ITRM20130237A1 - FORMULATION FOR ORAL ADMINISTRATION OF A COMBINATION OF FOOD SUPPLEMENTS USEFUL FOR ENJOY CORRECT CHOLESTEROL LEVELS - Google Patents
FORMULATION FOR ORAL ADMINISTRATION OF A COMBINATION OF FOOD SUPPLEMENTS USEFUL FOR ENJOY CORRECT CHOLESTEROL LEVELS Download PDFInfo
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- ITRM20130237A1 ITRM20130237A1 IT000237A ITRM20130237A ITRM20130237A1 IT RM20130237 A1 ITRM20130237 A1 IT RM20130237A1 IT 000237 A IT000237 A IT 000237A IT RM20130237 A ITRM20130237 A IT RM20130237A IT RM20130237 A1 ITRM20130237 A1 IT RM20130237A1
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- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 title claims description 24
- 235000015872 dietary supplement Nutrition 0.000 title claims description 18
- 239000000203 mixture Substances 0.000 title claims description 8
- 238000009472 formulation Methods 0.000 title claims description 6
- 230000000694 effects Effects 0.000 claims description 7
- 239000000284 extract Substances 0.000 claims description 7
- 229940068065 phytosterols Drugs 0.000 claims description 6
- 235000007189 Oryza longistaminata Nutrition 0.000 claims description 4
- 240000007594 Oryza sativa Species 0.000 claims description 4
- 235000007164 Oryza sativa Nutrition 0.000 claims description 4
- LGJMUZUPVCAVPU-UHFFFAOYSA-N beta-Sitostanol Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(C)CCC(CC)C(C)C)C1(C)CC2 LGJMUZUPVCAVPU-UHFFFAOYSA-N 0.000 claims description 4
- 239000008187 granular material Substances 0.000 claims description 4
- 229960001109 policosanol Drugs 0.000 claims description 4
- PCZOHLXUXFIOCF-UHFFFAOYSA-N Monacolin X Natural products C12C(OC(=O)C(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 PCZOHLXUXFIOCF-UHFFFAOYSA-N 0.000 claims description 3
- OILXMJHPFNGGTO-UHFFFAOYSA-N (22E)-(24xi)-24-methylcholesta-5,22-dien-3beta-ol Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(C)C=CC(C)C(C)C)C1(C)CC2 OILXMJHPFNGGTO-UHFFFAOYSA-N 0.000 claims description 2
- OQMZNAMGEHIHNN-UHFFFAOYSA-N 7-Dehydrostigmasterol Natural products C1C(O)CCC2(C)C(CCC3(C(C(C)C=CC(CC)C(C)C)CCC33)C)C3=CC=C21 OQMZNAMGEHIHNN-UHFFFAOYSA-N 0.000 claims description 2
- SGNBVLSWZMBQTH-FGAXOLDCSA-N Campesterol Natural products O[C@@H]1CC=2[C@@](C)([C@@H]3[C@H]([C@H]4[C@@](C)([C@H]([C@H](CC[C@H](C(C)C)C)C)CC4)CC3)CC=2)CC1 SGNBVLSWZMBQTH-FGAXOLDCSA-N 0.000 claims description 2
- ACTIUHUUMQJHFO-UHFFFAOYSA-N Coenzym Q10 Natural products COC1=C(OC)C(=O)C(CC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UHFFFAOYSA-N 0.000 claims description 2
- BTEISVKTSQLKST-UHFFFAOYSA-N Haliclonasterol Natural products CC(C=CC(C)C(C)(C)C)C1CCC2C3=CC=C4CC(O)CCC4(C)C3CCC12C BTEISVKTSQLKST-UHFFFAOYSA-N 0.000 claims description 2
- QNVSXXGDAPORNA-UHFFFAOYSA-N Resveratrol Natural products OC1=CC=CC(C=CC=2C=C(O)C(O)=CC=2)=C1 QNVSXXGDAPORNA-UHFFFAOYSA-N 0.000 claims description 2
- 240000001341 Reynoutria japonica Species 0.000 claims description 2
- 235000018167 Reynoutria japonica Nutrition 0.000 claims description 2
- LUKBXSAWLPMMSZ-OWOJBTEDSA-N Trans-resveratrol Chemical compound C1=CC(O)=CC=C1\C=C\C1=CC(O)=CC(O)=C1 LUKBXSAWLPMMSZ-OWOJBTEDSA-N 0.000 claims description 2
- HZYXFRGVBOPPNZ-UHFFFAOYSA-N UNPD88870 Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(C)=CCC(CC)C(C)C)C1(C)CC2 HZYXFRGVBOPPNZ-UHFFFAOYSA-N 0.000 claims description 2
- 229940076810 beta sitosterol Drugs 0.000 claims description 2
- NJKOMDUNNDKEAI-UHFFFAOYSA-N beta-sitosterol Natural products CCC(CCC(C)C1CCC2(C)C3CC=C4CC(O)CCC4C3CCC12C)C(C)C NJKOMDUNNDKEAI-UHFFFAOYSA-N 0.000 claims description 2
- 235000000431 campesterol Nutrition 0.000 claims description 2
- SGNBVLSWZMBQTH-PODYLUTMSA-N campesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CC[C@@H](C)C(C)C)[C@@]1(C)CC2 SGNBVLSWZMBQTH-PODYLUTMSA-N 0.000 claims description 2
- 235000017471 coenzyme Q10 Nutrition 0.000 claims description 2
- 229940110767 coenzyme Q10 Drugs 0.000 claims description 2
- ACTIUHUUMQJHFO-UPTCCGCDSA-N coenzyme Q10 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CC\C=C(/C)CCC=C(C)C)=C(C)C1=O ACTIUHUUMQJHFO-UPTCCGCDSA-N 0.000 claims description 2
- PCZOHLXUXFIOCF-BXMDZJJMSA-N lovastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 PCZOHLXUXFIOCF-BXMDZJJMSA-N 0.000 claims description 2
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims description 2
- 235000021283 resveratrol Nutrition 0.000 claims description 2
- 229940016667 resveratrol Drugs 0.000 claims description 2
- KZJWDPNRJALLNS-VJSFXXLFSA-N sitosterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CC[C@@H](CC)C(C)C)[C@@]1(C)CC2 KZJWDPNRJALLNS-VJSFXXLFSA-N 0.000 claims description 2
- 229950005143 sitosterol Drugs 0.000 claims description 2
- HCXVJBMSMIARIN-PHZDYDNGSA-N stigmasterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)/C=C/[C@@H](CC)C(C)C)[C@@]1(C)CC2 HCXVJBMSMIARIN-PHZDYDNGSA-N 0.000 claims description 2
- 229940032091 stigmasterol Drugs 0.000 claims description 2
- 235000016831 stigmasterol Nutrition 0.000 claims description 2
- BFDNMXAIBMJLBB-UHFFFAOYSA-N stigmasterol Natural products CCC(C=CC(C)C1CCCC2C3CC=C4CC(O)CCC4(C)C3CCC12C)C(C)C BFDNMXAIBMJLBB-UHFFFAOYSA-N 0.000 claims description 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 9
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 7
- 235000012000 cholesterol Nutrition 0.000 description 6
- 238000002560 therapeutic procedure Methods 0.000 description 5
- 230000002526 effect on cardiovascular system Effects 0.000 description 4
- CABVTRNMFUVUDM-VRHQGPGLSA-N (3S)-3-hydroxy-3-methylglutaryl-CoA Chemical compound O[C@@H]1[C@H](OP(O)(O)=O)[C@@H](COP(O)(=O)OP(O)(=O)OCC(C)(C)[C@@H](O)C(=O)NCCC(=O)NCCSC(=O)C[C@@](O)(CC(O)=O)C)O[C@H]1N1C2=NC=NC(N)=C2N=C1 CABVTRNMFUVUDM-VRHQGPGLSA-N 0.000 description 3
- 208000035150 Hypercholesterolemia Diseases 0.000 description 3
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- KJTLQQUUPVSXIM-ZCFIWIBFSA-N (R)-mevalonic acid Chemical compound OCC[C@](O)(C)CC(O)=O KJTLQQUUPVSXIM-ZCFIWIBFSA-N 0.000 description 2
- KJTLQQUUPVSXIM-UHFFFAOYSA-N DL-mevalonic acid Natural products OCCC(O)(C)CC(O)=O KJTLQQUUPVSXIM-UHFFFAOYSA-N 0.000 description 2
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
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- 208000032928 Dyslipidaemia Diseases 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 description 1
- 108090000895 Hydroxymethylglutaryl CoA Reductases Proteins 0.000 description 1
- 238000008214 LDL Cholesterol Methods 0.000 description 1
- 102000004316 Oxidoreductases Human genes 0.000 description 1
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- 230000007211 cardiovascular event Effects 0.000 description 1
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- 235000005911 diet Nutrition 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
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- 150000002148 esters Chemical class 0.000 description 1
- 229960000815 ezetimibe Drugs 0.000 description 1
- OLNTVTPDXPETLC-XPWALMASSA-N ezetimibe Chemical compound N1([C@@H]([C@H](C1=O)CC[C@H](O)C=1C=CC(F)=CC=1)C=1C=CC(O)=CC=1)C1=CC=C(F)C=C1 OLNTVTPDXPETLC-XPWALMASSA-N 0.000 description 1
- 239000003925 fat Substances 0.000 description 1
- 235000019197 fats Nutrition 0.000 description 1
- 229940125753 fibrate Drugs 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 235000012041 food component Nutrition 0.000 description 1
- 239000005417 food ingredient Substances 0.000 description 1
- 230000000260 hypercholesteremic effect Effects 0.000 description 1
- 230000031891 intestinal absorption Effects 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 229930185723 monacolin Natural products 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 229960003512 nicotinic acid Drugs 0.000 description 1
- 235000001968 nicotinic acid Nutrition 0.000 description 1
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- 239000000902 placebo Substances 0.000 description 1
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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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
-
- 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
- A61K31/05—Phenols
-
- 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
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds 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
-
- 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
-
- 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)
- A61K36/70—Polygonaceae (Buckwheat family), e.g. spineflower or dock
- A61K36/704—Polygonum, e.g. knotweed
Description
FORMULAZIONE PER SOMMINISTRAZIONE ORALE DI UNA COMBINAZIONE FORMULATION FOR ORAL ADMINISTRATION OF A COMBINATION
DI INTEGRATORI ALIMENTARI UTILE PER FAVORIRE CORRETTI LIVELLI DI OF FOOD SUPPLEMENTS USEFUL TO FAVOR CORRECT LEVELS OF
COLESTEROLO CHOLESTEROL
DESCRIZIONE DESCRIPTION
a) Campo della tecnica a cui il trovato fa riferimento a) Field of the art to which the invention refers
Il trovato fa riferimento al controllo dei valori di colesterolemia in tutte le condizioni in cui è indicato l’impiego di terapie alternative ai convenzionali prodotti farmaceutici ipolipemizzanti e in particolare alle statine. The invention refers to the control of cholesterol levels in all conditions in which the use of alternative therapies to conventional lipid-lowering pharmaceutical products and in particular to statins is indicated.
L’ipercolesterolemia è infatti condizione molto diffusa nella popolazione generale che rappresenta un rilevante fattore di rischio cardiovascolare per lo sviluppo della temibile aterosclerosi, malattia che ha come temibili complicanze l’infarto miocardico e l’ictus cerebrale. In fact, hypercholesterolemia is a very common condition in the general population which represents a significant cardiovascular risk factor for the development of the fearful atherosclerosis, a disease that has myocardial infarction and stroke as dreadful complications.
L’approccio terapeutico alia ipercolesterolemia è attualmente regolato da apposite linee-guida di diagnosi e terapia delle dislipidemie elaborate nel 2011 dalla Società Europea di Cardiologia {Reiner Z. et al. European Heart Journal 2011; 32: 1769-1818). The therapeutic approach to hypercholesterolemia is currently governed by specific guidelines for the diagnosis and therapy of dyslipidemias drawn up in 2011 by the European Society of Cardiology {Reiner Z. et al. European Heart Journal 2011; 32: 1769-1818).
Le linee-guida consentono ai medici di prescrivere farmaci ipolipemizzanti non indiscriminatamente ma solo quando il profilo di rischio cardiovascolare dei pazienti è particolarmente elevato. La terapia con statine è infatti raccomandata come parte della strategia complessiva di trattamento della popolazione adulta con rischio cardiovascolare globale assoluto (calcolato con la apposita carta europea SCORE del rischio cardiovascolare) del 10% o superiore di sviluppare malattie cardiovascolari entro 10 anni. In tutti gli altri casi, i medici devono prescrivere solo modifiche delle abitudini alimentari, aumentando il consumo di cibi poveri di grassi animali ed eventualmente ricorrendo a integratori alimentari per aumentare l'introito giornaliero di sostanze naturali che hanno un riconosciuto effetto ipocolesterolemizzante. The guidelines allow doctors to prescribe lipid-lowering drugs not indiscriminately but only when the cardiovascular risk profile of patients is particularly high. Statin therapy is in fact recommended as part of the overall treatment strategy of the adult population with absolute overall cardiovascular risk (calculated with the appropriate European Cardiovascular Risk Card SCORE) of 10% or greater of developing cardiovascular disease within 10 years. In all other cases, doctors must only prescribe changes in eating habits, increasing the consumption of foods low in animal fats and possibly resorting to food supplements to increase the daily intake of natural substances that have a recognized cholesterol-lowering effect.
Tra queste sostanze, le vigenti linee-guida della Società Europea di Cardiologia annoverano i fitosteroli, la soia, le fibre solubili, gli acidi grassi poliinsaturi n-3, il policosanolo e il riso rosso fermentato ( Reiner Z. et al. European Heart Journal 2011; 32: pagina 1787). Among these substances, the current guidelines of the European Society of Cardiology include phytosterols, soy, soluble fiber, polyunsaturated fatty acids n-3, policosanol and fermented red rice (Reiner Z. et al. European Heart Journal 2011; 32: page 1787).
Il ricorso a queste sostanze naturali con attività ipocolesterolemizzante viene poi raccomandato anche nei pazienti che hanno avuto un evento cardiovascolare e che quindi dovrebbero essere sottoposti a terapia cronica con farmaci ipolipemizzanti, e in particolare gli inibitori deH’HMG-CoA reduttasi, le cosiddette ‘statine’. Anche se le statine rappresentano ormai un presidio irrinunciabile in prevenzione secondaria, la loro somministrazione è sfortunatamente associata di frequente a reazioni avverse lievi o ad alterazioni di alcuni parametri di laboratorio che ne limitano la tollerabilità. Le indagini epidemiologiche dimostrano infatti che la terapia con statine viene interrotta dopo pochi mesi nella metà dei pazienti che presentano una bassa aderenza al trattamento. In questi casi, le linee guida vigenti raccomandano di ricorrere a soluzioni terapeutiche alternative, tra cui gli integratori naturali. The use of these natural substances with cholesterol-lowering activity is also recommended in patients who have had a cardiovascular event and who therefore should undergo chronic therapy with lipid-lowering drugs, and in particular the inhibitors of HMG-CoA reductase, the so-called 'statins. '. Although statins are now an indispensable aid in secondary prevention, their administration is unfortunately frequently associated with mild adverse reactions or alterations in some laboratory parameters that limit their tolerability. In fact, epidemiological investigations show that statin therapy is stopped after a few months in half of the patients who have low adherence to treatment. In these cases, current guidelines recommend resorting to alternative therapeutic solutions, including natural supplements.
b) Stato della tecnica preesistente b) Pre-existing state of the art
La prescrizione di integratori alimentari a base di piante e altri rimedi naturali si è notevolmente diffusa negli ultimi anni unitamente alle indispensabili modifiche allo stile di vita sotto controllo medico (Woolf KJ, et al. J Clin Hypertens 2011;13:829-835). Prescribing of plant-based dietary supplements and other natural remedies has spread considerably in recent years along with indispensable, medically supervised lifestyle changes (Woolf KJ, et al. J Clin Hypertens 2011; 13: 829-835).
L’elenco delle sostanze naturali che hanno dimostrato di possedere la proprietà di modulare i valori plasmatici di colesterolo è relativamente e comprende, come già indicato, i fitosteroli, la soia, le fibre solubili, gli acidi grassi poliinsaturi n-3, il poiicosanolo e il riso rosso fermentato. The list of natural substances that have been shown to have the property of modulating plasma cholesterol values is relatively and includes, as already indicated, phytosterols, soy, soluble fiber, n-3 polyunsaturated fatty acids, polychosanol and fermented red rice.
L’uso di integratori alimentari incontra sicuramente il favore dei pazienti ipercolesterolemici che sono usualmente riluttanti a iniziare un trattamento con statine e preferiscono in prima battuta valutare sistemi alternativi di controllo della colesterolemia. La prescrizione di integratori alimentari, tuttavia, è spesso considerata dai medici una soluzione terapeutica non risolutiva nella pratica clinica. La ragione è legata al fatto che tutte le ricerche scientifiche condotte hanno valutato l'efficacia di singoli composti mettendo in evidenza solo una modesta efficacia ipolipemizzante con conseguente registrazione di riduzioni minime dei livelli plasmatici di colesterolo. The use of food supplements certainly meets the favor of hypercholesterolemic patients who are usually reluctant to start a treatment with statins and prefer to first evaluate alternative cholesterol control systems. The prescription of dietary supplements, however, is often considered by doctors to be a non-decisive therapeutic solution in clinical practice. The reason is linked to the fact that all the scientific researches conducted have evaluated the efficacy of single compounds, highlighting only a modest lipid-lowering efficacy with consequent recording of minimal reductions in plasma cholesterol levels.
c) La soluzione proposta con ili nuovo ritrovato ai problemi posti dalle precedenti formulazioni e conseguenti effetti vantaggiosi attesi c) The solution proposed with the new invention to the problems posed by the previous formulations and consequent expected advantageous effects
Il nuovo ritrovato è stato ideato per ovviare alle limitazioni insite nella supplementazione a base di un solo ingrediente alimentare. Il nuovo trovato è infatti costituito da una formulazione basata sulla associazione di più integratori alimentari con comprovata azione ipocolesterolemizzante e rappresenta quindi un prodotto totalmente nuovo nel panorama italiano e internazionale. La soluzione proposta con il nuovo ritrovato, dunque, introduce per la prima volta il concetto dell’approccio multifattoriale al controllo dei livelli plasmatici di colesterolo con integratori alimentari. Questo approccio innovativo è in linea con quanto raccomandato dalle vigenti lineeguida scientifiche a proposito dei composti farmaceutici convenzionali. Secondo le linee-guida europee del 2011, infatti, è raccomandabile in tutti i casi in cui la monoterapia non risulti efficace o sia mal tollerata, ricorrere alla terapia di associazione, combinando statine e fibrati, statine e inibitori deN’assorbimento di colesterolo, statine e acido nicotinico. Pertanto è oggi scientificamente approvato il ricorso a sostanze ipolipemizzanti diverse con meccanismo di azione complementare piuttosto che a un unico principio ( Reìner Z. et al. European Heart Journal 2011; 32: pagina 1792). The new invention was designed to overcome the limitations inherent in supplementation based on a single food ingredient. The new invention is in fact constituted by a formulation based on the association of several food supplements with proven cholesterol-lowering action and therefore represents a totally new product in the Italian and international panorama. The solution proposed with the new invention, therefore, introduces for the first time the concept of the multifactorial approach to the control of plasma cholesterol levels with food supplements. This innovative approach is in line with what is recommended by current scientific guidelines regarding conventional pharmaceutical compounds. According to the European guidelines of 2011, in fact, it is recommended in all cases in which monotherapy is not effective or is poorly tolerated, to resort to combination therapy, combining statins and fibrates, statins and cholesterol absorption inhibitors, statins and nicotinic acid. Therefore, the use of different lipid-lowering substances with complementary mechanisms of action rather than a single principle is now scientifically approved (Reìner Z. et al. European Heart Journal 2011; 32: page 1792).
d) Breve descrizione del nuovo trovato d) Brief description of the new invention
Il nuovo trovato si caratterizza per una formulazione a base di una combinazione di integratori alimentari aventi effetto ipolipemizzante The new invention is characterized by a formulation based on a combination of food supplements having a lipid-lowering effect
Il ritrovato è composto dai seguenti tre integratori alimentari con documentata attività ipolipemizzante che si esplica attraverso differenti meccanismi di azione. The invention is composed of the following three food supplements with documented lipid-lowering activity that is expressed through different mechanisms of action.
in particolare, il nuovo trovato sarà composto da: in particular, the new invention will consist of:
- Monacolina (inibisce l’enzima 3-idrossi-3-metil-glutaril coenzima A ridottasi che consente la conversione epatica di 3-idrossi-3-metil-glutaril coenzima A in acido mevalonico, precursore del colesterolo) - Monacolin (inhibits the 3-hydroxy-3-methyl-glutaryl coenzyme A reduced enzyme which allows the hepatic conversion of 3-hydroxy-3-methyl-glutaryl coenzyme A into mevalonic acid, precursor of cholesterol)
- Fitosteroli (contrastano l'assorbimento a livello intestinale del colesterolo introdotto con la dieta alimentare) - Phytosterols (counteract the intestinal absorption of cholesterol introduced with the diet)
- Policosanolo (inibisce la sintesi dell’enzima FIMG-CoA reduttasi che è il substrato della conversione epatica di 3-idrossi-3-metil-glutaril coenzima A in acido mevalonico, precursore del colesterolo) - Policosanol (inhibits the synthesis of the FIMG-CoA reductase enzyme which is the substrate for the hepatic conversion of 3-hydroxy-3-methyl-glutaryl coenzyme A into mevalonic acid, precursor of cholesterol)
e) Descrizione dettagliata dei modo di attuazione del nuovo trovato e) Detailed description of the method of implementation of the new invention
In dettaglio, il nuovo trovato sarà rappresentato da capsule caratterizzate dal fatto di comprendere: In detail, the new invention will be represented by capsules characterized by the fact of comprising:
Monacolina K: 10 mg (pari a 200 mg di riso rosso fermentanto estratto secco titolato al 5%) Monacolin K: 10 mg (equal to 200 mg of fermenting red rice dry extract titrated at 5%)
Fitosteroli (esteri di beta-sitosterolo, campesterolo e stigma sterolo titolati al 75%): 300 mg Phytosterols (esters of beta-sitosterol, campesterol and stigma sterol titrated to 75%): 300 mg
Policosanoli (titolati al 90%): 12 mg Policosanols (titrated to 90%): 12 mg
Coenzima Q10: 20 mg Coenzyme Q10: 20 mg
Resveratrolo (Polygonum cuspidatum estratto secco titolato al 98%}: 26 mg Resveratrol (Polygonum cuspidatum dry extract titrated at 98%}: 26 mg
Il procedimento per la realizzazione del nuovo trovato comprenderà le seguenti fasi in successione tra loro: The process for the realization of the new invention will comprise the following phases in succession to each other:
- Miscelazione a secco degli estratti dei quattro prodotti componenti - Dry mixing of the extracts of the four component products
- Impasto a umido della miscela ottenuta - Wet mixing of the obtained mixture
- Granulazione a umido dell’impasto ottenuto - Wet granulation of the mixture obtained
- Essicazione e asciugatura dei granuli ottenuti - Drying and drying of the obtained granules
- Granulazione a secco dei granuli essicati - Dry granulation of dried granules
- Stabilizzazione dei granuli ottenuti. - Stabilization of the obtained granules.
f) Modalità in cui il nuovo preparato potrà essere utilizzato f) How the new preparation can be used
Il nuovo preparato sarà utilizzato dapprima in ambito scientifico e successivamente in ambito industriale. The new preparation will be used first in the scientific field and subsequently in the industrial field.
In una prima fase, il nuovo trovato sarà protagonista di uno studio scientifico multicentrico, randomizzato, a gruppi paralleli, controllato in cieco, dal titolo “Randomized comparison of thè CHOlesterol-lowering effects of nutraceuticaLs versus Ezetimibe in Statin-intolerant patientS", il cui acronimo è CHOLESS. li protocollo del trial, che sarà coordinato dall’Università Sapienza di Roma, è stato registrato presso la Food and Drug Administration ( ClinicalTnals.gov Identifìer: NCT01807078), Lo studio si propone di arruolare 200 pazienti con diagnosi di ipercolesterolemia che saranno randomizzati in due gruppi. Il primo gruppo sarà trattato con il nuovo trovato e il secondo gruppo riceverà placebo. Il trattamento durerà 90 giorni al termine del quale si valuterà quale percentuale di pazienti dei due gruppi avrà raggiunto una riduzione dei valori plasmatici di colesterolo totale e colesterolo LDL superiori al 10% dei valori iniziali pre-trattamento. In una seconda fase, è previsto l’uso del preparato in ambito industriale. Il nuovo trovato potrà essere commercializzato dalla rete distributiva degli integratori alimentari (parafarmacie, erboristerie e farmacie). In a first phase, the new invention will be the protagonist of a multicentre, randomized, parallel-group, blind-controlled scientific study entitled "Randomized comparison of the CHOlesterol-lowering effects of nutraceuticaLs versus Ezetimibe in Statin-intolerant patientS", whose acronym is CHOLESS.The trial protocol, which will be coordinated by the Sapienza University of Rome, was registered with the Food and Drug Administration (ClinicalTnals.gov Identifìer: NCT01807078), The study aims to enroll 200 patients diagnosed with hypercholesterolemia who will be randomized into two groups. The first group will be treated with the new invention and the second group will receive placebo. The treatment will last 90 days at the end of which it will be assessed which percentage of patients of the two groups will have achieved a reduction in plasma total cholesterol values and LDL cholesterol higher than 10% of the initial pre-treatment values or of the preparation in the industrial field. The new invention can be marketed by the distribution network of food supplements (parapharmacies, herbalists and pharmacies).
Claims (1)
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| IT000237A ITRM20130237A1 (en) | 2013-04-19 | 2013-04-19 | FORMULATION FOR ORAL ADMINISTRATION OF A COMBINATION OF FOOD SUPPLEMENTS USEFUL FOR ENJOY CORRECT CHOLESTEROL LEVELS |
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| IT000237A ITRM20130237A1 (en) | 2013-04-19 | 2013-04-19 | FORMULATION FOR ORAL ADMINISTRATION OF A COMBINATION OF FOOD SUPPLEMENTS USEFUL FOR ENJOY CORRECT CHOLESTEROL LEVELS |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070172468A1 (en) * | 2006-01-25 | 2007-07-26 | Reliv International Inc. | Dietary supplements for reducing cholesterol levels |
| US20110152221A1 (en) * | 2008-08-08 | 2011-06-23 | The Board Of Trustees Of The University Of Illinois | PAK1 Agonists and Methods of Use |
| US20110223250A1 (en) * | 2004-03-29 | 2011-09-15 | Wyeth Llc | Multi-vitamin and mineral nutritional supplements |
| WO2012137163A1 (en) * | 2011-04-08 | 2012-10-11 | Funcional Food Research S.R.L. | Flour-based functional food |
-
2013
- 2013-04-19 IT IT000237A patent/ITRM20130237A1/en unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110223250A1 (en) * | 2004-03-29 | 2011-09-15 | Wyeth Llc | Multi-vitamin and mineral nutritional supplements |
| US20070172468A1 (en) * | 2006-01-25 | 2007-07-26 | Reliv International Inc. | Dietary supplements for reducing cholesterol levels |
| US20110152221A1 (en) * | 2008-08-08 | 2011-06-23 | The Board Of Trustees Of The University Of Illinois | PAK1 Agonists and Methods of Use |
| WO2012137163A1 (en) * | 2011-04-08 | 2012-10-11 | Funcional Food Research S.R.L. | Flour-based functional food |
Non-Patent Citations (3)
| Title |
|---|
| ANONYMOUS: "Cho-Less - The Official Natura Health Products Blog", 22 January 2013 (2013-01-22), XP002720298, Retrieved from the Internet <URL:http://blog.naturahealthproducts.com/tag/cho-less/> [retrieved on 20140213] * |
| ANONYMOUS: "CHO-LESS_TERIN (90 Tabletten)", 5 February 2013 (2013-02-05), XP002720299, Retrieved from the Internet <URL:http://www.nahani.net/cho-less-terin-90-tabletten.html> [retrieved on 20140213] * |
| ANONYMOUS: "Cholesterol-lowering Effects of nutraceuticaLs Versus Ezetimibe in Statin-intolerant Patients", 6 March 2013 (2013-03-06), XP002720300, Retrieved from the Internet <URL:http://clinicaltrials.gov/show/NCT01807078> [retrieved on 20140213] * |
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