JPS5927824A - Antilipemic agent - Google Patents

Abstract

PURPOSE:An antilipemic agent, containing trimethylsteroid as a main component, and capable of exhibiting cholesterol reducing action in blood equal to that of a vegetable sterol, e.g. beta-sitosterol. CONSTITUTION:An antilipemic agent containing trimethylsteroid, particularly preferably cycloartenol and 24-methylenecycloartanol, as a main component. A carrier or adjuvant is added to the above-mentioned compounds and formulated into an agent for the oral administration, e.g. a tablet, powder, capsule or syrup, etc. The daily dose thereof is 0.2-15g, preferably 0.5-5g for adults.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an antilipemic agent containing trimethylsteroid as a main component.

Plant sterols such as β-sitosterol and campesterol are known to lower serum cholesterol levels, and their mechanism of action is generally thought to be inhibition of cholesterol absorption from the intestinal tract. That amount of 'A' in plant sterols.

It is known that when trimethylsteroids such as cycloartenol and 24-methylenecycloartanol are added and administered at ~'Ao/1oo, the same effect is obtained at doses less than 'Ao' of ordinary plant sterol agents. It is being (See %Kokai No. 57-18617).

However, it has been reported that alcohols in unsaponifiables of fat soybean oil, including trimethylsteroids, have no effect on lowering blood cholesterol (Nutrition and Food, Vol. 19, p. 439).
(1966), the present inventors investigated the blood cholesterol-lowering effect of trimethylsteroids and found that it had an effect equivalent to that of plant sterols such as β-sitosterol, thereby completing the present invention.

Examples of the trimethylsteroid used in the present invention include cycloartenol, cycloartenol, 24-methylenecycloartanol, and the like, with cycloartenol and 24-methylenecycloartanol being particularly preferred.

A method for preparing cycloartenol and 24-methylenecycloartanol is described in JP-A-57-48617.

The present invention is prepared in oral dosage forms such as tablets, powders, capsules, and syrups. The daily dose for adults is usually 0.2 to 15 g of the active ingredient, preferably 0.5 to 5 I.

Example Using Wistar male rats with an average weight of 125 g,
Each group of 10 animals in both the control group and other groups was allowed to freely consume the feed shown in Table 1 for 22 days. After the test, the rat was anesthetized with t-ether, blood was collected, and the improved smooth web method (Nutrition and Food, Vol. 28, 98 Negative, 1975)
Plasma cholesterol levels were measured according to 2010). As a result, Table 1 (Unit: CH) Table 2 a: F2ft? : Significant difference for &ζ P<o, o5 According to these results, it is clear that adding cycloartenol or 24-methylenecycloartanol to the feed reduces plasma cholesterol more than K.

[Acute toxicity]

For example, cycloartenol was administered to rats and mice by 5J.
Oral administration of il/Ky did not result in death.

[Formulation Example 1] Cycloartenol 260Ji', Vitamin 01 [ll
11 Citric acid 5g, cellulose calcium glycolate 20
,! i', sodium lauryl sulfate 10. ! i'.

Polyoxyethylene monostearate sy and methylene chloride 300- are taken, mixed well and stirred to form a cloudy liquid. Add Aerosil 200 to 400 (parts name) 1
8011 is added, mixed and stirred, and dried at 50 to 60°C, and the resulting lumps are crushed to obtain an adsorption powder. This adsorbed powder contains polyvinylpyrrolidone, 2-methyl-5-vinylpyridine-
Organic solvent soluble binder such as methacrylic acid/methyl ethyl acrylate copolymer 2011? : Add 3001 nl of the dissolved chlorocene/ethanol solution, knead, and then granulate using an Eck pelleter according to the usual method. Drying at about 50°C solidifies to obtain good granules without stickiness (active ingredients of about 5
(contains 1%). By adding a small amount of lubricant such as magnesium stearate to this product, an automatic capsule filling machine
Can be filled into 0 mfl hard capsules.

[Formulation Example 2] 260 g of 24-mef dichloroartanol was dissolved in 120 #K of 'a' rapeseed oil and filled into soft capsules according to a conventional method. 68.4 active ingredients in 1 capsule 100cm
Contains %.

[Formulation Example 3] DK Ester F 160 (trade name) and polysorbate 802 were added to 50% lnrbitol water if 100 Tnl, and the mixture was made to a 500% concentration with distilled water and stirred again to obtain an emulsion. (Contains about 10% active ingredient) Patent applicant: Sankyo Co., Ltd. Agent: Patent attorney Shoji Kashide

Claims (1)

[Claims] 1. An antilipemic agent containing trimethylsteroid as a main component. 2. The antilipemic agent according to claim 1, wherein the trimethylsteroid is cycloartenol or 24-methylenecycloartanol.