IT8922583A1 - ASPARTATES-BASED PHARMACEUTICAL AND DIETARY COMPOSITIONS - Google Patents
ASPARTATES-BASED PHARMACEUTICAL AND DIETARY COMPOSITIONS Download PDFInfo
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- IT8922583A1 IT8922583A1 IT1989A22583A IT2258389A IT8922583A1 IT 8922583 A1 IT8922583 A1 IT 8922583A1 IT 1989A22583 A IT1989A22583 A IT 1989A22583A IT 2258389 A IT2258389 A IT 2258389A IT 8922583 A1 IT8922583 A1 IT 8922583A1
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- IT
- Italy
- Prior art keywords
- aspartate
- tetrahydrate
- magnesium
- hemihydrate
- potassium
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims description 8
- 235000005911 diet Nutrition 0.000 title claims description 4
- 230000000378 dietary effect Effects 0.000 title claims description 3
- 235000018102 proteins Nutrition 0.000 claims description 12
- 102000004169 proteins and genes Human genes 0.000 claims description 12
- 108090000623 proteins and genes Proteins 0.000 claims description 12
- YKZPPPNXRZHVGX-PXYKVGKMSA-L dipotassium;(2s)-2-aminobutanedioate;hydron;hydrate Chemical compound [H+].[H+].O.[K+].[K+].[O-]C(=O)[C@@H](N)CC([O-])=O.[O-]C(=O)[C@@H](N)CC([O-])=O YKZPPPNXRZHVGX-PXYKVGKMSA-L 0.000 claims description 11
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 10
- CKLJMWTZIZZHCS-REOHCLBHSA-L aspartate group Chemical class N[C@@H](CC(=O)[O-])C(=O)[O-] CKLJMWTZIZZHCS-REOHCLBHSA-L 0.000 claims description 10
- WEYUEHTZQZGAHE-UHFFFAOYSA-N 3-(1,3-dioxolan-2-ylmethoxy)benzaldehyde Chemical compound O=CC1=CC=CC(OCC2OCCO2)=C1 WEYUEHTZQZGAHE-UHFFFAOYSA-N 0.000 claims description 8
- 235000015872 dietary supplement Nutrition 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 235000003704 aspartic acid Nutrition 0.000 claims description 7
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims description 7
- 230000015556 catabolic process Effects 0.000 claims description 7
- 229940068988 potassium aspartate Drugs 0.000 claims description 7
- 229910052751 metal Inorganic materials 0.000 claims description 6
- 239000002184 metal Substances 0.000 claims description 6
- 229960001983 magnesium aspartate Drugs 0.000 claims description 5
- CRSJYWPXKKSOCQ-CBAPHJFVSA-L magnesium;(2s)-2-aminobutanedioate;hydron;tetrahydrate Chemical compound O.O.O.O.[Mg+2].[O-]C(=O)[C@@H](N)CC(O)=O.[O-]C(=O)[C@@H](N)CC(O)=O CRSJYWPXKKSOCQ-CBAPHJFVSA-L 0.000 claims description 5
- CKLJMWTZIZZHCS-UHFFFAOYSA-N Aspartic acid Chemical compound OC(=O)C(N)CC(O)=O CKLJMWTZIZZHCS-UHFFFAOYSA-N 0.000 claims description 4
- 150000002739 metals Chemical class 0.000 claims description 4
- 150000007530 organic bases Chemical class 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 229940088594 vitamin Drugs 0.000 claims description 4
- 229930003231 vitamin Natural products 0.000 claims description 4
- 235000013343 vitamin Nutrition 0.000 claims description 4
- 239000011782 vitamin Substances 0.000 claims description 4
- 235000014633 carbohydrates Nutrition 0.000 claims description 3
- 150000001720 carbohydrates Chemical class 0.000 claims description 3
- 150000001860 citric acid derivatives Chemical class 0.000 claims description 3
- DTGRQRFFKHYRJG-UHFFFAOYSA-N magnesium tetrahydrate Chemical compound O.O.O.O.[Mg+2] DTGRQRFFKHYRJG-UHFFFAOYSA-N 0.000 claims description 3
- 229930091371 Fructose Natural products 0.000 claims description 2
- 239000005715 Fructose Substances 0.000 claims description 2
- RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 claims description 2
- FNAQSUUGMSOBHW-UHFFFAOYSA-H calcium citrate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O FNAQSUUGMSOBHW-UHFFFAOYSA-H 0.000 claims description 2
- 239000001354 calcium citrate Substances 0.000 claims description 2
- 230000004963 pathophysiological condition Effects 0.000 claims description 2
- 230000004962 physiological condition Effects 0.000 claims description 2
- 239000001509 sodium citrate Substances 0.000 claims description 2
- 150000004685 tetrahydrates Chemical class 0.000 claims description 2
- 239000004480 active ingredient Substances 0.000 claims 4
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- QYSXJUFSXHHAJI-YRZJJWOYSA-N vitamin D3 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-YRZJJWOYSA-N 0.000 claims 2
- 235000005282 vitamin D3 Nutrition 0.000 claims 2
- 239000011647 vitamin D3 Substances 0.000 claims 2
- 229940021056 vitamin d3 Drugs 0.000 claims 2
- 239000005913 Maltodextrin Substances 0.000 claims 1
- 229920002774 Maltodextrin Polymers 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000002650 habitual effect Effects 0.000 claims 1
- 244000144980 herd Species 0.000 claims 1
- 229940035034 maltodextrin Drugs 0.000 claims 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims 1
- 235000013337 tricalcium citrate Nutrition 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 16
- 229910052700 potassium Inorganic materials 0.000 description 14
- 239000011777 magnesium Substances 0.000 description 12
- 239000011591 potassium Substances 0.000 description 12
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 11
- 229910052749 magnesium Inorganic materials 0.000 description 11
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 10
- 229940091250 magnesium supplement Drugs 0.000 description 9
- 229910052757 nitrogen Inorganic materials 0.000 description 8
- 206010022998 Irritability Diseases 0.000 description 7
- 230000000694 effects Effects 0.000 description 7
- 229940009098 aspartate Drugs 0.000 description 6
- -1 magnesium aspartates Chemical class 0.000 description 6
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 5
- 229940109239 creatinine Drugs 0.000 description 5
- 230000002035 prolonged effect Effects 0.000 description 5
- 230000001225 therapeutic effect Effects 0.000 description 5
- 239000003795 chemical substances by application Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 230000000144 pharmacologic effect Effects 0.000 description 3
- 230000009467 reduction Effects 0.000 description 3
- 230000036325 urinary excretion Effects 0.000 description 3
- KPGXRSRHYNQIFN-UHFFFAOYSA-N 2-oxoglutaric acid Chemical compound OC(=O)CCC(=O)C(O)=O KPGXRSRHYNQIFN-UHFFFAOYSA-N 0.000 description 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 2
- 244000118350 Andrographis paniculata Species 0.000 description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- 208000007976 Ketosis Diseases 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- PNNCWTXUWKENPE-UHFFFAOYSA-N [N].NC(N)=O Chemical compound [N].NC(N)=O PNNCWTXUWKENPE-UHFFFAOYSA-N 0.000 description 2
- XKMRRTOUMJRJIA-UHFFFAOYSA-N ammonia nh3 Chemical compound N.N XKMRRTOUMJRJIA-UHFFFAOYSA-N 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 230000029142 excretion Effects 0.000 description 2
- 208000028867 ischemia Diseases 0.000 description 2
- 230000004140 ketosis Effects 0.000 description 2
- PFGPOPYOCNOUMS-KXAAMTCKSA-J magnesium dipotassium (2S)-2-aminobutanedioate (3S)-3-amino-4-hydroxy-4-oxobutanoate pentahydrate Chemical compound O.O.O.O.O.[Mg++].[K+].[K+].N[C@@H](CC([O-])=O)C(O)=O.N[C@@H](CC([O-])=O)C(O)=O.N[C@@H](CC([O-])=O)C([O-])=O PFGPOPYOCNOUMS-KXAAMTCKSA-J 0.000 description 2
- 230000035790 physiological processes and functions Effects 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 208000010444 Acidosis Diseases 0.000 description 1
- 208000002874 Acne Vulgaris Diseases 0.000 description 1
- 239000004475 Arginine Substances 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 206010014418 Electrolyte imbalance Diseases 0.000 description 1
- 208000019025 Hypokalemia Diseases 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 206010039792 Seborrhoea Diseases 0.000 description 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000007950 acidosis Effects 0.000 description 1
- 208000026545 acidosis disease Diseases 0.000 description 1
- 206010000496 acne Diseases 0.000 description 1
- 238000007792 addition Methods 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- HWXBTNAVRSUOJR-UHFFFAOYSA-N alpha-hydroxyglutaric acid Natural products OC(=O)C(O)CCC(O)=O HWXBTNAVRSUOJR-UHFFFAOYSA-N 0.000 description 1
- 229940009533 alpha-ketoglutaric acid Drugs 0.000 description 1
- 229910021529 ammonia Inorganic materials 0.000 description 1
- 229940124325 anabolic agent Drugs 0.000 description 1
- 230000001195 anabolic effect Effects 0.000 description 1
- 230000001548 androgenic effect Effects 0.000 description 1
- 208000022531 anorexia Diseases 0.000 description 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 230000000386 athletic effect Effects 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 235000011001 calcium citrates Nutrition 0.000 description 1
- 239000004202 carbamide Substances 0.000 description 1
- 230000000747 cardiac effect Effects 0.000 description 1
- 231100001012 cardiac lesion Toxicity 0.000 description 1
- 231100000457 cardiotoxic Toxicity 0.000 description 1
- 230000001451 cardiotoxic effect Effects 0.000 description 1
- 150000001768 cations Chemical class 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000008645 cold stress Effects 0.000 description 1
- 206010061428 decreased appetite Diseases 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000007812 deficiency Effects 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
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- 230000002526 effect on cardiovascular system Effects 0.000 description 1
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- 239000005556 hormone Substances 0.000 description 1
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- 230000003834 intracellular effect Effects 0.000 description 1
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- 208000010125 myocardial infarction Diseases 0.000 description 1
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- 239000001301 oxygen Substances 0.000 description 1
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- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 235000021317 phosphate Nutrition 0.000 description 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 208000024896 potassium deficiency disease Diseases 0.000 description 1
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- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
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- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
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Description
DESCRIZIONE DELL'INVENZIONE DESCRIPTION OF THE INVENTION
La presente invenzione ha per oggetto oonposizicni farmaceutiche e dietetiche per stati fisiopatologici o fisiologici in cui si manifesta un aumento del catabolismo proteico, quali il digiuno prolungato terapeutico, dieta dimagrante, l'anoressia, le malattie defedanti croniche, gli intensi allenamenti sportivi, l'esercizio fisico prolungato, specie di soggetti poco allenati,e simili.Le oonposizicni secondo l'invenzione sono caratterizzate dal fatto di contenere acido aspertico o suoi sali con metalli o basi organiche farmaceuticamente e/o dieteticamente accettabili, di preferenza un'associazione di aspartato di potassio e di aspartato di magnesio. The present invention relates to pharmaceutical and dietetic onposizicni for physiopathological or physiological states in which an increase in protein catabolism occurs, such as prolonged therapeutic fasting, weight loss diet, anorexia, chronic defying diseases, intense sports training, prolonged physical exercise, especially of poorly trained subjects, and the like. The onpositions according to the invention are characterized by the fact that they contain aspertic acid or its salts with pharmaceutically and / or dietetically acceptable metals or organic bases, preferably an association of aspartate of potassium and magnesium aspartate.
In particolare, l'invenzione riguarda composizioni farmaceutiche atte al trattamento degli stati teste citati,contenenti come principio attivo un'associazione di D,L oppure DL-aspartato di potassio emidrato e di D,L oppure DL-aspartato di magnesio tetraidrato in rapporti ponderali superiori a 2,5:1, preferibilmente in rapporti ponderali compresi fra 3,5:1 e 5,5:1,quando utilizzata come prodotto farmaceutico e in rapporti ponderali reciproci compresi fra 4:1 e 1:2, di preferenza fra 2:1 e 1:1,25 quando utilizzata come integratore dietetico. Beninteso, formano oggetto dell'invenzione anche composizioni contenenti aspartati di potassio e magnesio diversi dall'emidrato e, rispettivamente,dal tetraidrato,oppure aspartati di altri cationi,che siano tra loro in rapporti ponderali equivalenti a quelli teste citati. In particular, the invention relates to pharmaceutical compositions suitable for the treatment of the aforementioned states, containing as the active principle an association of D, L or DL-potassium aspartate hemihydrate and D, L or DL-aspartate of magnesium tetrahydrate in weight ratios higher than 2.5: 1, preferably in weight ratios ranging from 3.5: 1 to 5.5: 1, when used as a pharmaceutical product and in reciprocal weight ratios ranging from 4: 1 to 1: 2, preferably between 2 : 1 and 1: 1.25 when used as a dietary supplement. Of course, compositions containing potassium and magnesium aspartates other than hemihydrate and, respectively, tetrahydrate, or aspartates of other cations, which are in weight ratios equivalent to those mentioned above, also form the subject of the invention.
E' noto da tarpo l'impiego terapeutico di associazioni di aspartato di potassio e di aspartato di magnesio in tutti gli stati di carenza extracellulare e intracellulare di potassio e di magnesio. The therapeutic use of combinations of potassium aspartate and magnesium aspartate in all states of extracellular and intracellular deficiency of potassium and magnesium is known from tarpo.
L'anpia letteratura farmacologica relativa all'argomento pone in rilievo questo aspetto degli aspartati di K e Mg (cfr. per esempio Arzneimittel-Forsch. 18, 342-47; 347-50 (1968); 18, 1328-29 (1968) Med. Welt n?20, 1177-80 (1969); Therapeut. Arkh. 46, 84-88 (1974), e sottolinea altri effetti della associazione in oggetto, quali la riduzione dell'aggregazione piastrinica (Aqressologie 9, 591-96 (1968)), la funzione preservante del rene prima del trapianto (Arzeimittel-Forsch. 24, 1286-88 (1974)), la prevenzione della disintegrazione cellulare attraverso il rallentamento della timolisi e delle linfolisi (Arzneimittel-Forsch.16, 559-65 (1966)), la protezione dell'intossicazione da ammoniaca (Acta Physiol. Acad.Sci.Hung.37,416 (1970))e dallo stress da freddo (Arzeimittel-Forsch.15,88-90 (1965), e l'aumento della circolazione coronarica e periferica (Arzeneimittel-Forsch. 17, 502-05 (1967)), la conservazione dei fosfati ad alta energia durante l?ischemia (Arzeimittel-Forsch. 22, 909-12 (1972)), la riduzione delle lesioni cardiache da cardiotossici (Arzeimittel-Forsch. 19, 660-63 (1969); 25, 760-65 (1975); 25, 918-23 (1975);Arch. Parmakol.Exp.Pathol.260,124-25 (1968). The long pharmacological literature on the subject highlights this aspect of K and Mg aspartates (see for example Arzneimittel-Forsch. 18, 342-47; 347-50 (1968); 18, 1328-29 (1968) Med. Welt n? 20, 1177-80 (1969); Therapeut. Arkh. 46, 84-88 (1974), and underlines other effects of the association in question, such as the reduction of platelet aggregation (Aqressologie 9, 591-96 (1968)), the preservative function of the kidney before transplantation (Arzeimittel-Forsch. 24, 1286-88 (1974)), the prevention of cell disintegration through the slowing of thymolysis and lympholysis (Arzneimittel-Forsch. 16, 559- 65 (1966)), the protection of ammonia intoxication (Acta Physiol. Acad.Sci.Hung.37,416 (1970)) and cold stress (Arzeimittel-Forsch.15,88-90 (1965), and the increase in coronary and peripheral circulation (Arzeneimittel-Forsch. 17, 502-05 (1967)), conservation of high-energy phosphates during ischemia (Arzeimittel-Forsch. 22, 909-12 (197 2)), the reduction of cardiotoxic cardiac lesions (Arzeimittel-Forsch. 19, 660-63 (1969); 25, 760-65 (1975); 25, 918-23 (1975); Arch. Parmakol.Exp.Pathol.260,124-25 (1968).
Benefici effetti degli aspartati di K e Mg nel trattamento clinico delle arritmie cardiache e degli infarti sono altres? citati in Muench. Med.Wscr.110, 224-227 (1968); Med.Welt n? 44, 1768-71 (1971); n? 33-34, 1790-97 (1968); n? 35, 1848-52 (1964);n? 50, 2124-26 (1974); n? 38, 2236-43 (1967);n? 20, 739-42 (1972); Therapiewoche 15, 405-10 (1965);Wien. Med.Wschr. 117, 885-89 (1967); Med. Monatsschr. 25, 267-69 (197.1);e altrove.Ancora, ? noto l'impiego degli aspartati in questione per deprimere 11iperantnoniemia negli epatopazienti (Ther. Gegenwart 109, 1175, 1178, 80, 1182-83 (1970);Gastroenterology 56, 1223 (1969)). Beneficial effects of K and Mg aspartates in the clinical treatment of cardiac arrhythmias and heart attacks are also? mentioned in Muench. Med.Wscr. 110, 224-227 (1968); Med.Welt n? 44, 1768-71 (1971); n? 33-34, 1790-97 (1968); n? 35, 1848-52 (1964); no? 50, 2124-26 (1974); n? 38, 2236-43 (1967); n? 20, 739-42 (1972); Therapiewoche 15, 405-10 (1965); Wien. Med.Wschr. 117, 885-89 (1967); Med. Monatsschr. 25, 267-69 (197.1); and elsewhere. Again,? the use of the aspartates in question to depress hyperantnemia in hepatopatients is known (Ther. Gegenwart 109, 1175, 1178, 80, 1182-83 (1970); Gastroenterology 56, 1223 (1969)).
Complessivamente le propriet? farmacologiche sinora note dell'associazione degli aspartati di potassio e di magnesio si possono cos? riassumere: Overall the properties? so far known pharmacological of the association of potassium and magnesium aspartates can be cos? to summarise:
a) aumento del contenuto di potassio tissutale e capacit? di correggere l'ipopotassiemia; a) increase in tissue potassium content and capacity? to correct hypokalemia;
b) diminuzione del fabbisogno cardiaco di ossigeno in contrasto con gli effetti dell'ischemia; b) decrease in cardiac oxygen requirement in contrast with the effects of ischemia;
c) diminuzione dell'amnoniemia negli epatopazienti; c) decrease in amnonemia in hepatopatients;
d)diminuzione dell'acido alfa-chetoglutarico nei soggetti diabetici. d) decrease of alpha-ketoglutaric acid in diabetic subjects.
Le associazioni dei due aspartati sinora utilizzate contenevano quantit? equiponderali di aspartato potassico emidrato e di aspartato di magnesio tetraidrato; le dosi giornaliere previste per l?adulto erano di 1,8 g complessivi,pari quindi a 0,9 g di K-aspartato. 1/2 H20 e 0,9 g di Mg-aspartato.4 H2O. The associations of the two aspartates used up to now contained quantities? equiponderal of potassium aspartate hemihydrate and magnesium aspartate tetrahydrate; the daily doses foreseen for the adult were 1.8 g in total, therefore equal to 0.9 g of K-aspartate. 1/2 H20 and 0.9 g of Mg-aspartate. 4 H2O.
Si ? ora inaspettatamente trovato che in condizioni di accelerata degradazione proteica - quale si osserva in varie condizioni fisiologiche e fisiopatologiche, e che trova la sua pi? chiara esemplificazione nel digiuno prolungato - la souministrazione di acido aspartico (sia esso nella forma D,L oppure DL) o di suoi sali coi metalli farmaceuticamente accettabili (per esempio sodio, potassio, magnesio, calcio) o con basi organiche farmaceuticamente e/o dieteticamente accett?bili (per esempio arginine, lisina, omitina, etanolamrvLna,ecc.),e in particolare dell'associazione degli aspartati di potassio e magnesio in determinati rapporti, e a dosi elevate,? in grado di contrastare efficacemente il catabolismo proteico, com'? dimostrato dalla netta diminuzione dell'escrezione urinaria di ammonio e di urea rispetto ai valori determinabili in assenza di detta associazione.Si ? inoltre trovato che la nuova associazione esercita una interessante attivit? antichetogena, riducendo in misura rilevante la concentrazione ematica di acido ?-idrossibutirrico. Yup ? now unexpectedly found that in conditions of accelerated protein degradation - which is observed in various physiological and pathophysiological conditions, and which finds its pi? clear example in prolonged fasting - the subtraction of aspartic acid (be it in the D, L or DL form) or its salts with pharmaceutically acceptable metals (for example sodium, potassium, magnesium, calcium) or with pharmaceutically and / or dietetically organic bases acceptable (for example arginine, lysine, omithine, ethanolamrvLna, etc.), and in particular of the association of potassium and magnesium aspartates in certain ratios, and at high doses ,? able to effectively counteract protein catabolism, how? demonstrated by the net decrease in urinary excretion of ammonium and urea compared to the values that can be determined in the absence of this association. also found that the new association carries out an interesting activity? antichetogenic, significantly reducing the blood concentration of? -hydroxybutyric acid.
In particolare si ? travato che tali attivit? sono particolarmente accentuate allorch? si impiegano associazioni dei due aspartati nelle quali il rapporto ponderale aspartato di potassio emidrato: aspartato di magnesio tetraidrato ? compreso nei valori sopra citati. In particular yes? found that such activities? are particularly accentuated when? combinations of the two aspartates are used in which the weight ratio of potassium aspartate hemihydrate: magnesium aspartate tetrahydrate? included in the values mentioned above.
Secondo l'invenzione, inoltre, la dose efficace di associazione ? nettamente superiore a quelle precedentemente usate. I risultati pi? favorevoli si ottengono, dal punto di vista farmacologico, con dosi giornaliere (per l'adulto) conprese fra 5 e 30 g pi? favorevolmente 12-18 g di aspartato potassico emidrato e 3-4,5 g di aspartato di magnesio tetraidrato, quantunque si possano raggiungere buoni risultati anche sonministrando dosi equivalenti (corrispondenti cio? a circa 10-16 g di acido aspartico) di uno o pi? aspartati farmaceuticamente accettabili o, al limite, di acido aspartico. In altre parole, gli effetti sorprendentemente constatati appaiono dovuti a dosi elevate di ione aspartato, in qualunque forma esso si trovi. Tuttavia, cerne gi? posto in rilievo, si ? trovato particolarmente conveniente l'associazione di aspartati di potassio e di magnesio nei rapporti sopra citati. Furthermore, according to the invention, the effective dose of association? clearly superior to those previously used. The results more? favorable are obtained, from the pharmacological point of view, with daily doses (for the adult) with between 5 and 30 g more? favorably 12-18 g of potassium aspartate hemihydrate and 3-4.5 g of magnesium aspartate tetrahydrate, although good results can also be achieved by administering equivalent doses (corresponding to about 10-16 g of aspartic acid) of one or more ? pharmaceutically acceptable aspartates or, at least, aspartic acid. In other words, the surprisingly observed effects appear to be due to high doses of aspartate ion, in whatever form it is found. However, there are already emphasized, yes? the association of potassium and magnesium aspartates in the aforementioned ratios was found to be particularly convenient.
La capacit? manifestata da un'associazione di aspartati di potassio e magnesio nel contrastare efficacemente, e a livello clinicamente rilevante, la perdita di azoto (ammonico e areico) durante il digiuno totale,? stata dimostrata da sperimentazioni condotte su pazienti obesi. L'esempio che segue,non limitativo, illustra ulteriormente l'invenzione. The capacity manifested by an association of potassium aspartates and magnesium in effectively counteracting, and at a clinically relevant level, the loss of nitrogen (ammonium and areic) during total fasting ,? has been demonstrated in trials conducted on obese patients. The following non-limiting example further illustrates the invention.
ESEMPIO EXAMPLE
In 15 soggetti obesi sottoposti a digiuno, in assenza di scrministrazione orale di aspartato di potassio e magnesio, l'escrezione urinaria media giornaliera di azoto nel corso della seconda settimana di digiuno ? risultata di 3,5 ?0,4 (m?SE)g/g di creatinina per ci? che riguarda l'azoto ammoniacale e di 2,3 ? 0,2 g/g di creatinina per ci? che concerne l'azoto ureico. I corrispondenti valori ottenuti in un gruppo di altrettanti soggetti sottoposti a digiuno terapeutico, con saministrazione quotidiana orale di aspartato di potassio e di magnesio (in ragione di 15 g di DL-aspartato di potassio emiidrato e 3,6 g di DL-aspartato di magnesio tetraidrato) sono risultati: 1,7 ? 0,2 per ci? che riguarda l'azoto ammoniacale (P 0,001)e 1,5 per ci? che riguarda l'azoto ureico (P 0,005). In 15 obese subjects undergoing fasting, in the absence of oral excretion of potassium and magnesium aspartate, the average daily urinary excretion of nitrogen during the second week of fasting? result of 3.5? 0.4 (m? SE) g / g of creatinine for that? what about ammonia nitrogen and 2.3? 0.2 g / g of creatinine for that? concerning urea nitrogen. The corresponding values obtained in a group of as many subjects subjected to therapeutic fasting, with daily oral administration of potassium aspartate and magnesium (in the ratio of 15 g of DL-potassium aspartate hemihydrate and 3.6 g of DL-magnesium aspartate tetrahydrate) were found to be: 1.7? 0.2 for that? which concerns ammoniacal nitrogen (P 0.001) and 1.5 for that? concerning urea nitrogen (P 0.005).
La riduzione dell'escrezione giornaliera urinaria di azoto da 6 g/g di creatinina a 3,2 g/g di creatinina corrisponde ad un risparmio netto di 2,8 g/g di creatinina di azoto e quindi (2,8 N/g creat x 1,08 g creat/die)corrisponde al risparmio quotidiano di 3,02 g di azoto.Visto che 1 g di azoto corrisponde a 6,25 di proteine, tale risparmio pu? venir quantizzato in (3,02 g x 6,25) circa 18,9 g di proteine e quindi in circa (18,9 g proteine x 5) 95 g di massa magra al giorno. In un periodo terapeutico di 14 giorni ci? corrisponde a un risparmio netto di 1323 g di massa magra. The reduction of the daily urinary excretion of nitrogen from 6 g / g of creatinine to 3.2 g / g of creatinine corresponds to a net saving of 2.8 g / g of nitrogen creatinine and therefore (2.8 N / g creat x 1.08 g creat / day) corresponds to the daily saving of 3.02 g of nitrogen. Since 1 g of nitrogen corresponds to 6.25 of proteins, this saving can? be quantified in (3.02 g x 6.25) about 18.9 g of protein and then in about (18.9 g protein x 5) 95 g of lean mass per day. In a therapeutic period of 14 days there? corresponds to a net saving of 1323 g of lean mass.
La tollerabilit? dell'aspartato di potassio e magnesio secondo l'invenzione alle dosi impiegate si ? rivelata ottima. In nessun caso si sono dimostrati sintomi o segni riferibili alla somministrazione del prodotto n? si sono evidenziate anomalie dei comuni parametri di laboratorio. Alle dosi impiegate, inoltre, non si ? manifestato l'effetto lassativo del magnesio. Si ? constatato, per contro, un interessante effetto antichetogeno, evidenziato dalla diminuita concentrazione ematica di acido ?-idrossibutirrico. Tolerability of the potassium and magnesium aspartate according to the invention at the doses used yes? turned out to be excellent. In no case were symptoms or signs related to the administration of product n? anomalies of common laboratory parameters were highlighted. Furthermore, at the doses used, don't you? manifested the laxative effect of magnesium. Yup ? on the other hand, an interesting antichetogenic effect was noted, highlighted by the decreased blood concentration of? -hydroxybutyric acid.
Tale constatazione ? particolarmente interessante poich? ? noto che l'esercizio fisico,specie se prolungato, comporta inevitabilmente una chetosi:quest'ultima e l'acidosi che l'accompagna sono tra i fattori che inducono una perdita proteica. Such a finding? particularly interesting since? ? I note that physical exercise, especially if prolonged, inevitably involves ketosis: the latter and the acidosis that accompanies it are among the factors that induce protein loss.
Si prepone pertanto che L'associazione di aspartati secondo l'invenzione venga utilizzata,ai fini della ritenzione di azoto, anche come integratore dietetico in soggetti che si sottopongono ad allenamento o comunque a intenso sforzo muscolare,e che vanno quindi incontro a chetosi It is therefore proposed that the association of aspartates according to the invention be used, for the purposes of nitrogen retention, also as a dietary supplement in subjects who undergo training or in any case to intense muscular effort, and who therefore undergo ketosis
Gli integratori secondo l'invenzione sono infatti stati assunti,con ottimi risultati, da atleti sottoposti a sfoni particolarmente prolungati (sci di fondo, marcia, maratona,partite di calcio e di pallacanestro, atletica in generale). The supplements according to the invention have in fact been taken, with excellent results, by athletes subjected to particularly prolonged spells (cross-country skiing, walking, marathon, football and basketball matches, athletics in general).
Rispetto ai mezzi tradizionalmente usati allo stesso scopo, l'associazione secondo l'invenzione presenta i seguenti vantaggi: Compared to the means traditionally used for the same purpose, the association according to the invention has the following advantages:
a) il bicarbonato di sodio accoppiato al cloruro di potassio, usato da Hamaford (Am. J.Fhysiol. 243 (Endocrinol.Metab. 6)) nei soggetti obesi in digiuno terapeutico, riduce solamente l'escrezione di azoto ammoniacale e sovraccarica i pazienti della quota non necessaria di cloruro di sodio (come esplicitamente annesso dall'A. nella discussione del lavoro), con possibili conseguenze a livello cardiovascolare; a) sodium bicarbonate coupled with potassium chloride, used by Hamaford (Am. J.Fhysiol. 243 (Endocrinol.Metab. 6)) in obese subjects in therapeutic fasting, only reduces the excretion of ammonia nitrogen and overloads patients the unnecessary amount of sodium chloride (as explicitly annexed by the author in the discussion of the work), with possible consequences at the cardiovascular level;
b) il fruttosio contrasta gli effetti del digiuno ma apporta un considerevole quantitativo di calore (375 Cal/die)e non corregge lo squilibrio elettrolitico; b) fructose counteracts the effects of fasting but brings a considerable amount of heat (375 Cal / day) and does not correct the electrolyte imbalance;
c) gli anabolizzanti proteici di tipo steroideo sono derivati dagli ormoni maschili androgeni di cui mantengono, seppur ridotti, alcuni effetti indesider?bili (acne, seborrea, ?rsutismo); vengono inoltre attualmente proibiti nell'uso sportivo perch? considerati "doping". c) the steroid-type protein anabolics are derived from male androgenic hormones of which they maintain, although reduced, some undesirable effects (acne, seborrhea, rsutism); are also currently prohibited in sports use why? considered "doping".
La presente invenzione si riferisce anche tutti gli aspetti industrialmente applicabili connessi alla preparazione e all'impiego dell'associazione di aspartato di potassio e aspartato di magnesio come agente indicato negli stati fisiopatologici ad accresciuto catabolismo proteico owero come agente indicato negli stati fisiologici ad accresciuto catabol?SITO proteico (integratore dietetico). The present invention also refers to all the industrially applicable aspects connected to the preparation and use of the association of potassium aspartate and magnesium aspartate as an agent indicated in the pathophysiological states with increased protein catabolism or as an agent indicated in the physiological states with increased catabolism? Protein SITE (dietary supplement).
Pertanto, un aspetto essenziale dell*invenzione ? costituito da formulazioni farmaceutiche contenenti i due aspartati in rapporti tali da corrispondere ad almeno 2,5 parti in peso,preferibilmente da 3,5 a 5,5 parti in peso,e ancora pitipreferibilmente 4-4,30 parti in peso di aspartiato di potassio eraiidrato per 1 parte in peso di aspartato di magnesio tetraidrato. Tipiche formulazioni - non limitative - al riguardo sono bustine contenenti 5 g (eppure 7,5 g) di DL-aspartato di potassio emiidrato e 1,2 g (oppure, rispettivamente, 1,8 g) di DL-aspartato di magnesio tetraidrato. Un altro aspetto essenziale dell'invenzione ? costituito da formulazioni dietetiche (integratori dietetici)contenenti una quantit? in peso compresa tra 40 e 70%, di preferenza fra 45 e 60% in peso, di acido aspartico o suoi sali con metalli o basi organiche dieteticamente accettabili,preferibilmente di aspartato di K e aspartato di Mg, in combinazione con citrati di metalli o basi organiche dieteticamente accettabili,preferibilmente citrati di sodio e di calcio, ed inoltre carboidrati e vitamine. Therefore, an essential aspect of the invention? consisting of pharmaceutical formulations containing the two aspartates in ratios such as to correspond to at least 2.5 parts by weight, preferably from 3.5 to 5.5 parts by weight, and again preferably 4-4.30 parts by weight of potassium aspartate washyhydrate per 1 part by weight of magnesium aspartate tetrahydrate. Typical - non-limiting - formulations in this regard are sachets containing 5 g (yet 7.5 g) of DL-aspartate of potassium hemihydrate and 1.2 g (or, respectively, 1.8 g) of DL-aspartate of magnesium tetrahydrate. Another essential aspect of the invention? consisting of dietary formulations (dietary supplements) containing a quantity? by weight between 40 and 70%, preferably between 45 and 60% by weight, of aspartic acid or its salts with dietetically acceptable organic metals or bases, preferably of K aspartate and Mg aspartate, in combination with metal citrates or dietetically acceptable organic bases, preferably sodium and calcium citrates, as well as carbohydrates and vitamins.
Tipiche formulazioni sono bustine,sacchetti, compresse e cos? via contenenti o costituite dalle formulazioni sopra precisate, con eventuali aggiunti di aromatizzanti, edulcoranti, agenti di effervescenza e simili additivi ben noti all'esperto. Typical formulations are sachets, bags, tablets and so on. via containing or consisting of the formulations specified above, with possible additions of flavoring, sweeteners, effervescence agents and similar additives well known to those skilled in the art.
Un esempio non limitativo di integratore secondo l'invenzione ha la seguente composizione,riferita a 100 g complessivi: A non-limiting example of an integrator according to the invention has the following composition, referred to a total of 100 g:
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