JPS62265236A - Stomachic composition - Google Patents

Abstract

PURPOSE:A stomachic composition which is readily administered and has improved low-temperature stability, containing a surface active agent, a stomachic and methylated cyclodextrin. CONSTITUTION:1-50wt% at least one surface active agent (e.g. 10-20C alkyl or alkenyl-containing alkyl or alkenyl sulfate, soybean phospholipid, etc.) is blended with 0.001-10wt% stomachic (e.g. aniseed, aloe, fennel, Curcuma longa L., Isodon japonicus Hara, etc.) and 0.5-20 times as much as compound (e.g. methylated beta-cyclodextrin, etc.) shown by the formula (n is 6-9; at least one A among 3n A is methyl and the rest is H) as the stomachic by weight to give a stomachic composition. EFFECT:The stomachic composition is hardly observed to have characteristic smell of stomachic and is readily administered. The composition is well absorbed. The composition has improved low-temperature stability when it is processed into liquid and does not change with time.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a stomachic composition, and more particularly to a stomachic composition that is easy to take, has low-temperature stability, and the like.

[Conventional technology and its problems]

Since ancient times, Kenso-kei has been used in the form of decoctions, etc., and even today, a wide variety of Kenso-kei are in use.

However, the stomachic type has the disadvantage that it has a strong unique odor and taste, making it difficult to take. Among these drawbacks, odor is considered to be a solution to imparting a scent using a commonly prepared perfume, but this method does not easily solve the problem.

On the other hand, cyclodextrin is known to form clathrate compounds with various substances.

A method of suppressing the peculiar odor of t-menthol in oral medicine using this principle has been published, for example, in JP-A-52-1140.
It is disclosed in Publication No. 14. However, in such a composition, these odorous substances and cyclodextrin form an inclusion compound, and although the odor is alleviated, the intestinal absorption of the odorous substance is also suppressed.

Therefore, it has been thought that it would be theoretically difficult to solve the above-mentioned drawbacks and achieve sufficient absorption by adding cyclodextrin to drugs that are naturally absorbed from the gastrointestinal tract to exert their medicinal effects.

[Means for solving problems]

The present inventors have conducted various studies to overcome these problems, and have found that by blending Kensho-based with a specific cyclodextrin and surfactant, the characteristic odor and taste of Kenstomis-based can be suppressed, and the taste can be sufficiently suppressed. The present invention was completed based on the discovery that a medicinal effect can be obtained.

That is, the present invention uses the following three components (A) to (C) (A)
Surfactant from at least one company (B) Healthy stomach type (C) The following general formula (1) (where n represents a number from 6 to 9, and at least one of the 3n A's is a methyl group) The present invention provides a stomach-promoting drug composition containing a methylated cyclodextrin represented by:

In addition, the clathrate compound of the methylated cyclodextrin of general formula (I) and a stomachic compound has the property of being difficult to precipitate at low temperatures, and has excellent low-temperature stability when made into a liquid stomachic drug composition. I also found that there is.

Examples of the surfactant as component (A) used in the present invention include the following surfactants that are recognized as pharmaceutical additives.

(1) An alkyl or alkenyl sulfurized salt containing an alkyl group or alkenyl group having an average carbon number of 10 to 20.

(2) Fatty acid glycerin monoester or fatty acid glycerin diester consisting of a fatty acid having an average carbon number of 10 to 20 and glycerin.

(3) Sucrose fatty acid ester consisting of a fatty acid with an average carbon number of 10 to 20 and sucrose.

(4) A sorbitan fatty acid ester consisting of a fatty acid having an average carbon number of 10 to 2 o and norbitol or sorbitan.

(5) Does it contain an alkyl group or alkenyl group having an average carbon number of 10 to 20 and added with 1 to 20 moles of ethylene oxide? Rioquin ethylenenoalkyl or haalkenyl ether.

(ra) A fatty acid ester having an average carbon number of 10 to 20 and a glycol fatty acid ester.

(7) Consisting of a fatty acid with an average carbon number of 10 to 20 and 1 to 20 moles of ethylene oxide? Liethylene fatty acid ester 0 (8) Polyglycerin fatty acid ester consisting of a fatty acid with an average carbon number of 10 to 20 and 1 to 20 moles of glycerin 0 (9) Sorbitan fatty acid ester with an average carbon number of 10 to 20 and 1 to 20 moles of ethylene oxide Polyoxyethylene sorbitan fatty acid ester (0CX) consisting of hydrogenated castor oil and oxyethylene hydrogenated castor oil consisting of 1 to 20 moles of ethylene oxide.

Ill Soybean phospholipids.

Among these surfactants, nonionic surfactants such as sorbitan fatty acid ester, sucrose fatty acid ester, and polyoxyethylene sorbitan fatty acid ester are particularly preferred. Further, these surfactants are blended in the stomach-promoting drug composition of the present invention in a total amount of 1 to 50% by weight, preferably 10 to 20% by weight.

In the present invention, the herbal medicine that is component (B) includes the following crude drugs and drugs that are generally used as stomach medicines.

(1) Anise seed, (2) Aloe, (3) Fennel, (
4) Turmeric, (5) Uyaku, (6) Enmeiso, (7) Scutellariae, (8) Oren, (9) Processed Daiyu 1. (LO Gazoyutsu, old) Cuckoo, (13 Calamus roots, Q31 Dry-
91s (141f, t'j, (15) Kizotsu, (16
) Keihi, (17) Gentiana, (18) Collazine, (
19) Kouboku, (20) Goshuyu, (21) Gatehouse, (
22) Colon〆, (23) Konzurango, (24) Sansho, (25) Jiyo, (26) Shisoshi, (27) Shuksha, (28) Gingerbread% (29) Shozuku, (30) Cuticle, (31) ) stone fusuma root, (32) centaurimus grass, (33) common lily, (34) chinensis, (3
5) Soyo, (36) Escherichia incense, (37) Rhubarb, (3
8) Chikusetsunikuzuku% (39) Clove, (40
) Chimpi, (41) ) Ugarashi, (42) ) Uhi,
(43) Animal fat, (44) bittern, (45) nutmeg,
(46) Nikuzuku, (47) 71 Tsuka, (48) Bi%i
, (49) Byakujutsu, (50) Hop, (51
) Vomica extract, (52) Mana leaf, (53) Motsukoku,
(54) Yakuchi, (55) Ryutan, (56) Ryokiyo, (57) Fennel oil, (58) Cinnamon oil,
(59) Ginger oil, (60) Ginger oil, (
61) Clove oil, (62) Spruce oil, (63) Tsuka oil, (64) Lemon oil, (65) T-menthol,
(66) #-menthol, (67) Red bud phase, (68) Corydalis, (69) Licorice, (70) Berberine chloride (71) Carnitine chloride, (72) Marube Rikan, (
73) Sennen Ken, (74) Taishi Ginseng, (75) ↑ Summer, (76
) Sesho-ka, (77) Baekdu-kun (78), Higashine, (79)
Party ginseng, (80) Mingtang ginseng, (81) Roth extract, (82)
) Mizuna Kamu, (83) Ko Huangren, (84) Yamasu Seiko, (85
) Ryobanzi, (86) Hu Shizi, (87) Nibianzu, (88)
Bean bite, (89) malt, (90) red bean 'p'Ls (9
1) Soka, (92) Souzuku, (93) Byakujutsu,
(94) Large belly skin, (95) French palm reading, (96) humiliation,
(97) Eko Isosuke, (98) Shikiko, (99) Moktenjuku,
(100) Reiring Kao Among these stomach-friendly drugs, drugs with strong odors such as cinnamon bark, fennel, clove, nutmeg, nautsuka, and t-menthol are particularly preferred. These stomachic drugs are treated in advance with methylated cyclodextrin (1) and added to the stomachic drug composition at a final concentration of o, ooi to 10%, preferably 0.1 to 2%.

Methylated cyclodextrin (1) as component (C) of the present invention
), those where n is 6 are methylated α-cyclodextrin, those where n is 7 are methylated β-cyclodextrin, those where n is 8 are methylated γ-cyclodextrin, and n is 8.
is 9 is called methylated δ-cyclodextrin. All of these exhibit clathrate-forming properties.

Methylated cyclodextrin (11 is produced by methylating cyclodextrin. When cyclodextrin is methylated using a methylating agent such as dimethyl sulfate according to a conventional method, the hydroxyl group of the glucose residue is at the 6-position, the 2-position A mixture is obtained in which the methylation is carried out in the order of the 3- and 3-positions.

In the general formula (1), at least one of the three groups may be a methyl group, but preferably, the weight average degree of ether substitution is 8.0 to 11.0, and the degree of ether substitution is 8.0 to 11.0. Methylated β-cyclodextrin containing 50% by weight or more of the same is preferred.

Here, the degree of ether substitution refers to the number of methyl groups introduced per β-cyclodextrin molecule, and methylated β-cyclodextrin with different degrees of ether substitution is
For a mixture containing more than one species, the weight average degree of ether substitution is calculated from each degree of ether substitution and the weight percent of each component.

The methylated cyclodextrin (1) is used in an amount of 1/2 to 20 times, preferably 1 to 10 times, the weight of the stomachic system. Methylated cyclodextrin (summer) has almost no deodorizing or deodorizing effect even when added in an amount less than 1/2 by weight, and even when used in excess of 20 times the amount. No increase in deodorizing effect was observed.

Methylated cyclodextrin (methylated cyclodextrin)
A saturated aqueous solution method, a kneading method of kneading methylated cyclodextrin f11 and a healthy stomach type with a relatively small amount of water using a kneader or the like are employed.

In addition to the above-mentioned ingredients, the composition of the stomach medicine composition of the present invention includes well-known Kenso Kuwagumi by, antacids such as magnesium hydroxide and aluminum hydroxide, which are used as compounding ingredients, intestinal regulators such as lactic acid bacteria, amylase, etc. Digestive agents, mucosal agents such as L-glutamine, viscosity modifiers, emulsifiers, solubilizers, preservatives, stabilizers, flavoring agents, flavoring agents, water, etc. may be added as necessary.

When the stomach-promoting drug composition of the present invention is used as a medicine, it can be in any dosage form such as powder, granules, or liquid, but liquid is particularly preferred.

[Action and effect of the invention]

The stomach health drug composition of the present invention has almost no odor or taste peculiar to stomach health drugs and is easy to take, so it can be targeted at a wide range of users.

In addition, the absorption of mulberry in the composition of the present invention is also good. Furthermore, when the composition of the present invention is made into a liquid, it has excellent low-temperature stability and can be used as a health medicine that does not change over time. [Examples] The present invention will now be described with reference to Examples.

Example 1 The liquid stomach medicine compositions shown in Table 1 were subjected to Mu using a conventional method.

When blending menthol and methylated cyclodextrin (IJ), a clathrate compound was formed in advance with a saturated solution, and the mixture was blended so that the final concentration was as shown in Table 1. The menthol odor of these stomach medicines was evaluated according to the following criteria. The results are shown in Table 1.

Evaluation of menthol odor The surveyor evaluated the results using the following criteria.

◎: No menthol odor at all ○: Almost no menthol odor 62 Weak menthol odor ×: Obvious menthol odor XX: Strong menthol odor Example 2 A stomach drug composition was prepared, and the presence or absence of a specific odor was determined by 9 people and 10 people.

The results are shown in Table 2.

Composition> Invention product (8) Comparative product (4) - Cinnamon oil 0.10. Toukiyo oil 0.1
0. Rubitan tomonolaurate 10
10. Purified water 87.
8 89.8 or less margin table 2

Claims (1)

[Scope of Claims] 1. The following three components (A) to (C) (A) At least one surfactant (B) Stomach medicine (C) The following general formula (I) ▲ Numerical formula, chemical formula, table Methylated cyclodextrin represented by ▼(I) (where n represents a number from 6 to 9, at least one of the 3n A's represents a methyl group, and the rest represent a hydrogen atom) A stomachic medicine composition characterized by containing the following.