JP2003231647A - Oral liquid composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To obtain an oral liquid composition that can be deliciously taken, even after active ingredients of medicines and foods having unpleasant tastes, e.g. bitterness and peculiarly unpleasant smells are continuously ingested or can be smoothly ingested even by children without vomiting because of strange tastes and unbearable smells. <P>SOLUTION: The oral liquid composition comprises (a) the active ingredients of medicines and foods having unpleasant tastes and smalls, (b) fruit perfumes and (c) a sweetener in combination of potassium acesulfam and a stevia extract at a mass ratio of the acesulfam/the stevia extruct of 10/(1-4). <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral liquid composition, and more specifically, it gives an unpleasant taste such as bitterness, astringency, acrid taste and a unique unpleasant odor which the active ingredient of a medicinal food contains. The present invention relates to an oral liquid composition that can be improved and can be taken easily.

[0002]

2. Description of the Related Art Conventionally, many oral liquid preparations have been developed and widely put into practical use because of their ease of administration. In this case, in order to improve the unpleasant taste of the medicinal food active ingredient to be mixed in the oral liquid preparation or to mask the unique odor, it is practiced to add a sweetener such as a fragrance or sucrose to some extent. The taste is improved and the smell is masked.

However, it is still difficult to improve the taste and smell to such an extent that they are taken deliciously. For this reason, patients with illness may stop taking medications that they should continue to take during the course of the treatment, or children may spit out medications, resulting in delays in disease recovery and worsening of illness. There is a problem,
Further improvement is strongly desired.

[0004]

SUMMARY OF THE INVENTION It is an object of the present invention to solve the various problems in the prior art and achieve the following objects. That is, the present invention can be taken deliciously even if an oral solution containing a medicinal food active ingredient having an unpleasant taste such as bitterness or a unique unpleasant odor is continuously administered, and the oral solution even when taken by a child has It is an object of the present invention to provide an oral solution composition in which the taste and odor are prevented from being exhaled due to off-taste and off-odor.

[0005]

[Means for Solving the Problems] In order to solve the above problems, the present inventors have conducted intensive studies in combination with various sweeteners and flavors, and as a result, (a) a pharmaceutical food having an unpleasant taste and smell. By combining an active ingredient, (b) a fruit-based flavor, and (c) a sweetener in which acesulfame potassium and stevia extract are mixed in a fixed ratio, the synergistic effect of each of these ingredients results in a taste and flavor. It was found that an oral liquid composition having an extremely good aftertaste can be obtained, and the present invention has been completed.

That is, an object of the present invention is to provide the following oral solution composition to solve the above problems.

According to the invention of claim 1, (a) a medicinal food active ingredient having an unpleasant taste and smell, (b) a fruit-based flavor, (c) acesulfame potassium and stevia extract in a mass ratio, An oral solution composition comprising: acesulfame potassium: stevia extract = 10: 1 to 4; Claim 2
Of the invention, the active ingredient of medicinal food of component (a) is a cold medicine,
The oral liquid composition according to claim 1, which is one or more selected from antipyretics, analgesics, antiphlogistics, antitussives, expectorants, antihistamines, hemostatics, crude drugs, vitamin B groups and food additives. is there. In the invention of claim 3, the fruit-based flavor of the component (b) is one or more selected from the group consisting of citrus flavor, grape flavor, Prunus fruit flavor and apple flavor. The oral solution composition according to 1 or 2. In the invention of claim 4, the sweetener of the component (c) is 0.005 to 0.3 W / based on the total amount of the oral solution composition.
The oral liquid composition according to any one of claims 1 to 3, which is blended with V%. The invention of claim 5 is the oral liquid composition according to any one of claims 1 to 4, which has a pH of 2 to 5.

According to the present invention, acesulfame potassium, which expresses sweetness quickly, masks the bitterness that expresses quickly, while the active ingredient of medicinal foods having unpleasant tastes having bitterness, astringency and astringency is masked. Stevia extract that remains after sweetness develops slowly after ingestion, while improving the taste by suppressing the astringent taste, fruit flavors may mask the unpleasant odor of pharmaceutical food active ingredients, and by these synergistic effects , Having a very pleasant taste.

Further, when Stevia extract is not blended in the oral liquid composition, the unpleasantness masking of the fruit-based flavor is not sufficient, and Stevia extract is also used as a flavor enhancer (synergy improving agent for taste and smell). It is estimated to be working.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION The present invention will be described in more detail below. The oral liquid composition of the present invention contains (a) a medicinal food active ingredient having an unpleasant taste and smell, (b) a fruit-based flavor, and (c) a sweetener comprising acesulfame potassium and a stevia extract. However, other components are contained if necessary.

The active ingredient of medicinal foods having an unpleasant taste such as bitterness, astringency, and astringency of the above-mentioned component (a) and a unique unpleasant odor includes cold remedies, antipyretics, analgesics, antiphlogistics, antitussives,
Pharmaceuticals such as expectorants, antihistamines, hemostatics, crude drugs, B vitamins, food additives, etc.
The seeds may be used alone or in combination of two or more.

Examples of the above-mentioned pharmaceutical agents include acetaminophen, aspirin, phenacetin, mefenamic acid,
Antipyrine, phenylbutazone, sulpirine, diclofenac sodium, ibuprofen, ketoprofen, naproxen, epirizole, tiaramide hydrochloride, indomethacin, pentazocine, acetylcholine chloride, alimemazine hydrochloride, cyproheptadine hydrochloride, diphenhydramine hydrochloride, diphenhydramine hydrochloride, chlorpheniramine maleate, phosphoric acid phosphate. Dihydrocodeine phosphate, dextromethorphan hydrobromide, pentoxyberine citrate, theophylline, aminophylline, ephedrine hydrochloride, epinephrine hydrochloride, salbutamol sulfate,
Examples include trimethoquinol hydrochloride, procaterol hydrochloride, methylephedrine hydrochloride, phenylpropanolamine hydrochloride, guaifenesin, tranexamic acid, anhydrous caffeine, and caffeine. These may be used alone or in combination of two or more. You may.

The herbal medicines include, for example, aloe, fennel, turmeric, oyster, corydalis, ages, ougi, ousei, onji, guarana, kokushi, swordfish, touki, eucommia, carrot, amarogentin, sardine,
Oataku, Ouren, Gautu, Cascala Sagrada, Cuckoo, Cascalyllaceae, Crapeweed, Crowcon, Ginkgo, Pheasant, Kyounin, Kihada, Kuko, Kujin, Keigai, Keihi, Ketsumeishi, Kengoshi, Gentiana,
Gencho ginger, koujin, kobushi, koboku, gobo, goshitsu, goshuyu, gorushi, colombo, konzlango, psycho, sashishi, saffron, sandscon, dio, shikon, perilla, peony, shazin (tsuraiganenjin), shazen (plantain), jascent, jascent Gourd, gall, seihi, boiled ginger, senkyu, senkotsu, centaurium grass, senburi, senbou, senso, senna, sojutsu, sohakuhi, soyo, daioh, bamboo shoot ginseng, chimo, chillet grass, chimpi,
Spruce, tounin, turmeric, bittern, carrot, juniper, juniper, belladonnacon, henoposite oil,
Yakuchi, yutan, mugwort, mugwort, bitter tincture,
Jisyu, hop, homika, bowie, maoh, mokutsu, mokko, ryutan, gentian, luzonka, forsythia, carrot, senega, kyokyou, ginkgo,
Examples include royal jelly, and these may be used alone or in combination of two or more.

Examples of the vitamin B group include vitamin B ₁ group (for example, thiamine, thiamine nitrate, thiamine hydrochloride, vitamin B ₁ derivative, etc.), vitamin B ₂ group (for example, riboflavin, sodium riboflavin phosphate phosphate, butyric acid). Riboflavin, etc.), vitamin B ₆ group (for example,
Pyridoxine, pyridoxal, pyridoxamine and phosphoric acid or hydrochloride thereof, etc., vitamin B ₁₂ group (eg, cobalamin, cyanocobalamin, methylcobalamin, etc.) and the like, and these may be used alone or in combination of two kinds. You may use together the above.

Examples of the above-mentioned food additives include calcium pantothenate, potassium chloride, starch husk powder, niacinamide, biotin, seaweed powder, nicotinic acid amide, cyanocobalamin, and the like. Also, two or more kinds may be used in combination.

The active ingredient of medicinal foods having the unpleasant taste and smell of the above-mentioned component (a) is mixed in an effective amount range which produces a medicinal effect according to each purpose. It is preferable to add 0.001 to 1 W / V%.

Examples of the fruit-based fragrance as the component (b) include citrus-based fragrances such as mandarin orange, orange, lemon, grapefruit, and seaquat, red grape,
Grape flavors such as Muscat, Prunus fruit flavors such as peach, apricot, plum, apricots, apple flavors such as green apples, tropical fruit flavors such as passion fruit, pineapple, lychee and banana, and strawberry flavors. However, these may be blended alone or in combination of two or more. Among these,
Citrus-based flavors, grape-based flavors, Prunus fruit-based flavors, and apple-based flavors are particularly preferable in that they are suitable for improving the flavor.

The component (b), the fruit-based flavor, is preferably blended in an amount of 0.001 to 1.0 W / V%, preferably 0.05 to 0.5 W / V%, based on the total amount of the oral liquid composition. Is more preferable.

The sweetener (c) is a mixture of stevia extract and acesulfame potassium. Here, the compounding ratio of the acesulfame potassium and the stevia extract is a mass ratio of 1 to 4 stevia extract to 10 parts of acesulfame potassium, and particularly 1.5 to 3
Is preferred. When the amount of Stevia extract is less than 1, the taste is not sufficiently improved. On the other hand, when the amount of Stevia extract is more than 4, the stevia extract has a strong sweetness, resulting in a dull sweetness and a poor feeling of ingestion.

The component (c), stevia extract, is a perennial plant of the Asteraceae Stevia Rebaud.
iana) leaves are extracted and purified to have a sweetness component of 80% purity.
The above is a natural sweetener having a sweetness 300 times or more that of sugar. As this Stevia extract,
Also included are stevioside, rebaudioside A, rebaudioside C, rebaudioside D, rebaudioside E, zulcoside A alone, and α-glucosyl compounds obtained by reacting these with glucosyltransferase.

Acesulfame potassium [6-methyl-1,2,3-oxathiazine-4 (3) as the component (c).
H) -one-2,2-dioxide potassium salt (C ₄ H
₄ KNO ₄ S, molecular weight: 201.24)] is a synthetic sweetener having the following structural formula, and has a sweetness of about 200 times that of sucrose when compared to a 5% sucrose aqueous solution.

[0022]

[Chemical 1]

The sweetener consisting of the acesulfame potassium and the stevia extract of the above-mentioned component (c) can be blended in an amount depending on the components having an unpleasant taste and odor in the oral liquid composition. 0.005-
0.3 W / V%, preferably 0.01 to 0.15 W / V
%. When the compounding amount of the acesulfame potassium and the stevia extract is less than 0.005 W / V%, the taste improving effect becomes insufficient, while when it exceeds 0.3 W / V%, the sweetness is too strong and the taste is dull. , And it may be difficult to take.

In addition to the sweetener as the component (c), fructose, sucrose, and other ingredients may be used as long as the taste improving effect of the oral liquid composition of the present invention is not excluded.
Glucose, maltose and other sugar sweeteners may be blended, and in order to provide a refreshing sweetness, sugar alcohols such as maltitol, xylitol, erythritol, sorbitol, mannitol, aspartame, syclarose,
You may mix | blend high intensity sweeteners, such as saccharin.

The oral liquid composition of the present invention comprises the above (a) to
A liquid pH containing the necessary components of (c) and using an acid
2 to 5 to enhance the sourness, the refreshing feeling can be enhanced and the taste can be more easily taken.
In this case, in order to adjust the pH of the oral solution composition to 2 to 5, for example, an organic acid such as acetic acid, citric acid, malic acid, tartaric acid, ascorbic acid, or phosphoric acid is used as a pH adjuster. Is preferred.

The above-mentioned other components are not particularly limited and may be appropriately selected depending on the intended purpose. Examples thereof include preservatives, preservatives, fragrances, fragrances, cooling agents, surfactants, Solubilizers, emulsifiers, solvents, buffers, suspensions, thickeners, colorants, stabilizers, solubilizers and the like,
These may be used alone or in combination of two or more.

Examples of the preservatives and preservatives include sodium sorbate, benzoic acids (benzoic acid, sodium benzoate, etc.), parabens (ethyl paraoxybenzoate, butyl paraoxybenzoate, propyl paraoxybenzoate, etc.), etc. Is mentioned.

Examples of the surfactants, solubilizers, emulsifiers, and solvents include nonionic surfactants such as sucrose fatty acid esters, polyoxyethylene hydrogenated castor oils, polysorbates and pluronics, and ethanol. , Distilled water for injection, purified water and the like.

Examples of the suspending agent and thickening agent include gum arabic, crystalline cellulose, bee gum, xanthan gum, gelatin, metrose and edible salts thereof, carmellose and edible salts thereof, and the like. Examples of the colorant include caramel, β-carotene, various food colors (food yellow No. 1, food red No. 2, etc.) and the like. Examples of the stabilizer include an edible salt of edetic acid, sodium chloride, and an edible salt of pyrosulfite.

Other ingredients (preservatives, preservatives, flavors, fragrances, cooling agents, surfactants, solubilizers, emulsifiers, solvents, buffers, suspending agents, thickeners, coloring agents) , Stabilizers, solubilizing agents, etc.) in the oral liquid composition are not particularly limited, and are preferably appropriately contained in the conventional oral solutions.

The method for preparing the oral solution composition is not particularly limited, and each component is usually mixed with a part of a solvent such as purified water and dissolved, and the remaining solvent is added to prepare a liquid amount. If necessary, the pH is adjusted using acid or alkali.

The oral liquid composition of the present invention may be a drug, quasi drug, or health food that is orally administered in a liquid form, such as a liquid agent (for example, syrup or drink), a suspension,
It can be formulated into emulsions, granules, powders, capsules, etc., and is used for medicinal purposes such as nourishing tonics, gastric-sensing agents, antipyretic analgesics, bronchodilators, etc. Applicable.

[0033]

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

[Example 1] Oral solution Add the ingredients shown in Table 1 below, purified water, polyoxy hydrogenated castor oil and sodium benzoate, and further add citric acid to adjust the pH.
Of the present invention 1
2 and comparative liquids 1 to 4 were manufactured.

Next, the panelists 17 for each oral liquid preparation
The sensory evaluation of the four items of bitterness / astringency / astringency, good aftertaste, good front taste, and unique discomfort by name was performed according to the following evaluation criteria, and the average value of the evaluation results was calculated. The results are shown in Table 1.

<Evaluation criteria> 5 points: excellent 4 points: somewhat excellent 3 points: Normal 2 points: somewhat inferior 1 point: inferior

[0037]

[Table 1]

[Example 2] Oral syrup The components shown in Table 2 below, purified water, polyoxyethylene hydrogenated castor oil and sodium benzoate were added, and the pH was adjusted to 100 mL with citric acid to prepare the product 3 of the present invention. 4 and comparative products 5 to 7 were manufactured.

Next, for each oral syrup, 18 panelists selected the bitterness, astringency, astringency, and good aftertaste.
The sensory evaluations of the four items of the good taste and unique discomfort were performed in the same manner as in Example 1 above, and the average value of the evaluation results was calculated. The results are shown in Table 2.

[0040]

[Table 2]

[Example 3] Oral liquid agent The components shown in Table 3 below, polyoxyethylene hydrogenated castor oil, sodium benzoate and purified water were added, and the pH was adjusted to 3.5 with citric acid. 50 mL of oral liquid
Got

[0042]

[Table 3]

[Example 4] Oral liquid formulation The components shown in Table 4 below, propylene glycol, sodium benzoate and purified water were added, and the pH was adjusted to 4 with citric acid.
As a result, 50 mL of the oral liquid preparation of Example 4 was obtained.

[0044]

[Table 4]

[Example 5] Oral liquid agent The components shown in Table 5 below, polyoxyethylene hydrogenated castor oil, sodium benzoate and purified water were added, and the pH was adjusted to 3.2 with citric acid. Oral liquid medicine 30mL
Got

[0046]

[Table 5]

Each of the oral liquid preparations of Examples 3 to 5 was able to be taken deliciously because unpleasant tastes such as bitterness of the active ingredient of medicinal foods and unique unpleasant odors were suppressed.

[0048]

As described above, according to the present invention,
It can be taken deliciously even if an oral solution containing a medicinal food active ingredient having an unpleasant taste such as bitterness or a unique unpleasant odor is continuously administered, and it is exhaled due to the offensive taste and odor of the oral solution even when administered to children. An oral liquid composition with improved taste and odor that does not end up being obtained is obtained.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61K 47/12 A61K 47/12 47/14 47/14 47/26 47/26 47/46 47/46 A61P 11/00 A61P 11/00 // A61K 31/137 A61K 31/137 31/167 31/167 31/4402 31/4402 31/485 31/485 31/522 31/522 F term (reference) 4B018 MD61 MD94 ME14 MF02 4C076 AA22 BB01 CC01 CC03 CC09 CC15 DD08F DD41R DD46F DD61T DD68T FF12 FF16 FF39 FF52 FF61 4C086 AA01 AA02 BC17 CB07 CB23 MA03 MA05 MA23 MA52 NA09 MA03 NA03 MA03 NA03 MA03 NA03 MA03 NA03 MA03 NA03 MA10 NA02 MA10 NA03 MA10

Claims (5)

[Claims] 1. Acesulfame potassium: stevia extract in a mass ratio of (a) a medicinal food active ingredient having an unpleasant taste and smell, (b) a fruit-based flavor, and (c) acesulfame potassium and stevia extract in a mass ratio. = 10: 1 to 4 and a sweetener blended so as to be contained therein. 2. The active ingredient of medicinal food of component (a) is selected from cold medicines, antipyretics, analgesics, antiphlogistics, antitussives, expectorants, antihistamines, hemostatics, herbal medicines, vitamin B group and food additives. The oral liquid composition according to claim 1, which is one kind or two or more kinds. 3. The fruit-based flavor as the component (b) is one or more selected from the group consisting of citrus-based flavor, grape-based flavor, Prunus fruit-based flavor and apple-based flavor. The oral liquid composition according to 2. 4. The internal-use liquid composition according to claim 1, wherein the sweetener as the component (c) is added in an amount of 0.005 to 0.3 W / V% based on the total amount of the internal-use liquid composition. 5. The oral liquid composition according to claim 1, which has a pH of 2 to 5.