JP2001213764A - Oral solution - Google Patents

Abstract

PROBLEM TO BE SOLVED: To easily mask a peculiar unpleasant flavor in an oral solution containing polyvinylpyrrolidone in a certain amount or more. SOLUTION: In the internal liquid containing 0.4% by mass or more of polyvinylpyrrolidone, polyvinylpyrrolidone 1
An oral liquid preparation comprising citric acid and / or a pharmaceutically acceptable salt thereof in an amount of 0.15 parts by mass or more in terms of citric acid with respect to parts by mass.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an oral solution containing polyvinylpyrrolidone. More specifically, mask the unpleasant flavor unique to polyvinylpyrrolidone,
The present invention relates to a liquid medicine for oral administration that has ensured good ingestibility.

[0002]

2. Description of the Related Art Polyvinylpyrrolidone (hereinafter abbreviated as "PVP"), which is widely used as an internal liquid agent as a stabilizer, solubilizer, solubilizing agent, etc., is known to have a unique unpleasant flavor. Had been. Conventionally, this PVP
Additives such as sweeteners have been added to mask the unique unpleasant flavor, but the effect is not yet sufficient, and when a certain amount or more of PVP is blended, the particular unpleasant flavor is still present. Was a problem.

[0003]

SUMMARY OF THE INVENTION It is an object of the present invention to provide a liquid medicine for internal use which easily masks the unpleasant flavor peculiar to PVP and has good ingestibility.

[0004]

Means for Solving the Problems As a result of intensive studies to solve the above-mentioned problems, the present inventor has found that a certain amount or more of PVP is blended into an oral solution having a peculiar unpleasant flavor. It has been found that by mixing citric acid and / or a pharmaceutically acceptable salt thereof, an unpleasant flavor peculiar to PVP is masked, and an oral solution with good ingestibility can be prepared. The present invention completed based on such knowledge,
0.15 parts by mass or more of citric acid and / or a pharmaceutically acceptable salt thereof is converted to citric acid with respect to 1 part by mass of polyvinyl pyrrolidone in an oral liquid containing 0.4% by mass or more of polyvinyl pyrrolidone. It is an internal liquid solution characterized by having done.

[0005] The polyvinylpyrrolidone (hereinafter referred to as "PVP") in the present invention is used as a stabilizing agent, a solubilizing agent, a solubilizing agent and the like in an oral liquid preparation and has a unique unpleasant flavor. When the content is 0.4% by mass or more with respect to the whole oral liquid preparation, the flavor affects the ingestibility, and when the content is 1.0% by mass or more, the unpleasant flavor becomes remarkable.

[0006] The citric acid or a pharmaceutically acceptable salt thereof according to the present invention is mainly used as a pH adjuster in an oral solution. The amount of citric acid or a pharmaceutically acceptable salt thereof is PVP1 in terms of citric acid.
It is usually at least 0.15 part by mass, preferably at least 0.5 part by mass, particularly preferably at least 0.7 part by mass with respect to parts by mass.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION An oral solution according to the present invention is prepared by a conventional method for preparing an oral solution by mixing PVP and citric acid and / or a pharmaceutically acceptable salt thereof in addition to the active ingredient. Can be. Further, in the present invention, as a carrier used in the preparation of an oral solution, a buffer solution other than citric acid, an organic acid-based / inorganic acid-based pH adjuster of a phosphate buffer, and other solubilizing agents as necessary, Buffers, preservatives, flavors, dyes, sweeteners and the like can be used.

[0008]

The present invention will be described in more detail with reference to Test Examples, Examples and Comparative Examples.

(Test Example 1) 10% by mass of sucrose was blended.
Prepare an aqueous solution in which the amount of PVP is changed,
A dosing test was performed on 10 persons (10 men and 10 women), and the flavors were compared to obtain the results shown in Table 1.

[0010]

[Table 1]

Test Example 2 Sucrose 10% by mass, PVP
Based on a 1.0% by mass aqueous solution, an aqueous solution was prepared by changing the amount of citric acid and adjusting the pH to 3 with sodium hydroxide. 20 adult men and women (10 men, 10 women
2) was taken, and the flavor was compared. The results in Table 2 were obtained.

[0012]

[Table 2]

(Example 1) 2 ml of kokushi flow extract (2000 mg in terms of crude drug) 2 ml of elephantology flow extract (2000 mg in terms of crude drug) Royal jelly 500 mg taurine 1500 mg L-arginine hydrochloride 300 mg inositol 400 mg carnitine chloride 100 mg anhydrous caffeine 50 mg nicotinamide 60 mg thiamine nitrate 25 mg sodium riboflavin phosphate 12 mg pyridoxine hydrochloride 10 mg sucrose 14000 mg D-sorbitol solution 5000 mg sodium benzoate 65 mg fragrance 100 mg polyvinylpyrrolidone 1000 mg citric acid and sodium citrate so as to be 900 mg in terms of citric acid Was dissolved in purified water to adjust the pH to 2.7, and a total amount of 100 mL of the internal solution It was prepared.

(Example 2) Eleuthero flow extract 2 mL (prototype equivalent 2000 mg) Ousei flow extract 2.4 mL (prototype 2400 mg) Guarana flow extract 0.525 mL (prototype conversion 525 mg) Licorice extract 125 mg (prototype conversion 500 mg) 2) Kokushi flow extract (2000 mg in terms of crude drug) Keihi flow extract 0.15 mL (in terms of crude drug 150 mg) Kojin flow extract 1.5 mL (in terms of crude drug 1500 mg) Hawthorn extract 10 mg (in terms of crude drug 30 mg) Sanyaku flow extract 0.8 mL Peony extract 30 mg (raw drug equivalent 120 mg) Ginger extract 111 mg (raw drug equivalent 1000 mg) Joteishi soft extract 250 mg (raw drug equivalent 1000 mg) Kiss 37.5 mg (150 mg in terms of crude drug) Soft Radix Extract 230 mg (750 mg in terms of crude drug) Chimney Extract 20 mg (100 mg in terms of crude drug) Touki Flow Extract 0.6 mL (600 mg in terms of crude drug) Toshishi Extract 33 mg (300 mg in terms of crude drug) 0.6 mL of liquid (600 mg of crude drug) Citrus extract 758 mg (2500 mg of crude drug) Carrot extract 450 mg (3000 mg of crude drug) 133 mg of garlic extract (400 mg of crude drug) Bulk extract 17.2 mg (550 mg of crude drug) Muirapuama extract 37.5 mg (750 mg in crude drug equivalent) Yokuinin dry extract 400 mg (10000 mg in crude drug equivalent) Ryugannik extract 0.3 mL (300 in crude drug equivalent) g) Royal jelly 500 mg taurine 1500 mg L-arginine hydrochloride 300 mg inositol 400 mg carnitine chloride 100 mg anhydrous caffeine 50 mg nicotinamide 60 mg thiamine nitrate 25 mg riboflavin sodium phosphate 12 mg pyridoxine hydrochloride 10 mg sucrose 10,000 mg sodium odoritol 50 mg sodium odoritol Polyoxyethylene hydrogenated castor oil 250 mg Polyvinyl pyrrolidone 2000 mg Citric acid and sodium citrate were dissolved in purified water so that the above components and citric acid would be 1000 mg, and the pH was adjusted to 3.5. An oral solution was prepared.

(Example 3) Ammonium iron citrate 30 mg Magnesium aspartate 200 mg Calcium gluconate 1000 mg Aminoethylsulfonic acid 500 mg Anhydrous caffeine 50 mg Thiamine nitrate 10 mg Riboflavin sodium phosphate 15 mg Pyridoxine hydrochloride 25 mg Nicotinamide 40 mg Yoquinin flow extract 2 mL ( Royal jelly 500 mg ground yellow extract 300 mg (crude drug equivalent 600 mg) sugar 4000 mg glucose 4000 mg trehalose 2000 mg sorbitol (70%) 2000 mg erythritol 1000 mg maltitol 2500 mg xylitol 1200 mg sodium stevia extract 30 mg dextrin g Butylparaben 3.5 mg Propylparaben 3.5 mg Fragrance 50 mg Polyvinylpyrrolidone 1000 mg Citric acid and sodium citrate are dissolved in purified water so as to be 400 mg in terms of citric acid, and the pH is adjusted to 3.5. It was adjusted to prepare a total of 50 mL of an oral solution.

(Test Example 3) 20 adult men and women (10 males)
(10 women) were tested for the oral administration of the liquid preparations prepared in Examples 1 to 3, and the flavor was evaluated. As a result, the unpleasant flavor of polyvinylpyrrolidone was masked.

Claims (1)

[Claims] 1. An oral liquid preparation containing 0.4% by mass or more of polyvinylpyrrolidone, wherein polyvinylpyrrolidone 1
An oral liquid preparation comprising 0.15 parts by mass or more of citric acid and / or a pharmaceutically acceptable salt thereof in terms of citric acid with respect to parts by mass.