative, post-infection, post-trauma, post-chemotherapy, chronic respiratory failure, the elderly, the newborn
• prediabetes or diabetics hyperlipemia or in the treatment of heart disease (angina, heart failure), liver failure, cirrhosis.
• These compositions can also be used in hemodialysis patients.
• compositions according to the invention can constitute a nutritional supplement in convalescent subjects, the elderly, the occasional or high-level sportsperson, pregnant women and, in general, in any asthenic person who presents functional muscular disturbances ( hypoexcitability and hypocontractility).
• L-lysine base but also by all the organic or inorganic acid salts of L-lysine which are biologically acceptable.
• L-lysine following: hydrochloride, acetate, succinate,
• the combination L-lysine and L-carnitine is a direct combination in the form of a salt.
• Such salts can be prepared according to traditional methods, for example by mixing L-carnitine with L-lysine in the form of hydrochloride in water and crystallization of the resulting salt by addition of an organic polar solvent immiscible in the water.
• the relative proportions of L-carnitine and L-lysine can vary between 1: 0.5 and 1:20 in moles.
• the doses per 24 h of L-lysine are between 0.5 g and
• the 20 g dose of L-lysine corresponds to the 24-hour supply of certain amino acid solutions used in artificial parenteral nutrition.
• the products are dissolved in 0.9% isotonic saline.
• Neuromuscular preparation (sciatic nerve - rocnemian gastric muscle in situ)
• the animal is anesthetized with veterinary sodium pentobarbital at a dose of 30 mg / kg, i.p. (0.05 ml per 100 g body weight).
• the right femoral vein is catheterized (Abbocath catheter, T 22G x 32 mm) and perfused with a dilute solution (1%) of veterinary sodium pentobarbital.
• an automatic infuser B. Braun, Melsungen is used at the speed of 0.380 ml / h.
• the nerve-muscle preparation is bathed in a modified Liley solution suitably oxygenated (95% O 2 and 5% CO 2 ) at 37 ° C, (137 mM / l NaCl; 5 mM / l KCl; 2 mM / l CaCl 2 ; 1 mM / l MgCl 2 ; 24 mM / l NaHCO 3 ; 1 mM / l sodium glutamate and 10 mM / l BES (N, N-b ⁇ s [2-hydroxyethyl] -2-aminoethanesulfonic acid).
• a modified Liley solution suitably oxygenated (95% O 2 and 5% CO 2 ) at 37 ° C, (137 mM / l NaCl; 5 mM / l KCl; 2 mM / l CaCl 2 ; 1 mM / l MgCl 2 ; 24 mM / l NaHCO
• Neuro-muscular excitability is determined by measuring 3 parameters: rheobase, chronaxia and useful time according to the methods described by LABORIT H. and LABORIT G., (1955), mentioned above and LAPICQUE L. (1926) "Excitability as a function of time.” 1 vol. Presses Universitaires éd., Paris.
• Rheobase is the threshold of electrical intensity capable of provoking the minimum functional response of the muscle when the current passage time lengthens indefinitely. This minimum intensity remains the same beyond a certain time limit called useful time. If the current passage time becomes less than the useful time. the intensity of the current capable of provoking a functional response becomes stronger and stronger. For a current of double intensity of the rheobase, the shortest duration of the passage of the exciting current is the chronaxie.
• Muscle contractility is determined by measuring the force of contraction caused by a stimulation of frequency 10 Hz compared to the force of contraction caused by a stimulation of frequency 100 Hz (maximum force of contraction).
• n 8 aaa aa aaa aaa aaa
• n 8 b NSb NSb NSb
• n 8 bb ce NSb NSc NSb NSc NSb c
• the minimum active dose is close to 20 ⁇ M / kg.
• the maximum activity is reached at a dose of 77.5 ⁇ M / kg.
• n 8 bbb bbb b bbbb
• L-carnitine or DL-carnitine with L-lysine on neuromuscular excitability and on muscle contractility of the fasted rat
• n 8 aaa aa aa aa aaaa
• n 8 NSb b NSb NSb
• n 8 bbb bbb bbbb
• n 8 bbb NSb NSb bb
• n 8 aaa aa aa aa aaaa
• n 8 NSb NSb NSb NSb
• n 8 bbb bb bb bbb
• n 8 NSb NSb NSb NSb
• n 8 bbb NSb NSb NSb
• n 8 NSb c NSb c NSb NSc NSb c
• n 8 bbb dddd bb NSd bbb NSd bbb d a: sound comparison with fed controls; a: 0.01 ⁇ P ⁇ 0.1 aa: 0.001 ⁇ P ⁇ 0.02 aaa: P ⁇ 0.001 NSa: not significant.
• b comparison with fasting witnesses; b, bb, bbb, NSb: see a.
• c comparison between DL-carnitine + L-lysine and L-carnitine + L-lysine (38.75 ⁇ M / kg); c, cc, ccc, NSc: see a.
• d identical to c for the dose of 77.50 ⁇ M / kg; d, dd, ddd, NSd: see a.
• L-carnitine and L-lysine according to the invention can be presented in various forms intended for pharmaceutical or dietetic use.
• the presentations can be intended:
• oral solutions ampoules, vials, pack, bags
• drops syrups, sachets, oral lyophilisates (lyocs)
• capsules tablets, chewable tablets, reconstituting drinks.
• parenteral artificial nutrition solutions (carbohydrates, amino acids, peptides, lipids, electrolytes, trace elements, vitamins).
• Example 2 Drinkable ampoules
• the invention also relates to a process for the preparation of a pharmaceutical and / or dietetic composition, characterized in that L-carnitine is combined with L-lysine or one of its salts of organic or inorganic acid and in that this combination is mixed with pharmaceutically or dietically acceptable excipients.
• L-carnitine is combined with L-lysine or one of its salts of organic or inorganic acid and in that this combination is mixed with pharmaceutically or dietically acceptable excipients.
• the particular embodiments are in accordance with those previously described for the composition.
• the invention finally relates to a method of treating mammals, in particular a human or an animal, characterized in that a mammal is administered a combination of L-carnitine and L-lysine or one of its organic acid salts or inorganic.

Landscapes

• Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• Animal Behavior & Ethology (AREA)
• Pharmacology & Pharmacy (AREA)
• General Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Diabetes (AREA)
• Obesity (AREA)
• Hematology (AREA)
• Endocrinology (AREA)
• Emergency Medicine (AREA)
• Nutrition Science (AREA)
• Urology & Nephrology (AREA)
• Reproductive Health (AREA)
• Gastroenterology & Hepatology (AREA)
• Epidemiology (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicinal Preparation (AREA)
• Coloring Foods And Improving Nutritive Qualities (AREA)

Applications Claiming Priority (2)

Publications (1)

Family

ID=9369324

Family Applications (1)

Country Status (10)

Families Citing this family (7)

Citations (1)

Family Cites Families (5)

• 1988
  • 1988-08-12 FR FR8810886A patent/FR2635264B1/fr not_active Expired - Fee Related
• 1989
  • 1989-08-01 CA CA000607172A patent/CA1341260C/fr not_active Expired - Fee Related
  • 1989-08-10 EP EP89402257A patent/EP0354848B1/fr not_active Expired - Lifetime
  • 1989-08-10 WO PCT/FR1989/000419 patent/WO1990001316A1/fr not_active Ceased
  • 1989-08-10 PT PT91430A patent/PT91430B/pt not_active IP Right Cessation
  • 1989-08-10 DE DE8989402257T patent/DE68903448T2/de not_active Expired - Fee Related
  • 1989-08-10 JP JP1508982A patent/JP2785989B2/ja not_active Expired - Lifetime
  • 1989-08-10 ES ES89402257T patent/ES2043062T3/es not_active Expired - Lifetime
  • 1989-08-10 EP EP89909580A patent/EP0428608A1/fr active Pending
  • 1989-08-10 AT AT89402257T patent/ATE82122T1/de not_active IP Right Cessation
  • 1989-08-10 DE DE198989402257T patent/DE354848T1/de active Pending
• 1991
  • 1991-09-27 GR GR90300149T patent/GR900300149T1/el unknown
• 1992
  • 1992-12-21 GR GR920403006T patent/GR3006598T3/el unknown

Patent Citations (1)

Non-Patent Citations (2)

Also Published As

Similar Documents

Legal Events