ES2528331A1 - Composición con efecto en la salud ósea y cardiovascular - Google Patents
Composición con efecto en la salud ósea y cardiovascular Download PDFInfo
- Publication number
- ES2528331A1 ES2528331A1 ES201331232A ES201331232A ES2528331A1 ES 2528331 A1 ES2528331 A1 ES 2528331A1 ES 201331232 A ES201331232 A ES 201331232A ES 201331232 A ES201331232 A ES 201331232A ES 2528331 A1 ES2528331 A1 ES 2528331A1
- Authority
- ES
- Spain
- Prior art keywords
- beta
- composition
- cryptoxanthin
- campesterol
- stigmasterol
- 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.)
- Granted
Links
- 239000000203 mixture Substances 0.000 title abstract description 13
- 230000036996 cardiovascular health Effects 0.000 title 1
- 230000004821 effect on bone Effects 0.000 title 1
- 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 abstract description 13
- DMASLKHVQRHNES-UPOGUZCLSA-N (3R)-beta,beta-caroten-3-ol Chemical compound C([C@H](O)CC=1C)C(C)(C)C=1/C=C/C(/C)=C/C=C/C(/C)=C/C=C/C=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C DMASLKHVQRHNES-UPOGUZCLSA-N 0.000 abstract description 7
- NBZANZVJRKXVBH-ITUXNECMSA-N all-trans-alpha-cryptoxanthin Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CC(O)CC1(C)C)C=CC=C(/C)C=CC2C(=CCCC2(C)C)C NBZANZVJRKXVBH-ITUXNECMSA-N 0.000 abstract description 7
- 235000002360 beta-cryptoxanthin Nutrition 0.000 abstract description 7
- DMASLKHVQRHNES-ITUXNECMSA-N beta-cryptoxanthin Natural products CC(=C/C=C/C=C(C)/C=C/C=C(C)/C=C/C1=C(C)CC(O)CC1(C)C)C=CC=C(/C)C=CC2=C(C)CCCC2(C)C DMASLKHVQRHNES-ITUXNECMSA-N 0.000 abstract description 7
- 239000011774 beta-cryptoxanthin Substances 0.000 abstract description 7
- 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 abstract description 5
- 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 abstract description 5
- 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 abstract description 5
- 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 abstract description 5
- 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 abstract description 5
- NJKOMDUNNDKEAI-UHFFFAOYSA-N beta-sitosterol Natural products CCC(CCC(C)C1CCC2(C)C3CC=C4CC(O)CCC4C3CCC12C)C(C)C NJKOMDUNNDKEAI-UHFFFAOYSA-N 0.000 abstract description 5
- 235000000431 campesterol Nutrition 0.000 abstract description 5
- 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 abstract description 5
- 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 abstract description 5
- 229950005143 sitosterol Drugs 0.000 abstract description 5
- 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 abstract description 5
- 235000016831 stigmasterol Nutrition 0.000 abstract description 5
- 229940032091 stigmasterol Drugs 0.000 abstract description 5
- BFDNMXAIBMJLBB-UHFFFAOYSA-N stigmasterol Natural products CCC(C=CC(C)C1CCCC2C3CC=C4CC(O)CCC4(C)C3CCC12C)C(C)C BFDNMXAIBMJLBB-UHFFFAOYSA-N 0.000 abstract description 5
- 229940076810 beta sitosterol Drugs 0.000 abstract description 4
- VGSSUFQMXBFFTM-UHFFFAOYSA-N (24R)-24-ethyl-5alpha-cholestane-3beta,5,6beta-triol Natural products C1C(O)C2(O)CC(O)CCC2(C)C2C1C1CCC(C(C)CCC(CC)C(C)C)C1(C)CC2 VGSSUFQMXBFFTM-UHFFFAOYSA-N 0.000 abstract description 3
- ARYTXMNEANMLMU-UHFFFAOYSA-N 24alpha-methylcholestanol Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(C)CCC(C)C(C)C)C1(C)CC2 ARYTXMNEANMLMU-UHFFFAOYSA-N 0.000 abstract description 3
- 208000024172 Cardiovascular disease Diseases 0.000 abstract description 3
- LGJMUZUPVCAVPU-JFBKYFIKSA-N Sitostanol Natural products O[C@@H]1C[C@H]2[C@@](C)([C@@H]3[C@@H]([C@H]4[C@@](C)([C@@H]([C@@H](CC[C@H](C(C)C)CC)C)CC4)CC3)CC2)CC1 LGJMUZUPVCAVPU-JFBKYFIKSA-N 0.000 abstract description 3
- ARYTXMNEANMLMU-ATEDBJNTSA-N campestanol Chemical compound C([C@@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@H](C)CC[C@@H](C)C(C)C)[C@@]2(C)CC1 ARYTXMNEANMLMU-ATEDBJNTSA-N 0.000 abstract description 3
- LGJMUZUPVCAVPU-HRJGVYIJSA-N stigmastanol Chemical compound C([C@@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@H](C)CC[C@@H](CC)C(C)C)[C@@]2(C)CC1 LGJMUZUPVCAVPU-HRJGVYIJSA-N 0.000 abstract description 3
- 238000011282 treatment Methods 0.000 abstract description 3
- 208000001132 Osteoporosis Diseases 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 230000002265 prevention Effects 0.000 abstract 2
- 235000015872 dietary supplement Nutrition 0.000 abstract 1
- 239000004615 ingredient Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 239000000047 product Substances 0.000 abstract 1
- 235000002378 plant sterols Nutrition 0.000 description 3
- BDCFUHIWJODVNG-UHFFFAOYSA-N Desmosterol Natural products C1C=C2CC(O)C=CC2(C)C2C1C1CCC(C(C)CCC(CC)C(C)C)C1(C)CC2 BDCFUHIWJODVNG-UHFFFAOYSA-N 0.000 description 2
- AVSXSVCZWQODGV-DPAQBDIFSA-N desmosterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@@H](CCC=C(C)C)C)[C@@]1(C)CC2 AVSXSVCZWQODGV-DPAQBDIFSA-N 0.000 description 2
- KZJWDPNRJALLNS-VPUBHVLGSA-N (-)-beta-Sitosterol 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)CC)C)CC4)CC3)CC=2)CC1 KZJWDPNRJALLNS-VPUBHVLGSA-N 0.000 description 1
- CSVWWLUMXNHWSU-UHFFFAOYSA-N (22E)-(24xi)-24-ethyl-5alpha-cholest-22-en-3beta-ol Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(C)C=CC(CC)C(C)C)C1(C)CC2 CSVWWLUMXNHWSU-UHFFFAOYSA-N 0.000 description 1
- KLEXDBGYSOIREE-UHFFFAOYSA-N 24xi-n-propylcholesterol Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(C)CCC(CCC)C(C)C)C1(C)CC2 KLEXDBGYSOIREE-UHFFFAOYSA-N 0.000 description 1
- LPZCCMIISIBREI-MTFRKTCUSA-N Citrostadienol Natural products CC=C(CC[C@@H](C)[C@H]1CC[C@H]2C3=CC[C@H]4[C@H](C)[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C)C(C)C LPZCCMIISIBREI-MTFRKTCUSA-N 0.000 description 1
- ARVGMISWLZPBCH-UHFFFAOYSA-N Dehydro-beta-sitosterol Natural products C1C(O)CCC2(C)C(CCC3(C(C(C)CCC(CC)C(C)C)CCC33)C)C3=CC=C21 ARVGMISWLZPBCH-UHFFFAOYSA-N 0.000 description 1
- MJVXAPPOFPTTCA-UHFFFAOYSA-N beta-Sistosterol Natural products CCC(CCC(C)C1CCC2C3CC=C4C(C)C(O)CCC4(C)C3CCC12C)C(C)C MJVXAPPOFPTTCA-UHFFFAOYSA-N 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000005115 demineralization Methods 0.000 description 1
- 230000002328 demineralizing effect Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 235000015500 sitosterol Nutrition 0.000 description 1
- NLQLSVXGSXCXFE-UHFFFAOYSA-N sitosterol Natural products CC=C(/CCC(C)C1CC2C3=CCC4C(C)C(O)CCC4(C)C3CCC2(C)C1)C(C)C NLQLSVXGSXCXFE-UHFFFAOYSA-N 0.000 description 1
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
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Pharmacology & Pharmacy (AREA)
- Mycology (AREA)
- Polymers & Plastics (AREA)
- Food Science & Technology (AREA)
- Nutrition Science (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
Abstract
La presente invención hace referencia a una composición que comprende beta-criptoxantina, campesterol, beta-sitosterol, estigmasterol, sitostanol, campestanol y, de al menos un excipiente farmacéuticamente aceptable. La presente invención además comprende el uso de dicha composición para la manufactura de un medicamento; en concreto de un medicamento para la prevención y/o tratamiento de osteoporosis y enfermedades cardiovasculares. Adicionalmente, la presente invención también comprende un producto comestible, preferentemente como suplemento dietético, que comprende una cantidad efectiva de beta-criptoxantina, campesterol, beta-sitosterol, estigmasterol, sitostanol, campestanol y cantidades adecuadas de otros ingredientes comestibles, para el tratamiento y/o prevención de enfermedades cardiovasculares y osteoporosis.
Description
P201331232
06-08-2013
En la tabla 2 se muestra la bioaccesibilidad de la beta-criptoxantina y de los esteroles vegetales totales e individuales de las composiciones 1, 2 y 3 del ejemplo 1.
Tabla 2. Bioaccesibilidad (%), expresada como media y en paréntesis el intervalo de confianza al nivel de probabilidad del 95%.
- Composición
- 1
- 2 3
- beta-criptoxantina
- 83 (70-93) -- 90 (84-97)
- Campesterol
- -- 8.31 (6.70-9.93) 6.66 (5.99-7.33)
- Estigmasterol
- -- 5.96 (4.47 7.45) 4.02 (3.75-4.29)
- Sitosterol
- -- 6.42 (5.18-7.66) 4.15 (4.05-4.25)
- Campestanol
- -- 6.82 (5.40-8.24) 5.79 (4.42-7.16)
- Sitostanol
- -- 6.05 (4.29-7.81) 4.41 (4.16-4.66)
- EV totales
- -- 6.48 (5.19-7.77) 4.35 (4.20-4.50)
EV= esteroles vegetales
Los intervalos de confianza de la Tabla 2 muestran que no hay diferencias en la
10 biodisponibilidad in vitro cuando las beta-criptoxantina y los esteroles vegetales de las composiciones están solos (composición 1 y 2, respectivamente) o juntos (composición 3).
Ejemplo 3: Evaluación de la biodisponibilidad in vivo
15 Se proporcionaron las tres composiciones del ejemplo 1 a 36 sujetos. En concreto, se seleccionaron mujeres en edad post-menopáusica, grupo de alto riesgo de desmineralización ósea y desarrollo de enfermedad cardiovascular. La selección se realizó mediante muestreo no-probabilístico. Se administró cada una de las
20 composiciones del ejemplo 1 una vez al día durante 4 semanas (t=4), dejando un
10
P201331232
06-08-2013
Tabla 3. Concentraciones séricas de los compuestos durante los tratamientos
- t=0
- t=4 % de cambio t=0, t=4) Incremento neto
- Composición 1
- Beta-criptoxantina
- 16.9 (13.7-20.1) 56.5 (50.0-63.0)a 310 (222-398) 36.4 (29.9-43.0)
- Composición 2
- Beta-sitosterol
- 4.0 (3.46-4.54) 6.34 (4.7-7.98) 64.32 (34.4392.21) 10 2.36 (0.94-3.78)
- Campesterol
- 3.06 (2.7-4.20) 3.28 (2.943.62) 12.7 (4.42, 20.98) 0.29 (0.04-5.54)
- Estigmasterol
- 0.50 (0.38-0.58) 0.48 (0.380.58) 14.2 (8.06,36.46) 15 -0.01 (-0.12-0.10)
- Desmosterol
- 0.58 (0.45-0.64) 0.65 (0.59,0.71) 15.48 (8.61, 22.35) 0.07 (0.03-0.11)
- Latosterol
- 2.91 (2.47-3.35) 3.13 (2.673.59) 14.86 (2.41, 27.31) 20 0.17 (-0.16-0.50)
- Composición 3
- Beta-criptoxantina
- 17.8 (13.921.6) 53.2 (47.3-59.0)a 282 (198365) 34.5 (29.939.2)
- Beta-sitosterol
- 3.91 (3.45-4.37) 5. 46 (4.39-6.53) 49.36 (24.8173.92) 25 1.56 (0.65-2.47)
- Campesterol
- 2.91 (2.66-3.16) 3.25 (2.83-3.67) 10.75 (3.07, 18.43) 0.34 (0.08-0.60)
- Estigmasterol
- 0.5 (0.41-0.58) 0.48 (0.40-0.55) 8.94 (-8.12, 26.0) 30 -0.02 (-0.11-0.07)
- Desmosterol
- 0.62 (0.58-0.66) 0.63 (0.62-0.65) 2.91 (-3.71, 9.53) 0.01 (-0.03-0.05)
- Latosterol
- 3.21 (2.74-3.68) 3.13 (2.70-3,56) 1.29 (-7.8810.46) 35 -0.08 (-0.36-0.20)
12
Claims (1)
-
imagen1 imagen2
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES201331232A ES2528331B1 (es) | 2013-08-06 | 2013-08-06 | Composición con efecto en la salud ósea y cardiovascular |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES201331232A ES2528331B1 (es) | 2013-08-06 | 2013-08-06 | Composición con efecto en la salud ósea y cardiovascular |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2528331A1 true ES2528331A1 (es) | 2015-02-06 |
| ES2528331B1 ES2528331B1 (es) | 2015-12-02 |
Family
ID=52440049
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES201331232A Active ES2528331B1 (es) | 2013-08-06 | 2013-08-06 | Composición con efecto en la salud ósea y cardiovascular |
Country Status (1)
| Country | Link |
|---|---|
| ES (1) | ES2528331B1 (es) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008154294A1 (en) * | 2007-06-07 | 2008-12-18 | Unicity International, Inc. | Method and composition for providing controlled delivery of biologically active substances |
| US20090264520A1 (en) * | 2008-04-21 | 2009-10-22 | Asha Lipid Sciences, Inc. | Lipid-containing compositions and methods of use thereof |
-
2013
- 2013-08-06 ES ES201331232A patent/ES2528331B1/es active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008154294A1 (en) * | 2007-06-07 | 2008-12-18 | Unicity International, Inc. | Method and composition for providing controlled delivery of biologically active substances |
| US20090264520A1 (en) * | 2008-04-21 | 2009-10-22 | Asha Lipid Sciences, Inc. | Lipid-containing compositions and methods of use thereof |
Non-Patent Citations (1)
| Title |
|---|
| ALEMANY LAIA et al. Effect of simulated gastrointestinal digestion on plant sterols and their oxides in enriched beverages.FOOD RESEARCH INTERNATIONAL ELSEVIER APPLIED SCIENCE, BARKING, GB // Junio 2013; VOL: 52 No: 1 Pags: 1 - 7 ISSN 0963-9969 Doi: doi:10.1016/j.foodres.2013.02.024 Gong Joshua; Goff H Douglas * |
Also Published As
| Publication number | Publication date |
|---|---|
| ES2528331B1 (es) | 2015-12-02 |
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