FIBROUS-LIPONUTRITIONAL COMPLEXES AND COMPOSITIONS CONTAINING THEM

Abstract: Fibrous-liponutritional complexes comprising one or more nutritional substances capable of promoting health and therapeutical beneficial activities together with one or more phospholipid component and one or more fibrous polysaccharide component; pharmaceutical formulations and foodstuffs containing said fibrous-liponutritional complexes; processes for the preparation of said complexes which are capable of inducing a surprisingly higher increase in the health and therapeutical beneficial activities than that expected for the single nutritional substances used.

Description: FIBROUS-LIPONUTRITIONAL COMPLEXES AND COMPOSITIONS CONTAINING THEM The present invention relates to fibrous- liponutritional complexes consisting of one or more beneficial and therapeutical nutritional substances (proteins and/or peptides obtained by hydrolysis of said proteins and/or optionally by synthesis, a ino acids, vitamins, oligosaccharidess , minerals, bioflavones, phytosterols, lactobacilli , lactospores, yeasts, etc.), together with one or more phospholipid compounds and one or more species of vegetable and/or animals fibers, as well as the pharmaceutical and dietetic compositions, and the functional foodstuffs containing said fibrous- liponutritional complexes. Some specific nutrients capable of promoting different, beneficial nutritional and therapeutical activities have been studied and identified for some time in common food, both from animal and vegetable sources. Non limiting examples of this class of therapeutical nutrients are: a) lactoferrin, a protein isolated from milk, having antioxidant, antiinflammatory, immunostimulating activities and also capable of promoting iron bioavailability (C.C. interbourn et al . , 1990, Biochem. Biophys . Acta, 1055, 179; B.E. Britigan et al . , 1994, Advances in Experimental Medicine and Biology, 357 , 143); b) casomorphines , small peptides of 4-10 amino acids isolated from casein and having opioid activity. These peptides proved to modulate intestinal motility and to stimulate the synthesis of anabolic hormones (J.L. Manbois et al., 1989, Lait, 69, 245); c) peptides capable of inhibiting anqiotensin I converting enzyme and therefore having antihypertensive activity. Said peptides have been isolated from milk protein, wheat flour and fish (Y. Aryoshi, 1993, Trends in Food science and Technology, 4, 139); d) peptides isolated from caseins, having immunostimulating activity (A.M. Fiat et al . , 93, J. Dairy Sci. , 76, 301) ; e) glycomacropeptides isolated from caseins, having nutritional properties promoting the development of intestinal bacteria (lactobacilli, bifidus, etc.), antiviral and antithrombotic activities (M. Yvon et al . , 1994, Reprod. Nutr. Dev. , 34, 527; P. Jolles et al . , 1991, Trends in Food Sci. and Technology, February issue, 42); f) caseinphosphopeptides capable of promoting the bioavailability of Ca, Mg and Zn and of preventing the onset of osteoporosis (Y.S. Lee, 1980, Br. J. Nutr. 43 , 457; R. Sato et al . , 1991, Bioche . Biophys . Acta, 1077, 413) ; g) peptides with high glutamine content obtainable from wheat flour proteins and capable of promoting glycogen muscle storage in athletes (M. Varnier, 1995, Am. J. Physiol. , 269, 309) ; h) purified peptide fractions from colostrum (or from milk serum) containing growth factors such as the "insulin-like growth factors", capable of stimulating protein anabolism (A. Mero et al . , 1997, J. Appl . Physiol., 83 (4), 1144); i) peptides from milk serum having antioxidizing activity (L.B. Colbert et al . , 1991, T.H. Food Sci., 56 (5) , 1248) ; 1) glutathione , a tripeptide present in various species of foods (or obtainable by synthesis) and capable of promoting an effective antioxidizing activity; m) carnosine, a dipeptide mainly present in animal meat (or obtainable by synthesis) having high antioxidizing activity as well; n) lactobacilli and/or lactospores present in milk enzymes, having regulating activity on the intestinal functionality as well as antioxidizing, liver-protecting and hypolipidemizing activities; o) bioflavones and carotenoids mainly present in fruits and in vegetables, having antioxidizing, immunostimulating and vasodilating activities; p) phytosterols mainly present in cereal seeds and in leguminous plants, having antioxidizing, hypolipidemizing and sometimes hormone-like activities; q) vitamins having antioxidizing activity such as vitamin C, vitamin E, vitamin D, β-carotenes, etc. r) S-adenosyl-methionine and the salts thereof. However, the nutritional and therapeutical beneficial activities of these nutritional substances greatly decrease upon oral administration, in that such substances are either inactivated by proteolytic enzymes in the stomach and in the intestine or they are altered or adversely affected by the acid pH in the stomach and/or by bile surfactants in the intestine. The present invention has surprisingly found that the fibrous-liponutritional complexes of the invention, containing one or more of these nutritional substances having health and therapeutical beneficial activities, together with at least one animal and/or vegetable phospholipid and one or more species of vegetable and/or animal fibers, when administered orally, are an effective, well -tolerated nutritional supplement capable of induce a surprisingly higher increase in the health and therapeutical beneficial activities than what expected for the single nutritional substances used. Preferably, the nutritional substance is 1 to 50% by weight of the fibrous-liponutritional complexes whereas the phospholipid components together with the fiber fraction are 50 to 99% by weight of said complexes. Examples of therapeutical nutrients usable for the preparation of the fibrous-liponutritional complexes are all protein nutritional substances, even those not already mentioned above. Examples of phospholipids from animal and/or vegetable sources are represented by phosphatidylcholine, phosphatidylethanolamine, mono- and dimethylphosphatidyl - ethanolamine, phosphatidylserine, phosphatidylinositol and derivatives, phosphatidylglycerol , cardiolipins, lysophospholipids of said compounds and/or mixtures thereof . Examples of fibers of vegetable and/or animal origin are represented by: oat, tomato, guar, potato fibers, different species of cellulose, chitins and chitosans, pectins, inulins, fructooligosaccharides, lignins and derivatives, cyclodextrins and derivatives, amides of various origin and mixtures thereof. The present invention further relates to the pharmaceutical and dietetic formulations (such as tablets, sugar-coated pills, lozenges, sachets, chewable or effervescent tablets, syrups, chewing gums and the like) and functional foodstuffs (bread, pasta, crakers, pizzas pies, biscuits, juices, soft drinks, milk and derivatives, honey, butter and margarine, various dressings and seasonings, mayonnaise, creams and the like) containing the fibrous-lipoprotein complexes and the compositions mentioned above, which can be used for the oral administration. Finally, the invention relates to the processes for the preparation of the fibrous-liponutritional complexes described above . Example 1 Fibrous-liponutritional complexes consisting of: a) 100 g of caseinphosphopeptides containing Ca isolated from cow milk caseins; b) 100 g of commercial soy lecithins containing 40% of phosphatidylcholines, 35% of phosphatidylethanolamine, 18% of phosphatidylinositol and smaller amounts of other phospholipids; c) 300 g of commercial oat fibers. Soy lecithins are dissolved in hexane and placed in a rotary evaporator containing glass microbeads of diameter 1-2 mm, the solvent is evaporated under vacuum at 25°C to obtain a film of phospholipid monomers adhered to glass microbeads. An aqueous solution buffered at physiological pH, containing the oat fibers is added to the mono-layered phospholipid-coated microbeads and subjected to mild stirring for 30 minutes at 25°C. The solution becomes progressively cloudy as fibrous- lipid complexes form, is added with caseinphosphopeptides and then centrifuged at 3000 xg for 5 minutes to separate the glass microbeads in the sediment; the resulting supernatant is then spray-dried to a powder. Said powder is the fibrous-liponutritional complex and can be used as it is both for the preparation of the pharmaceutical (or dietetic) compositions and for the preparation of different functional foodstuffs. Example 2 Fibrous-liponutritional complexes consisting of: a) 50 g of lactoferrin; b) 100 g of commercial soy lecithin containing 40% of phosphatidylcholine, 35% of phosphatidylethanolamine, 18% of phosphatidylinositol and smaller amounts of other phospholipids ; c) 300 g of commercial oat fibers. The three powders are mixed thoroughly by mechanical stirring and subsequently slowly dissolved in an aqueous solution under strong stirring. After that, the resulting emulsion is spray-dried to a powder. Said powder is the fibrous-liponutritional complex and can be used as it is both for the preparation of the pharmaceutical (or dietetic) compositions and for the preparation of different functional foodstuffs. Example 3 Fibrous-liponutritional complexes consisting of: a) 160 g of caseinphosphopeptides containing Ca isolated from cow milk caseins; b) 100 g of commercial egg lecithins containing 50% of phosphatidylcholines, more than 35% of phosphatidylethanolamine and smaller amounts of other phospholipids ; c) 200 g of fiber: 150 g of oat fibers and 50 g of fructooligosaccharides . The fibrous-liponutritional complexes of these three compositions are obtained as described in Example 2 above. Example 4 Fibrous-liponutritional complexes consisting of: a) 10 g of glutathione; b) 25 g of soy lysolecithins obtained by hydrolysis of lecithins of composition similar to that reported in Example 2 above, point b) ; c) 165 g of fibers: 100 g of oat fibers and 65 g of chitosan. The fibrous-liponutritional complexes of these three components are obtained as described in Example 2 above. Example 5 Fibrous-liponutritional complexes consisting of: a) 16 g of dried lactobacilli casei (or lactospore) ; b) 100 g of soy lecithins as in Example 1; c) 165 g of oat fibers. The fibrous-liponutritional complexes of these three components are obtained as described in Example 2. Example 6 Fibrous-liponutritional complexes consisting of: a) 20 g of bioflavones (green tea epicatechins) ; b) 100 g of soy lecithins of Example 1; c) 200 g of oat fibers. The fibrous-liponutritional complexes of these three components are obtained as described in Example 2. Example 7 Fibrous-liponutritional complexes consisting of: a) 25 g of vitamin C (ascorbic acid) ; b) 75 g of soy lecithins of Example 1; c) 150 g of oat fibers. The fibrous-liponutritional complexes of these three components are obtained as described in Example 2.

Claims: CLAIMS 1. Fibrous-liponutritional complexes consisting of: a) nutritional substances; b) a phospholipid compound; c) vegetable or animal fibers. 2. Complexes as claimed in claim 1, wherein the nutritional substances are selected from: lactoferrin, casomorphins, peptides capable of inhibiting angiotensin I converting enzyme, peptides isolated from caseins, glycomacropeptides, caseinphosphopeptides, peptides with high glutamine content, purified peptide fractions from colostrum (or milk serum) , peptides from milk serum, glutathione, carnosine, lactobacilli, lactospores, bioflavones, carotenoids, phytosterols, vitamins, S- adenosyl-methionine and the salts thereof. 3. Complexes as claimed in claim 1 or 2 , wherein the phospholipids are selected from phosphatidylcholine, phosphatidylethanolamine, mono- and dimethylphosphatidylethanolamine, phosphatidylserine, phosphatidylinositol and derivatives, phosphatidylglycerol, cardiolipins, lysophospholipids of said compounds and/or mixtures thereof . 4. Complexes as claimed in any one of claims 1 to 3, wherein the fibers are selected from oat, tomato, guar, potato fibers, cellulose, chitins and chitosans, pectins, inulins, fructooligosaccharides, lignins and derivatives, cyclodextrins and derivatives, amides or mixtures thereof. 5. Complexes as claimed in any one of claims 1 to 4 wherein the nutritional substance is 1 to 50% by- weight of the fibrous-liponutritional complexes and the phospholipid components together with the fiber fraction are 50 to 99% by weight of said complexes. 6. Pharmaceutical compositions containing the complexes of claims 1-5. 7. Foodstuffs containing the complexes of claims 1 to 5.

Inventors: CESTARO BENVENUTO, PISTOLESI ELVIRA, CESTARO, BENVENUTO, PISTOLESI, ELVIRA
Applicants: CESTARO BENVENUTO, HUNZA DI MARIA CARMELA MARAZZI, PISTOLESI ELVIRA, CESTARO, BENVENUTO, HUNZA DI MARIA CARMELA MARAZZITA S.A.S., PISTOLESI, ELVIRA
Application year: 2000
Main classification: A23L1
IPC codes: A23J7, A23L1, A61K31, A61K35, A61K36, A61K38, A61K45, A61P3