JP2003089638A - Pharmaceutical composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an agent for the treatment of common cold symptoms having improved action to suppress the promotion of the secretion of the respiratory tract for mitigating various symptoms of common cold (especially pituita symptoms caused by the inflammation of the nasal mucosa). SOLUTION: This pharmaceutical composition contains (a) pseudoephedrine or its salt and (b) one or more compound selected from belladonna (total) alkaloid, belladonna extract, scopolia extract, isopropamide iodide and datura extract.

Description

Description: BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to various symptoms associated with cold syndrome, hay fever, hay fever, allergic rhinitis and the like.
In particular, the present invention relates to a pharmaceutical composition having an improved effect on nasal discharge (nose nose). [0002] Pseudoephedrine is a sympathomimetic and is used for the purpose of removing edema or swelling of mucous membrane. Belladonna (total) alkaloid, belladonna extract, funnel extract, isopropamide iodide and datsura extract are parasympathetic nerves. These are commonly used drugs for the purpose of suppressing mucosal secretion with blockers. [0003] However, a composition combining (a) pseudoephedrine and (b) one or more selected from belladonna (total) alkaloids, belladonna extract, funnel extract, isopropamide iodide and datsura extract has not yet been known. . [0004] On the other hand, although many compositions for treating rhinitis have been known, any of them is a nasal mucosal hyperplasia symptom, which is an abnormally increased secretory gland of the nasal mucosa associated with cold syndrome, hay fever, hay fever, allergic rhinitis and the like. There is a need for a composition that has a stronger effect on odor. SUMMARY OF THE INVENTION The present invention provides a pharmaceutical composition which can reliably eliminate or alleviate nasal overdose symptoms among various symptoms associated with colds, allergic rhinitis and the like. To provide things. Means for Solving the Problems The inventors of the present invention have made intensive studies for the above purpose, and as a result, have found that certain active antiallergic drugs, sympathomimetics and parasympathomimetics are compounded as active ingredients. As a result, the present inventors have found that the present invention has a dramatic effect on the elimination or alleviation of the symptoms of excessive nasal discharge (nose nose) in the nasal mucosa, and completed the present invention. That is, the present invention provides a pharmaceutical composition comprising (a) pseudoephedrine or a salt thereof, and (b) one or more selected from belladonna (total) alkaloids, belladonna extract, funnel extract, isopropamide iodide and datsura extract. Things. Further, when cetirizine or a salt thereof is further added, it is useful for eliminating nasal polyps. In the present invention, pseudoephedrine is also called pseudoephedrine. In the present invention, the belladonna (total) alkaloid is a herbal medicine belladonna (Atoropa belladonn).
a Linne) are tropane-based alkaloids contained in the roots or leaves of Linne), and include both veradonan alkaloids and belladonna total alkaloids. Further, in the present invention, the salts include hydrochloride,
Inorganic salts such as nitrates, sulfates, phosphates, oxalates, maleates, fumarates, tosylates, hydrobromides and the like, and organic salts can be mentioned. BEST MODE FOR CARRYING OUT THE INVENTION The pharmaceutical composition of the present invention can usually be 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. [0012] The amount of each compound per day for adults, (a) pseudoephedrine or its salts
The dose is preferably 0 to 240 mg, and more preferably 36 to 180 mg. (B) Belladonna (total) alkaloids are 0.06-
1.0 mg is good, preferably 0.1 to 0.6 mg,
Belladonna extract is preferably 6-100 mg, preferably 1 mg.
0 to 60 mg is preferable, the funnel extract is preferably 6 to 100 mg, preferably 10 to 60 mg, and the isopropamide iodide is preferably 0.75 to 10 mg, preferably 1.0 to 1.0 mg.
The amount is preferably 7.5 mg, and the amount of datsura extract is preferably 0.06 to 1.0 mg, and more preferably 0.1 to 0.6 mg. When cetirizine or a salt thereof is blended, the amount of cetirizine is preferably 2.5 to 25 mg, and more preferably 5 to 20 mg. [0014] The pharmaceutical composition of the present invention comprises a tablet,
It is used as a formulation for oral administration forms such as capsules, granules, fine granules, powders, chewables, foaming agents, drops, dissolving agents in the mouth, dry syrups, and oral liquids. These preparations can be prepared by a conventional method. In the solid preparation, carriers used for preparing a preparation include excipients such as lactose, starch, sugar, mannitol, crystalline cellulose, binders such as hydroxypropylcellulose, hydroxypropylmethylcellulose, gelatin, PVP, and carboxy. There are disintegrants such as methylcellulose calcium and low-substituted hydroxypropylcellulose, lubricating agents such as magnesium stearate, hydrogenated castor oil, and talc.In addition, if necessary, dissolution aids, buffers, preservatives, fragrances, and dyes And flavoring agents can be used. [0016] In the liquid preparation for internal use, carriers used for preparation of the preparation include sucrose fatty acid esters, polyoxyl stearate, polyoxyethylene polyoxypropylene glycols, and polyoxyethylene monofatty acid esters. 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. The pharmaceutical composition of the present invention may contain, if necessary, components in addition to the above components. The guidelines for the manufacture of over-the-counter drugs (2000 edition, supervised by the Pharmaceutical Affairs Committee, published by Jiho Co., Ltd.) It is formulated according to the internal medicine for rhinitis and cold medicine standards listed in the above. The present invention will be described in more detail with reference to examples and test examples, but the present invention is not limited to the following examples. Example 1 After weighing each component and its amount, mixing well and sieving, tablets were produced using a tableting machine (Clean Press Collect 19, manufactured by Kikusui Seisakusho). Each tablet weighs 200 mg,
A 7.5 mm diameter flat-faced punch was used. 5 g of cetirizine hydrochloride 30 g of pseudoephedrine hydrochloride 30 g of isopropamide iodide 5 g of anhydrous caffeine 100 g of lactose 100 g of microcrystalline cellulose (AVICEL PH201) 98 g of magnesium stearate 2 g Tablets were made according to Example 1. In addition, each tablet weighed 200 mg, and a 9 mm diameter corner flat punch was used. Cetirizine hydrochloride 7.5 g Pseudoephedrine hydrochloride 45 g Belladonna total alkaloid 0.6 g Dipotassium glycyrrhizinate 200 g Anhydrous caffeine 75 g Lactose 120.4 g Microcrystalline cellulose 109.5 g Magnesium stearate 2 g Example 3 Weigh each component and amount and suffice After mixing and sieving, tablets were prepared according to Example 1. The weight of one tablet was 200 mg, and an 8 mm-diameter corner flat punch was used. Cetirizine hydrochloride 10 g Pseudoephedrine hydrochloride 60 g Belladonna extract 50 g Anhydrous caffeine 100 g Tablets 75 g Low-substituted hydroxypropylcellulose 93 g Magnesium stearate 2 g Example 4 After weighing each component and amounts, mixing uniformly and sieving, Example Tablets were prepared according to 1. Each tablet weighed 200 mg, and a 9.5 mm diameter flat-cornered punch was used. Cetirizine hydrochloride 10 g Pseudoephedrine hydrochloride 60 g Roth extract three-fold trituration 150 g Dipotassium glycyrrhizinate 160 g Anhydrous caffeine 120 g Lactose 100 g Microcrystalline cellulose 95 g Magnesium stearate 5 g (Screen diameter: 1mm) and mixed and pulverized material 3 in 1st hard capsule
00 mg was filled to make a capsule. However, the capsules were filled by hand. Cetirizine hydrochloride 15 g Pseudoephedrine hydrochloride 60 g Datsura extract 0.6 g Tranexamic acid 395 g Calcium hydrogen phosphate 53 g Microcrystalline cellulose 74 g Magnesium stearate 2.4 g Example 6 An aqueous solution in which a pH adjuster (phosphate buffer solution) is dissolved is used. After adding sucrose fatty acid ester uniformly to the solution, adding and dissolving naproxen and other chemicals, adding purified water to make a total volume of 60 liters. did. Cetirizine hydrochloride 10 g Pseudoephedrine hydrochloride 50 g Belladonna extract 60 g Lysozyme chloride 90 g (titer) Anhydrous caffeine 75 g Sucrose fatty acid ester 15 g Xylitol 15 g Stevia 10 g Ethyl aminobenzoate 5 g Orange flavor 1 g Orange flavor 1 g After mixing and sieving, tablets were produced using a tableting machine (Clean Press Collect 19; manufactured by Kikusui Seisakusho). Each tablet weighs 200 mg,
A 7.5 mm diameter flat-faced punch was used. Isotipendyl hydrochloride 10 g Pseudoephedrine hydrochloride 30 g Isopropamide iodide 5 g Anhydrous caffeine 80 g Lactose 100 g Microcrystalline cellulose (Avicel PH201) 90 g Magnesium stearate 5 g Example 8 After weighing and thoroughly mixing and sieving each component and amount, Tablets were made according to Example 7. In addition, each tablet weighed 200 mg, and a 9 mm diameter corner flat punch was used. Triprolidine hydrochloride 6 g Pseudoephedrine hydrochloride 45 g Belladonna total alkaloids 0.6 g Dipotassium glycyrrhizinate 200 g Anhydrous caffeine 75 g Lactose 116.4 g Microcrystalline cellulose 110 g Magnesium stearate 7 g After that, tablets were produced according to Example 7. The weight of one tablet was 200 mg, and an 8 mm-diameter corner flat punch was used. Metzilazine hydrochloride 8 g Pseudoephedrine hydrochloride 60 g Belladonna extract 50 g Anhydrous caffeine 100 g Tablets 75 g Low-substituted hydroxypropylcellulose 92 g Magnesium stearate 5 g Example 10 After weighing and uniformly mixing and sieving each component and amount, the example was used. Tablets were prepared according to 1. Each tablet weighed 200 mg, and a 9.5 mm diameter flat-cornered punch was used. Alimemazine tartrate 5 g Pseudoephedrine hydrochloride 60 g Roth extract three-fold trituration 150 g Dipotassium glycyrrhizinate 160 g Anhydrous caffeine 120 g Lactose 100 g Microcrystalline cellulose 97 g Magnesium stearate 8 g (Screen diameter: 1mm) and mixed and pulverized material 3 in 1st hard capsule
00 mg was filled to make a capsule. However, the filling into the capsule was performed by manual filling. Promethazine hydrochloride 15 g Pseudoephedrine hydrochloride 60 g Datsura extract 0.5 g Tranexamic acid 395 g Calcium hydrogen phosphate 53 g Microcrystalline cellulose 71.5 g Magnesium stearate 5 g After adding sucrose fatty acid ester uniformly to the solution, adding and dissolving naproxen and other chemicals, adding purified water to make a total volume of 60 liters. did. Diphenylpyraline teocoleate 4 g Pseudoephedrine hydrochloride 50 g Belladonna extract 60 g Lysozyme chloride 90 g (titer) Anhydrous caffeine 75 g Sucrose fatty acid ester 15 g Xylitol 15 g Stevia 10 g Ethyl aminobenzoate 11 g Orange flavor 1 g Test example of formulation Effect on Normal Rat Airway Secretion] Test Method The components and amounts shown in Table 1 were diluted in 100 mL of purified water for each of the groups A to E, and 2 mL were added to three ddY male rats in each group.
Each was orally administered. Two hours after administration, the chest was incised and the airway was excised, the amount of airway fluid was measured, and the average value was calculated. The average value was compared with the average value of Group F (2 mL of purified water was orally administered) as a control group. [Table 1] Table 2 shows the test results. The degree of suppression of the amount of airway fluid secretion is determined by the groups A and B
The group was superior to the other groups and showed an excellent inhibitory effect on secretory gland responses. [Table 2] Industrial Applicability The present invention is a pharmaceutical composition which has a great effect on the elimination and alleviation of nasal hyperplasia (nose nose) symptom associated with abnormal secretory gland in the nasal mucosa. A significantly useful drug could be provided for nasal symptoms such as syndrome or rhinitis.

Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat II (Reference) A61P 11/02 A61P 11/02 27/16 27/16 37/08 37/08 (72) Inventor Joji Nakagami Tokyo 3-24-1, Takada, Toshima-ku, Tokyo Taisho Pharmaceutical Co., Ltd. (72) Inventor Katsuyoshi Aikawa 3-24-1, Takada, Toshima-ku, Tokyo Taisho Seiyaku Co., Ltd. (72) Inventor Yasushi Nakagawa Tokyo 3-24-1, Takada, Toshima-ku Taisho Seiyaku Co., Ltd. F-term (reference) 4C088 AB48 AC05 AC11 BA08 MA08 NA05 ZA34 ZB13 ZC54 ZC75 4C206 AA01 FA10 GA09 GA22 MA03 MA04 NA05 ZA34 ZB13 ZC54 ZC75

Claims (1)

Claims: 1. A method comprising (a) pseudoephedrine or a salt thereof, and (b) at least one selected from belladonna (total) alkaloids, belladonna extract, funnel extract, isopropamide iodide and datsura extract. A pharmaceutical composition characterized by: