JP2001010977A - Composition for oral administration - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for oral administration having decreased discomfortable feeling by including an antipyretic analgesic agent giving discomfortable feeling to the palate and laryngopharynx part in taking in combination with a local anesthetic. SOLUTION: This composition contains (A) an antipyretic analgesic agent giving discomfortable feeling to the palate and laryngopharynx part in taking (e.g. ibuprofen, ketoprofen, ethenzamide, naproxen, dichlofenac and loxoprofen) and (B) preferably 0.0001-1 pt.wt. (based on 1 pt.wt. of the component A) of a local anesthetic (e.g. lidocaine, dibucaine, tetracaine, procaine and camphor). As a result of the formulation of the above components, the composition can be used as cold remedy, antitussive expectorant, agent for rhinitis, agent for laryngopharynx, analgesic antispasmodic agent, gastrointestinal agent, quasi-drug, health food, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an oral composition for reducing discomfort caused by taking an antipyretic analgesic which causes discomfort in the oral cavity and throat.

[0002]

BACKGROUND OF THE INVENTION In everyday life, one often encounters the need to take a preparation containing an antipyretic analgesic. Antipyretic analgesics are used in a wide range of pain diseases such as headache, toothache, menstrual pain, arthralgia, muscle pain, fever due to various causes, and chills. However, some antipyretic analgesics are unpleasant in the oral cavity and throat when taking the drug, so that they often hesitate to take the drug. This has led to a decrease in compliance (compliance with medication). Even if a drug with a high potency has been developed with difficulty, the expected effect will not be obtained unless the drug is taken according to the usage and dosage.

[0003] In this regard, pharmaceutical preparations for improvement have been conventionally made, but no preparations satisfying the compliance have been obtained yet.

[0004]

SUMMARY OF THE INVENTION An object of the present invention is to provide an oral anti-pyretic analgesic which has a reduced discomfort in the oral cavity and pharyngeal region when the drug is taken. .

[0005]

Means for Solving the Problems In order to solve the above problems, the present inventors have focused on nerves that transmit discomfort caused by taking antipyretic analgesics, and as a result of intensive studies, they have found that The present inventors have found that the drug significantly inhibits the transmission of discomfort and that the feeling of taking the antipyretic analgesic is remarkably improved, thereby completing the present invention. That is, the present invention is an oral composition containing an antipyretic analgesic and a local anesthetic which cause discomfort in the oral cavity and throat when taken.

[0006] It is not clear at present how the local anesthetic acts on discomfort in the oral cavity and pharynx when taking antipyretic analgesics. Its use is not known.

[0007]

BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, the oral cavity / pharynx and larynx are a general term for the oral cavity, pharynx and larynx, and refer to the parts that cause discomfort when taking antipyretic analgesics. Here, the unpleasant sensation refers to an unpleasant flavor such as bitterness and irritating taste felt in the oral cavity, an unpleasant burning sensation felt in the throat head, and the like. In the present invention, the antipyretic analgesic causing discomfort in the oral cavity and throat,
Examples include ibuprofen, ketoprofen, etensamide, naproxen, diclofenac, loxoprofen, and salts thereof, and one or more of these may be blended.

[0008] The dose of these antipyretic analgesics can be used within the range normally used as pharmaceuticals, and can be appropriately increased or decreased depending on age, weight, and medical condition.

In the present invention, a local anesthetic refers to a drug used as a drug, and includes lidocaine, dibucaine, tetracaine, procaine and salts thereof, and one or more of them can be used. In addition, camphor, creosote, eucalyptus oil, cauliflower oil, clove oil, which are known to have a local anesthetic effect in addition to the above, as well as extracts from goshyu, sanshishi, ginger, and gingerbread, can be appropriately blended. And especially camphor.

In the oral composition of the present invention, the mixing ratio of the local anesthetic to the antipyretic analgesic which causes discomfort in the oral cavity and the throat can be varied in a wide range depending on the type and dosage of the antipyretic analgesic and the local anesthetic. It can be selected and can contain 0.0001 to 1 part by weight of a local anesthetic for 1 part by weight of an antipyretic analgesic.

In the oral composition of the present invention, if necessary, an antiallergic drug, an antihistamine, an anti-inflammatory enzyme, a bronchodilator, an antitussive, an expectorant, a sympathomimetic, an anticholinergic, a caffeine, etc. Ingredients such as vitamins and vitamins can be appropriately blended.

The oral composition of the present invention includes, for example, a powder,
It can be used as a dosage form such as fine granules, granules, dry syrups, lozenges, drops, lozenges, oral dissolving agents, dissolving agents at the time of use, suspensions, streams, liquids for internal use, etc. .

These preparations can be prepared by a conventional method and are not particularly limited. Excipients in the case of solid preparations,
Lubricants, disintegrants, surfactants, antioxidants, coating agents, and the like, and other perfumes, pigments, flavoring agents, and the like can be used as necessary. In the case of a liquid preparation for internal use, a solubilizing agent, a surfactant, a thickener, a pH adjuster, etc., as required, a preservative, a fragrance, a pigment, a sweetener, a sweetener, a refreshing agent,
A coloring agent or the like can be used.

The oral composition of the present invention may further comprise a cold medicine, an antitussive expectorant, a drug for rhinitis,
It can be used for pharyngolaryngeal drugs, analgesic / spasmodic drugs, gastrointestinal drugs, etc., and can be used in a wide range of forms such as quasi-drugs and health foods if necessary.

[0015]

According to the present invention, it has become possible to reduce the discomfort and to maintain and improve the compliance of antipyretic analgesics which cause discomfort in the oral cavity and pharynx during taking.

[0016]

The present invention will be described in detail with reference to the following examples and test examples, but the present invention is not limited to the following examples.

Example 1 The following components and amounts were weighed and uniformly mixed with a V-type mixer for 10 minutes.
m). The pulverized powder obtained was mixed with a vertical granulator at a rotation speed of 150 rpm and a cross screw 1
Under conditions of 000 rpm, 60 g of ethanol was added and granulated. The granulated product is put into a fluidized bed drier,
Let dry for hours. After drying, the mixture was sieved using a 24 mesh sieve to obtain a powder.

Lidocaine hydrochloride 30 g Sodium citrate 100 g Ketoprofen 450 g Stevia 30 g Example 2 The following components were weighed so as to have the following concentrations, and dissolved in purified water to give an oral solution.

Tetracaine hydrochloride 10 mM Sodium citrate 10 mM Diclofenac sodium 150 mM Example 3 The following components and amounts were weighed, dissolved in purified water, and adjusted to pH 4.5 with citric acid. did.

Procaine hydrochloride 4 g Sodium citrate 5 g Ibuprofen 45 g Polysorbate 80 1 g Dipotassium glycyrrhizinate 10 g Example 4 The following components and amounts were weighed, dissolved in purified water, and adjusted to pH 4.2 with citric acid. 5 L was used as an oral liquid preparation.

Lidocaine hydrochloride 5 g Sodium citrate 5 g Naproxen 30 g Polysorbate 80 1 g Example 5 The following components and amounts were weighed, dissolved in purified water, adjusted to pH 4.5 with citric acid, and made up to 5 L with a total volume of 5 L. And

Procaine hydrochloride 2.5 g Sodium citrate 5 g Loxoprofen sodium 15 g Polysorbate 80 1 g Dipotassium glycyrrhizinate 10 g Test example 1 Study on improvement of discomfort in the oral cavity and pharynx larynx 38 healthy subjects (18 males, 20 females, average Age 2
9.4 years old) were randomly divided into two groups of 19 persons each, and 10 ml of the following test drug or comparative drug was taken.

Test drug: 10.3 g of ibuprofen and 10 mg of lidocaine hydrochloride were added to a solution obtained by dissolving 50 g of polysorbate 80 in 500 mL of purified water, followed by stirring and dissolving, and the total amount was made up to 1000 mL with purified water.

Comparative drug: A drug prepared by removing lidocaine hydrochloride from the above test drug was prepared in the same manner as the test drug.

The relative intensity of the discomfort remaining in the oral cavity and throat after 30 seconds is rated on a scale of 100 (the highest discomfort that can be imagined 100, the strong discomfort 48, the moderate discomfort 2
5, weak discomfort 10, slight discomfort 4, discomfort 0), quantified and evaluated (BG Gre)
en, et al. Chemical SensesV
ol. 18 (6) 683-702, 1993). The results are shown in Table 1. As is clear from Table 1, the test drug showed a significant discomfort reduction effect as compared with the comparative drug.

[0026]

[Table 1]

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 31/196 A61K 47/14 47/14 47/18 47/18 47/22 47/22 47/44 47 / 44 47/46 47/46 A61P 1/00 A61P 1/00 11/02 11/02 11/04 11/04 11/10 11/10 11/14 11/14 29/00 29/00 A61K 9/14 (72) Inventor Kenji Tsunoda 3-24-1, Takada, Toshima-ku, Tokyo F-term in Taisho Pharmaceutical Co., Ltd. ZA592 ZA622 ZA632 ZA662 ZB332 4C206 AA01 AA02 DA23 DA24 DA25 FA31 FA37 FA38 GA08 GA31 MA02 MA05 MA14 MA72 NA06 ZA07 ZA08 ZA29 ZA34 ZA59 ZA62 ZA63 ZA66 ZB33

Claims (5)

[Claims] An oral composition containing an antipyretic analgesic and a local anesthetic which cause discomfort in the oral cavity and pharynx when taken. 2. The antipyretic analgesic which causes discomfort in the oral cavity and pharynx when taken, is one or more selected from ibuprofen, ketoprofen, etensamide, naproxen, diclofenac, loxoprofen, and salts thereof. 2. The composition for oral use according to item 1. 3. The oral composition according to claim 1, wherein the local anesthetic is one or more selected from lidocaine, dibucaine, tetracaine, procaine and salts thereof. 4. A local anesthetic of 0.0001 to 1 part by weight of an antipyretic analgesic which causes discomfort in the oral cavity and throat during administration.
The oral composition according to claim 1, which contains 1 part by weight. 5. The oral composition according to claim 1, wherein the discomfort of the antipyretic analgesic which causes discomfort in the oral cavity and pharynx during administration is reduced.