JPH0952838A - Composition for oral use - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a preparation for oral use with masked bitter taste and having good administration feeling and taste. SOLUTION: This composition contains one or more kinds of gastrointestinal medicines selected from tiquizium bromide, scopolia extract, butylscropolamine bromide and timepidium bromide and stevia which is a sweatener ingredient as active ingredients. Effective blend ratio of stevia is 5-100mg, preferably 10-50mg/day.adult. Blend amount of stevia is 0.1-10 pts.wt., preferably 0.5-3 pts.wt. based on 1 pt.wt. tiquizium bromide, though it differs by component of gastrointestinal medicines. As necessary, other well-known additive is blended and the blend can be contained in preparation for oral uses such as granules, particles, powdery preparation, capsule, tablet, chewable preparation, dry syrup, liquid agent, etc. The preparation is relatively stable to heat and acid and has high safety and can be used without anxiety and has mild quality of sweetness, slight after-taste and non-fermentanting property and causes no browning by heat treatment.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an oral composition containing a specific gastrointestinal drug component and having improved ingestion and flavor.

[0002]

2. Description of the Related Art Stevia is Stevia Rebaudiana Berton
It is a sweetener composed mainly of the sweetening ingredients contained in the leaves of the perennial family Asteraceae i. On the other hand, the gastrointestinal drug components thixidium bromide, funnel extract, butylscopolamine bromide and timepidium bromide have a bitter taste, and therefore it is preferable to improve the feeling of ingestion. However, conventionally, masking of bitterness has been achieved by using a capsule, but it has no rapid effect, and when sucrose is blended into fine granules, the sweetness remains after administration and becomes dull. There was an inconvenience, and the feeling of taking and the improvement of flavor were not sufficient.

[0003]

SUMMARY OF THE INVENTION An object of the present invention is to provide an oral preparation containing a gastrointestinal drug component in which bitterness is masked and ingestion and flavor are improved.

[0004]

Means for Solving the Problems In order to solve the above problems, the present inventors have conducted various studies using various sweeteners, and as a result, when stevia and a specific gastrointestinal drug component were combined as a sweetening component, The present invention has been completed by finding that an oral preparation having a good feeling and taste can be obtained. That is,
The present invention relates to (a) one or more gastrointestinal drug components selected from the group consisting of thixidium bromide, funnel extract, butylscopolamine bromide and timepidium bromide, and (b)
An oral composition comprising stevia.

[0005]

BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, stevia means stevioside, rebaudioside A, sulcoside A, sulcoside B, rebaudioside E, rebaudioside D, steviorbioside, rebaudioside B. , A mixture of known stevia extracts such as steviol, or an isolated one of these components, and also includes the above-mentioned known stevia extract that has been subjected to an enzyme treatment to increase sweetness. Among these, those having a high content of rebaudioside A are preferable. The effective compounding amount of stevia is 5 mg to 100 mg, preferably 10 mg to 50 mg per day in healthy adults. The content of stevia varies depending on the type of gastrointestinal drug component, for example, with respect to 1 part by weight of tiquidium bromide, 0.1 parts by weight to 10 parts by weight of stevia, preferably 0.5 parts.
Parts by weight to 3 parts by weight.

The stevia-containing composition of the present invention may be used as it is or as required with other known additives such as excipients, disintegrating agents, binders, lubricants, antioxidants, coating agents, and coloring agents. Orals such as granules, fine granules, powders, capsules, tablets, chewable agents, dry syrups, liquids (drinks), etc. by mixing agents, flavoring agents, surfactants, plasticizers, etc., according to a conventional method It can be a formulation.

Examples of the excipient include mannitol, xylitol, sorbitol, glucose, sucrose, lactose, crystalline cellulose, crystalline cellulose / carboxymethyl cellulose sodium, calcium hydrogen phosphate, wheat starch, rice starch, corn starch, potato starch, carboxy. Sodium methyl starch, dextrin, α-cyclodextrin, β-cyclodextrin, carboxyvinyl polymer, light anhydrous silicic acid, titanium oxide, magnesium aluminometasilicate,
Examples thereof include polyethylene glycol and medium chain fatty acid triglyceride. Examples of the disintegrator include low-substituted hydroxypropyl cellulose, carboxymethyl cellulose, carboxymethyl cellulose calcium, carboxymethyl cellulose sodium, croscarmellose sodium type A (actizol), starch, crystalline cellulose, hydroxypropyl starch, partially pregelatinized starch and the like. To be

Examples of the binder include methylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone, gelatin, gum arabic, ethylcellulose, polyvinyl alcohol, pullulan, pregelatinized starch, agar, tragacanth,
Examples include sodium alginate and propylene glycol alginate.

Examples of the lubricant include stearic acid, magnesium stearate, calcium stearate, polyoxyl stearate, cetanol, talc, hardened oil, sucrose fatty acid ester, dimethylpolysiloxane,
Examples include microcrystalline wax, beeswax, and beeswax.

Examples of the antioxidant include dibutylhydroxytoluene (BHT), propyl gallate, butylhydroxyanisole (BHA), α-tocopherol,
Citric acid and the like.

Examples of the coating agent include hydroxypropylmethylcellulose, hydroxypropylcellulose, methylcellulose, ethylcellulose, hydroxypropylmethylcellulose phthalate, hydroxypropylmethylcellulose acetate succinate, carboxymethylethylcellulose, cellulose acetate phthalate, polyvinyl acetal diethylaminoacetate and aminoalkyl meta. Examples thereof include acrylate copolymer, hydroxypropylmethyl cellulose acetate succinate, methacrylic acid copolymer, cellulose acetate trimellitate (CAT), polyvinyl acetate phthalate, shellac and the like.

Examples of the coloring agent include tar dyes, titanium oxide and the like.

Examples of the surfactant include polyoxyethylene hydrogenated castor oil, sorbitan monostearate, sorbitan monopalmitate, sorbitan monolaurate, polyoxyethylene polyoxypropylene block copolymers, polysorbates, sodium lauryl sulfate, and macrogoles. , Sucrose fatty acid ester and the like.

Examples of the plasticizer include triethyl citrate, triacetin, cetanol and the like.

When the dosage form is a drink, it can be made to have a palatability by mixing with other physiologically active ingredients, hormones, nutritional ingredients, flavors and the like, if necessary.

In the present invention, saccharides such as sucrose may be added within a range that does not impair the effects of the present invention. Further, when a bitterness component other than gastrointestinal drug components such as tiquidium bromide is blended in the formulation, with respect to 1 part by weight of the bitterness component, stevia 0.005 parts by weight to 5 parts by weight, preferably 0.
Add 01 to 3 parts by weight.

[0017]

According to the present invention, it is relatively stable to heat and acid, highly safe, can be used with confidence, has a mild sweetness, a low aftertaste, and is non-fermentable.
It has become possible to provide an oral preparation containing a gastrointestinal drug component which does not cause a browning effect by heat treatment and has an excellent ingestion feeling and flavor.

[0018]

EXAMPLES The present invention will be specifically described below with reference to examples and test examples. Example 1 (Formulation example) Tiquidium bromide 5 mg The above drug and stevia (7.5 mg), isomerized sugar, sodium benzoate, citric acid, phosphoric acid, sodium hydrogenphosphate, dipotassium phosphate, and purified water were mixed. And 30m
1 liquid formulation.

Example 2 (Formulation Example) Tikidium bromide 5 mg Synthetic hydrotalcite 300 mg Magnesium oxide 250 mg The above-mentioned drug and stevia (10 mg), lactose, hydroxypropylcellulose, magnesium stearate and Avicel were weighed and uniformly mixed. 4 tablets were obtained from the obtained mixed powder.

Example 3 (Formulation Example) Timepidium bromide 5 mg Alumina hydroxide magnesium 30 mg The above drug and stevia (10 mg), D-sorbitol solution, benzoic acid, sodium citrate, polyoxyethylene hydrogenated castor oil and purified water were mixed. To give a 30 ml solution. Test Example 1 (Experimental Material) As the experimental material, the liquid agent of Example 1 (Sample A) and the liquid agent of Example 1 from which Stevia was removed (Sample B) were used. (Test method) Questionnaire survey regarding dose and flavor 1) Panelists: healthy adults in their 20s to 50s: 30
First name (male: 13 people, female: 17 people). 2) Content: Panelists use Sample A and Sample B, and then fill out a questionnaire form. The questionnaire is evaluated according to the evaluation items (smell / scent, sweetness, sourness, bitterness, astringency, and astringency). aftertaste,
Furthermore, (i) Deliciousness (ii) Medication-likeness (iii) Efficacy (iv) Repeated drinking (v) Purchase motive (vi) Overall evaluation)
Was classified into 7 levels (very good, relatively good, somewhat good, neither, slightly bad, relatively bad, and very bad). In addition, the sample administration is performed in double blind, the contents are not understood by the panelist,
An absolute evaluation method based on the SD method was used for data analysis.

(Test Results) Using a panel, the sample A,
With respect to the sample B, the feeling and preference were evaluated for odor / aroma, sweetness, sourness, spiciness, bitterness, astringency, acridness, body, and aftertaste. The results are shown in FIGS. 1, 2 and 3.

Specimen A using stevia for both feeling and preference
Shows a tendency of improving effect on the specimen B in all the evaluation groups. In terms of feeling, there were significant differences in the effects of improving sweetness, bitterness, and aftertaste (p <0.05). Regarding taste, sweetness, bitterness, spiciness and aftertaste (p <0.0
The improvement effect was shown in 5).

Further, as a flavor evaluation, (i) deliciousness,
Evaluations were also made regarding (ii) drug-likeness, (iii) feeling of efficacy, (iv) repeated drinking, (v) purchase motive, and (vi) comprehensive evaluation.

As a result, the improvement effect of the sample A on the sample B was obtained. Particularly, regarding the deliciousness and the overall evaluation, the sample A produced a significant difference from the sample B (p <
0.05).

From the above results, it was suggested that the use of stevia as a sweetener masks the bitterness of gastrointestinal drug components and improves the feeling of taking and the taste.

[Brief description of drawings]

FIG. 1 is a graph showing flavor evaluation (how to feel) when samples A and B are taken.

FIG. 2 is a graph showing flavor evaluation (preference) when the samples A and B are taken.

FIG. 3 is a graph showing flavor evaluation when the samples A and B are taken.

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Claims (1)

[Claims] 1. A composition containing (a) one or more gastrointestinal drug components selected from the group consisting of thixidium bromide, funnel extract, butylscopolamine bromide and timepidium bromide, and (b) stevia. Oral composition.