JPH09286735A - Liquid drug for internal use - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain Kakkonto (a Chines herbal drug) effective for the mitigation of various symptoms of cold in the form of a liquid drug for internal use having good taste and flavor by compounding a specific sweetener of natural origin to an extract of Kakkonto. SOLUTION: An extract of Kakkonto is compounded with stevia. Kakkonto is a Chinese herbal drug preparation composed of kakkon (root of Pueraria lobata), Maou (stalk of Ephedar sinica), Taisou (fruit of Zizyphus vulgaris), Keihi (bark of Cinnamomum cassia), Shakuyaku (root of Paeonia albiflora), Kanzou (root of Glycyrrhiza glabra) and Kankyou (rhizome of Zingiber officinale) or Shoukyou (rhizome of Zingiber officinale). Stevia is a sweetener composed mainly of a sweetener component existing in the leaf of Stevia Rebaudiana Bertoni which is a perennial plant of the family Compositae. The main components of the sweetener are stevioside, rebaudioside A, dulcoside A, rebaudioside E, steviolbioside, steviol, etc., and especially a sweetener composed of 100% rebaudioside A is most preferable. The amount of the stevia is preferably 5-100mg, especially 10-50mg per 30mL of the liquid drug for internal use from the viewpoint of the taste and flavor of the drug. The weight ratio of the raw crude drug of the Kakkonto to stevia is preferably (100-3,500):1. The liquid drug may be incorporated with an antipyretic analgesic agent, an antitussive agent, etc., at need.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an oral liquid preparation containing Kakkonto.

[0002]

2. Description of the Related Art Most of the cold syndromes are caused by viral infections and are characterized by systemic symptoms such as fever, chills, inflammation of respiratory mucosa, and various pain symptoms. However, to date, no fundamental cure for colds has been developed, so symptomatic treatment is mainly used. Therefore, drugs effective against various symptoms including antipyretic analgesics, bronchodilators, antitussive expectorants, and anti-inflammatory agents have been developed. However, elderly people, children, people with weak stomachs, pregnant women, etc. tend to avoid these drugs due to anxiety about side effects and prefer Chinese medicine used since ancient times. Kakkonto, which is a Kampo formula, is known to be particularly useful for alleviating the early symptoms of a cold.

[0003]

Although Kakkonto is an excellent Kampo medicine, it often does not produce the expected therapeutic effect in actual patients. The present inventors have investigated the cause, and as a result, have found that the cause is low compliance (drug compliance). The decrease in compliance is
It is presumed that this is due to the poor taste of Kakkonto due to the unique astringency of astringency, fishy taste, and sourness of Kakkonto, and if Kakkonto is improved, compliance improves, resulting in a therapeutic effect. I also thought that it would improve.

[0004] In general, the simplest method in which an oral preparation does not feel unpleasant taste is to make a solid preparation (tablet, capsule, etc.) in which taste is hard to feel. But,
Since elderly people and children have weak swallowing ability, it is preferable to use an oral liquid preparation rather than a solid preparation in terms of ease of drinking. Therefore, it is necessary to improve the feeling of ingestion of Kakkonto liquid, but in the past, a method of cheating the unpleasant taste with sweetness such as sucrose and sorbitol was used to improve the feeling of ingestion of liquid. However, in such a method, if a sufficient amount of sweetness to cheat the taste is used, the sweetness remains in the mouth after taking, and the overall flavor is deteriorated, and if the sweetness is suppressed, the taste is sufficiently reduced. However, there was a drawback that the taste remained.

An object of the present invention is to provide Kakkonto, which is effective in alleviating various symptoms of a cold, as an oral liquid preparation having a good taste.

[0006]

[Means for Solving the Problems] The inventors of the present invention have conducted various studies to solve the above problems, and as a result, when stevia was added to an oral solution containing Kakkonto extract, a unique taste The present invention has been completed by finding that the feeling of irritation is obviously reduced and the feeling of ingestion is significantly improved. That is, the present invention is an oral liquid preparation containing Kakkonto extract and stevia.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION Kakkonto used in the present invention is Kakkon,
It is a Chinese herbal prescription consisting of mahuang, oju, cabbage, peony, licorice, and ginger or ginger, and the mixing ratio is 4
8 parts by weight, mahuang 3-4 parts by weight, Ojumu 3-4 parts by weight,
Katsura 2 to 3 parts by weight, peony 2 to 3 parts by weight, licorice 1.
An extract having a formulation of 5 to 2.5 parts by weight, dry ginger or ginger of 1 to 4 parts by weight is used. The extract can be obtained by a conventional method, and there is also a commercially available Kakkonto extract.

In the present invention, stevia is Stevi.
a Rebaudiana Bertoni is a sweetener mainly composed of the sweetening component contained in the leaves of the perennial plant of the Asteraceae family. Stevioside, rebaudioside A, dulcoside A, dulcoside B, rebaudioside E, and re It contains baudioside D, steviorbioside, rebaudioside B, steviol, etc., or one or more of these components are separated, and a known stevia extract is treated with an enzyme. It also includes those that have been chemically treated. Among these, those having a rebaudioside A content of 36% by weight or more are preferable in terms of flavor, and rebaudioside A is 1
The most preferable one is 00%.

From the viewpoint of flavor, the effective amount of stevia is preferably 5 mg to 100 mg, more preferably 10 mg to 50 mg in 30 ml of the oral liquid preparation. From the viewpoint of improving the feeling of ingestion, the compounding ratio is preferably in the range of 100: 1 to 3500: 1 in the weight ratio of the raw drug of Kakkonto to stevia.

In addition to Kakkonto and Stevia, the oral solution of the present invention may be an antipyretic analgesic, a bronchodilator, an antitussive, if necessary.
Expectorants, anticholinergic agents, antihistamines or antiallergic agents, anti-inflammatory or anti-inflammatory enzymes, caffeines,
Vitamins, other crude drugs, antacids and the like can be added.

Antipyretic analgesics include acetaminophen, aspirin or salts thereof, etenzamid, sazapyrine, isopropylantipyrine, ibuprofen, ketoprofen, naproxen, loxoprofen or salts thereof, diflunisal, flurbiprofen, fenoprofen or salts thereof, Planoprofen, fenbufen, diclofenac or salts thereof, alclofenac, amphenac or salts thereof, flufenamic acid, tolfenamic acid, mefenamic acid, tenoxicam, piroxicam and the like.

Bronchodilators include methylephedrine hydrochloride (including d-form and dl-form), ephedrine hydrochloride, methoxyphenamine hydrochloride, trimethoquinol hydrochloride, theophylline, aminophylline, diprophylline, proxyfilin, orciprenaline hydrochloride, chlorprenaline hydrochloride. , Isoprenaline hydrochloride, hexoprenaline sulfate, salbutamol sulfate, formoterol fumarate, tulobutenol hydrochloride, fenoterol hydrobromide, procaterol hydrochloride, clenbuterol hydrochloride, probuterol hydrochloride, mabuterol hydrochloride, terbutaline sulfate, pyrbuterol hydrochloride and the like.

The antitussives include codeine phosphate, dihydrocodeine phosphate, dextromethorphan hydrobromide, noscapine or its salts, dimemorphan or its salts, cloperastine or its salts, epradinone hydrochloride, clobutinol hydrochloride, oxerazine or its salts, Examples include isoaminyl citrate, pentoxyberine citrate, sodium dibnate, hydrocotarnine, hominoben hydrochloride, clofedanol hydrochloride, benproperin phosphate and the like.

The expectorant is potassium guaiacolsulfonate, bromhexine hydrochloride, ambroxol hydrochloride, L-methylcysteine hydrochloride, L-ethylcysteine hydrochloride,
Carbocysteine, acetylcysteine and the like.

The anticholinergics include belladonna (total) alkaloids, isopropamide iodide, ipratropium bromide, flutropium bromide, oxitropium bromide and the like.

The antihistamine or antiallergic agent means diphenhydramine or a salt thereof, promethazine hydrochloride, isothipendyl hydrochloride, clemastine fumarate,
Iproheptin hydrochloride, cyproheptadine hydrochloride, diphenylpyraline or salts thereof, dimethindene maleate, triprolidine hydrochloride, homochlorcyclidine hydrochloride,
Azelastine hydrochloride, ibudilast, sodium cromoglicate or salts thereof, oxatomide, amlexanox, ketotifen fumarate, astemizole, epinastine hydrochloride, carbinoxamine maleate, chlorpheniramine maleate (including d-form and dl-form), mequitazine, tranilast, feprinast, fumulinast Emedastine acid, ozagrel hydrochloride, tazanolast, pemirolast or salts thereof, suplatast tosilate and the like.

The anti-inflammatory agent or anti-inflammatory enzyme agent includes lysozyme chloride, serrapeptase, bromelain, semi-alkaline proteinase, pronase, tranexamic acid, glycyrrhizinic acid and related substances or salts thereof.

[0018] The caffeines are caffeine, anhydrous caffeine and the like.

The vitamins include vitamin B ₁ or a derivative thereof or salts thereof, vitamin B ₂ or a derivative thereof or salts thereof, vitamin C and the like.

Other crude drugs include cinnamon, saiko, bellflower, senega, senshi, carrot, chin peel, omiza, soybean leaf, half-summer, fine spicy pineapple, cabbage, ream, yellow rice, apricot kernel, peach kernel, Bakumon winter, river cucumber, spicy sauce etc.

Antacids include magnesium carbonate, magnesium oxide, magnesium silicate, magnesium hydroxide,
Synthetic aluminum silicate, aluminum sulfate, dihydroaluminum / aminoacetate, aluminum hydroxide / sodium bicarbonate coprecipitate, synthetic hydrotalcite, sucralfate and the like.

The oral solution of the present invention can be usually orally administered to an adult once or several times a day in divided doses. This dose can be appropriately adjusted depending on the age, weight, and medical condition.

The oral liquid preparation of the present invention can be prepared into a preparation by a conventional method. Further, in the preparation of an oral liquid preparation, sucrose fatty acid esters, polyoxyl stearate,
Emulsions can also be made with emulsifiers such as polyoxyethylene polyoxypropylene glycols and polysorbates. In addition, sucrose, sorbitol, saccharides such as mannitol, a thickener, a solubilizer, a buffer, a preservative, a fragrance, a coloring matter, a flavoring agent, a coloring agent, etc. are used as long as the effects of the present invention are not impaired. Can be.

[0024]

The present invention will be described in more detail with reference to the following examples and test examples.

Example A suitable amount of preservative (sodium benzoate) was added to and dissolved in a phosphate buffer solution adjusted to pH 3.5. Further, as an emulsifier, polysorbate 80 (NIKKOL TO10M),
Add appropriate amount of xanthan gum as a thickener and disperse evenly. Converted into a crude drug, Kakkon 8g, Mao 4
g, Ooju 4g, Katsura 3g, Peony 3g, Licorice 2
Kakkonto extract (made by Matsuura Yakugyo Co., Ltd.) that will be 1 g of ginger and 1 g of ginger
20 ml and Stevia (manufactured by Maruzen Pharmaceutical Co., Ltd.) of 15 mg were mixed, and the whole mixture was uniformly dispersed by a homomixer. Thereafter, the total amount was adjusted to 30 ml with purified water to prepare an oral liquid preparation.

Comparative Example 1 A control liquid preparation was prepared in the same manner as in Example 1 except that stevia was omitted.

Comparative Example 2 A control liquid preparation was prepared in the same manner as in Example 1, except that the stevia of Example 1 was changed to 1.2 g of D-sorbitol.

Test Examples Questionnaire Survey on Flavor 1) Panelists: 13 adults (6 men, 7 women) with cold symptoms in their 20s to 50s 2) Test method: Examples, Comparative Example 1 and In order to maintain the objectivity of the test, the liquid formulation of Comparative Example 2 was arbitrarily ordered and was blinded.
It was taken (the contents were not known to the panelists) and then the questionnaire was answered.

[Panel panel 1)
Liquid smell / aroma, 2) bitterness, 3) astringency / astringency, 4) sweetness, 5) sourness, 6) pungent, 7) body, 8) irritation, 9)
Aftertaste, 10) effect, 11) overall flavor impression, 1
2) Each item of preference (comprehensive evaluation) was scored on a scale of 10 out of 10 (10 points, 9 points,... 0 points from the one with the best feeling of taking), and the average points of each item were compared.

The results are shown in Table 1.

[0031]

[Table 1]

[0032]

EFFECTS OF THE INVENTION As is clear from the above test examples, the present invention has made it possible to provide an oral liquid preparation in which the unique taste of Kakkonto has been improved.

Claims (1)

[Claims] 1. An oral liquid preparation containing Kakkonto extract and stevia.