JPH024710A - Pharmaceutical for treating infected root canal and apical periodontitis - Google Patents

Abstract

PURPOSE:To obtain the subject pharmaceutical, containing a pharmacologically active substance in a pharmaceutically acceptable water-soluble or water- swellable high polymer substance and capable of mainly enhancing retention properties of a drug in affected parts of infected root canals and apical periodontitis and improving persistence of the drug treating effects. CONSTITUTION:A pharmaceutical for treating infected root canals and apical periodontitis, obtained by containing a pharmacologically active substance, such as anti-inflammatory and analgesic agent, in a pharmaceutically acceptable water-soluble or water-swellable high polymer substance, preferably capable of dissolving or gelatinizing in water and exhibiting about 2-6000cP viscosity, e.g., cellulosic derivative, natural high polymer, polyacrylic acid and salts thereof, acrylic acid copolymers and/or polyvinylpyrrolidone, especially hydroxypropyl cellulose and capable of sustaining retention time of the drug in root canal parts or apical parts utilizing the viscosity of the above-mentioned high polymer substance, prolonging the action time and remarkably enhancing treating effects with simple operation.

Description

Detailed Description of the Invention [Field of Industrial Application] The present invention relates to a preparation applied to the treatment of infected root canals and apical periodontitis, and more specifically to a water-soluble or water-swellable polymer. Infected root canals and apical periodontitis, the main purpose of which is to maintain drug treatment effects by increasing the retention of drugs in infected root canals and apical periodontitis affected areas using the viscosity of the substance. It provides periodontal tissue treatment.

[Prior art] The infected root canal as used in the present invention is a general term for a root canal under an infected state (the tubular part containing the dental pulp in Fig. 1). A general term for a condition in which the dentin surrounding the canal is infected to the depths. Furthermore, apical periodontitis refers to tooth/periodontitis that occurs at the root apex of the tooth (the part with the apical foramen in FIG. 1).

Conventionally, in the treatment of infected root canals and apical periodontitis, sufficient therapeutic effects have not been obtained when administered internally due to the low ability to migrate to the local area of the tooth root, and external preparations generally do not contain phenols, Aldehydes are frequently used as therapeutic agents, but they are highly irritating to the skin and mucous membranes, and their therapeutic effects are not satisfactory.

[Problems to be Solved by the Invention] Infected root canals and apical periodontitis are usually treated once a week, and the affected area is kept sealed until the next treatment, so there is no need to use drugs. It is necessary to maintain the retention time in the root apex or root canal and to prolong the action time of the drug.

Although the purpose of treatment is different from that of the present invention, it is already known to mix a drug with water-soluble or water-swellable polymeric substances in order to impart sustained release properties to the drug (Japanese Patent Laid-Open No. 58-2137).
09, JP-A-62201-806, and JP-A-62-298521).

However, in JP-A No. 58-213709 and JP-A No. 62-298521, both are aimed at treating alveolar 1 excretion, which is different from the present invention.
Since it is intended to be attached to the surface of the gingiva or inserted into periodontal pockets, it is used in the form of a sheet or strip.
In Publication No. 1806, it is necessary to mix and cure a polyacrylic acid ester monomer, a polymerization initiator, and a drug, and this is applicable to infected root canals and apical periodontitis, which is the purpose of the present invention. Whether or not it would be possible was completely unexpected.

The present invention provides a treatment method that is effective and simple to treat infected root canals and apical periodontitis, for which no effective treatment method has hitherto been available.

[Means to solve the problem]

As a result of intensive research in order to solve the above problems, the present inventor has discovered that simply applying a drug to a water-soluble or water-swellable polymeric substance can reduce the risk of infection in root canals and apical periodontitis. It was discovered that a surprising therapeutic effect can be obtained.

That is, the present invention provides a method for infected root canals and apical periodontal tissues containing one or more pharmacologically active substances selected from the group of pharmaceutically acceptable water-soluble or water-swellable polymer substances. It's a treatment.

Pharmaceutically acceptable water-soluble or water-swellable polymeric substances used in the practice of the present invention include those that exhibit viscosity when dissolved or gelled in water (viscosity of about 2 to about 6.000
cps) is preferred. Examples of cellulose derivatives include hydroxypropyl cellulose (hereinafter abbreviated as RPC), methyl cellulose, hydroxypropyl alkyl cellulose, and sodium carboxymethyl cellulose; natural polymers include sodium alginate, gum arabic, pullulan, and dextrin; and other polyacrylics. A copolymer of acids, their salts, and acrylic acid.

Examples include polyvinylpyrrolidone. Among these, RPC is particularly preferred. These polymeric substances may be used alone or in combination of two or more.

Examples of drugs as pharmacologically active substances used in the present invention include anti-inflammatory analgesics such as aniline drugs such as acetaminophen, anthrani drugs such as mefenamic acid, and pyrazolone drugs such as sulpirin. Salicylic acid drugs such as aspirin, phenylacetic acid drugs such as alclofenac, basic drugs such as thiaramide hydrochloride, other antibacterial drugs such as indomethacin, protidic acid, sulindac, piroxicam fentiazac, etc. Antibacterial agents include penicillin drugs. .

Hepphalosvorin series, macrolide series, chloramphenicol series, tetracycline series, lincomycin series, aminoglycoside series, etc. as antibiotics and quinolones, chemotherapeutic agents such as sulfa drug 2 synthetic chemical antibacterial agents, and steroid drugs as various steroid drugs. There is. The concentrations used are not particularly limited.

In the present invention, in addition to the above-mentioned water-soluble or water-swellable polymeric substances and drugs, glycerin, propylene glycol, polyethylene glycol, etc. can be used as humectants. Usually, the amount used is from about 0.1% to about 10% by weight of the formulation width.

The preparation of the present invention is in the form of a solution or gel, and has a viscosity of 20
from about 2 to about 6.000 cps, preferably from about 5 to about 6.000 cps at °C
Approximately 3. OO0cps.

In addition, in order to use the preparation of the present invention for the treatment of an affected area, it can be injected directly into the root canal or root apex using a syringe, or it can be applied by soaking it in strands of cotton or the like. Usually, about 0.05 d to about 0.5 mR of the formulation is used per dose.

[Examples] The present invention will be explained below with reference to Examples, but the present invention is not limited to these in any way.

<Example 1> Antibacterial agent ofloxacin (quinolone type) and anti-inflammatory analgesic agent Amfenac Na (
Aqueous liquid preparation containing phenylacetic acid (phenylacetic acid) (1) Preparation method: Dissolve 1 g ofloxacin in 198 ml of distilled water to make a saturated solution (pH 7,13), and add lN NaOH solution 3 to this.
, 4 ml was added to make a complete dissolution solution (P H1
1,24). Next, 20% phosphoric acid was added dropwise to adjust the pH to 7.15. Add 1 g of Amfenac Na to this solution and 0.0 g of Amfenac Na.
2 ml of an ethanol solution containing 5% methylparahen was added to make a pH 7.35 mixed solution, which was filtered using a 0.2 μm filter. 4.5 g of RPC-M (manufactured by Nippon Soda ■) was added to this filtrate and stirred to obtain an aqueous base having uniform viscosity.

The viscosity of this aqueous solution was approximately 500 cps at 20°C.

(2) Clinical case Targeting approximately 30 patients with refractory infected root canals, 90% of the patients had stranded cotton soaked in the aqueous solution prepared in (1) above and applied to the affected area with tweezers. However, the remaining 10% of patients received direct injection using a syringe.

After one week, approximately 80% of the patients showed a therapeutic effect, and almost all of them were completely cured within two weeks.

<Example 2> Aqueous liquid preparation (1) Preparation method in which the antibacterial agent talindamycin hydrochloride (lincomycin series) and the anti-inflammatory agent dexamethison (steroid agent) are blended into an aqueous solution of the water-soluble polymer substance HPC (1) salt 1 clidamycin 0. Dissolve 5 g of dexamethacin in 91 ttdl of distilled water and 0.1 g of dexamethacin in 2 ml of ethanol to prepare a mixed solution. Furthermore, ethanol solution containing 0.5% methylparaben? & l ml was added and mixed to make a total volume of 100 ml, and filtered through a 0.2 μm filter. 2.25 g of RPC-M was added to the filtrate, stirred, and stored at room temperature. The viscosity of this aqueous solution is approximately 4 at 20°C.
It was 50 cps.

(2) Clinical example Targeting approximately 20 patients with apical periodontitis, 90% of the patients were treated with the aqueous solution prepared in item (1) above soaked in strands of cotton and using tweezers to remove the affected area. and the remaining patients were injected directly with a syringe.

Approximately 80% of patients showed a therapeutic effect after about one week, and almost all of them were completely cured within two weeks.

〔effect〕

As shown in the examples, it is possible to treat infected root canals and apical periodontitis, for which there have been no effective treatment methods, in a short period of time by simply using a water-soluble or water-swellable polymeric substance mixed with a drug. It becomes possible to provide a remarkable therapeutic effect in a short period of time.

[Brief explanation of the drawing]

FIG. 1 is a diagram showing teeth and periodontal tissues.

Claims (1)

[Scope of Claims] 1) A preparation for treating infected root canals and apical periodontitis, characterized by containing a pharmacologically active substance in a pharmaceutically acceptable water-soluble or water-swellable polymeric substance. . 2) The water-soluble or water-swellable polymeric substance is one or more selected from the group of cellulose derivatives, natural polymers, polyacrylic acid and its salts, acrylic acid copolymers, and polyvinylpyrrolidone. The preparation for treating infected root canals and apical periodontitis according to item 1.