HK1141245A - Oral liquid preparation with reduced unpleasant taste and odor - Google Patents

Description

Oral liquid preparation with reduced unpleasant taste and smell

Technical Field

The present invention relates to a vitamin B-derived food₁An oral liquid preparation with reduced unpleasant taste and smell.

Background

The drugs often have unpleasant tastes such as bitter taste, astringent taste, and pungent taste, and most of them cannot be taken directly. In addition, the medicine itself is often smelled with unpleasant odor, and thus is often taken with unpleasant feeling. For this reason, it is necessary to reduce unpleasant taste and/or odor in the oral cavity when taken.

Vitamin B₁Is a useful medicine which is used as food, health food, special nutritional food, quasi-drug, new quasi-drug and drug in the mode of oral liquid preparation. However, vitamin B₁When used as an active substance of a preparation such as a quasi drug, a new quasi drug, a drug or the like in a high concentration as an oral liquid preparation, unpleasant tastes such as bitterness, astringency, and pungency are enhanced, and further an unpleasant odor called thiamine odor is generated, so that there is a disadvantage that it is difficult to take.

To reduce vitamin B₁For example, a method of blending a gluconate salt and a calcium salt of an organic acid (patent document 1), a method of blending a fruit-based flavor, acesulfame potassium and a stevioside extract (patent document 2), a method of using electrolytic reduced water obtained by electrolyzing an electrolyte (patent document 3), a method of adding a convertible syrup to reduce bitterness (patent document 4), and a method of adding at least one of menthol and polyoxyethylene-polyoxypropylene-ethylene glycol (patent document 5) have been conventionally attempted.

However, so far on vitamin B derived products₁Even if it is possible to mask a low concentration of vitamin B₁Unpleasant taste of, but for high concentrations of vitamin B₁The unpleasant taste-reducing effect of (c) is still unsatisfactory.

In addition, especially for vitamin B-containing compositions having high vitamin B concentration₁Not only unpleasant taste but also strong sensation from vitamin B due to the liquid form of the oral liquid preparation of (1)₁Has a problem of extremely poor feeling of taking an oral liquid preparation because of the smell of thiamine.

[ patent document 1 ] Japanese patent application laid-open No. 2003-335679

[ patent document 2 ] Japanese patent application laid-open No. 2003-231647

[ patent document 3 ] Japanese patent application laid-open No. 2002-338498

[ patent document 4 ] Japanese patent application laid-open No. 2002-322062

[ patent document 5 ] Japanese patent application laid-open No. Hei 11-139992

Disclosure of Invention

Accordingly, an object of the present invention is to provide a vitamin B-derived food₁Has reduced unpleasant taste and smell, and contains vitamin B at high concentration₁The oral liquid preparation of (1).

The present inventors have conducted various studies to solve the above problems and as a result, have found that by incorporating a specific amount of carbon dioxide in an oral liquid preparation, the amount of vitamin B derived from a high concentration can be effectively reduced₁The unpleasant taste and smell of the above substances, and thus the present invention has been completed.

Namely, the present invention provides a vitamin B-derived food₁Has reduced unpleasant taste and smell, and contains vitamin B1 μ g/mL or more₁And the gas internal pressure is 1.0 to 4.0kg/cm³Carbon dioxide (c).

In addition, the invention also provides vitamin B₁Oral liquid containing vitamin B₁In a method for reducing unpleasant taste and smell, vitamin B is contained in an amount of 1. mu.g/mL or more₁The oral liquid preparation has a gas internal pressure of 1.0 to 4.0kg/cm³Contains carbon dioxide.

According to the present invention, the content of vitamin B in a high concentration can be reduced₁From vitamin B in oral liquid preparations₁Unpleasant taste and smell. Therefore, the oral liquid preparation of the present invention has excellent feeling of taking and vitamin B₁Is useful as a refreshing drink, a quasi-drug, and particularly a drug.

Detailed Description

In the present invention, vitamin B is used as vitamin B₁Examples thereof include vitamin B such as thiamine, thiamine hydrochloride, thiamine nitrate, thiamine disulfide nitrate (dithioamin nitrate), thiamine disulfide, thiamine dicetyl sulfate, thiamine hydrochloride, furethiamine, oxytetramine, thiocoramine, sulbutiamine, bisfenthionamide, prosulethiamine, benfotiamine, decarboxylated coenzyme, and dibenzoylthioamine₁And one or more selected from salts and derivatives thereof.

In the present invention, vitamin B₁The content of (b) is 1. mu.g/mL or more, preferably 10 to 800. mu.g/mL, more preferably 25 to 800. mu.g/mL, and further preferably 45 to 200. mu.g/mL, based on the whole oral liquid preparation.

In the present invention, carbon dioxide may be used alone, or two or more kinds of gases other than carbon dioxide, such as oxygen, hydrogen, and nitrogen, may be mixed, but carbon dioxide is preferably used alone.

In the present invention, of carbon dioxideThe content of the active ingredient is 1.0 to 4.0kg/cm in terms of the internal pressure of the gas (the amount of gas dissolved in a unit volume) of the oral liquid as a whole³Preferably 2.2 to 3.7kg/cm³More preferably 2.5 to 3.5kg/cm³More preferably 3.0 to 3.4kg/cm³。

The pressure in the gas is lower than 1.0kg/cm³When the vitamin B derivative is used, vitamin B is not sufficiently obtained₁Unpleasant taste and/or odor reducing effect of (a) and is therefore not preferred.

Examples of the solvent of the oral liquid preparation of the present invention include water, ethanol, propylene glycol, and glycerin. Among them, water is preferably used.

In addition, in the oral liquid preparation of the present invention, vitamin B is excluded₁In addition to carbon dioxide, other components such as vitamin B which can be incorporated into a conventional oral liquid preparation may be incorporated as required₂Nicotinic acid, pantothenic acid and vitamin B₆Vitamin B₁₂Vitamins such as vitamin C; taurine; amino acids such as carnitine hydrochloride and cysteine; minerals such as crude drug, caffeine, diisopropylamine dichloroacetate, ferrum, and calcium; chondroitin, glucosamine, gamma-oryzanol, inositol, alpha-lipoic acid, biotin, folic acid, ursodeoxycholic acid, royal jelly, sodium aspartate, glucuronolactone, additives and the like.

As the above vitamin B₂Examples thereof include vitamin B such as riboflavin, riboflavin butyrate, riboflavin sodium phosphate, flavin adenine dinucleotide and the like₂And one or more selected from salts and derivatives thereof. Vitamin B₂The content of (b) is preferably 20 to 240 [ mu ] g/mL.

Examples of the nicotinic acid include one or more selected from nicotinic acid, nicotinamide, inositol hexanicotinate, decanoate and other nicotinic acids, salts thereof, and derivatives thereof. The content of nicotinic acid is preferably 120. mu.g/mL-6 mg/mL.

Examples of the pantothenic acid include one or more members selected from pantothenic acid such as calcium pantothenate, sodium pantothenate, panthenol, and pantethine, salts thereof, and derivatives thereof. The content of pantothenic acid is preferably 50. mu.g/mL-3 mg/mL.

As the above vitamin B₆Examples thereof include vitamin B compounds such as pyridoxine, pyridoxal, pyridoxamine, pyridoxine phosphate, pyridoxal phosphate and pyridoxamine phosphate₆And one or more selected from salts and derivatives thereof. Vitamin B₆The content of (B) is preferably 20. mu.g/mL-1 mg/mL.

As the above vitamin B₁₂Examples thereof include vitamin B such as cobalamin, cyanocobalamin, hydroxycobalamin acetate and methylcobalamin₁₂And one or more selected from salts and derivatives thereof. Vitamin B₁₂The content of (b) is preferably 0.01 to 6 [ mu ] g/mL.

Examples of the additives include a taste-improving agent, a sweetener, a stabilizer, a thickener, a dissolution aid, a pH adjuster, a colorant, and a perfume.

Examples of the taste-modifying agent include povidone, menthol, dipotassium glycyrrhizinate, malic acid, sodium malate, tartaric acid, sodium tartrate, succinic acid, sodium succinate, acetic acid, glutamic acid, sodium glutamate, citric acid, sodium citrate, gluconolactone, and sodium chloride.

Examples of the sweetener include sucrose, fructose, glucose, lactose, sorbitol, maltitol, erythritol, xylitol, trehalose, sucralose, honey, saccharin sodium, a stevioside extract, aspartame, acesulfame potassium, brown sugar, sweet protein, and licorice.

Examples of the stabilizer include povidone, glycerin, erythorbic acid and salts thereof, edetic acid and salts thereof, and metaphosphoric acid.

Examples of the thickener include sodium carboxymethylcellulose, agar, povidone, polyvinyl alcohol, and xanthan gum.

Examples of the dissolution aid include polysorbate, polyethylene glycol, polyoxyethylene hardened castor oil, povidone, and sodium hydroxide.

Examples of the pH adjuster include citric acid, sodium citrate, lactic acid, sodium hydroxide, hydrochloric acid, malic acid, sodium malate, tartaric acid, sodium tartrate, succinic acid, sodium succinate, acetic acid, gluconic acid, and phosphoric acid.

Examples of the coloring agent include tar coloring matter, ferric oxide, and caramel.

Examples of the essence include Apple Tea essence (Apple Tea Flavor), Apricot Tea essence (Apricot Tea Flavor), Rose Tea essence (Rose Tea Flavor), black Tea essence, Apple essence, pineapple essence, and the like.

As the pH of the oral liquid preparation of the present invention, to ensure vitamin B₁From the viewpoint of stability of pharmacological action of (3), the pH is preferably 1 to 6, more preferably 2.0 to 4.5. The pH adjustment may be performed by a conventionally known method, for example, by adding an acid or a base.

The oral liquid preparation of the present invention can be produced by a method for producing an oral liquid preparation which is a common method.

The oral liquid preparation of the present invention can be administered in the same manner as a conventional liquid preparation.

Examples

The present invention will be described in further detail below with reference to examples, but the scope of the present invention is not limited to the examples.

Production example 1 containing vitamin B₁And production of a comparative liquid preparation

Mixing vitamin B₁(nitrate salt) 0.4g, 1g, 2g, 10g were dissolved in 40L of pure water, respectively, and degassing was performed.

Then, any 8L of each of the obtained solutions or degassed pure water was placed in a pressure-resistant vessel, and carbon dioxide was introduced thereinto under pressure so that the gas internal pressure became 1.2kg/cm³、2.2kg/cm³、3.2kg/cm³. The liquid was filled into a washed brown glass bottle, and the bottle was capped to obtain an oral liquid preparation.

Test example 1

The oral liquid preparation of the manufacturing example or the oral liquid preparation of the comparative liquid preparation was taken to be about 5mL in the mouth of 5 healthy subjects, and carefully not swallowed so as to spread over the tongue, and then expectorated after about 15 seconds. The degree of unpleasant tastes such as astringency, pungency, bitterness, astringency, and harshness and the degree of unpleasant odor at this time were evaluated on 5 scales shown below.

Taste of the product

1: very unpleasant taste was perceived

2: unpleasant taste was felt

3: an unpleasant taste was slightly felt

4: it seems that unpleasant taste is felt

5: nothing is felt

Smell(s)

1: an extremely unpleasant smell was felt

2: unpleasant smell was felt

3: an unpleasant smell was slightly felt

4: an unpleasant smell seems to be felt

5: nothing is felt

Will contain vitamin B₁The taste evaluation of the oral liquid preparation of (1) is shown in table 1, and the odor evaluation is shown in table 2.

TABLE 1

TABLE 2

Preparation example 2 containing vitamin B₁And B₂And production of a comparative liquid preparation

Mixing vitamin B₁(nitrate) and vitamin B₂0.4g each, 0.8g in total, 1g each, 2g in total, 4g in total, 10g in total, and 20g in total of (phosphoric ester) were dissolved in 40L of pure water, and degassing was performed.

Then, any 8L of each of the obtained solutions or degassed pure water was placed in a pressure-resistant vessel, and carbon dioxide was introduced thereinto under pressure so that the gas internal pressure became 3.2kg/cm³. The liquid was filled into a washed brown glass bottle, and the bottle was capped to obtain an oral liquid preparation.

Test example 2

The degree of unpleasant taste and the degree of unpleasant odor of the oral liquid preparation produced in production example 2 were evaluated in 5 healthy subjects in the same manner as in test example 1.

Will contain vitamin B₁And B₂The taste evaluation of the oral liquid preparation of (4) is shown in Table 3, and the odor evaluation is shown in Table 4.

TABLE 3

TABLE 4

Preparation example 3 containing vitamin B₁And B₆And production of a comparative liquid preparation

Mixing vitamin B₁(nitrate) and vitamin B₆(hydrochloride salt) 0.4g each, 0.8g in total, 1g each, 2g in total, 4g in total, 10g in total, and 20g in total were dissolved in 40L of pure water, and degassing was performed.

Then, any 8L of each of the obtained solutions or degassed pure water was placed in a pressure-resistant vessel, and carbon dioxide was introduced thereinto under pressure so that the gas internal pressure became 3.2kg/cm³. The liquid was filled into a washed brown glass bottle, and the bottle was capped to obtain an oral liquid preparation.

Test example 3

The degree of unpleasant taste and the degree of unpleasant odor of the oral liquid preparation produced in production example 3 were evaluated by 5 healthy subjects in the same manner as in test example 1.

Will contain vitamin B₁And B₆The taste evaluation of the oral liquid preparation of (4) is shown in Table 5, and the odor evaluation is shown in Table 6.

TABLE 5

TABLE 6

Preparation example 4 containing vitamin B₁、B₂And B₆And production of a comparative liquid preparation

Mixing vitamin B₁(nitrate), vitamin B₂(phosphoric acid ester), vitamin B₆(hydrochloride salt) 0.4g each, 1.2g total, 1g total, 3g total, 2g total, 6g total, 10g total, 30g total were dissolved in 40L of pure water, and the solution was degassed.

Then, any 8L of each of the obtained solutions or degassed pure water was placed in a pressure-resistant vessel, and carbon dioxide was introduced thereinto under pressure so that the gas internal pressure became 3.2kg/cm³. The liquid was filled into a washed brown glass bottle, and the bottle was capped to obtain an oral liquid preparation.

Will contain vitamin B₁、B₂And B₆The taste evaluation of the oral liquid preparation of (4) is shown in Table 7, and the odor evaluation is shown in Table 8.

TABLE 7

TABLE 8

Claims (2)

1. A vitamin B₁Has reduced unpleasant taste and smell, and contains vitamin B1 μ g/mL or more₁And the gas internal pressure is 1.0 to 4.0kg/cm³Carbon dioxide (c).

2. Vitamin B₁Oral liquid containing vitamin B₁In a method for reducing unpleasant taste and smell, vitamin B is contained in an amount of 1. mu.g/mL or more₁The oral liquid preparation has a gas internal pressure of 1.0 to 4.0kg/cm³ComprisesCarbon dioxide.