Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
  • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
  • A61K9/1605—Excipients; Inactive ingredients
  • A61K9/1629—Organic macromolecular compounds
  • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K9/4841—Filling excipients; Inactive ingredients
  • A61K9/4866—Organic macromolecular compounds
• • 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
  • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Definitions

• the present invention relates to the use of a vegetable extract Englerina lecardii for the manufacture of a pharmaceutical composition for the treatment of diabetes, more particularly for the treatment of type II diabetes.
• Diabetes is a chronic condition that occurs when the pancreas does not secrete enough insulin, so-called type I diabetes, or when the body misuses the insulin it produces, so-called diabetes.
• Insulin is a hormone that regulates the concentration of sugar in the blood.
• Hyperglycemia a high blood sugar concentration, is a common effect of diabetes which, over time, causes serious damage to many parts of the body, especially the heart, blood vessels, eyes, kidneys or nerves.
• Type II diabetes accounts for 90% of the world's diabetes and is mainly caused by diet problems, overweight, lack of exercise and genetic factors. Fortunately, type I diabetes is a rare death and is rapidly fatal without the daily administration of insulin.
• the World Health Organization estimates that there are more than 180 million diabetics in the world, including 4 million in France alone, and that there will be more than double that in 2030. D ' after estimates, 1, 1 million people died of diabetes in 2005 and WHO predicts that deaths from diabetes will increase by more than 50% over the next 10 years if urgent action is not taken .
• the most used treatment for diabetes is to administer a glucophage to the patient. It is usually metformin, a chemical obtained by semisynthesis from a plant called Galega.
• the metformin molecule usually used under form of tablets, has several disadvantages.
• Metformin is particularly contraindicated in case of diabetes ketoacidosis, diabetic precoma, even moderate renal disorders (or pathologies causing them), liver disorders, explorations using iodinated contrast media, insufficiency cardiac or respiratory failure. It should not be given in children and lactating women and can only be taken under medical supervision by elderly and pregnant women. Finally, the prolonged use of metformin potentiates the risk of the appearance of its undesirable effects.
• Metformin can also cause many side effects, including gastrointestinal symptoms such as nausea, vomiting, diarrhea, abdominal pain and loss of appetite. In some people, mild erythema, reduced vitamin B12 absorption with reduced serum levels and lactic acidosis have also been observed, with in the most severe cases acidotic dyspnea, abdominal pain, and hypothermia followed by coma.
• Metformin which is difficult to dose depending on each individual, can also cause, in case of overdose, an excessive drop in blood glucose, with consequences as serious as hyperglycemia.
• metformin is an expensive drug, which poses a serious economic problem for diabetics from the poorest countries. Indeed, it should be remembered that almost 80% of diabetes deaths occur in low- and middle-income countries. However, the high cost of conventional diabetes treatments makes it difficult to access care in developing countries. Access to diabetes treatment is therefore limited to a very small proportion of those concerned.
• metformin is a fragile molecule that requires strict conservation conditions, which is extremely problematic in hot and / or humid countries, particularly in Africa and Asia.
• the invention teaches the use of a vegetable extract Englerina lecardii for the manufacture of a pharmaceutical composition for the treatment of diabetes.
• composition according to the invention has no or very few side effects and is much less expensive than conventional diabetes medications. It is thus much better accepted by patients for long-term regular treatment.
• the antidiabetic pharmaceutical composition of the invention makes it possible to treat diabetes from a level of 1.05 g / l of sugar in the blood.
• the active principle of the antidiabetic pharmaceutical composition of the invention is directly derived from a natural plant extract, without chemical modification of its molecules, it is much better supported by the body and causes fewer side effects.
• the active principle of the antidiabetic pharmaceutical composition of the invention has very low risks of overdose, which considerably reduces the risk of excessive hypoglycaemia due to taking the medicine.
• Englerina lecardii or Loranthus lecardii whose vernacular name is sattaga bowal, is a sub-woody, hemiparasitic plant of the family Loranthaceae. It grows on savannah trees and is widely distributed in Senegal, Mali, Guinea-Bissau and Guinea. It has opposite or subopposed leaves, petiolate; and an ovate to elliptical or lanceolate leaf blade with cuneate base and acute to subacumine, glabrous and penninerve, with four to six pairs of lateral veins.
• a plant extract is used Englerina lecardii.
• This extract is preferably obtained from the leaves of Englerina lecardii and has a hypoglycemic activity, as well as an antioxidant and cytoprotective phytotherapeutic effect.
• the leaf extract of Englerina lecardii contains many active ingredients, many of which have been identified.
• a phytochemical screening was carried out by means of general tests and by thin layer chromatography. It revealed that the plant extract Englerina lecardii contains proanthocyanidins, saponosides, reducing compounds and carotenoids. Column chromatography revealed the presence of oligosaccharides and mainly polyphenols.
• the plant extract Englerina lecardii used in the context of the invention is preferably a vegetable solution or a liquid plant extract and for example according to its concentration a mother tincture, an officinal dye or a liquid extract 6'Englerina lecardii.
• This solution or liquid extract is obtained by any appropriate means and in particular by extraction, preferably aqueous, alcoholic or hydro-alcoholic, by maceration, infusion, decoction, digestion, leaching or the like.
• a liquid plant extract is prepared from Englerina lecardii leaves by means of hydro-alcoholic extraction by a stirring percolation technique. Its alcohol content is preferably between 30 and 70 °.
• Englerina lecardii mother tincture with an ethanol content of about 70% VA / was prepared from Englerina lecardii dry leaves by exhaustive cold percolation followed by concentration under vacuum. on the rotary evaporator.
• composition according to the invention can adopt different galenic forms. It can for example be in the form of tea bags containing for example about 5 grams of Englerina lecardii leaves roughly crushed.
• It may also be in the form of tablets, preferably orodispersible, soft capsules, granules, capsules, powder, ampoules, syrup or any other appropriate dosage form, preferably oral, imaginable by the human being. job.
• the composition according to the invention is formulated in the form of microspheres, also called spheroids, preferentially grouped into capsules in an amount corresponding for example to a unit dose.
• microspheres also called spheroids
• microspheres can be made by different methods.
• a first method consists for example in making a peripheral layer containing the plant extract Englerina lecardii around a neutral nucleus, formed for example of a mixture of sugar and starch or a crystal of sugar, mannitol or sorbitol.
• the layer containing the plant extract Englerina lecardii can advantageously be made by coating, impregnation, spraying or spraying, the active ingredient being for this purpose preferably mixed with a mounting agent or a binder.
• the microspheres or spheroids can be formed by extrusion and spheronization.
• the vegetable extract of Englerina lecardii is first mixed with an absorbent and adsorbent substance, preferentially of natural or synthetic polymer type, having plastic properties compatible with the extrusion and spheronization steps of the rest of the process.
• microcrystalline cellulose for example microcrystalline cellulose, microfine cellulose, a weakly substituted hydroxypropyl cellulosic polymer, starch, modified starch, polysaccharides or any other suitable substance or mixture.
• an aqueous or non-aqueous humidifying liquid may also be added to obtain a homogeneous, malleable paste that can undergo the next steps of the process.
• the moistening liquid also serves as a vehicle for transporting and depositing the active ingredient to the heart of the absorbent and adsorbent substance in the microcavities of the polymer.
• extrudates The manufacturing process then consists of extruding the wet mass through a die with calibrated orifices. This produces compact filaments of generally cylindrical and defined section, called "extrudates".
• These two methods may further comprise at least one drying step and / or a calibration step.
• the drying can be done by light heating for example at a temperature between 30 and 40 ° C or by simple exposure to the open air for a sufficient time.
• the resulting spheroids may optionally be coated on the periphery of an outer skin to protect for example external moisture, heat, aggressive body conditions or delayed effect.
• the plant extract of leaves Englerina lecardii advantageously has, in addition to its antidiabetic properties, antibacterial, cytoprotective and antioxidant properties.
• the polar methanol extract of Englerina lecardii leaves shows modest activity on Candida albicans with a MIC of 28.12 mg / ml.
• the present inventors have conducted two studies which have led to the conclusion of a significant decrease in blood glucose levels in diabetic patients treated with a decoction of leaves of Englerina lecardii. .
• the first study is a preliminary ethno-therapeutic evaluation that was conducted in sixteen diabetic patients (nine men and seven women), aged 36 to 70 years.
• the second study is a clinical trial that was performed in the Endocrinology-Diabetology and Metabolic Diseases Department of the DONKA National Hospital in Conakry, Guinea. This controlled clinical trial has demonstrated the efficacy and good tolerance of a composition based on Englerina lecardii in the treatment of diabetes in adults. The details of this test are described below.
• the patients included in the trial were treated with three strips of 5 g of Englerina lecardii leaves daily for three months.
• Glucose averages before inclusion and after six and twelve weeks of treatment are shown in Table I below.
• Bilirubin (mmol / l) 13.26 1 1, 77 1 1, 16 -2.10 (-15.84%) 0.31
• the composition according to the invention may contain one or more other suitable compounds or excipients such as for example extracts of one or more other plants, vitamins, minerals, trace elements , compounds increasing the effectiveness of the active ingredient, protecting it or assisting in its rapid release, flavorings, mounting agents, binding compounds, slippery compounds, lubricating compounds, surfactants, sugars, lactose, sorbitol, mannitol, modified starches or starches, maltodextrins, carbonates, citrates, gelatin, polyvinylpyrrolidone, polysaccharides, cellulose derivatives, cross-linked sodium carboxymethylcellulose, microcrystalline cellulose, microfine cellulose , low substituted hydroxypropyl cellulosic polymers or any other suitable compound.
• suitable compounds or excipients such as for example extracts of one or more other plants, vitamins, minerals, trace elements , compounds increasing the effectiveness of the active ingredient, protecting it or assisting in its rapid release, flavorings, mounting agents, binding compounds, slippery compounds, lubric
• Spheroids were made by the extrusion and spheronization process described above, from a hydroalcoholic extract of Englerina lecardii leaves, prepared according to the European Pharmacopoeia, with an ethanol content of 70% VA / and a residue. dry about 10%. These spheroids were collected in capsules of 350 mg.
• the spheroids obtained were grouped into capsules of 350 mg corresponding to a unit dose of composition, for a preferred dosage of three capsules per day.
• This trace element is a facilitator that activates the fight against diabetes.
• This incorporation can be carried out in various ways including the simple addition to the extract or the microcrystalline cellulose powder or even in the wetting liquid.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Medicinal Chemistry (AREA)
• Chemical & Material Sciences (AREA)
• Engineering & Computer Science (AREA)
• Veterinary Medicine (AREA)
• Animal Behavior & Ethology (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Natural Medicines & Medicinal Plants (AREA)
• Epidemiology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Diabetes (AREA)
• Botany (AREA)
• Mycology (AREA)
• Microbiology (AREA)
• Medical Informatics (AREA)
• Biotechnology (AREA)
• Alternative & Traditional Medicine (AREA)
• Endocrinology (AREA)
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• Obesity (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Medicines Containing Plant Substances (AREA)
• Medicinal Preparation (AREA)

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• 2009
  • 2009-11-23 FR FR0905623A patent/FR2952824B1/fr not_active Expired - Fee Related
• 2010
  • 2010-11-23 WO PCT/IB2010/055374 patent/WO2011061725A1/fr active Application Filing
  • 2010-11-23 US US13/511,411 patent/US8703213B2/en not_active Expired - Fee Related
  • 2010-11-23 EP EP10801273A patent/EP2504018A1/de not_active Withdrawn

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