Enzyme in a dosage form for oral use in mammals,...

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical

Reexamination Certificate

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C424S441000, C424S442000, C424S094600

Reexamination Certificate

active

06699496

ABSTRACT:

BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to an enzyme in an oral dosage form, a food material(food stuff) containing the enzyme and a method for administering the enzyme in a dosage form; more specifically, the invention relates to an enzyme in a dosage form for oral use in mammals, a food material (food stuff) containing the enzyme and a method for administering the enzyme, wherein the enzyme is effective for decreasing the increased body fat and internal fat in mammals including humans, cattle, pet animals, when these increased fats are useless or harmful.
2. Description of the Related Art
The frequency of obesity in humans has been increasing due to excess calorie intake based on the recent change in their diets. The obesity functions as one cause for the induction of adult diseases. Because fat in particular readily accumulates in fat cells and is of high calorie, the individuals now pay significant attention to the fat intake from their diets. Alternatively, excessive accumulation of body fat in cattle such as cows and pigs is sometimes avoided from the respects of unpalatability as edible meat and nutritive control. Furthermore, the obesity of pet animals such as cats and dogs due to the ingestion of highly nutritious pet foods in recent years has been worrying their owners.
Recently, the physiological action and function of fat in mammals including humans, and the structure and the digestion and absorption of fat have been elucidated and reported. For example, JP-A-4-300825 remarks that 1,3-diglyceride (abbreviated to 1,3-DG hereinafter) suppresses more the increase in serum neutral fat after food ingestion and decreases more body fat, compared with triglyceride (abbreviated to TG hereinafter). In other words, it is suggested that the ingestion of 1,3-DG can effectively decrease body fat and internal fat (particularly, liver fat).
The reason is possibly as follows; 2-monoglyceride (abbreviated to 2-MG hereinafter) is primarily produced, with the action of the digestive juice in bodies, after TG ingestion. Then, 2-MG is readily converted to TG in the small intestines, which is then incorporated as TG (depot fat) in the liver and the like. Alternatively, 1-monoglyceride (hereinafter abbreviated to 1-MG) is produced with the action of the digestive juice, after 1,3-DG ingestion. However, the 1-MG is hardly converted into TG and is therefore hardly absorbed and stored as fat. In this case, additionally, fat incorporation in the liver is made principally via fatty acids from the portal vein. Accordingly, ketone bodies produced via &bgr; oxidation enhanced in the liver are excreted in urine. Thus, liver fat is decomposed and decreased.
With attention focused on what have been described above, conventionally, attempts have been made to procure the fat decreasing effect in humans or mammals, by a method comprising administering 1,3-DG extracted from natural materials or synthesized by chemical or enzymatic esterification (ester interchange reaction) and then contained in common edible oils and oil-containing foods, or comprising directly administering 1,3-DG in a dosage form.
However, the method comprising administering 1,3-DG separately from fat contained in food materials can hardly suppresses sufficiently 2-MG production per se derived from the fat contained in food materials, essentially, although the effects of 1,3-DG and 1-MG per se can be procured. Thus, the method can exert only limited effect on the decrease in body fat and internal fat.
Because 1-MG per se is so unstable that 1-MG can hardly be contained in such edible oils or oil-containing food materials, disadvantageously, the aforementioned method per se is hardly established in a practical sense.
SUMMARY OF THE INVENTION
It is an object of the invention to provide a means for effectively decreasing body fat and internal fat in mammals, by sufficiently utilizing the above findings about 1,3-DG and/or 1-MG. The present inventors have found that a certain enzyme conventionally never used for oral administration in mammals including humans can be used for the object. Thus, the invention has been achieved.
A first aspect of the invention relates to an enzyme in a dosage form for oral use in mammals, wherein the enzyme is capable of converting triglyceride in food materials into 1,3-diglyceride (1,3-DG) and/or 1-monoglyceride (1-MG).
According to the first aspect of the invention, the enzyme in an oral dosage form functions to convert the fat (TG) per se in the food materials into 1,3-DG and/or 1-MG which is hardly convertible to body fat or internal fat. Thus, the production of 2-MG from fat in food materials can sufficiently be suppresed. Consequently, the enzyme in an oral dosage form can satisfactorily decrease body fat and internal fat.
The inventors have not yet found any evidence that an enzyme having an activity of converting triglyceride into 1,3-DG and/or 1-MG has been utilized in a dosage form for oral use in mammals or any report telling the possibility. The function and advantage described above may be applied generally to mammals including humans, because mammals have common biological properties in terms of the structures of the digestive system including the liver and the physiological functions.
A second aspect of the invention relates to an enzyme in a dosage form for oral use in mammals, wherein the enzyme in the first aspect of the invention comprises at least one selected from the group consisting of lipase and esterase derived from the following microorganisms and biological organism 1 to 10.
1
. Geotrichum candidum
2
. Candida rugosa
3
. Candida lipolytica
4. Pseudomonas sp.
5
. Aspergillus niger
6
. Fhizopus oryzae
7. Rhizopus sp.
8
. Mucor javanicus
9. Porcine pancreas
10
. Penicillium camembertii
The lipase or esterase derived from the 1 to 10 microorganisms and biological organism and the like is particularly effective as the enzyme in the oral dosage form. Additionally, because the enzyme per se has been well known conventionally and because of the oral dosage form, the lipase or esterase never exerts side effects harmful for mammals including humans.
A third aspect of the invention relates to a food material (food stuff) containing the enzyme according to the first aspect or the second aspect of the invention.
In accordance with the third aspect of the invention, the enzyme is contained in a food material. Thus, the resulting food material has the same advantage as those in the first and second aspects of the invention (without separately ingesting or administering the enzyme), and exhibits the same activity toward the fat contained in the resulting food material per se, or the fat in a fat-containing food material concurrently ingested with the resulting food material even when the food material only slightly contains fat.
A fourth aspect of the invention relates to a food material according to the third aspect of the invention, wherein the food material contains fat and the enzyme of 500 to 100,000 units per 100 g of fat [one unit of the enzyme generates 1 &mgr;mol fatty acid per one minute, as assayed at 37° C., pH 7 according to the fat digestion test described in the Section General Tests of the Japanese Pharmacopoeia; the definition applicable hereinafter].
In accordance with the fourth aspect of the invention, the enzyme is contained in an amount of 500 to 100,000 units per 100 g of fat in the enzyme-containing food material containing fat, whereby very excellent effect on the decrease in body fat or internal fat can be expected.
A fifth aspect of the invention relates to a method for administering the enzyme in an oral dosage form according to the first aspect or the second aspect of the invention, with a food material containing fat before, during or after meal.
The method for administering the enzyme in an oral dosage form according to the fifth aspect of the invention can bring function and advantage almost at the same levels as those in the first and second aspects of the invention.


REFERENCES:
patent: 5178864 (1993-

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