JPH0621063B2 - Dental painkiller composition - Google Patents

Description

FIELD OF THE INVENTION The present invention relates to dental analgesic compositions, and more particularly,
The present invention relates to a dental analgesic composition used by filling a caries hole. The composition of the present invention exhibits a synergistic analgesic effect due to the combination of specific drugs contained in a predetermined base.

BACKGROUND OF THE INVENTION Various drugs have been conventionally known as dental analgesics. However, none of these alone have been sufficiently effective. That is, when the local anesthetic is used alone, the perception of dentin in the tooth does not disappear, and the analgesic effect is insufficient. In addition, the phenols used as root canal anti-inflammatory analgesics have strong irritation and may cause side effects when they are applied in effective doses alone.

Therefore, various proposals have been made to obtain higher effects by combining two or more of these drugs in combination. For example, dental therapy, Vol. 5, No. 1, pp. 30-37, 1986, dibucaine hydrochloride, parabutylaminobenzoic acid diethylaminoethyl hydrochloride, isothipendyl hydrochloride and eugenol were blended to prepare an ethanol-based liquid agent to study its analgesic effect. The results of doing so are disclosed.

However, such liquid analgesics are unsatisfactory in terms of local retention and sustained effect of the drug. Therefore, as a dosage form of a dental pain reliever, in recent years,
Ointment-like products are becoming mainstream rather than liquid products. Carboxyvinyl polymers, hydrophilic ointments, or castor oil are usually used as the base of such ointment-type dental pain relievers. However, even if these are used as a base, the adhesiveness to the caries pores or the development of a continuous analgesic effect are still insufficient, and no analgesic having an excellent analgesic effect has been obtained.

That is, in the combination of the conventional base and the active ingredient,
There is a problem in compatibility, stability as a preparation, etc., the drugs that can be mixed are limited depending on the nature of the base, and an effective combination of drugs has not been achieved. Further, it is considered that the action of the drug to be blended may be inhibited by the ointment base.

SUMMARY OF THE INVENTION Accordingly, the present inventors have made various studies on an ointment base that fully exerts the effects of ethyl aminobenzoate, which has an excellent effect as a local anesthetic, and eugenol, which is an excellent root canal analgesic and anti-inflammatory agent. I did. As a result, they have found that an excellent analgesic effect can be obtained by blending ethyl aminobenzoate and eugenol together with a hydrophobic base containing tragacanth gum powder, and completed the present invention.

That is, the present invention is a hydrophobic base, tragacanth rubber powder,
Further, the present invention provides a dental analgesic composition comprising ethyl aminobenzoate and eugenol as active ingredients.

The present invention surprisingly not only exerts the effects of the individual active ingredients by blending ethyl aminobenzoate and eugenol into a hydrophobic base containing tragacanth gum powder, but also provides a dental analgesic composition. As a result, an extremely excellent expression of synergistic effect was observed.

In the present invention, if desired, a local anesthetic, an anti-inflammatory agent, a fragrance, or one or more of these may be mixed and mixed with the base. Further, when these are water-soluble drugs, it is preferable to further add lanolin, preferably purified lanolin, to the hydrophobic base.

Ethyl aminobenzoate used in the present invention is known as a local anesthetic, and eugenol is known as a root canal anti-inflammatory analgesic, and a dental analgesic containing either of them is already commercially available. There is no suggestion for the combination.

Detailed Description of the Invention The amount of ethyl aminobenzoate used in the dental analgesic composition of the present invention is 5 to 20% by weight, preferably 8 to 15% by weight, based on the entire composition. If the blending amount is less than 5% by weight, an effective analgesic effect cannot be obtained. On the other hand, if it is more than 20% by weight, irritation of the oral mucosa occurs, and
The ointment has poor operability in terms of formulation, leading to a decrease in stability of the analgesic composition or a deterioration in usability.

The content of eugenol is 3 to 8% by weight, preferably 4 to 6% by weight, based on the entire composition. If the compounding amount is less than 3% by weight, an effective analgesic effect cannot be obtained. Also,
If the blending amount is more than 8% by weight, oral mucous membrane irritation occurs, and there is a difficulty in formulation of the ointment, and the stability of the formulation decreases or the usability deteriorates.

As the tragacanth rubber powder blended in the present invention, 200
A mesh pass is preferable. When the particle size of the tragacanth rubber powder is 200 mesh or more, it gives an unpleasant feeling such as roughening in the mouth during use.

The amount of tragacanth rubber powder is 10 to the total composition.
It is 40% by weight, preferably 30 to 35% by weight. Compounding amount
If it is less than 10% by weight, the desired effect cannot be obtained because the adhesion to the wet surface is insufficient. On the other hand, the compounding amount is 8
If it exceeds 5% by weight, the graininess becomes remarkable and the usability deteriorates.

As a hydrophobic base, white petrolatum, plastibase,
Zelen 50W, vegetable oil, a mixture thereof, or the like is used, but a mixture of white petrolatum and plastibase is preferable in order to obtain sufficient drug effects such as releasability and local retention. In this case, it is desirable from the viewpoint of usability that the weight ratio of white petrolatum / plastibase is 1/4 to 2/1. If the blending ratio is less than 1/4, the adhesiveness is poor and the composition tends to peel off from the coated surface. On the other hand, if it is larger than 2/1, the adhesiveness becomes too high and the application becomes difficult.

The composition of the present invention may further contain the following local anesthetic, anti-inflammatory agent, and fragrance.

Examples of such a local anesthetic include dibucaine hydrochloride, parabutylaminobenzoic acid diethylaminoethyl hydrochloride, lidocaine hydrochloride, tetracaine hydrochloride and the like. Generally, the blending amount of these is preferably 0.1 to 2% by weight.

Examples of the anti-inflammatory agent include diphenhydramine hydrochloride and isothipendyl hydrochloride. The blending amount of these is 0.1
It is preferably ˜2% by weight.

As the fragrance, those having a bactericidal / preservative action such as peppermint oil, cinnamon oil, menthol, thymol, borneol are preferable. The blending amount of these is preferably 0.1 to 3% by weight.

The composition of the present invention is produced by uniformly mixing the above components by a conventional method. For example, ethyl aminobenzoate is rubbed with diethyl ether and the diethyl ether is evaporated to a powder. The aminoaminobenzoate is kneaded with a base (in the case of a mixed base, it is preferable to mix it first), eugenol is further added, and finally, tragacanth gum powder is added little by little and kneaded to obtain the whole quality. Equal.

The obtained analgesic composition has an ointment-like form, and when licked, it paralyzes the tongue.

As described above, ethyl aminobenzoate and eugenol, which are the active ingredients of the present invention, are commercially available as anesthetics and analgesics as described above, and do not show toxicity to the human body. The dose of these active ingredients is within the conventionally known range, but it is usually preferable to be 0.1 to 0.2 g per tooth.

EXAMPLES The present invention will be described in more detail based on examples.

Example 1 Ethyl aminobenzoate was triturated with a little diethyl ether and the diethyl ether was evaporated to a powder. White petrolatum and plastibase were added to and kneaded to this, and eugenol was further added and kneaded. Finally, tragacanth rubber powder was added and kneaded to uniformly produce the whole quality. The resulting composition is a very pale brown ointment that fragrances and numbs the tongue when licked.

Example 2 Dibucaine hydrochloride was dissolved in a small amount of distilled water and absorbed in purified lanolin (A). Separately, ethyl aminobenzoate was rubbed with a small amount of diethyl ether, the diethyl ether was evaporated to a powder, and plastibase was added thereto and kneaded (B). (A) and (B)
Was mixed, and white petrolatum and eugenol were further added to make a total of 70 g, which was kneaded. Finally, tragacanth rubber powder was added and kneaded to uniformly produce the whole quality. The resulting composition is a very pale brown ointment that fragrances and numbs the tongue when licked.

Comparative Example 1 By the same method as in Example 1, an analgesic composition having the following composition was produced.

Comparative Example 2 In the same manner as in Example 1, an analgesic composition having the following composition was produced.

Comparative Example 3 In the same manner as in Example 1, an analgesic composition having the following composition was produced.

Effect of the Invention The analgesic action of the ointment analgesic compositions obtained in Examples 1 to 2 and Comparative Examples 1 to 5 was examined.

Test method (guinea pig blink reaction method): An analgesic composition was applied on the cornea or eyelid conjunctiva of guinea pigs (5 animals per group) using the spatula's back, and wiped off after 90 seconds. Then, the cornea was stimulated with pig hair at a predetermined time, and the blink reaction rate was examined. The results are shown in the following Table 1 and FIG.

As is clear from Table 1 and FIG. 1, the analgesic compositions obtained in Examples 1 and 2 of the present invention show an analgesic action for a long time. On the other hand, when one of ethyl aminobenzoate and eugenol is blended (Comparative Examples 1 and 2), or when both are blended together and no tragacanth rubber powder is blended (Comparative Example 3). ) Has a short duration of analgesic effect.

As described above, the dental analgesic composition of the present invention effectively adheres to teeth and exerts an excellent analgesic effect continuously for a long period of time.

[Brief description of drawings]

FIG. 1 is a graph showing changes over time in the blink reaction inhibition rate of guinea pigs when various analgesic compositions were applied.

Claims (7)

[Claims] 1. A dental analgesic composition comprising a hydrophobic base, tragacanth gum powder, and ethyl aminobenzoate and eugenol as active ingredients. 2. The composition according to item (1), wherein the amount of ethyl aminobenzoate is 5 to 20% by weight based on the total weight of the composition. 3. The composition according to item (1), wherein the amount of eugenol is 3 to 8% by weight based on the total weight of the composition. 4. The composition according to item (1), wherein the particle size of the tragacanth rubber powder is 200 mesh pass. 5. The composition according to item (1), wherein the content of the tragacanth rubber powder is 10 to 40% by weight based on the whole composition. 6. A composition according to claim 1, wherein the hydrophobic base is white petrolatum, plastibase or a mixture thereof. 7. The composition according to item (6), wherein the blending weight ratio of white petrolatum / plastibase is 1/4 to 2/1.