JPH09151127A - Composition for pharyngopathy - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for pharyngopathy increased in the sustainability of its analgesic effect, also safe even after long-term use, by formulating a specific compound in a system composed of an iodine-based bactericide and a local anesthetic. SOLUTION: This composition for pharyngopathy comprises 0.01-5.0wt.% of an iodine-based bactericide (esp. pref. povidone iodine or a combination of iodine with potassium iodide at the weight ratio of (1:2)), 0.01-10wt.% of a local anesthetic (pref. procaine, lidocaine, dibucaine, or their salts, or ethyl aminobenzoate), and 10-95wt.% of a polyhydric alcohol (pref. glycerol, propylene glycol or polyethylene glycol). The composition is effective for throat disinfection/sterilization, tonsillitis, stomatitis, foul breath removal, throat chapping, throat pain, throat swelling, uncomfortable feeling of throat, etc.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition for pharyngeal diseases in which the duration of analgesic effect is enhanced.

[0002]

2. Description of the Related Art As a conventional composition for pharyngeal diseases, a composition in which an iodine bactericidal agent and a local anesthetic are mixed is known in German Publication No. 3234350, but the pain during application is eliminated. Regarding sustainability, satisfactory results were not obtained.

[0003]

When a local anesthetic is mixed with an iodine fungicide, the local anesthetic must be used many times in a short time because it is quickly absorbed. The dose of anesthetic increases and side effects such as nausea and drowsiness occur. Therefore, it has been desired to develop a composition for pharyngeal diseases which contains a local anesthetic and is durable.

[0004]

Means for Solving the Problems As a result of intensive studies to solve the above-mentioned problems, the present inventors have found that an iodine bactericide contains a local anesthetic and a polyhydric alcohol to improve sustainability. Then, they have completed the present invention.

That is, the present invention is a composition for pharyngeal diseases, which contains an iodine fungicide, a local anesthetic and a polyhydric alcohol.

The iodine fungicides include iodine or
A complex of iodine, for example, povidone iodine can be used. Preferably, povidone iodine, or iodine and potassium iodide are used, and the weight ratio thereof is 0.5: 1 to 0.5: 5, and particularly preferably,
Povidone-iodine or iodine / potassium iodide in a weight ratio of 1: 2 is preferable.

Local anesthetics include ester types such as procaine and amide types such as lidocaine and other classes such as dibucaine. As the ester type local anesthetic, for example, in addition to procaine, tetracaine,
Examples thereof include oxybuprocaine, thecaine and salts thereof (eg, hydrochloride), and examples of the amide type include lidocaine, bupivacaine, mepivacaine,
Propitocaine and its salts (for example, hydrochloride etc.) are mentioned. Other classifications include, for example, dibucaine, ethyl aminobenzoate, dibucaine hydrochloride,
Examples include oxesazein and ethyl piperidinoacetylaminobenzoate. Preferred are procaine, lidocaine, dibucaine and their salts or ethyl aminobenzoate. Particularly preferred is lidocaine or lidocaine hydrochloride.

The polyhydric alcohol is preferably glycerin, ethylene glycol, propylene glycol, butylene glycol, polyethylene glycol or sorbitol, more preferably glycerin, propylene glycol or polyethylene glycol. Most preferably, glycerin is used alone or in combination with propylene glycol. The weight mixing ratio of glycerin and propylene glycol is 5: 2 to 5: 5, preferably 5: 3 to 5: 4.

In the present invention, the iodine bactericide, the local anesthetic and the polyhydric alcohol are blended in amounts of 0.01 to 5.0% by weight of the iodine bactericide, 0.01 to 10% by weight of the local anesthetic. The content of the polyhydric alcohol is 10 to 95% by weight, preferably 0.1 to 2.0% by weight of iodine bactericide, 0.01 to 0.5% by weight of local anesthetic, and 60 of polyhydric alcohol.
~ 90% by weight.

Further, 300 to 2000 parts by weight of polyhydric alcohol is added to 1 part by weight of the local anesthetic, preferably 600 to 12 parts of polyhydric alcohol is added to 1 part by weight of the local anesthetic.
Add 00 parts by weight.

The composition for pharyngeal diseases of the present invention is used as a preparation such as a solution, a spray, and a gel.

These formulations can be prepared by a conventional method. The solvent used for the preparation of the preparation, such as purified water and alcohol, other known additives, if necessary,
For example, antioxidants, surfactants, pH adjusters, preservatives,
A flavoring agent or the like can be used.

Examples of the antioxidant include dibutylhydroxytoluene (BHT), propyl gallate, butylhydroxyanisole (BHA), α-tocopherol, citric acid and the like.

Examples of the surfactant include polyoxyethylene hydrogenated castor oil, sorbitan monostearate, sorbitan monopalmitate, sorbitan monolaurate, polyoxyethylene polyoxypropylene block copolymers, polysorbates, sodium lauryl sulfate and macrogol. And sucrose fatty acid esters.

Examples of preservatives include sodium benzoate, paraoxybenzoic acid ester, sorbic acid and the like.

Examples of the flavoring agents include l-menthol, peppermint water, peppermint oil, eucalyptus oil and the like.

The pH of the pharyngeal disease composition of the present invention is usually about 1 to 4, preferably about 2 to 3, and can be adjusted using a conventional pH adjusting agent. As a pH adjuster,
For example, edible organic acids such as citric acid, malic acid, tartaric acid, acetic acid, succinic acid, lactic acid, fumaric acid, and ascorbic acid; inorganic acids such as hydrochloric acid and phosphoric acid; and salts thereof (for example, sodium salt, potassium salt). Etc.).

[0018]

EFFECTS OF THE INVENTION The composition for pharyngeal diseases according to the present invention is for throat sterilization / disinfection, tonsils, stomatitis, removal of halitosis, throat,
It is a safe and persistent composition for pharyngeal diseases, which is effective for sore throat, sore throat, discomfort in throat, and vocalization.

[0019]

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

Example 1 Lidocaine 0.1 g Iodine 0.5 g Potassium iodide 1.0 g Glycerin 85.0 g Ethanol 12.7 g l-Menthol 0.3 g Hydrochloric acid Appropriate amount The above components were weighed, mixed and dissolved, and then purified water was added. Was added to bring the total volume to 100 ml.

Example 2 Lidocaine 0.1 g Iodine 0.5 g Potassium iodide 1.0 g Glycerin 50.0 g Propylene glycol 35.0 g Ethanol 12.7 g l-Menthol 0.5 g The above ingredients were weighed and mixed and dissolved. Purified water was added to bring the total volume to 100 ml.

Example 3 Lidocaine 0.1 g Iodine 0.5 g Potassium iodide 1.0 g Glycerin 45.0 g Propylene glycol 30.0 g Polyethylene glycol 10.0 g Ethanol 12.7 g l-Menthol 0.2 g Hydrochloric acid Appropriate amount of the above components After weighing, mixing and dissolving, purified water was added to make a total volume of 100 ml.

Example 4 Lidocaine hydrochloride 0.1 g Iodine 0.5 g Potassium iodide 1.0 g Glycerin 60.0 g Propylene glycol 30.0 g Ethanol 7.7 g l-Menthol 0.3 g The above ingredients were weighed and mixed and dissolved. Then, purified water was added to make a total volume of 100 ml.

Example 5 Lidocaine 0.1 g Povidone iodine 0.45 g Glycerin 85.0 g Ethanol 12.7 g l-Menthol 0.3 g Hydrochloric acid Appropriate amount The above components were weighed, mixed and dissolved, and purified water was added. The total volume was 100 ml.

Example 6 Lidocaine 0.1 g Povidone iodine 0.45 g Glycerin 50.0 g Propylene glycol 35.0 g Ethanol 12.7 g l-Menthol 0.5 g The above ingredients were weighed, mixed and dissolved, and then purified. Water was added to bring the total volume to 100 ml.

Example 7 Lidocaine 0.1 g Povidone iodine 0.45 g Glycerin 45.0 g Propylene glycol 30.0 g Polyethylene glycol 10.0 g Ethanol 12.7 g l-Menthol 0.2 g Hydrochloric acid Appropriate amount of the above components After weighing, mixing and dissolving, purified water was added to make a total volume of 100 ml.

Example 8 Lidocaine hydrochloride 0.1 g Povidone iodine 0.45 g Glycerin 60.0 g Propylene glycol 30.0 g Ethanol 7.7 g l-Menthol 0.8 g The above components were weighed, mixed and dissolved, and purified water was added. The total volume was 100 ml.

Test Example 1 (Experimental material) Examples 1 to 3 and the following comparative example were used as experimental materials.

Comparative Example 1 Lidocaine 0.1 g Iodine 0.5 g Potassium iodide 1.0 g Ethanol 12.7 g 1-menthol 0.3 g The above components were weighed, mixed and dissolved, and purified water was added to make a total amount of 100 ml. (Test method) Subjects; patients with pharyngitis and pharyngeal discomfort 25
The number of adult subjects (15 males and 10 females) was used.

2. Content: 500 μl of each of Examples 1 to 3 and Comparative Example 1 was spray-applied to the pharynx of a subject, and the intensity of pain was evaluated with time according to the following criteria.
We used the method of answering the questionnaire.

(Evaluation) 5 ... Very strong feeling 4 ... Strong feeling 3 ... Feeling 2 ... Slight feeling 1 ... Slight feeling 0 ... Not feeling (Test result) The average value of the scores of the pain intensity of the test subject over time The changes are as shown in FIGS.

As is clear from these results, compared with Comparative Example 1, in Examples 1 to 3 in which the polyhydric alcohol and the local anesthetic were mixed, the effect of suppressing pain and the enhancement of its persistence were observed.

Test Example 2 (Experimental materials) Examples 5 to 7 and the following comparative examples were used as experimental materials.

Comparative Example 2 Lidocaine 0.1 g Povidone iodine 0.45 g Ethanol 12.7 g 1-menthol 0.3 g The above components were weighed, mixed and dissolved, and purified water was added to make a total amount of 100 ml. (Test method) Subjects; patients with pharyngitis and pharyngeal discomfort 25
The number of adult subjects (15 males and 10 females) was used.

2. Content: 500 μl of each of Examples 5 to 7 and Comparative Example 2 was spray-applied to the subject's pharynx, and the intensity of pain was evaluated with time according to the following criteria.
We used the method of answering the questionnaire.

(Evaluation) 5 ... Very strong feeling 4 ... Strong feeling 3 ... Feeling 2 ... Slight feeling 1 ... Slightly feeling 0 ... Not feeling (Test results) The average value of the scores regarding the pain intensity of the test subject over time The changes are as shown in FIGS.

As is clear from these results, compared with Comparative Example 2, in Examples 4 to 7 in which the polyhydric alcohol and the local anesthetic were mixed, the effect of suppressing pain and the enhancement of its durability were observed.

[Brief description of the drawings]

FIG. 1 is a graph showing the analgesic evaluation when Example 1 and Comparative Example 1 are applied by spraying.

FIG. 2 is a graph showing the analgesic evaluation when Example 2 and Comparative Example 1 are applied by spraying.

FIG. 3 is a graph showing analgesic evaluation when Example 3 and Comparative Example 1 are applied by spraying.

FIG. 4 is a graph showing an analgesic evaluation when Example 5 and Comparative Example 2 are applied by spraying.

FIG. 5 is a graph showing analgesic evaluation when Example 6 and Comparative Example 2 are applied by spraying.

FIG. 6 is a graph showing analgesic evaluation when Example 7 and Comparative Example 2 are applied by spraying.

─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. ⁶ Identification code Internal reference number FI Technical display area A61K 45/00 AAQ A61K 45/00 AAQ 45/06 ACD 45/06 ACD ACK ACK 47/10 47 / 10 N // (A61K 33/18 31:24) (A61K 33/18 31: 165) (A61K 33/18 31:47)

Claims (4)

[Claims] 1. A composition for pharyngeal diseases comprising an iodine fungicide, a local anesthetic and a polyhydric alcohol. 2. The composition for pharyngeal diseases according to claim 1, wherein the local anesthetic is procaine, lidocaine, dibucaine and salts thereof or ethyl aminobenzoate. 3. The composition for pharyngeal diseases according to claim 1, wherein the polyhydric alcohol is glycerin, propylene glycol or polyethylene glycol. 4. A local anesthetic selected from (A) lidocaine or lidocaine hydrochloride, and (B) a polyhydric alcohol selected from the group consisting of glycerin and propylene glycol.
Composition for pharyngeal diseases, characterized in that