JPH0952829A - Muscle relaxant - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a muscle relaxant having an excellent ingesting feeling. SOLUTION: This muscle relaxant contains one or more kinds selected from chlorophenesin carbamate, methocarbamol, chlorzoxazone and chlormezanone as a muscle relaxant and stevia as a sweetening component. The blending amount of the stevia is different according to the muscle relaxant component, but e.g. 0.01-0.1 pts.wt., preferably 0.01-0.05 pts.wt. stevia is used based on 1 pt.wt. chlorophenesin carbamate. As necessary, by blending other conventional additives, preparations for oral administration such as granules, powder, capsules, tablets, dry syrups and liquid formulations are prepared. This muscle relaxant is relatively stable to a heat and an acid, has a high safety, can be used without a worry, has a mild sweetness quality with less after taste and no fermenting property, does not develop a browning effect by a heat treatment and further does not give too much calories.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to improving the flavor of an oral drug containing a specific muscle relaxant component.

[0002]

BACKGROUND OF THE INVENTION Stevia is a Stevia Rebau.
diana Bertoni is a sweetener mainly composed of a sweetening ingredient contained in leaves of a perennial plant of the Asteraceae family.

On the other hand, since the muscle relaxant component which is the active ingredient of the muscle relaxant, such as chlorphenesin carbamate, has a bitter taste, it is preferable to improve the feeling of ingestion by making it difficult to drink. However, although conventional techniques (eg, incorporating sucrose) can achieve the purpose of masking bitterness to some extent, other problems occur (eg, when incorporating sucrose, the sweetness in the mouth is increased after administration). Due to the inconvenience such as remaining sickness, etc., the feeling of ingestion could not be improved sufficiently.

[0004]

An object of the present invention is to improve the feeling of taking a muscle relaxant.

[0005]

[Means for Solving the Problems] In order to solve the above problems, the present inventors have repeatedly studied using various sweeteners, and as a result, when stevia and a specific muscle relaxant component were combined as a sweetening component, The present invention has been completed by finding that a muscle relaxant having a good feeling of taking can be obtained.

That is, the present invention is a muscle relaxant characterized by containing stevia and one or more drugs selected from the group consisting of chlorphenesin carbamate, metocarbamol, chlorzoxazone and chlormezanone. .

In the present invention, stevia means stevioside, rebaudioside A, sulcoside A, sulcoside B, rebaudioside E, rebaudioside D, steviorbioside, rebaudioside B,
It refers to a mixture of known stevia extracts such as steviol or the one obtained by isolating one of these components, and also includes the above-mentioned known stevia extract that has been subjected to an enzyme treatment in order to increase the sweetness. Among these, those having a high content of rebaudioside A are preferable. The compounding amount of stevia varies depending on the type of muscle relaxant component.
The amount is 01 parts by weight to 0.1 parts by weight, preferably 0.01 parts by weight to 0.05 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. Oral preparations such as granules, powders, capsules, tablets, dry syrups, and liquids (drinks) can be prepared by mixing agents, flavoring agents, surfactants, plasticizers, and the like according to a conventional method.

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. Methylstarch sodium, 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. As the disintegrant, low-substituted hydroxypropyl cellulose, carboxymethyl cellulose, carboxymethyl cellulose calcium, carboxymethyl cellulose sodium, croscarmellose sodium / A type (actizol), starch, crystalline cellulose,
Examples thereof include hydroxypropyl starch and partially pregelatinized starch.

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

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

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

As the coating agent, for example, hydroxypropylmethylcellulose, hydroxypropylcellulose, methylcellulose, ethylcellulose, hydroxypropylmethylcellulose phthalate, hydroxypropylmethylcellulose acetate succinate, carboxymethylethylcellulose, cellulose acetate phthalate, polyvinyl acetal diethylaminoacetate, amino. Examples thereof include alkyl methacrylate copolymer, hydroxypropylmethyl cellulose acetate succinate, methacrylic acid copolymer, cellulose acetate trimellitate (CAT), polyvinyl acetate phthalate and shellac.

Examples of colorants include tar dyes and titanium oxide.

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 given 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. When a bitterness component other than the specific muscle relaxant component is mixed in the formulation, stevia 0.001 part by weight to 0.1 part by weight, preferably 0.007 part by weight, per 1 part by weight of the bitterness component. ˜0.03 parts by weight are compounded.

[0018]

EFFECTS OF THE INVENTION 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 a muscle relaxant that does not cause a browning effect by heat treatment and that does not take too much calories and has an excellent feeling of ingestion.

[0019]

EXAMPLES The present invention will be specifically described with reference to Examples and Test Examples.

Example 1 (Formulation Example) Ibuprofen 450 mg Chlorphenesin carbamate 750 mg Anhydrous caffeine 50 mg Vitamin B ₁ nitrate 24 mg Vitamin B ₂ 12 mg The above drug and stevia (15 mg), D-sorbitol solution, benzoic acid, sodium citrate , Polyoxyethylene hydrogenated castor oil and distilled water were mixed to prepare a 50 ml liquid agent.

Example 2 (Formulation Example) Ibuprofen 432 mg Ethenzamide 252 mg Chlorphenesin carbamate 500 mg Anhydrous caffeine 50 mg The above drug and stevia (10 mg), crystalline cellulose, hydroxypropyl cellulose, magnesium stearate, hardened oil were weighed and uniformly mixed. Then, 9 tablets were obtained with the obtained mixed powder.

Example 3 (Formulation example) Aluminum flufenamic acid 750 mg Chlorphenesin carbamate 750 mg Stevia (10 mg), crystalline cellulose, hydroxypropyl cellulose, magnesium stearate and hardened oil were weighed and uniformly mixed. Then, 6 plain tablets were obtained from the obtained mixed powder.

Example 4 (Formulation example) Oxaprozin 400 mg Metocarbamol 250 mg Anhydrous caffeine 50 mg The above drug and stevia (15 mg), D-sorbitol solution, benzoic acid, sodium citrate, polyoxyethylene hydrogenated castor oil and distilled water were added. The mixture was mixed to give a 30 ml solution.

Example 5 (Formulation Example) Ibuprofen 450 mg Chlorphenesin carbamate 750 mg Anhydrous caffeine 50 mg d-α-tocopherol 100 mg The above drug and stevia (15 mg), monoglyceride, lecithin, D-sorbitol solution, ethanol and distilled water were added. In addition, make 50 ml, mix with a mixer, then emulsify with a homogenizer at 200 kg / cm ³ to 50 ml.
Was used as a liquid agent.

Test Example 1 (Experimental Material) As the experimental material, the liquid agent of Example 1 was used as a specimen containing stevia.

(Test Method) Questionnaire Survey Regarding Flavor 1) Panelists: healthy adults in their 20s to 50s: 20
First name (male: 13; female: 7). 2) Content: A method was used in which the sample A using stevia and the sample B not using stevia were drunk, and then the questionnaire was answered.

The evaluation method of the questionnaire was as follows. The panelist asked each evaluation item (smell / fragrance, sweetness, sourness, spiciness, bitterness, astringency, astringency, aftertaste, and (a) deliciousness (b) medicinalness (c) repeated effectiveness (d) Drinking (e) purchase motive (f) overall evaluation) is divided into 7 levels (very good, relatively good, moderately good, neither, somewhat bad, relatively bad, very bad). It was In addition, the sample administration was performed in a double blind, and the contents were not understood by the panelists. An absolute evaluation method based on the SD method was used for data analysis.

(Test Results) Using a panel, the sample A,
About B Smell / aroma, sweetness, sourness, spiciness,
The feeling and taste of bitterness, astringency, acridness, body, and aftertaste were evaluated. The results are shown in FIGS.
Shown in In terms of feeling, sweetness, sourness, spiciness, bitterness, astringency
There was a tendency for improvement in acridness and aftertaste, and there was a significant difference in bitterness, aftertaste and pungency (p <
0.05).

Regarding the taste, an improvement tendency was observed in all the evaluation groups, and in particular, bitterness (p <0.01), sweetness,
Aftertaste, pungency, body and aftertaste (p <0.05) showed significant improvement effects.

Further, as flavor evaluation, taste, medicinalness, efficacy, repeated drinking, purchase motive,
The overall evaluation was also performed.

As a result, the sample A showed an improving effect on the sample B, and particularly, the tasting property was significantly improved (p <0.05). From the above results, it was suggested that using stevia as a sweetener masks the bitterness component of the drug derived from the active ingredient.

[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 samples A and B are taken.

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

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification code Internal reference number FI technical display location C07D 279/06 C07D 279/06

Claims (1)

[Claims] 1. A muscle relaxant comprising one or more drugs selected from the group consisting of chlorphenesin carbamate, metocarbamol, chlorzoxazone and chlormezanone and stevia.