JP2003081828A - Medicine composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a medicine composition which can surely remove or alleviate excessive nosal drip (snotter) symptoms among symptoms caused by viral cold, bacterial cold, influenza, tonsillitis, allergy, pollinosis and atopy. SOLUTION: This medicine composition having enhanced effect on excessive nosal drip symptoms is obtained by formulating (a) one kind selected from the group consisting of zafirlukast and its salts and (b) one kind selected from the group consisting of belladonna alkaloid or belladonna total alkaloids, belladonna essence, scopolia extract, isopropamide iodide and stramonium essence.

Description

Description: BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a pharmaceutical composition having an improved effect on nasal hyperplasia (nose nose) associated with cold syndrome or rhinitis. 2. Description of the Related Art Zafilkast is used as an antiallergic drug, and is also known as belladonna (total) alkaloid,
Belladonna extract, funnel extract, isopropamide iodide or datura extract have long been widely used as parasympathetic blockers. As described above, various drugs are known, but a pharmaceutical composition combining zafilkast and belladonna (total) alkaloid, belladonna extract, funnel extract, isopropamide iodide or datura extract is not known. On the other hand, many pharmaceutical compositions have been known so far, but all have insufficient effects on nasal hyperplasia as a nasal mucosa hypersecretion lesion associated with cold syndrome and the like, and thus a sufficiently satisfactory clinical effect is obtained. I didn't. [0003] The cold syndrome is a respiratory infection. Generally, it is a disease accompanied by various systemic symptoms such as malaise and local inflammatory symptoms centering on the upper respiratory tract. Although the development of a drug having an antiviral effect that suppresses the infection and proliferation of the virus that causes a cold is desired as a causative therapy, at present the state of the art is still developing effective ones. Rather, symptomatic treatments aimed at improving individual symptoms are central to the treatment of colds. This is the same when caused by bacterial infection. The core of symptomatic treatment is relief of various symptoms by antipyretic analgesic components, antitussive components, bronchodilator components, etc. Belladonna (total) alkaloids, belladonna extract, funnel extract, isopropamide iodide, datura extract, etc. Are originally used for such purposes. Therefore, especially in the medical setting, the use of the combination formulation has not been performed. However, colds and rhinitis have various symptoms at the same time when they become ill, and they change simultaneously.Therefore, in order to cure various symptoms early, reduce the frequency of drug use and prevent the occurrence of side effects, There has been a demand for the development of a compounding agent in which the compounding amount of the components is reduced and the effect is enhanced, and it has been important how to formulate a compound that achieves such purpose. [0005] Especially in daily life, among the various symptoms caused by colds, excessive nasal discharge, especially nasal symptoms, causes respiratory failure, distracts the concentration of things and causes unexpected accidents. Not only have the danger of causing
Must be compensated by oral respiration, and the direct uptake of fresh air into the lungs leads to secondary infection with new viruses and bacteria, leading to the disadvantage of prolonged symptoms. This is exactly the same in the case of nasal discharge caused by allergic rhinitis. In other words, how to eliminate nasal overdose symptoms as early as possible and prevent new secondary infections or sensitization of allergens beforehand to relieve or cure the symptoms is an important point in the actual treatment. ing. The present invention has, therefore, been made in view of the above-mentioned prior art, and has as its object the purpose of viral cold, bacterial cold, influenza, tonsillitis,
It is an object of the present invention to provide a pharmaceutical composition capable of reliably removing or alleviating nasal overuse (nose nose) among various symptoms caused by allergy, hay fever and atopy. Means for Solving the Problems The inventors of the present invention have conducted intensive studies for the above purpose, and as a result, by combining a specific antiallergic drug and a parasympathetic blocker as active ingredients, the nasal mucosa has been improved. The present inventors have found that the present invention has a dramatic effect on eliminating or alleviating the symptoms of excessive nasal discharge (nose nose), and completed the present invention. That is, the present invention relates to (a) one kind selected from the group consisting of zafilukast and salts thereof and (b) one kind selected from the group consisting of belladonna (total) alkaloids, belladonna extract, funnel extract, isopropamide iodide and datsura extract. It is a pharmaceutical composition having an enhanced effect on nasal polyp symptoms, which is formulated. In the present invention, zafirlukast is also referred to as zafirlukast, and all substances having the same structural formula including stereoisomers are referred to regardless of the name. Further, in the present invention, the belladonna (total) alkaloid refers to both a belladonna alkaloid or a belladonna total alkaloid,
It is an alkaloid extracted from the herbal medicine Belladonna (Atoropa belladonna Linne). In the present invention, the salts include hydrochloride, nitrate, sulfate, phosphate, oxalate, maleate,
Fumarate, tosylate, besylate, hydrobromide and the like. The pharmaceutical composition of the present invention can be usually orally administered to an adult once or several times a day. This dose can be appropriately increased or decreased depending on the age, weight, and medical condition. The amount is 1 for each adult
Per day, (a) zafilkast is preferably from 10 to 80 mg, and more preferably from 20 to 80 mg. Similarly,
(B) Belladonna (total) alkaloids are 0.06-1.
0 mg is good, preferably 0.1-0.6 mg is good,
Belladonna extract is preferably 6 to 100 mg, preferably 10 to 60 mg, and the funnel extract is 6 to 100 mg.
, Preferably 10 to 60 mg, isopropamide iodide is preferably 0.75 to 10 mg, preferably 1.0 to 7.5 mg, and datsura extract is 0.06 to 10 mg.
1.0 mg is preferred, and preferably 0.1 to 0.6 mg. The amount of each component (b) is usually 0.0001 to 10 parts by weight, preferably 0.0002 to 3 parts by weight, based on 1 part by weight of the component (a). DETAILED DESCRIPTION OF THE INVENTION The pharmaceutical composition of the present invention is prepared in the form of tablets, capsules, granules, fine granules, powders, chewables, foaming agents, drops, mouth dissolving agents, dry syrups. It is used as a preparation for oral administration such as an oral solution.
These preparations can be prepared by a conventional method. In the solid preparation, carriers used for preparation of the preparation include lactose, starch, sugar, mannitol, excipients such as crystalline cellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, gelatin, binders such as PVP, carboxymethylcellulose calcium, Disintegrators such as low-substituted hydroxypropylcellulose, magnesium stearate, hydrogenated castor oil, lubricating agents such as talc, and other solubilizing agents as necessary, buffers,
Preservatives, flavors, dyes, flavoring agents and the like can be used. [0011] In the oral liquid preparation, the carrier used for the preparation of the preparation includes sucrose fatty acid esters, polyoxyl stearate, polyoxyethylene polyoxypropylene glycols, polyoxyethylene monofatty acid esters and the like. Agents, thickeners such as synthetic aluminum silicate, magnesium silicate, magnesium carbonate, magnesium oxide, and magnesium aluminate metasilicate; organic acid and inorganic acid pH adjusters such as citrate buffer and phosphate buffer In addition, if necessary, a solubilizing agent, a buffer, a preservative, a flavor, a pigment, a sweetener, and the like can be used. These components can be used singly or as a mixture of each other. Usually, cold medicine standards and rhinitis listed in the over-the-counter drug manufacturing guidelines (2000 edition, supervised by the Pharmaceutical Affairs Committee, published by Jiho Co., Ltd.) Manufactured in compliance with internal medicine standards. The present invention will be described in more detail with reference to the following Examples and Test Examples, but the present invention is not limited to the following Examples. (Example 1) The following components and amounts were weighed and thoroughly mixed, and then tablets were produced using a tableting machine (Clean Press Collect 19; manufactured by Kikusui Seisakusho). Each tablet weighs 200
mg, and a punch having an 8 mm-diameter corner plane was used. Zafilkast 40 g Belladonna extract 50 g Anhydrous caffeine 75 g Lactose 150 g Microcrystalline cellulose (Avicel PH201) 100 g Magnesium stearate 10 g (Example 2) The following components and amounts are weighed and thoroughly mixed, and then according to Example 1. Then tablets were prepared. The weight of one tablet was 200 mg, and an 8 mm-diameter corner flat punch was used. Zafirkast 40 g Isopropamide iodide 5 g Lysozyme chloride 90 g (titer) Anhydrous caffeine 75 g Lactose 150 g Microcrystalline cellulose 130 g Magnesium stearate 10 g (Example 3) The following components and amounts are weighed and thoroughly mixed. Tablets were made according to Example 1. The weight of one tablet was 200 mg, and an 8 mm-diameter corner flat punch was used. Zafilkast 50 g Datsura extract 0.5 g Bromelain 80000 units Tabrates 80 g Low-substituted hydroxypropylcellulose 100 g Magnesium stearate 15.5 g (Example 4) The following components and amounts were weighed and uniformly mixed. To obtain a tablet of 150 mg. Zafirkast 60 g Roth extract 50 g Dipotassium glycyrrhizinate (200 g as glycyrrhizic acid) Caffeic anhydride 75 g Lactose 100 g Microcrystalline cellulose 100 g Magnesium stearate 20 g Hardened castor oil 5 g (Example 5) pH adjuster (phosphate buffer)
After preservatives, sweeteners, and flavors are added to the aqueous solution in which the sucrose fatty acid ester is uniformly dispersed, pranlukast hydrate and other drugs are added and dissolved. , Purified water was added to make the total volume 60 L, and an oral liquid preparation was produced. Zafilkast 50 g Belladonna total alkaloid 0.3 g Anhydrous caffeine 75 g Sucrose fatty acid ester 15 g Mannitol 15 g Stevia 10 g Ethyl aminobenzoate 5 g Orange flavor 3 g Grapefruit flavor 3 g (Test Example 1) [Test Example 1] <Test method> The components and amounts shown in Table 1 were
The mixture was diluted in 00 mL of purified water, and orally administered to 6 ddY male rats (5 weeks old, body weight 80 to 120 g) in groups of 6 in each group. Two hours after administration and 12 hours after administration, the chest was incised and the airway was excised, and the amount of airway fluid was measured and the average value was calculated.
Group (6 animals): In addition to oral administration of 2 mL of purified water, the same treatment as in the test group was performed and measurement was performed. ). [Table 1] <Test Results> The results are shown in Table 2. [Table 2] As described above, the degree of suppression of the amount of secretion of airway fluid is enhanced in group A as compared with the other groups, and the pharmaceutical composition comprising the active ingredient of the present invention is excellent in the response of airway secretory glands. In addition, the inhibitory effect was shown, and the effect was continued. Thus, the present invention can provide a useful drug having an enhanced effect on nasal hyperplasia in the case of cold syndrome or rhinitis.

Continuation of front page    (72) Inventor Joji Nakagami             Taisho, 3-24-1, Takada, Toshima-ku, Tokyo             Yakuhin Co., Ltd. (72) Inventor Yasuo Nakagawa             Taisho, 3-24-1, Takada, Toshima-ku, Tokyo             Yakuhin Co., Ltd. (72) Inventor Katsuyoshi Aikawa             Taisho, 3-24-1, Takada, Toshima-ku, Tokyo             Yakuhin Co., Ltd. F term (reference) 4C086 AA01 AA02 BC13 MA02 MA17                       MA35 MA52 ZA34                 4C088 AB12 BA08 MA02 MA17 MA35                       MA52 ZA34                 4C206 AA01 AA02 GA28 MA02 MA37                       MA55 NA05 ZA34

Claims (1)

Claims: 1. A group selected from the group consisting of (a) zafilkast and salts thereof and (b) a group consisting of belladonna (total) alkaloids, belladonna extract, funnel extract, isopropamide iodide and datura extract. A pharmaceutical composition comprising one or more compounds selected from the group and having an enhanced effect on nasal hyperplasia.