JPH08333246A - Ibuprofen suspension liquid - Google Patents

Abstract

PURPOSE: To obtain an ibuprofen suspension liquid having improved stability of ibuprofen, eliminating or alleviating an irritating feeling and bitterness during administration. CONSTITUTION: This ibuprofen-containing suspension liquid comprises menthol or menthol and an essence of a crude medicine. An antiseptic and a sweetener are completely dissolved in an aqueous solution having pH 2 to pH 5 in which a pH adjuster (e.g. phosphoric acid buffer solution) is dissolved. The crude medicine, menthol and optionally an antiseptic and a thickening agent are uniformly dispersed into the solution, which is mixed with ibuprofen and other pharmacodynamically effective components, a spice, etc., if required. The solution is heat-treated at 55-65 deg.C for 10-20 minutes to give the objective ibuprofen suspension liquid. The amount of menthol for one administration is 1-45mg, the amount of the crude medicine [e.g. KANNZOU (root of Glycyrrhiza glabra)] is 0.0001-0.1wt.% based on the whole amount of a preparation and that of ibuprofen is 1-60mg/ml.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an ibuprofen suspension for internal use in which the stability of ibuprofen is improved and the irritation sensation and bitterness upon administration are eliminated or reduced.

[0002]

BACKGROUND OF THE INVENTION Suspensions containing ibuprofen are
Due to the strong irritation and bitter taste of ibuprofen when taken, a satisfactory feeling of taking was not obtained. It is considered that the stimulating sensation and bitterness are caused by the release of ibuprofen, the growth of the crystals, and the precipitation / aggregation.
Regarding the masking of the bitterness of the ibuprofen suspension agent, JP-A-1-258618 and JP-A-2-258618 are known.
Although the technology described in No. 286615 is known,
I still don't get a satisfactory feeling.

[0003]

DISCLOSURE OF THE INVENTION The present invention provides a stable ibuprofen suspension which suppresses the release of ibuprofen, that is, an ibuprofen suspension in which the irritation sensation and bitterness upon administration are eliminated or reduced. With the goal.

[0004]

Means for Solving the Problems The present inventors have conducted a study on the bitterness of an ibuprofen oral liquid medication, and as a result, dl-form or l-form menthol was added, and a crude drug was added. The present invention has been completed by finding that irritation and bitterness when taking ibuprofen are eliminated or reduced.

The present invention is an ibuprofen suspension containing ibuprofen, characterized in that menthol or both menthol and a crude drug are blended. Still another aspect of the present invention is the ibuprofen suspension agent, which is characterized by being heat-treated in the coexistence of ibuprofen, menthol, and a herbal medicine.

In the present invention, menthol can be used in the form of dl or l, and the blending amount thereof is 1.0 to 45.0 mg per dose, preferably 2.0 per dose.
~ 18.0 mg.

In the present invention, the crude drug is a crude drug such as licorice, jellyfish, cinnamon syrup, peony, peony, valerian, salamander, ginger, chimp and the like, and one or more kinds of them are blended. The compounding amount of these crude drugs and their extracts is 0.0001 to 0.1% by weight, preferably 0.001 to 0.1% by weight based on the total amount of the preparation.
It is 02% by weight.

The surfactant in the present invention is a surfactant which is difficult to dissolve in ether such as sucrose fatty acid esters, polyoxyl stearates, polyoxyethylene polyoxypropylene glycols and polyoxyethylene monofatty acid esters. , And blend one or more of these. The blending amount of these surfactants is 0.001 to 10% by weight, preferably 0.0025, based on the total amount of the preparation.
~ 2% by weight.

The suspension of the present invention includes xanthan gum, pullulan, dextran, hyaluronic acid, chondroitin sulfate, carrageenan, guar gum, tara gum,
One or more thickeners having a small emulsion stability effect such as locust bean gum, sodium alginate, chito acid, and tamarind gum may be blended. The blending amount of these thickeners is 0.001 to 10 with respect to the total amount of the preparation.
%, Preferably 0.01 to 3% by weight.

The suspension of the present invention contains 1 part of ibuprofen.
˜60 mg / ml, anhydrous caffeine or caffeine 0.5 to 30 mg / ml can be blended. If necessary, other antipyretic analgesics, muscle relaxants, antispasmodics, antihistamines, sympathomimetics and the like can be added.

The suspension of the present invention can be manufactured by the following method. A preservative and a sweetener are added to an aqueous solution (pH 2.0 to 5.0) in which an organic acid-based or inorganic acid-based pH adjusting agent such as a citrate buffer solution or a phosphate buffer solution is dissolved, and the ingredients are completely dissolved. A crude drug, menthol, if necessary, a surfactant and a thickening agent are added to the solution and uniformly dispersed. Etc. are added, and the whole mixture is uniformly dispersed with a homomixer. Furthermore, after adding purified water to adjust the total amount to 100% by weight,
Heat treatment for 10 to 20 minutes.

The temperature of the heat treatment is in the range of 55 to 65 ° C, preferably 60 ° C. The pH range of the suspension of the present invention is 2.0 to 5.0, preferably 2.5 to 4.0.

[0013]

INDUSTRIAL APPLICABILITY According to the present invention, a stable ibuprofen suspension which suppresses the release of ibuprofen is provided, and an ibuprofen suspension in which irritation and bitterness during administration are removed or reduced is provided.

[0014]

EXAMPLES Next, the present invention will be described in detail by showing Examples and Test Examples.

Example 1 An aqueous solution (pH: pH adjusting agent (phosphate buffer))
Preservatives and sweeteners were added to 3.5) and completely dissolved. To the solution, TO10M as a surfactant and xanthan gum as a thickening agent were added and uniformly dispersed, then ibuprofen and other drugs were added, and the entire mixture was uniformly dispersed with a homomixer. Purified water was added to adjust the total amount to 100%, and then heat treatment was performed at 55 to 65 ° C. for 20 minutes. (In 30 ml) ibuprofen 144 mg anhydrous caffeine 50 mg l-menthol 1.0 mg TO10M 3.75 mg xanthan gum 60 mg sweetener 10000 mg preservative proper amount.

Example 2 In the same manner as in Example 1, a suspension containing the following components was obtained. (In 30 ml) ibuprofen 144 mg anhydrous caffeine 50 mg l-menthol 2.25 mg TO10M 3.75 mg xanthan gum 60 mg sweetener 10000 mg preservative proper amount.

Example 3 In the same manner as in Example 1, a suspension containing the following components was obtained. (In 30 ml) ibuprofen 144 mg anhydrous caffeine 50 mg l-menthol 4.5 mg TO10M 3.75 mg xanthan gum 60 mg sweetener 10000 mg preservative proper amount.

Example 4 In the same manner as in Example 1, a suspension containing the following components was obtained. (In 30 ml) Ibuprofen 144 mg Anhydrous caffeine 50 mg l-Menthol 9.0 mg TO10M 3.75 mg Xanthan gum 60 mg Sweetener 10000 mg Preservative A suitable amount.

Example 5 In the same manner as in Example 1, a suspension containing the following components was obtained. (In 30 ml) ibuprofen 144 mg anhydrous caffeine 50 mg l-menthol 4.5 mg licorice soft extract 166.7 mg TO10M 3.75 mg xanthan gum 60 mg sweetener 10000 mg preservative proper amount.

Example 6 A suspension was obtained by the same formulation and method as in Example 1 except that the heat treatment was not carried out.

Example 7 In the same manner as in Example 1, a suspension containing the following components was obtained. (In 30 ml) Ibuprofen 150 mg Anhydrous caffeine 25 mg l-Menthol 4.5 mg Keihi extract 100 mg TO10M 3.75 mg Xanthan gum 60 mg Sweetener 10000 mg Preservative proper amount.

Example 8 In the same manner as in Example 1, a suspension containing the following components was obtained. (In 30 ml) Ibuprofen 150 mg Anhydrous Caffeine 25 mg l-Menthol 4.5 mg Ginger extract 50 mg Dihydrocodeine phosphate 8 mg Methylephedrine hydrochloride 20 mg Chlorpheniramine maleate 2.5 mg TO10M 3.75 mg Xanthan gum 60 mg Sweeteners 10000 mg Sweeteners 10000 mg.

Example 9 In the same manner as in Example 1, a suspension containing the following components was obtained. (In 30 ml) ibuprofen 150 mg anhydrous caffeine 25 mg l-menthol 4.5 mg button pi extract 75 mg dihydrocodeine phosphate 8 mg methylephedrine hydrochloride 20 mg chlorpheniramine maleate 2.5 mg lysozyme chloride 20 mg (potency) TO10M 3.75 mg chondrotin sulfate 30 mg Agent 10000mg Preservative Suitable amount.

Example 10 In the same manner as in Example 1, a suspension containing the following components was obtained. (In 30 ml) ibuprofen 100 mg acetaminophen 150 mg anhydrous caffeine 25 mg l-menthol 4.5 mg carrot extract 25 mg dihydrocodeine phosphate 8 mg ambroxol hydrochloride 15 mg methylephedrine hydrochloride 20 mg chlorpheniramine maleate 2.5 mg lysozyme chloride 20 mg (potency) ) TO10M 3.75 mg Chondroitin sulfate 30 mg Sweetener 10000 mg Preservative Suitable amount.

Test Example [Sensory Evaluation Test] <Test Method> For each of the formulation examples in Table 1, 1
All doses were taken and evaluated. The evaluation was performed by 6 healthy adult volunteers. For sensory evaluation, the intensity of irritation to the throat was digitized by the following criteria and compared with each other.

Sensory evaluation 1: No irritation to the throat is felt. 2: Almost no irritation to the throat is felt. 3: Feels a little weak to the throat. 4: Feeling weak irritation. 5: I feel irritation to my throat. 6: I feel a little strong irritation to the throat. 7: I strongly feel irritation to my throat. 8: I feel a strong irritation to the throat.

<Results> As shown in Table 2, by incorporating 1-menthol or a herbal medicine extract (liquorice extract) or both, the ingestibility of the ibuprofen suspension was improved.

[0028]

[Table 1]

[0029]

[Table 2]

Continuation of the front page (51) Int.Cl. ⁶ Identification code Reference number within the agency FI Technical display location A61K 47/26 A61K 47/26 H 47/34 47/34 H 47/46 47/46 J (72) Inventor Toshiaki Nakajima 3-24-1, Takada, Toshima-ku, Tokyo Within Taisho Pharmaceutical Co., Ltd. (72) Inventor Kenji Tsunoda 3-24-1, Takada, Toshima-ku, Tokyo Within Taisho Pharmaceutical Co., Ltd.

Claims (6)

[Claims] 1. An ibuprofen suspension containing ibuprofen, wherein menthol is added to the ibuprofen suspension. 2. The ibuprofen suspension agent according to claim 1, which is heat-treated in the coexistence of ibuprofen and menthol. 3. An ibuprofen suspension containing ibuprofen, wherein menthol and a crude drug extract are blended. 4. The ibuprofen suspension agent according to claim 3, which is heat-treated in the coexistence of ibuprofen, menthol and a crude drug. 5. The ibuprofen suspension agent according to claim 4, which is heat-treated in the coexistence of ibuprofen, menthol, a crude drug, and a surfactant. 6. The surfactant is sucrose fatty acid ester,
The ibuprofen suspension agent according to claim 5, which is a polyoxyl stearate, a polyoxyethylene polyoxypropylene glycol, or a polyoxyethylene monofatty acid ester.