JP2005041832A - Gargle containing local anesthetic - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a preparation achieving sufficient effects by a low drug level when a local anesthetic is utilized as a gargle, that is, the gargle containing the local anesthetic exhibiting good absorption efficiency through oral mucous membrane, and high absorption rate. <P>SOLUTION: The preparation has the effects of the local anesthetic improved by regulating the pH of the preparation of the gargle containing the local anesthetic. <P>COPYRIGHT: (C)2005,JPO&NCIPI

Description

The present invention relates to a local anesthetic drug-containing gargle. Specifically, the present invention relates to a local anesthetic drug-containing gargle which is remarkably effective in reducing pain in the mouth such as stomatitis.

  Cancer patients are expected to be treated or prolong their lives by developing anti-cancer drugs and radiation therapy, but on the other hand, they often feel mental and physical distress due to side effects of such treatments as anti-cancer drugs. As a side effect of such cancer treatment, refractory severe stomatitis is known. From the beginning of chemotherapy, dry mouth, abnormal taste, pain, etc. have appeared, causing problems such as deterioration of nutritional status and interruption of chemotherapy. Local anesthetic drugs are very effective as countermeasures against such stomatitis pain.

In fact, in recent years, it is known that a preparation obtained by jelly-forming lidocaine, which is a local anesthetic drug, in a hospital prescription with carrageenan is used for pain relief of stomatitis in cancer patients.

These local anesthetic-containing preparations for pain relief of stomatitis include patches, ointments, gargles and the like, but it is thought that mouthwashes due to side effects of cancer treatment have a wide affected area and gargles are suitable.

  However, when local anesthetics are used as gargles, local anesthetics such as lidocaine are known to have serious side effects such as shock symptoms and convulsions, and recently allergic problems of lidocaine have been pointed out. For example, there is a need for a formulation that does not consume more than the required amount of drug. Specifically, there is a demand for a preparation capable of obtaining a sufficient effect with a smaller drug concentration, a preparation capable of obtaining a sufficient effect even if the drug is removed by rinsing with water after the drug is impregnated. That is, a local anesthetic drug-containing gargle having a high absorption efficiency of the local anesthetic into the oral mucosa and a high absorption rate is desired.

  From the situation as described above, the problem to be solved by the present invention is that when a local anesthetic is used as a gargle, the local anesthetic has a good absorption efficiency for the oral mucosa and has a high absorption rate. To provide gargle.

As a result of intensive studies, the present inventors have found that the efficacy of the local anesthetic drug is improved by adjusting the pH of the preparation of the gargle containing the local anesthetic drug. Thus, the present invention was completed.
The present invention encompasses the following.

A local anesthetic drug-containing gargle characterized by having a formulation pH of less than 8.0.

[2] The local anesthetic drug-containing gargle according to [1], wherein the local anesthetic drug is lidocaine or a pharmaceutically acceptable salt thereof.

[3] The local anesthetic drug-containing gargle according to [1] to [2], wherein the formulation pH is 6.0 or more and less than 8.0.

[4] The local anesthetic drug-containing gargle according to [1] to [3], wherein the preparation pH is 6.5 or more and less than 7.5.

  An object of the present invention is to provide a local anesthetic drug-containing gargle having a high absorption efficiency of the local anesthetic to the oral mucosa and a high absorption rate.

  The pH of the preparation of the local anesthetic drug-containing gargle of the present invention includes less than 8.0, preferably 6.0 to 8.0, and particularly preferably 6.5 to 7.5. . Precipitation of a local anesthetic drug is observed at pH 8.0 or higher, and the efficacy of the local anesthetic is low, and it is not established as a gargle because of a suspended substance due to the drug. When the pH is less than 6.5, the efficacy of the local anesthetic is slightly weakened, and when the pH is less than 6, the efficacy is further reduced.

Examples of the local anesthetic drug used in the local anesthetic drug-containing gargle of the present invention include lidocaine, ethyl paraaminobenzoate, oxybuprocaine, tetracaine, procaine, diethylaminoethyl parabutylaminobenzoate, or a pharmaceutically acceptable salt thereof. Or a mixture thereof. Particularly preferred is lidocaine hydrochloride. This is because the effect is demonstrated in this embodiment.

  A pH adjuster can be used in the local anesthetic drug-containing gargle of the present invention. Examples of the pH adjuster include acids such as hydrochloric acid, dilute hydrochloric acid, boric acid, sulfuric acid, phosphoric acid and salts thereof, citric acid, succinic acid, malic acid, tartaric acid, lactic acid, ascorbic acid, fumaric acid, maleic acid, gluconic acid. , Organic acids such as glucuronic acid, acetic acid and salts thereof, and bases such as potassium hydroxide, calcium hydroxide, sodium hydroxide, magnesium hydroxide, sodium carbonate, sodium hydrogen carbonate, and a mixture thereof. . Particularly preferred is a mixture of citric acid, an organic acid of malic acid, and sodium hydroxide and sodium bicarbonate.

  The local anesthetic drug-containing gargle of the present invention can contain sweeteners such as aspartame, saccharin, saccharin sodium, stevia, thaumatin, erythritol, sorbitol, xylitol, and in this case, a more preferable feeling of administration can be obtained.

  The local anesthetic drug-containing gargle of the present invention can be blended with a fragrance such as lemon, orange, grapefruit, pine, banana, chocolate, yogurt, vanilla, menthol, etc. In this case, a more preferable feeling of administration can be obtained.

  In the local anesthetic drug-containing gargle of the present invention, a pharmaceutically acceptable non-toxic and inert additive can also be added. These additives include sodium alginate, carboxyvinyl polymer, carmellose sodium, xanthan gum, propylene glycol, glycerin, concentrated glycerin, hydroxyethylcellulose, hydroxyethylmethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone, polyacrylic acid, Examples include thickeners such as sodium polyacrylate and polyvinyl alcohol, other buffers, colorants, flavoring agents, adsorbents, stabilizers, suspending agents, antioxidants, and preservatives.

Hereinafter, the present invention will be described more specifically with reference to examples and experimental examples, but the present invention is not necessarily limited thereto. In addition, the value of the compounding quantity in a present Example and a comparative example is all the mass%.

(Example 1) Preparation of a local anesthetic drug-containing gargle The local anesthetic drug-containing gargle of the present invention was prepared in the following amounts.
The blending amount and formulation pH are shown in Table 1.

(Experimental example 1) Sensory test The sensory test was implemented using the formulation shown in Example 1.

Ten subjects were grated for 30 seconds with 10 mL of each formulation, followed by 3 times of maturation with 30 mL of water. The effect of the local anesthetic drug after 5 minutes was determined by the following index.
"I don't feel at all"
"I feel a little"
"feel"
"I feel strongly"
more than

Each sensory test was performed on at least 2 hours withdrawn from the same subject.
Table 2 shows the number of subjects corresponding to each index.

From the above results, the drug effect was significantly improved by adjusting the formulation pH of the local anesthetic drug-containing gargle.

Claims (4)

A local anesthetic drug-containing gargle characterized by having a formulation pH of less than 8.0. The local anesthetic drug-containing gargle according to claim 1, wherein the local anesthetic drug is lidocaine. The local anesthetic drug-containing gargle according to any one of claims 1 to 2, wherein the preparation pH is 6.0 or more and less than 8.0. 4. The local anesthetic drug-containing gargle according to any one of claims 1 to 3, wherein the formulation pH is 6.5 or more and less than 7.5.