US20040241249A1 - Krill and/or marine extracts for prevention and/or treatment of cardiovascular diseases arthritis, skin cancer diabetes, premenstrual syndrome and transdermal transport - Google Patents

Krill and/or marine extracts for prevention and/or treatment of cardiovascular diseases arthritis, skin cancer diabetes, premenstrual syndrome and transdermal transport Download PDF

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US20040241249A1
US20040241249A1 US10/481,040 US48104004A US2004241249A1 US 20040241249 A1 US20040241249 A1 US 20040241249A1 US 48104004 A US48104004 A US 48104004A US 2004241249 A1 US2004241249 A1 US 2004241249A1
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composition
patient
krill
acid
effective amount
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Tina Sampalis
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Aker Biomarine Antarctic AS
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Priority to US10/481,040 priority Critical patent/US20040241249A1/en
Assigned to NEPTUNE TECHNOLOGIES & BIORESSOURCES INC. reassignment NEPTUNE TECHNOLOGIES & BIORESSOURCES INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: SAMPALIS, TINA
Publication of US20040241249A1 publication Critical patent/US20040241249A1/en
Priority to US11/640,235 priority patent/US8057825B2/en
Priority to US13/216,694 priority patent/US20110305771A1/en
Priority to US14/152,603 priority patent/US20140199414A1/en
Priority to US15/267,988 priority patent/US20170224742A1/en
Assigned to AKER BIOMARINE ANTARCTIC AS reassignment AKER BIOMARINE ANTARCTIC AS ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: Neptune Technologies & Bioressources, Inc.
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/56Materials from animals other than mammals
    • A61K35/612Crustaceans, e.g. crabs, lobsters, shrimps, krill or crayfish; Barnacles
    • AHUMAN NECESSITIES
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    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/07Retinol compounds, e.g. vitamin A
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    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/20Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
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    • A61K31/201Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having one or two double bonds, e.g. oleic, linoleic acids
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    • A61K31/202Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids having three or more double bonds, e.g. linolenic
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    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/23Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
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    • A61K31/232Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
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    • 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 
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    • A61K31/575Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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    • A61K31/688Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols both hydroxy compounds having nitrogen atoms, e.g. sphingomyelins
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    • A61K33/24Heavy metals; Compounds thereof
    • A61K33/30Zinc; Compounds thereof
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
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Definitions

  • This invention relates to multi-therapeutic extracts derived from krill and/or marine, which can prevent and/or treat several diseases.
  • Krill is the common name for small, shrimp-like crustaceans, however not shrimp, that swarm in dense shoals, especially in Antarctic waters. It is one of the most important food source for fish, some kind of birds and especially for baleen whales as being an important source of protein. Krill is also a good source of omega-3 fatty acid, which are well known for their health benefits.
  • krill and/or marine oil may be used for the treatment of autoimmune murine lupus and other autoimmune diseases and can also be used for treating cardiovascular diseases.
  • the krill and/or marine oil used for these treatments has only conserved its omega-3 fatty acids as active ingredients, which is a very small part of all the active ingredients of the krill and/or marine itself. This fact reduces the potential of the krill and/or marine oil as a treatment for these diseases.
  • a method of prevention, therapy and/or treatment of several disease comprising the administration of a therapeutically effective amount of krill and/or marine oil to a patient.
  • the krill and/or marine oil is obtained from a process comprising the steps of:
  • the krill and/or marine oil comprises Eicosapentanoic acid, Docosahexanoic acid, Linolenic acid, Alpha-linolenic acid, Linoleic acid, Arachidonic acid, Oleic acid, palmitic acid, palmitoleic acid, stearic acid, nervonic acid, Phosphatidylcholine, Phosphatidylinositol, Phosphatidylserine, Phosphatidylethanolamine, Sphingomyelin, Cholesterol, Triglycerides, Monoglycerides, a-tocopherol, all-trans retinol, Astaxanthin, Canthaxanthin, ⁇ -carotene, flavonoid, Zinc, Selenium, sodium, potassium and calcium.
  • the krill and/or marine oil comprises Eicosapentanoic acid, Docosahexanoic acid, Linolenic acid, Alpha-linolenic acid, Linoleic acid, Arachidonic acid, Oleic acid, palmitic acid, palmitoleic acid, stearic acid, Phosphatidylcholine, Phosphatidylinositol, Phosphatidylserine, Phosphatidylethanolamine, Sphingomyelin, Cholesterol, Triglycerides, Monoglycerides, a-tocopherol, all-trans retinol, Astaxanthin, Canthaxanthin, ⁇ -carotene, Zinc and Selenium.
  • compositions for the treatment and/or prevention and/or therapy of the previously mentioned diseases comprising a therapeutically effective amount of krill and/or marine oil in association with a pharmaceutically acceptable carrier.
  • a multi-therapeutic oil extract free of enzyme is derived from krill and/or marine, found in any marine environment around the world, for example, the Antarctic ocean (euphasia superba), the Pacific ocean (euphasia pacifica), the Atlantic ocean, the Indian ocean, in particular coastal regions of Mauritius Island and/or Reunion Island of Madagascar, Canadian West Coast, Japanese Coast, St-Lawrence Gulf and Fundy Bay, and this oil extract is a free fatty acid lipid fraction.
  • the active components of the enzyme-free krill and/or marine oil extract are:
  • the neutral lipids of the krill and/or marine extract also comprises:
  • ⁇ -tocopherol (vitamin E) >1.0 IU/100 g
  • ⁇ -carotene >3000 ⁇ g/100 ml
  • Astaxanthin >20 mg/100 g
  • Canthaxanthin >2 mg/100 g
  • the krill and/or marine extract also comprises:
  • Flavonoids >0.5 mg/100 g
  • Oil Stability index ⁇ 0.1 after 50 hours at 97.8° C.
  • Table 1 is showing the results obtained from the previously described tests: TABLE 1 Paired Samples Test Paired Differences 95% Confidence Std. Interval of the Parameter Error Difference Sig. (2- tested Mean SD. Mean Lower Upper t-value df tailed) Cholesterol .4954 .55800 .15476 .1582 .8326 3.201 12 .008 Triglycerides .3538 .54543 .15127 .0242 .6834 2.339 12 .037 HDL ⁇ .2108 .29859 .08281 ⁇ .3912 ⁇ .0303 ⁇ 2.545 12 .026 LDL .2846 .47333 .13128 ⁇ .0014 .5706 2.168 12 .051 Chol/HDL .3600 .53446 .14823 .0370 .6830 2.429 12 .032
  • the inclusion criteria for the study are being aged between 50 and 65 years, both genders being admissible, having a clinical diagnosis of primary osteoarthritis (mild to moderate) 6 to 12 months prior to study enrollment including pain and stiffness, radiographic confirmation of illness prior to enrollment. It also include evidence of measurable symptoms of OA for at least 3 months prior to study enrollment requiring the use of acetaminophen, anti-inflammatory agents or opioid analgesics. Patients were asked to stop the use of all “pain-killers” the week prior to initiation of the trial for wash-out purposes.
  • the Exclusion criteria were a severe osteoarthritis, unavoidable sustained use of NSAID's, aspirin or other medicines for anti-inflammatory use, use of topical analgesics within 4 weeks of randomization visit, steroid injection into either knee within past 3 months, initiation of physical therapy or muscle conditioning within 3 months, seafood allergies, use of anticoagulants or salicylates, alcohol consumption exceeding 3 mixed drinks per day, concurrent medical/arthritic disease that could confound or interfere with the evaluation of pain, prior surgery (including arthroscopy) of either knee, a known “secondary” cause of osteoarthritis.
  • Evaluation was based on daily dose of NSAIDs and/or analgesics and/or SAARDs, number of painful joints, number or swollen joints, duration of morning stiffness, visual analog scale (0-100) WOMACscale and SF36. Preliminary results have been obtained after 2 months. The number of NSAIDs and/or analgesics and/or SAARDs required for daily functioning has been recorded at initiation and at 2 months after initiation.
  • Results shown at Table 2 demonstrate the effect of an uptake of krill extract on the relief of arthritis. TABLE 2 Frequency % Valid % Cumulative % No change 3 23.1 23.1 23.1 Pain relief 10 76.9 76.9 100.0 Total 13 100.0 100.0
  • Nutrition was fat-free chow for the first week and was modified accordingly with the assigned group as described below for the following 2-20 weeks in the quantity of 1 ml of oil per day.
  • mice were divided in six groups as follows:
  • Group E fat free chow (100% of calories)+local application of krill and/or marine oil 2 times per day
  • Group F fat-free chow with supplementation or krill and/or marine oil (20% of total calories)+local application of krill and/or marine oil 2 times per day
  • mice had been submitted to UVB radiation using a fluorescent test lamp, emission spectrum 270400 nm during weeks 2-20.
  • the essay were performed during 30 minutes of UVB exposure per day and the test lamp was at a distance of 30 cm from the mice.
  • mice were anesthetized with ether and sacrificed. Skin was examined blind by pathologists for signs of carcinogenesis.
  • Krill and/or marine oil can be used to enhance transdermal transportation as a substrate for dermatological topical cosmetic applications where cosmetic applications relate to skin hydration, anti-wrinkle, keratolytics, peeling and mask via creams, ointments, gels, lotions or oils.
  • a blood glucose decrease of 20% was obtained for the patients taking krill extract, which shows that an uptake of krill extract is controlling blood glucose content and therefore controlling diabetes in human patients.
US10/481,040 2001-06-18 2002-06-07 Krill and/or marine extracts for prevention and/or treatment of cardiovascular diseases arthritis, skin cancer diabetes, premenstrual syndrome and transdermal transport Abandoned US20040241249A1 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
US10/481,040 US20040241249A1 (en) 2001-06-18 2002-06-07 Krill and/or marine extracts for prevention and/or treatment of cardiovascular diseases arthritis, skin cancer diabetes, premenstrual syndrome and transdermal transport
US11/640,235 US8057825B2 (en) 2001-06-18 2006-12-18 Krill extracts for treatment of cardiovascular diseases
US13/216,694 US20110305771A1 (en) 2001-06-18 2011-08-24 Krill Extracts for Treatment of Cardiovascular Diseases
US14/152,603 US20140199414A1 (en) 2001-06-18 2014-01-10 Krill and/or marine extracts for prevention and/or treatment of cardiovascular diseases, arthritis, skin cancer, diabetes, premenstrual syndrome and transdermal transport
US15/267,988 US20170224742A1 (en) 2001-06-18 2016-09-16 Phospholipid-containing marine extracts for treatment of cardiovascular diseases

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US29838301P 2001-06-18 2001-06-18
PCT/CA2002/000843 WO2002102394A2 (en) 2001-06-18 2002-06-07 Krill and/or marine extracts for prevention and/or treatment of cardiovascular diseases, arthritis, skin cancer, diabetes, premenstrual syndrome and transdermal transport
US10/481,040 US20040241249A1 (en) 2001-06-18 2002-06-07 Krill and/or marine extracts for prevention and/or treatment of cardiovascular diseases arthritis, skin cancer diabetes, premenstrual syndrome and transdermal transport

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US11/640,235 Expired - Fee Related US8057825B2 (en) 2001-06-18 2006-12-18 Krill extracts for treatment of cardiovascular diseases
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US15/267,988 Abandoned US20170224742A1 (en) 2001-06-18 2016-09-16 Phospholipid-containing marine extracts for treatment of cardiovascular diseases

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