EP2964207A1 - Composition destinée à être utilisée dans le traitement du syndrome des ovaires polykystiques - Google Patents

Composition destinée à être utilisée dans le traitement du syndrome des ovaires polykystiques

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Publication number
EP2964207A1
EP2964207A1 EP14719069.8A EP14719069A EP2964207A1 EP 2964207 A1 EP2964207 A1 EP 2964207A1 EP 14719069 A EP14719069 A EP 14719069A EP 2964207 A1 EP2964207 A1 EP 2964207A1
Authority
EP
European Patent Office
Prior art keywords
formulation
lipoic acid
polycystic ovary
ovary syndrome
present
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP14719069.8A
Other languages
German (de)
English (en)
Inventor
Lorenzo Secondini
Luigi Amelotti
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Laborest Italia SRL
Original Assignee
Laborest Italia SRL
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 Laborest Italia SRL filed Critical Laborest Italia SRL
Publication of EP2964207A1 publication Critical patent/EP2964207A1/fr
Withdrawn legal-status Critical Current

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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
    • A61K36/06—Fungi, e.g. yeasts
    • A61K36/062—Ascomycota
    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
    • 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)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/899—Poaceae or Gramineae (Grass family), e.g. bamboo, corn or sugar cane
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Definitions

  • composition for use in the treatment of polycystic ovary syndrome Composition for use in the treatment of polycystic ovary syndrome
  • the present invention relates to a pharmaceutical composition or a nutraceutical composition or a medical device or a supplement product for use in the preventive and/or curative treatment of polycystic ovary syndrome (PCOS) and of the metabolic disorders deriving from or connected to polycystic ovary syndrome.
  • PCOS polycystic ovary syndrome
  • the present invention relates to a pharmaceutical composition or a nutraceutical composition or a medical device or a supplement product for use in reducing the lipid profile and the degree of hirsutism in insulin resistant and hyperandrogenous women affected by polycystic ovary syndrome.
  • PCOS Polycystic Ovary Syndrome
  • PCOS Polycystic Ovary Syndrome
  • the physiological hyperinsulinaemia of adolescence may constitute a triggering factor that brings about the development of hyperandrogenism and anovulation.
  • Polycystic ovary syndrome has a basic etiology linked to an oxidative syndrome with insulin resistance.
  • the insulin resistance and consequent hyperinsulinaemia that are often associated with this syndrome play an important role not only in the pathogenesis of the syndrome itself, but also in the clinical symptomatology.
  • HOMA glucose (mmol/l) x insulin (mU/ml) / 22.5. Values > 2.5 indicate insulin resistance.
  • patients with this syndrome have an increased risk of developing pathologies such as type 2 diabetes, the metabolic syndrome in connection with hypertension, dislipidaemia and cardiovascular diseases, obesity, high plasma levels of C-Reactive Protein (CRP) and triglycerides with low levels of cholesterol.
  • CRP C-Reactive Protein
  • Reversible gastrointestinal side effects occur in 30% of the cases in patients who take metformin. These include abdominal discomfort characterized by diarrhoea, nausea, abdominal swelling, loss of appetite, anorexia and a metallic taste in the mouth.
  • the Applicant has given a response to the above-mentioned needs thanks to a selected combination of active compounds, which unexpectedly show an unexpected mutual synergistic action.
  • the present invention therefore relates to a pharmaceutical composition or a nutraceutical composition or a supplement product for use in a preventive treatment of polycystic ovary syndrome and/or the metabolic disorders deriving from or connected to polycystic ovary syndrome - said disorders being selected from among insulin resistance, dislipidaemia and hormonal alterations - and having the characteristics set forth in the appended claim.
  • the present invention relates to a pharmaceutical composition or a nutraceutical composition or a supplement product for use in a curative treatment for reducing and/or eliminating the symptoms of polycystic ovary syndrome and of the metabolic disorders deriving from or connected to polycystic ovary syndrome - said disorders being selected from among insulin resistance, dislipidaemia and hormonal alterations - and having the characteristics set forth in the appended claim.
  • formulation means a pharmaceutical composition or a medical device or a nutraceutical composition or a supplement product, in accordance with the present invention.
  • the formulation of the present invention comprises a mixture which comprises or, alternatively, consists of the compounds (i) and (iii) (binary formulation) in various proportions to each other, as described and/or claimed below.
  • Said mixture is formulated with excipients, technological additives, co-formulations, polar and/or semipolar polymeric matrices, carriers and stabilizers of pharmaceutical or food grade, which must be suitable for preparing a solid formulation, such as, for example, a formulation in powder or granular form, in tablets or in capsules; or a liquid solution; or a suspension in syrup.
  • the compound based on red yeast rice (Monascus purpureus) is titrated in monacolin and is in the form of a powder extract.
  • the formulation of the present invention which comprises said mixture comprising or, alternatively, consisting of the compounds (i) and (iii) (binary formulation) has valid application for use in: (a) a preventive treatment of polycystic ovary syndrome and the metabolic disorders deriving from or connected to polycystic ovary syndrome, having the characteristics as set forth in the appended claim, and/or
  • the formulation of the present invention comprises a mixture which comprises or, alternatively, consists of the compounds (i), (ii) and (iii) (ternary formulation) in various proportions to one another, as described and/or claimed below.
  • Said mixture is formulated with excipients, technological additives, co-formulations, polar and/or semipolar polymeric matrices, carriers and stabilizers of pharmaceutical or food grade, which must be suitable for preparing a solid formulation, such as, for example, a formulation in powder or granular form, in tablets or in capsules; or a liquid solution; or a suspension in syrup.
  • a lipoic acid compound or a derivative thereof, in a therapeutically effective amount is advantageously indicated for use in treatments (a) and (b), as specified below.
  • the compound based on red yeast rice is titrated in monacolin, for example it is titrated in monacolin at 3% or 5% or 10%, and is in the form of a powder extract.
  • preventive treatment for PCOS is tied to the fact that treating subjects with PCOS preventively can correct altered metabolic parameters which represent possible risk factors.
  • the combination of the three compounds (i), (ii) and (iii) together acts by improving the entry of glucose into cells, on the consequent reduction in insulin resistance and in reducing LDL cholesterol with a mechanism similar to that of statins.
  • monacolin K and myo-inositol are together capable of combating insulin resistance and the increase in cholesterol, as well as being capable of controlling lipid metabolism.
  • Inositol D-chiro inositol or myo-inositol
  • monacolin K D-chiro inositol or myo-inositol
  • monacolin K D-chiro inositol or myo-inositol
  • monacolin K D-chiro inositol or myo-inositol
  • Monacolin K, or a derivative thereof by reducing cholesterol, as a precursor of androgen synthesis, can improve the hyperandrogenous symptoms that affect women suffering from this syndrome.
  • lipoic acid which has a marked antioxidant action through the formation of glutathione, contributes positively.
  • the formulation comprises a mixture which comprises or, alternatively, consists of the compounds (i) and (iii) or, alternatively, the compounds (i), (ii) and (iii) in various proportions by weight to one another, as described and/or claimed below.
  • Said mixture is formulated with excipients, technological additives, co- formulations, polar and/or semipolar polymeric matrices, carriers and stabilizers of pharmaceutical or food grade, which must be suitable for preparing a solid formulation, such as, for example, a formulation in powder or granular form, in tablets or in capsules; or a liquid solution; or a suspension in syrup.
  • the pharmacologically acceptable excipients are selected from among thickening agents, such as, for example, xanthan gum and guar gum; edulcorants, such as, for example, sorbitol and sucralose; acidifiers, such as, for example citric acid; maltodextrins; anti-agglomerants, such as, for example silicon dioxide and magnesium stearate; antioxidants and flavourings.
  • the compound based on red yeast rice (Monascus purpureus) present in the binary or ternary formulation is obtained using methods and apparatus known to the person skilled in the art.
  • the compound based on red yeast rice ⁇ Monascus purpureus) is titrated in monacolin, for example it is titrated in monacolin at 3% or 5% or 10%, using methods and apparatus known to the person skilled in the art.
  • the D-chiro inositol compound (ii), present in the ternary formulation is also known as 1 D-chiro-inositol or D-(+)-chiro-inositol). Examples of D-chiro inositol derivatives or analogues are, for example, pinitol, e.g. D- pinitol, or D-chiro-inositol-prtosphate.
  • the lipoic acid compound present in the binary or ternary formulation contains alpha lipoic acid (thioctic acid 1077-28-7) in the R(+) configuration (R(+) enantiomer) or as a racemic R(+)/S(-) mixture.
  • the racemic mixture can contain the R(+) enantiomer in an amount comprised from 50% to 100%, relative to the lipoic acid present, and the S(-) enantiomer in an amount comprised from 50% to 0%, relative to the lipoic acid present.
  • the lipoic or alpha lipoic acid (iii) can be present in the binary or ternary formulation only in the form of the R(+) enantiomer, or as a 50/50, or 60/40, 70/30, 80/20 or 90/10 or 100/0 racemic R-(+)-alpha lipoic acid/S- (-)-alpha lipoic acid mixture.
  • the binary or ternary formulation of the present invention contains a 50/50 racemic R-(+)-alpha lipoic acid/S-(-)-alpha lipoic acid mixture.
  • the inositol can be present as myo-inositol in combination with the compound based on red yeast rice (Monascus purpureus) (i) and lipoic acid (iii).
  • the binary or ternary formulation of the present invention contains alpha lipoic acid (iii) in non-dissociated acid form or in the form of a pharmaceutically acceptable salt, for example a sodium salt.
  • Said excipients are present in an amount comprised from 50 to 20% by weight, relative to the total weight of the binary or ternary formulation, preferably from 40 to 20% by weight, relative to the total weight of the formulation.
  • the binary or ternary formulation of the present invention contains a compound based on red yeast rice (Monascus purpureus) titrated in monacolin at 3%.
  • red yeast rice Monascus purpureus
  • the red yeast rice is present in the formulation in a percentage by weight comprised from 3.3 to 16%, relative to the final weight of the binary or ternary formulation.
  • the binary or ternary formulation of the present invention contains a compound based on red yeast rice (Monascus purpureus) titrated at 10% in monacolin.
  • red yeast rice Monascus purpureus
  • the red yeast rice is present in the formulation in a percentage by weight comprised from 0.034 to 5%, relative to the final weight of the formulation.
  • Said D-chiro inositol or myo-inositol (ii) present in the binary or ternary formulation is present in an amount comprised from 30 to 60% by weight, relative to the total weight of the formulation, preferably from 40 to 50% by weight, relative to the total weight of the ternary formulation.
  • the ternary formulation comprises D- chiro inositol or myo-inositol in an amount comprised from 30 to 60% by weight, relative to the total weight of the formulation, preferably from 40 to 50% by weight, relative to the total weight of the ternary formulation.
  • Said lipoic acid (iii) present in the binary or ternary formulation is present in an amount comprised from 10 to 35% by weight, relative to the total weight of the formulation, preferably from 15 to 20% by weight, relative to the total weight of the formulation.
  • the binary or ternary formulation comprises alpha lipoic acid in the R(+) configuration (R(+) enantiomer) or as a racemic R(+)/S(-) mixture [where the racemic mixture contains the R(+) enantiomer in an amount comprised from 50% to 100%, relative to the lipoic acid present] in an amount comprised from 5 to 35% by weight, relative to the total weight of the formulation, preferably from 15 to 20% by weight, relative to the total weight of the binary or ternary formulation.
  • Said D-chiro inositol or myo-inositol compound is administered, via the ternary formulation of the present invention, at a concentration comprised from 0.5 to 5 grams/daily dose, preferably from 1 to 4 grams/daily dose.
  • 0.6 g of D-chiro inositol can be substituted with 1 g or else 2 g of myo-inositol.
  • the binary or ternary formulation of the present invention contains lipoic acid or alpha lipoic acid as the R(+) enantiomer, or as a 50/50 or 60/40, 70/30, 80/20 or 90/10 racemic mixture of R-(+)-alpha lipoic acid and S-(-)-alpha lipoic acid. Preferably, it is a 50/50 racemic mixture.
  • the lipoic or alpha lipoic acid (iii) is protected to avoid pyrosis in the mouth, esophagus, and stomach (gastric pyrosis) of the subject undergoing treatment. Furthermore, the lipoic or alpha lipoic acid is protected so as to release the lipoic acid in a gradual and controlled manner in the body of the subject treated with the formulation of the present invention.
  • the lipoic or alpha lipoic acid be released in the stomach within 30 minutes after administration and the remaining 50%, preferably 40%, be released in the gastrointestinal tract.
  • This release mode ensures a level of lipoic or alpha lipoic acid in blood serum for a period comprised from 0 to less than 4 hours.
  • lipoic acid makes it possible, on the one hand, to obtain levels of lipoic acid in blood serum that are comparable to those that would be obtained with a single injectable dose or with a formulation containing non-controlled release (non-protected) lipoic acid and, on the other hand, to maintain, over a period of time comprised from 0 to less than 4 hours, a level of lipoic acid in blood serum comprised from 20 to 80 ng/ml of plasma, preferably from 30 to 60 ng/ml of plasma, even more preferably from 45 to 55 ng/ml of plasma.
  • the lipoic or alpha lipoic acid (iii) present in the binary or ternary formulation can be in microencapsulated or coated form (protected form) so as to ensure a gradual and controlled release of lipoic acid in a time interval comprised from 0 to less than 4 hours.
  • the lipoic or alpha lipoic acid (iii) is present in said binary or ternary formulation not in a microencapsulated or coated form, but rather immersed in a matrix, for example of a polymeric nature, which in any case ensures a gradual and controlled release of the lipoic acid over time, in a time interval comprised from 0 to less than 4 hours (protected form).
  • a matrix for example of a polymeric nature, which in any case ensures a gradual and controlled release of the lipoic acid over time, in a time interval comprised from 0 to less than 4 hours (protected form).
  • the choice will depend on the type of pharmaceutical administration it is desired to achieve with the formulation of the present invention.
  • the binary or ternary formulation of the present invention is prepared for oral administration, for example in the form of a tablet, granules for tablets or granules for sachets.
  • 2 sachets per day or 2 tablets per day are administered, having a formulation as shown below:
  • a formulation in sachets can have the following composition:
  • red yeast rice ⁇ Monascus purpureus titrated in monacolin at 3%: 150 mg (equal to 4.5 mg of monacolin) D-chiro inositol: 600 mg, or else myo-inositol: 1000 mg
  • a formulation in tablets can have the following composition:
  • red yeast rice (Monascus purpureus) titrated in monacolin at 5%: 100 mg (equal to 5 mg of monacolin) D-chiro inositol: 600 mg, or else myo-inositol: 1000 mg
  • a formulation in sachets can have the following composition:
  • red yeast rice (Monascus purpureus) titrated in monacolin at 3%: 150 mg (equal to 4.5 mg of monacolin) D-chiro inositol: 600 mg, or else myo-inositol: 2000 mg
  • a formulation in tablets can have the following composition:
  • red yeast rice (Monascus purpureus) titrated in monacolin at 5%: 100 mg (equal to 5 mg of monacolin) D-chiro inositol: 600 mg, or else myo-inositol: 2000 mg
  • Lipoic acid 400 mg.
  • the lipoic or alpha lipoic acid that is present in said formulation in tablet form is mixed together with polymers, for example polymers selected from among microcrystalline cellulose, hydroxypropyl cellulose and hydroxypropyl methyl cellulose at a different molecular weight, and together with additives such as magnesium stearate, silicon dioxide, talc and dicalcium phosphate so as to achieve a coating that enables a controlled and gradual release of the lipoic acid.
  • the coating is made using apparatus and technologies known to a person skilled in the art, who is undoubtedly capable of selecting the most suitable polymers among those commercially available and the best operating conditions.
  • the tablet is externally coated with a thin layer of a coating or film (film coating) to provide a coated tablet that ensures a controlled and gradual release in a period of from 0 to 4 hours.
  • a coating or film film coating
  • a tablet comprising the binary or ternary formulation of the present invention is coated (protected tablet) with a thin layer of a coating or film (film coating) using one or more enteric coatings.
  • the coating or film has a pH-dependent solubility capable of enabling release according to the pH value in a given segment of the gastrointestinal tract, and of ensuring a rapid absorption of the lipoic acid.
  • the enteric coating is realized with coating compounds known to persons skilled in the art, for example hydroxypropyl cellulose, hydroxypropyl methylcellulose phthalate or polyvinyl acetate-phthalate.
  • the coating is applied using apparatus and technologies known to a person skilled in the art, who is undoubtedly capable of selecting the most suitable coating compounds among those commercially available.
  • a tablet it is desirable that at least 50%, preferably 60%, of lipoic or alpha lipoic acid be released in the stomach within 30 minutes after administration and the remaining 50%, preferably 40%, be released in the gastrointestinal tract in the following 3-4 hours.
  • This release mode ensures a level of lipoic or alpha lipoic acid in blood serum for a period comprised from 0 to less than 4 hours.
  • the tablet of the present invention can be said to have a 50/50 fast/slow controlled release.
  • the lipoic or alpha lipoic acid is present in said formulation in microencapsulated or coated form (encapsulated or coated lipoic acid) to provide a controlled and gradual release in a period of from 0 to 4 hours.
  • the lipoic acid is microencapsulated or coated (protected form) to a degree of at least 92%, preferably 96%, by weight.
  • the microencapsulation or coating is applied on the lipoic or alpha lipoic acid using apparatus and technologies known to a person skilled in the art, who is undoubtedly capable of selecting the most suitable coating compounds among those commercially available.
  • the lipoic or alpha lipoic acid is microencapsulated or coated with a combination of lacquer gum, triethylcitrate and talc.
  • granules for sachets it is desirable that at least 50%, preferably 60%, of lipoic or alpha lipoic acid be released in the stomach within 30 minutes after administration and the remaining 50%, preferably 40%, be released in the gastrointestinal tract in the following 3-4 hours.
  • This release mode ensures a level of lipoic or alpha lipoic acid in blood serum for a period comprised from 0 to less than 4 hours.
  • the granules for sachets of the present invention can be said to have a 50/50 fast/slow controlled release.
  • Said lipoic acid is administered, via the binary or ternary formulation of the present invention, at a concentration comprised from 100 to 1200 milligrams/daily dose, preferably from 300 to 800 milligrams/daily dose.
  • the lipoic acid or alpha lipoic acid is administered, via the binary or ternary formulation of the present invention, at a concentration comprised from 100 to 1200 milligrams/daily dose, preferably from 300 to 600 milligrams/daily dose, as the R(+) enantiomer or as a 50/50 or 60/40, 70/30, 80/20 or 90/10 racemic mixture of R-(+)-alpha lipoic acid and S-(-)-alpha lipoic acid.
  • the binary or ternary formulation of the present invention contains R-(+)-alpha lipoic acid or a 50/50 or 60/40, 70/30, 80/20 or 90/10 racemic mixture of R-(+)-alpha lipoic acid and S-(-)-alpha lipoic acid in a microencapsulated or coated form (protected form for granules for sachets) or coated using a polymeric matrix (protected form for tablets) in the form of a non- dissociated acid or a salt, preferably a sodium salt.
  • the formulation of the present invention both in the form of tablets and of granules per sachets, must have a controlled and gradual release over time to ensure a level of lipoic acid in blood serum from 0 to less than 4 hours.
  • the formulation has a concentration comprised from 100 to 1200 milligrams/daily dose, even more preferably from 300 to 800 milligrams/daily dose.
  • the formulation of the present invention in the form of granules for sachets or hard capsules, consists of red yeast rice ⁇ Monascus purpureus) titrated in monacolin, for example it is titrated in monacolin at 3% or 5% or 10%; D-chiro inositol and/or myo-inositol and R-(+)-alpha lipoic acid or a 50/50 racemic mixture, the latter in a microencapsulated or coated form (alpha lipoic acid protected for granules or for tablets) with a controlled and gradual release over a period of from 0 to less than 4 hours.
  • the binary or ternary formulation of the present invention comprises a qualitative/quantitative chemical composition having the characteristics as set forth above, in combination with one or more excipients or additives, as described above.
  • the formulation is prepared using apparatus and methods known to a person skilled in the art, who is undoubtedly capable of selecting the best operating conditions according to the type of formulation to be realized.
  • Said mixture will comprise red yeast rice (Monascus purpureus) titrated in monacolin, for example it is titrated in monacolin at 3% or 5% or 10%, D-chiro inositol and alpha lipoic acid and/or excipients and/or technological additives and/or co-formulants and/or polar and/or semipolar polymeric matrices and/or carriers and/or stabilizers according to the form of administration it is desired to prepare.
  • red yeast rice Monascus purpureus
  • Said mixture is prepared by adding the various components in sequence inside a container equipped with stirring means and heating means.
  • lipid matrices selected from among lipid matrices, carboxymethyl cellulose, carboxypropyl cellulose, hydroxypropyl cellulose and lacquer gum in order to formulate the composition in the desired form of administration.
  • a formulation is prepared in solid, granular or powder form, which is suitable for oral administration in the form of pills, tablets, softgels or orosoluble pharmaceutical forms.
  • the pharmaceutical composition or supplement product of the present invention shows a surprisingly positive effect in the treated subjects.
  • the pharmaceutical composition or the supplement product of the present invention can be administered once or twice a day for the purpose of administering to the subject undergoing treatment a daily dose as described above for each individual active component.
  • composition or supplement product of the present invention can be administered both as a background therapy and a periodic therapy.
  • ternary formulation of the present invention by administering, twice a day, a 3 g sachet (granular ternary formulation) comprising:
  • Coated lipoic acid 400 mg (weight of the lipoic acid prior to coating);
  • Stabilizers sorbitol, guar gum
  • Thickening agents xanthan gum, maltodextrins
  • Acidifier citric acid
  • Anti-agglomerant silicon dioxide
  • the ternary granular formulation of the present invention was tested in vivo on a group of 10 non-diabetic patients suffering from polycystic ovary syndrome (PCOS) in order to evaluate the effects of administering said ternary granular formulation on several specific parameters of the polycystic ovary syndrome.
  • the control group was made up of 10 healthy subjects.
  • the 10 treated subjects showed considerable improvements compared to the control group subjects who took a placebo.
  • glucose tolerance based on the HOMA and Quicki indexes
  • the Applicant also evaluated the administration of the ternary formulation on the lipid profile and degree of hirsutism in insulin resistant and hyperandrogenous women affected by PCOS.
  • the objective of the present study was to evaluate whether the administration of a ternary formulation of the present invention, in the form of a sachet containing a mixture consisting of: red yeast rice (Monascus purpureus) titrated at 5%: 150 mg; myo-inositol: 1000 mg and lipoic acid: 400 mg, was capable of reducing cholesterol levels and hyperandrogenous symptoms in insulin resistant women of fertile age with PCOS and an average degree of hirsutism (Ferriman-Gallwey > 8).

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Abstract

La présente invention porte sur une composition pharmaceutique, une composition nutraceutique, un dispositif médical ou un produit de complément destinés à être utilisés dans le traitement préventif et/ou curatif du syndrome des ovaires polykystiques (PCOS) et des troubles métaboliques dérivés du syndrome des ovaires polykystiques ou liés à celui-ci. De plus, la présente invention porte sur une composition pharmaceutique, une composition nutraceutique, un dispositif médical ou un produit de complément destinés à être utilisés dans la réduction du profil lipidique 3 et du degré d'hirsutisme chez des femmes souffrant d'insulinorésistance et d'hyperandrogénie atteintes du syndrome des ovaires polykystiques (PCOS).
EP14719069.8A 2013-03-07 2014-03-07 Composition destinée à être utilisée dans le traitement du syndrome des ovaires polykystiques Withdrawn EP2964207A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT000349A ITMI20130349A1 (it) 2013-03-07 2013-03-07 Composizione per uso nel trattamento della sindrome dell ovaio policistico
PCT/IB2014/000257 WO2014135956A1 (fr) 2013-03-07 2014-03-07 Composition destinée à être utilisée dans le traitement du syndrome des ovaires polykystiques

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EP2964207A1 true EP2964207A1 (fr) 2016-01-13

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EP14719069.8A Withdrawn EP2964207A1 (fr) 2013-03-07 2014-03-07 Composition destinée à être utilisée dans le traitement du syndrome des ovaires polykystiques

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CN113164396B (zh) 2018-11-26 2023-11-03 宝洁公司 含有硫辛酸的固体药物制剂及其用途
CN109517740B (zh) * 2018-12-05 2020-11-27 广东天益生物科技有限公司 一株紫色红曲霉诱变株和一种水溶性功能红曲及其制备方法和应用
IT201900025063A1 (it) * 2019-12-20 2021-06-20 Idi Integratori Dietetici Italiani S R L Composizioni gastroresistenti comprendi inositolo e/o estratto di gymnema sylvestre, loro composizioni farmaceutiche e nutraceutiche e loro uso
US11918018B2 (en) 2022-05-17 2024-03-05 Provation Life LLC Nutraceutical compositions and methods for dietary alleviation of polycystic ovary syndrome

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