Method for producing a fat mixture

Details Method for producing a fat mixture Method for producing a fat mixture

2000-11-13

2003-03-11

Badio, Barbara P. (Department: 1616)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

C514S170000

Reexamination Certificate

active

06531463

ABSTRACT:

FIELD OF THE INVENTION
The present invention relates to a method for producing a fat mixture of &bgr;-sitosterol, which mixture is health beneficial, homogeneous and stable, lowers the serum total cholesterol and LDL-cholesterol levels, and contains the &bgr;-sitosterol in a partly dissolved and/or microcrystalline form.
BACKGROUND OF THE INVENTION
A high serum total cholesterol level, hypertension and smoking are the main risk factors associated with a heart disease (1). There are several sterols of plant origin that are distinguished from cholesterol only by side chain substituents and by the degree of saturation. Most of the higher plants produce 24&agr;-substituted sterols (24-methyl- and 24-ethylsterols). Sitosterols are mixtures of &bgr;-sitosterol (stigmasta-5-en-3&bgr;-ole) and certain saturated sterols, such as &bgr;-sitostanol, containing sterols not less than 95%, and unsaturated sterols not less than 85%. Sitosterols are broadly present in plants, such as in wheat and rye germ oils, corn oil, and commonly in seed oils. Sitosterols are antihypercholesterolemic agents that inhibit absorption of cholesterol in the intestine, and through the inner walls of blood vessels (2). Sitosterols play a role in the treatment of atherosclerosis when administered in doses of 2-3 grams., three times a day. In the western diet, the daily intake of &bgr;-sitosterol, stigmasterol and campesterol from food is about 200-400 mg (3), which is of about the same order as our daily cholesterol intake from food.
At the beginning of 1950's, it was recognized that as a result of the addition of &bgr;-sitosterol to the feed of cholesterol fed chicken and rabbits, the cholesterol levels were lowered in both test animals, and moreover, this addition of &bgr;-sitosterol prevented atherogenesis in rabbits (4). The use of sitosterol and soy bean sterols for lowering cholesterol levels was studied intensely in 1950's and 1960's (5), and indeed, preparations thereof lowered cholesterol levels by about 10% (6). It was then discovered that the activity of &bgr;-sitosterol was based on the inhibition of absorption of cholesterol, and that sterols of plant origin were themselves poorly absorbed (7). The mechanism which inhibits the cholesterol absorption was considered to be based on crystallization and coprecipitation of cholesterol and &bgr;-sitosterol. Mattson et al. (8) showed that 1 gram of &bgr;-sitosterol reduces by 42% the absorption of cholesterol from food containing 500 mg of cholesterol. The reduction of plasma cholesterol may be due to the increased activity of LDL-receptors.
&bgr;-Sitosterol is a lipophilic compound. In contact with the lipid membranes of intestinal walls, &bgr;-sitosterol will not be absorbed due to its poor water solubility, or only a minor proportion of it will be absorbed; when administered orally, only less than 5% of it will be absorbed (9). The activity of &bgr;-sitosterol is based on competitive inhibition of cholesterol absorption in the intestine (10). &bgr;-sitosterol interferes with cholesterol resorption and reresorption in the small intestine (11). It is considered that this results from the similarity between the chemical structures of cholesterol and &bgr;-sitosterol (12). Several studies carried out under various conditions have shown that phytosterols lower LDL-cholesterol levels. It is further recognized that serum phytosterols correlate with HDL-levels. &bgr;-sitosterol reduces synthesis of cholesterol in the liver by affecting the gene expression of HMG-CoA reductase (13). Richter W et al. (14) have shown that &bgr;-sitosterol lowers by 10-15% the total serum cholesterol level, and by 19% the LDL-cholesterol level, by inhibiting the absorption of cholesterol in the intestine. In a study, nine adult patients were administered for 5 days with 500 mg of cholesterol, as well as with 1 gram of &bgr;-sitosterol, or 2 grams of &bgr;-sitosteryl oleate. The absorption of cholesterol was decreased by 42% when administering &bgr;-sitosterol, and by 33% when administering &bgr;-sitoteryl oleate (15). Uchita et al. (16) have recognized that in female rats, sitosterol inhibits absorption of cholesterol, and lowers cholesterol balance in plasma and liver. Vahouny et al. (17) have discovered that sitosterol inhibits absorption of cholesterol in rats by 54%.
Finnish patent application No. 964951 discloses an agent for lowering the cholesterol level in serum, and the use thereof. This application relates to the use of an ester of &bgr;-sitostanol with a fatty acid or a mixture of esters of &bgr;-sitostanol with a fat acid as a fat component or as a fat substitute in food products, to the use thereof as such, complementing the diet, and to the compound itself.
Finnish patent publication No. 98 730 discloses a method for producing a substance to lower high serum cholesterol levels. In the method &bgr;-sitostanol, obtained from &bgr;-sitosterol by hydrogenating in an organic solvent in the presence of palladium on carbon as a catalyst, and a plant oil are used to produce an ester of &bgr;-sitostanol with a fatty acid, or a mixture of such esters, employing the transesterification technique in the presence of a sodium ethylate catalyst.
Both of these patent publications mentioned above disclose a method for modifying &bgr;-sitosterol to obtain a derivative thereof soluble in fats, wherein soluble &bgr;-sitostanol fatty acid esters are produced therefrom, as well as the use of the compounds obtained as agents to lower serum cholesterol levels.
Naturally occurring &bgr;-sitosterol is a crystalline compound. As is known, free sterols like &bgr;-sitosterol are dissolved only scarcely in oil and fat, and therefore, derivatives of &bgr;-sitosterol, for instance esters that are significantly more soluble in fats are produced for practical reasons, even though, according to some studies (15), these derivatives do not inhibit the absorption of cholesterol as effectively as the free &bgr;-sitosterol. Such derivatives soluble in fats may be mixed much more easily into nutrition products to form a homogeneous mixture than a solid, insoluble, coarse &bgr;-sitosterol powder. However, such processing to obtain a &bgr;-sitosterol derivative entails additional costs for the product. Further, the hydrogenation of &bgr;-sitosterol to &bgr;-sitostanol is necessarily carried out using an organic solvent so that traces of it, as well as traces of the metal catalysts used, may be present in the esterified end product. In addition, the esterified product is no longer a naturally occurring substance but a man made artificial chemical compound.
An object of the invention is to provide a method for producing a fat mixture of &bgr;-sitosterol, which is health beneficial, homogeneous and stable, lowers the total serum cholesterol and LDL-cholesterol levels, and contains the &bgr;-sitosterol in a partly dissolved and/or in a microcrystalline form. Another object of the invention is to use such a homogeneous stable fat mixture of &bgr;-sitosterol containing it in a partly dissolved and/or in a microcrystalline form in fat preparations or food products as an agent that lowers the cholesterol level in serum, as well as to use this mixture as such to complement the diet.
The main characteristic features of the method and use according to the present invention are disclosed in the appended claims.
We have discovered that &bgr;-sitosterol may be made partly soluble and/or micro-crystalline with the following procedure. The problems and disadvantages associated with the state of the art may be avoided with the solution of the present invention. According to the method of the invention, &bgr;-sitosterol and food grade oil are mixed, and this mixture is heated until all solids are dissolved in oil. After cooling, water is added into the mixture at the temperature thereof, thereby dispersing it. The result will be a homogeneous, stable, fat-like, almost white mass with a consistency closely resembling that of butter, or an oily mixture, depending on the amounts of the components. This homogeneous and

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