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WO2011099031A1 - Active antioxidants for all age group - Google Patents

Active antioxidants for all age group Download PDF

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Publication number
WO2011099031A1
WO2011099031A1 PCT/IN2010/000872 IN2010000872W WO2011099031A1 WO 2011099031 A1 WO2011099031 A1 WO 2011099031A1 IN 2010000872 W IN2010000872 W IN 2010000872W WO 2011099031 A1 WO2011099031 A1 WO 2011099031A1
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Prior art keywords
folic acid
dha
recited
epa
folate
Prior art date
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Ceased
Application number
PCT/IN2010/000872
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French (fr)
Inventor
Kamlesh Rajnikant Zota
Sanjay Agrawal
Ketan Chandulal Zota
Manukant Chandulal Zota
Himanshu Muktilal Zota
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ZOTA HEALTH CARE Ltd
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ZOTA HEALTH CARE Ltd
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Filing date
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Publication of WO2011099031A1 publication Critical patent/WO2011099031A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/01Hydrocarbons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P39/06Free radical scavengers or antioxidants

Definitions

  • FIELD OF INVENTION This invention is based on active antioxidants which are useful for all age group like adult, kids thereof.
  • a method of providing controlled release of a biologically active substance within a subject's digestive system comprising administering a biologically active substance to a subject's digestive system.
  • the biologically active substance is administered concurrently with one or more soluble fibers in an oral dosage unit.
  • the soluble fibers interact with the biologically active substance within the subject's digestive system to moderate and control the release of the biologically active substances in the subject's bloodstream. This provides more constant blood concentrations of the biologically active substances.
  • the amount of soluble fibers in the oral dosage unit is greater than 40% by weight, and in some cases greater than 50% by weight of the oral dosage unit.
  • the oral dosage unit typically contains from about 1 to 15g of soluble fiber, and in some cases from about 3 to 5g of soluble fiber.
  • the biologically active substance may contain phytonutrients that promote the subject's cardiovascular system, immune system, or weight management.
  • the main object of the invention is to provide an active antioxidant for the all age group.
  • Prior antioxidants targeted on the particular age group. This is one of the strong antioxidant as comparative to others. Deficiency of antioxidants or low level of the same can cause oxidative stress and hence eventually kill cells. For all this reasons antioxidants are so important for the body metabolism and it also helps in lowering down the cell aging.
  • STATEMENT OF INVENTION This invention is based on active antioxidants which are useful for all age group like adult, kids thereof. These are active antioxidants. They work on whole body as well as its metabolism.
  • This invention is based on the strong antioxidants which are essential for all age group.
  • Oxidation is a chemical reaction that transfers electrons from a substance to an oxidizing agent. Oxidation reactions can produce free radicals, which start chain reactions that damage cells. Antioxidants terminate these chain reactions by removing free radical intermediates, and inhibit other oxidation reactions by being oxidized themselves. As a result, antioxidants are often reducing agents such as thiols, ascorbic acid or polyphenols. Antioxidants are also widely used as ingredients in dietary supplements in the hope of maintaining health and preventing diseases such as cancer and coronary heart disease. Although initial studies suggested that antioxidant supplements might promote health, later large clinical trials did not detect any benefit and suggested instead that excess supplementation may be harmful.
  • antioxidants In addition to the uses of natural antioxidants in medicine, oxidation reactions are crucial for life, they can also be damaging; hence, plants and animals maintain complex systems of multiple types of antioxidants, such as glutathione, vitamin C, and vitamin E as well as enzymes such as catalase, superoxide dismutase and various peroxidases.
  • EPA Eicosapentaenoic acid (EPA or also icosapentaenoic acid) is an omega-3 fatty acid. EPA and its metabolites act in the body largely by their interactions with the metabolites of arachidonic acid; It is obtained in the human diet by eating oily fish or fish oil— cod liver, herring, mackerel, salmon, menhaden and sardine. It is also found in human milk. It's beneficial potential in mental conditions, such as schizophrenia.. EPA may affect depression, and importantly, suicidal behavior. EPA has inhibitory effect on CYP2C9 and CYP2C19 hepatic enzymes.
  • DHA Docosahexaenoic acid is an omega-3 fatty acid. DHA is metabolized to form the docosanoids, which comprise several families of potent hormones. DHA is a major fatty acid in sperm and brain phospholipids, particularly in the retina. Dietary DHA may reduce the risk of heart disease by reducing the level of blood triglycerides in humans. Low levels of DHA have been associated with Alzheimer's disease.
  • Folic acid also known as vitamin B9 or folacin
  • folate the naturally occurring form
  • pteroyl-L-glutamic acid and pteroyl-L-glutamate are forms of the water-soluble vitamin B9.
  • Folic acid is itself not biologically active, but its biological importance is due to tetrahydrofolate and other derivatives after its conversion to dihydrofolic acid in the liver.
  • Heart disease - Folic acid is a safe and effective supplement that targets large artery stiffness and may prevent isolated systolic hypertension, it may improve the integrity of the vascular endothelium.
  • Bone loss in Parkinson's disease (PD)-Folate lowers homocysteine (Hey) levels which in turn prevents bone loss in Parkinson's disease (PD) patients taking levodopa (a psychoactive drug taken to treat Parkinson's disease). Improvements in bone health include increased BMD at the lumbar spine, total femur, and femur shaft.
  • Schizophrenia-Folate deficiency may increase the risk of schizophrenia because by increasing homocysteine levels folate also increases interleukin 6 and tumor necrosis factor alpha levels and these two cytokines are involved in the development of schizophrenia.
  • Renal disease-Folic acid supplements may reduce the risk of children developing renal diseases or injuries such as microalbuminuria.
  • Lycopene It's a symmetrical tetraterpene assembled from 8 isoprene units. Their antioxidant property, substantial scientific and clinical research has been devoted to a possible correlation between lycopene consumption and general health. Early research suggested some amelioration of cardiovascular disease, cancer, diabetes, osteoporosis, and even male infertility. Lycopene helps neutralize harmful free radicals, which are implicated in cancer, heart disease, macular degeneration and other age-related illnesses. The evidence for a benefit was strongest for cancers of the prostate, lung, and stomach. Data were also suggestive of a benefit for cancers of the pancreas, colon and rectum, esophagus, oral cavity, breast, and cervix

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Toxicology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

This invention is based on strong antioxidants which are useful for all age group. The basic composition of ingredients are-EPA 150 mg, DHA 100 mg, Folic Acid 5 mg and Lycopene 50 mg. DHA is a major fatty acid in sperm and brain phospholipids, particularly in the retina. Dietary DHA may reduce the risk of heart disease by reducing the level of blood triglycerides in humans. Low levels of DHA have been associated with Alzheimer's disease. Vitamin B9 (folic acid and folate inclusive) is essential to numerous bodily functions ranging from nucleotide biosynthesis to the remethylation of homocysteine. The human body needs folate to synthesize DNA, repair DNA, and methylate DNA as well as to act as a cofactor in biological reactions involving folate. It is especially important during periods of rapid cell division and growth. Both children and adults require folic acid to produce healthy red blood cells and prevent anemia. Folate and folic acid derive their names from the Latin word folium (which means "leaf"). Leafy vegetables are a principal source, although in Western diets fortified cereals and bread may be a larger dietary source. EPA has inhibitory effect on CYP2C9 and CYP2C19 hepatic enzymes. At high dose, it may also inhibit the activity of CYP2D6 and CYP3A4, important enzymes involved in drug metabolism. EPA improves the response of patients to chemotherapy, possibly by modulating the production of eicosanoid. It might also reduce the risk of developing certain types of cancer; including multiple myeloma. Lycopene helps neutralize harmful free radicals, which are implicated in cancer, heart disease, macular degeneration and other age- related illnesses. The evidence for a benefit was strongest for cancers of the prostate, lung, and stomach. Data were also suggestive of a benefit for cancers of the pancreas, colon and rectum, esophagus, oral cavity, breast, and cervix.

Description

TITLE OF INVENTION: Active antioxidants for all age group.
FIELD OF INVENTION: This invention is based on active antioxidants which are useful for all age group like adult, kids thereof.
PRIOR ART:
In the existing system as given in IPC8 Class: AA61K4706FI and USPC Class: 424 944 wherein A method of providing controlled release of a biologically active substance within a subject's digestive system. The biologically active substance is administered concurrently with one or more soluble fibers in an oral dosage unit. The soluble fibers interact with the biologically active substance within the subject's digestive system to moderate and control the release of the biologically active substances in the subject's bloodstream. This provides more constant blood concentrations of the biologically active substances. The amount of soluble fibers in the oral dosage unit is greater than 40% by weight, and in some cases greater than 50% by weight of the oral dosage unit. The oral dosage unit typically contains from about 1 to 15g of soluble fiber, and in some cases from about 3 to 5g of soluble fiber. The biologically active substance may contain phytonutrients that promote the subject's cardiovascular system, immune system, or weight management.
In the existing system as given in United States Patent 6649195 wherein A powerful formulation for preventing and treating macular degeneration, cataracts, glaucoma and other eye diseases, and contains over thirty naturally effective vitamins, minerals, phytonutrients and amino acids, which have all been found to demonstrate a powerful protective effect on the health of the eye.
In the existing system as given in WO/2009/053824 wherein the present invention concerns a new composition based on pellets of lipoic acid in a lipophilic medium, if necessary combined with other active ingredients.
OBJECT OF THE INVENTION: The main object of the invention is to provide an active antioxidant for the all age group. Prior antioxidants targeted on the particular age group. This is one of the strong antioxidant as comparative to others. Deficiency of antioxidants or low level of the same can cause oxidative stress and hence eventually kill cells. For all this reasons antioxidants are so important for the body metabolism and it also helps in lowering down the cell aging. STATEMENT OF INVENTION: This invention is based on active antioxidants which are useful for all age group like adult, kids thereof. These are active antioxidants. They work on whole body as well as its metabolism.
DETAILED DESCRIPTION AND SCOPE OF THE INVENTION: This invention is based on the strong antioxidants which are essential for all age group.
ANTIOXIDANT An antioxidant is a molecule capable of slowing or preventing the oxidation of other molecules. Oxidation is a chemical reaction that transfers electrons from a substance to an oxidizing agent. Oxidation reactions can produce free radicals, which start chain reactions that damage cells. Antioxidants terminate these chain reactions by removing free radical intermediates, and inhibit other oxidation reactions by being oxidized themselves. As a result, antioxidants are often reducing agents such as thiols, ascorbic acid or polyphenols. Antioxidants are also widely used as ingredients in dietary supplements in the hope of maintaining health and preventing diseases such as cancer and coronary heart disease. Although initial studies suggested that antioxidant supplements might promote health, later large clinical trials did not detect any benefit and suggested instead that excess supplementation may be harmful. In addition to the uses of natural antioxidants in medicine, oxidation reactions are crucial for life, they can also be damaging; hence, plants and animals maintain complex systems of multiple types of antioxidants, such as glutathione, vitamin C, and vitamin E as well as enzymes such as catalase, superoxide dismutase and various peroxidases.
EPA 150 mg
DHA 100 mg
Folic Acid 5 mg
Lycopene 50 mg
EPA Eicosapentaenoic acid (EPA or also icosapentaenoic acid) is an omega-3 fatty acid. EPA and its metabolites act in the body largely by their interactions with the metabolites of arachidonic acid; It is obtained in the human diet by eating oily fish or fish oil— cod liver, herring, mackerel, salmon, menhaden and sardine. It is also found in human milk. It's beneficial potential in mental conditions, such as schizophrenia.. EPA may affect depression, and importantly, suicidal behavior. EPA has inhibitory effect on CYP2C9 and CYP2C19 hepatic enzymes. At high dose, it may also inhibit the activity of CYP2D6 and CYP3A4, important enzymes involved in drug metabolism. EPA improves the response of patients to chemotherapy, possibly by modulating the production of eicosanoid. It might also reduce the risk of developing certain types of cancer, including multiple myeloma. DHA Docosahexaenoic acid is an omega-3 fatty acid. DHA is metabolized to form the docosanoids, which comprise several families of potent hormones. DHA is a major fatty acid in sperm and brain phospholipids, particularly in the retina. Dietary DHA may reduce the risk of heart disease by reducing the level of blood triglycerides in humans. Low levels of DHA have been associated with Alzheimer's disease.
Folic acid Folic acid (also known as vitamin B9 or folacin) and folate (the naturally occurring form), as well as pteroyl-L-glutamic acid and pteroyl-L-glutamate, are forms of the water-soluble vitamin B9. Folic acid is itself not biologically active, but its biological importance is due to tetrahydrofolate and other derivatives after its conversion to dihydrofolic acid in the liver.
(1 ) Human reproduction - Folate deficiency during pregnancy can increase the risk of preterm delivery, infant low birth weight, and fetal growth retardation. Folate deficiency in the mother increases homocysteine level in the blood which may lead to spontaneous abortion and pregnancy complications such as placental abruption and preeclampsia.
(2) Heart disease - Folic acid is a safe and effective supplement that targets large artery stiffness and may prevent isolated systolic hypertension, it may improve the integrity of the vascular endothelium.
(3) Stroke - Folic acid appears to reduce the risk of stroke. Folic supplements are inexpensive and relatively safe to use and that is why stroke or hyperhomocysteinemia patients are encouraged to consume daily B vitamins including folid acid.
(4) Infectious disease-Folate deficiency is linked to anemia causing Plasmodium falciparum malaria in areas such as Colombia where malaria has reached endemic proportions.
(5) Bone loss in Parkinson's disease (PD)-Folate lowers homocysteine (Hey) levels which in turn prevents bone loss in Parkinson's disease (PD) patients taking levodopa (a psychoactive drug taken to treat Parkinson's disease). Improvements in bone health include increased BMD at the lumbar spine, total femur, and femur shaft.
(6) Schizophrenia-Folate deficiency may increase the risk of schizophrenia because by increasing homocysteine levels folate also increases interleukin 6 and tumor necrosis factor alpha levels and these two cytokines are involved in the development of schizophrenia.
(7) Renal disease-Folic acid supplements may reduce the risk of children developing renal diseases or injuries such as microalbuminuria. Lycopene - It's a symmetrical tetraterpene assembled from 8 isoprene units. Their antioxidant property, substantial scientific and clinical research has been devoted to a possible correlation between lycopene consumption and general health. Early research suggested some amelioration of cardiovascular disease, cancer, diabetes, osteoporosis, and even male infertility. Lycopene helps neutralize harmful free radicals, which are implicated in cancer, heart disease, macular degeneration and other age-related illnesses. The evidence for a benefit was strongest for cancers of the prostate, lung, and stomach. Data were also suggestive of a benefit for cancers of the pancreas, colon and rectum, esophagus, oral cavity, breast, and cervix
Procedure of Manufacturing
QUANTITATIVE FORMULA:
Figure imgf000005_0001
Figure imgf000006_0002
Figure imgf000006_0001
Figure imgf000007_0001
MANUFACTURING PROCESS:
Figure imgf000008_0001

Claims

1. Active antioxidants for all age group.
2. Active antioxidants comprise of EPA, DHA, Folic acid and lycopene.
3. Active antioxidants as recited in Claim 2 wherein EPA 150 mg,
4. Active antioxidants as recited in Claim 2 wherein DHA 100 mg,
5. Active antioxidants as recited in Claim 2 wherein Folic Acid 5 mg
6. Active antioxidants as recited in Claim 2 wherein Lycopene 50 mg.
7. Active antioxidant as recited in Claim 4 wherein DHA is a major fatty acid in sperm and brain phospholipids, particularly in the retina. Dietary DHA may reduce the risk of heart disease by reducing the level of blood triglycerides in humans
8. Active antioxidants as recited in Claim 5 wherein folic acid is essential to numerous bodily functions ranging from nucleotide biosynthesis to the remethylation of homocysteine. The human body needs folate to synthesize DNA, repair DNA, and methylate DNA as well as to act as a cofactor in biological reactions involving folate. It is especially important during periods of rapid cell division and growth. Both children and adults require folic acid to produce healthy red blood cells and prevent anemia. Folate and folic acid derive their names from the Latin word folium (which means "leaf"). Leafy vegetables are a principal source, although in Western diets fortified ce"reals and bread may be a larger dietary source.
9. Active antioxidants as recited in Claim 6 wherein Lycopene helps neutralize harmful free radicals, which are implicated in cancer, heart disease, macular degeneration and other age-related illnesses. The evidence for a benefit was strongest for cancers of the prostate, lung, and stomach. Data were also suggestive of a benefit for cancers of the pancreas, colon and rectum, esophagus, oral cavity, breast, and cervix.
10. Active antioxidants as recited in Claim 3 wherein EPA has inhibitory effect on CYP2C9 and CYP2C19 hepatic enzymes. At high dose, it may also inhibit the activity of CYP2D6 and CYP3A4, important enzymes involved in drug metabolism. EPA improves the response of patients to chemotherapy, possibly by modulating the production of eicosanoid. It might also reduce the risk of developing certain types of cancer, including multiple myeloma.
PCT/IN2010/000872 2010-02-11 2010-12-30 Active antioxidants for all age group Ceased WO2011099031A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN373/MUM/2010 2010-02-11
IN373MU2010 2010-02-11

Publications (1)

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WO2011099031A1 true WO2011099031A1 (en) 2011-08-18

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2759044C1 (en) * 2020-09-23 2021-11-09 Федеральное государственное бюджетное учреждение "Российский научно-исследовательский институт гематологии и трансфузиологии Федерального медико-биологического агентства" (ФГБУ РосНИИГТ ФМБА России) Method for correcting anemia in preoperative period in patients with gastric cancer

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6649195B1 (en) 2002-07-11 2003-11-18 Vitacost.Com, Inc. Eyesight enhanced maintenance composition
WO2007076416A2 (en) * 2005-12-20 2007-07-05 Alcon Research, Ltd. Composition and methods for inhibiting the progression macular degeneration and promoting healthy vision
WO2009020595A2 (en) * 2007-08-03 2009-02-12 Shaklee Corporation Nutritional supplement system
DE202009002126U1 (en) * 2009-02-13 2009-04-16 Orthomol Pharmazeutische Vertriebs Gmbh Trace element-containing composition
WO2009053824A1 (en) 2007-10-23 2009-04-30 Laboratorio Chimico Internazionale S.P.A. Lipoic acid pellet composition
GB2458466A (en) * 2008-03-18 2009-09-23 Kartar Singh Lalvani Composition for hair, skin and nail health maintenance

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6649195B1 (en) 2002-07-11 2003-11-18 Vitacost.Com, Inc. Eyesight enhanced maintenance composition
WO2007076416A2 (en) * 2005-12-20 2007-07-05 Alcon Research, Ltd. Composition and methods for inhibiting the progression macular degeneration and promoting healthy vision
WO2009020595A2 (en) * 2007-08-03 2009-02-12 Shaklee Corporation Nutritional supplement system
WO2009053824A1 (en) 2007-10-23 2009-04-30 Laboratorio Chimico Internazionale S.P.A. Lipoic acid pellet composition
GB2458466A (en) * 2008-03-18 2009-09-23 Kartar Singh Lalvani Composition for hair, skin and nail health maintenance
DE202009002126U1 (en) * 2009-02-13 2009-04-16 Orthomol Pharmazeutische Vertriebs Gmbh Trace element-containing composition

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2759044C1 (en) * 2020-09-23 2021-11-09 Федеральное государственное бюджетное учреждение "Российский научно-исследовательский институт гематологии и трансфузиологии Федерального медико-биологического агентства" (ФГБУ РосНИИГТ ФМБА России) Method for correcting anemia in preoperative period in patients with gastric cancer

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