JPH11302189A - Composition for cold - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject composition capable of being easily prepared into preparations, masking the bitter taste of an antiallergic medicine without relying on a sweetener and thereby having an excellent oral administration taste by compounding an Echinacea plant and the antiallergic medicine. SOLUTION: This composition contains (A) an Echinacea plant and (B) an antiallergic medicine preferably in an amount of 0.0005-0.2 pt.wt. per pt.wt. of the component A. The component A is an Echinacea plant which is a kind of herb originated in the North American continent and belongs to the family Compositae. The use form of the composition includes powder preparations, teas, extracts and solid preparations. The Echinacea plant is exemplified by Echinacea purpurea and Echinacea angustifolia. The component B is exemplified by carbinoxamine maleate, chlorpheniramine maleate, brompheniramine maleate, ketotifen fumarate and mequitazine.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a medicament for the so-called cold syndrome, and to a common cold composition having an improved feeling of taking.

[0002]

2. Description of the Related Art The so-called cold syndrome is a viral respiratory infection, which is characterized by systemic symptoms such as fever and chills, inflammation of respiratory mucosa, various pain symptoms and malaise. , Is one of the acute inflammatory diseases. For such diseases, the development of a drug having an antiviral action is most effective because various viruses cause the onset. However, the cold virus is prone to mutation, and effective antiviral drugs have not been put to practical use so far. Therefore, in order to alleviate individual symptoms, compositions for colds have been conventionally developed mainly for symptomatic treatment.

[0003] The main components of these symptomatic drugs are:
Antipyretic analgesics, antiallergic drugs (including antihistamines), bronchodilators, antitussive expectorants, nonsteroidal anti-inflammatory drugs, etc. have been used, and these are mainly effective against the central nervous system. Common cold compositions are at the center of development.

[0004] However, none of these drugs is satisfactory in the feeling of taking. In particular, carbinoxamine maleate, phenylamine maleate, ketotifen fumarate, epinastine hydrochloride, mequitazine, and the like, which are antiallergic agents, are known to have a unique bitter taste. For this reason, a technique for improving the feeling of taking a drug is regarded as important from the viewpoint of improving compliance. Examples thereof include pharmaceutical devising such as sugar coating and coating with a film coating, and a bitterness masking technique by adding a sweetener such as sugar.

[0005]

However, these bitterness masking techniques require the use of a sweetener when a plurality of steps are required for the preparation of a preparation or when a plurality of drugs are compounded with emphasis on the efficacy. However, there were problems such as insufficient bitterness masking of the drug.

[0006] Accordingly, an object of the present invention is to provide a cold-receiving composition which is easy to prepare and has an excellent feeling of taking, which masks the bitter taste of antiallergic drugs without relying on sweeteners.

[0007]

Means for Solving the Problems The present inventors have made intensive studies to solve the above-mentioned problems, and as a result, by adding echinacea, that is, an extract of a plant belonging to the genus Echinacea or a crude drug, to an antiallergic drug. It was found that the feeling of taking was significantly improved.

[0008] That is, the present invention is a common cold composition comprising echinacea and an antiallergic drug.

The echinacea referred to in the present invention is a plant belonging to the genus Echinacea belonging to the family Asteraceae, which is a kind of herb native to the continent of North America. In Europe, in particular, it is used for the purpose of preventing colds and reducing the symptoms of colds. It is widely used as a crude drug material having an activating effect. Examples of the use form include powders, teas, extracts, and solid preparations, which have a strong astringency peculiar to plants, particularly a so-called green odor, and therefore, it is hard to say that the feeling of taking Echinacea itself is good. It is.

Surprisingly, however, the simultaneous combination of echinacea having such a peculiar taste and an antiallergic drug having a peculiar bitterness cancels out the peculiar taste of each, and as a result, This makes it possible to prepare a cold composition having an improved feeling of taking.

The echinacea plants used in the present invention include Echinacea purpura.
ea ), Echinacea angustifolia ( Echinacea)
angustifolia ), Echinacea parida ( Echinacea pall)
ida , Echinacea paradox
a ), Echinacea tennessensis
sseensis ), Echinacea sanguinea ( Echinacea sang)
uinea ), Echinacea simulat
a ), Echinacea atroluvens ( Echinaceaatrorube )
ns ) and the like. In the present invention, these related plants can also be used.

[0012] These extracts of Echinacea spp.
Water, hot water, an organic solvent such as ethanol, or a mixture thereof can be used, which is prepared by a general extraction method. In particular, when the present invention is made into a solid preparation, a powder of a crude drug can be used.

Examples of the antiallergic drug which can be used in the present invention include carbinoxamine maleate, pheniramine maleate, chlorpheniramine maleate, brompheniramine maleate, ketotifen fumarate, epinastine hydrochloride, mequitazine and the like. Is suitable for chlorpheniramine maleate, ketotifen fumarate and mequitazine.

In the present invention, in order to prepare an anti-cold composition having a good feeling of taking, it is necessary to adjust the mixing ratio of echinacea to an antiallergic drug. Although the ratio varies slightly depending on the antiallergic drug, the antiallergic drug is generally 0.0005 per 1 part by weight of the echinacea component.
What is necessary is just to adjust within the range of -0.2 weight part. For example, carbinoxamine maleate 0.005 to 0.5 parts by weight, chlorpheniramine maleate and related substances 0.005 to 0.75 parts by weight, ketotifen fumarate 0.0005 to 0.1 parts by weight, 0.01 to 0.75 parts by weight for epinastine hydrochloride, 0.01 to 0.75 parts by weight for mequitazine
What is necessary is just 0.2 weight part.

[0015]

BEST MODE FOR CARRYING OUT THE INVENTION As a dosage form of the composition for colds of the present invention, any liquid or solid preparation can be used as long as it is an oral medicine, but from the viewpoint of feeling of administration, tablets and capsules can be used. And the like. As a production method at that time, it is possible to use various excipients according to the dosage form and to produce by a general method.

Further, in the present invention, various drugs can be blended in addition to the echinacea and the antiallergic drug. For example, drugs such as antipyretic analgesics, anti-inflammatory enzymes, bronchodilators, antitussives, expectorants, sympathomimetics, anticholinergics, caffeines, vitamins, other crude drugs, antacids, etc. It can be compounded in accordance with the standard of cold medicine etc. described in the production guidelines (1995 edition, Pharmaceutical Industry News).

The composition for colds of the present invention may contain various excipients, lubricants, surfactants, solubilizers, buffers, preservatives, fragrances, dyes, sweeteners, depending on the final dosage form. Flavoring agents, coloring agents and the like can be used.

[0018]

According to the present invention, it is possible to obtain a cold remedy composition which does not exhibit the bitter taste peculiar to antiallergic drugs and has a remarkably improved feeling upon taking.

[0019]

<Example 1> The following components and amounts were weighed and uniformly mixed.
Tablets were obtained by tableting to a tablet weight of 300 mg.

Acetaminophen 900 g (the same applies to the following units) Dihydrocodeine phosphate 24 Methylephedrine hydrochloride 60 Chlorpheniramine maleate 6 Echinacea soft extract 24 (manufactured by Nattermann, 3.0 g equivalent to crude drug, same as the following examples) ) Guaifenesin 125 anhydrous caffeine 50 lactose 275 low-substituted hydroxypropylcellulose 275 magnesium stearate 35 hydrogenated castor oil 26 <Example 2> The following components and amounts were weighed and uniformly mixed. Weight per tablet 30 by direct hitting method
Tablets were obtained by tableting so as to be 0 mg.

Acetaminophen 900 g (the same applies to the following units) Codeine phosphate 18 Methylephedrine hydrochloride 60 Carbinoxamine maleate 12 Echinacea soft extract 24 Guaiphenesin 125 Anhydrous caffeine 50 Lactose 275 Low-substituted hydroxypropylcellulose 275 Magnesium stearate 32 Hardened castor oil 29 <Example 3> The following components and amounts were weighed and uniformly mixed, and then the obtained mixed powder was weighed by a direct compression method to a tablet weight of 30.
Tablets were obtained by tableting so as to be 0 mg.

Acetaminophen 900 g (the same applies to the following units) Benproperin phosphate 30 Methylephedrine hydrochloride 60 Mequitadine 4 Echinacea soft extract 24 Guaiphenesin 125 Anhydrous caffeine 50 Lactose 275 Low-substituted hydroxypropylcellulose 271 Magnesium stearate 32 Hardened castor oil 29 < Example 4> The following components and amounts were weighed and uniformly mixed, and then the obtained mixed powder was weighed by a direct compression method to a tablet weight of 30.
Tablets were obtained by tableting so as to be 0 mg.

Ibuprofen 450 g (the same applies to the following units) Benproperin phosphate 30 Methylephedrine hydrochloride 60 Ketotifen fumarate 2 Echinacea soft extract 24 Guaifenesin 125 Lactose 374 Low-substituted hydroxypropylcellulose 360 Magnesium stearate 40 Hardened castor oil 35 <Example 5> The following components and amounts were weighed and uniformly mixed, and the resulting mixed powder was weighed by a direct compression method to a tablet weight of 30 tablets.
Tablets were obtained by tableting so as to be 0 mg.

Ibuprofen 450 g (the same applies to the following units) Hominobene hydrochloride 80 Methylephedrine hydrochloride 60 Epinastine hydrochloride 20 Echinacea soft extract 24 Lysozyme chloride 90 (titer) Lactose 360 Low-substituted hydroxypropylcellulose 343 Magnesium stearate 40 Hardened castor oil 35 <Test Example> Comparative Example 1 prepared by replacing the echinacea soft extract of Example 1 with an equal amount of lactose, and Comparative Example 2 similarly prepared by replacing the echinacea soft extract of Example 3 with an equal amount of lactose were prepared according to the respective examples. did.

Examples 1 and 3 of the present invention, Comparative Example 1,
Comparative Example 2 was taken by 25 people suffering from a cold, and the impression at the time of taking "A: very easy" and "B:
"Easy", "C: Neither of these", or "D: Difficult to see".
Table 1 shows the results.

[0026]

[Table 1]

────────────────────────────────────────────────── ─── Continued on the front page (51) Int.Cl. ⁶ Identification code FI C07D 453/02 C07D 453/02 487/04 150 487/04 150 // C07D 409/04 211 409/04 211

Claims (2)

[Claims] 1. A cold composition comprising echinacea and an antiallergic drug. 2. The antiallergic agent according to claim 1, wherein the antiallergic agent is at least one selected from the group consisting of carbinoxamine maleate, chlorpheniramine maleate, brompheniramine maleate, ketotifen fumarate, epinastine hydrochloride, and mequitazine. Cold remedy composition.