JP6549428B2 - Oral composition - Google Patents

Description

  The present invention relates to oral compositions and, more particularly, to oral compositions which contain butyl scopolamine bromide while masking its unpleasant taste.

  Butylscopolamine bromide has the effect of relieving stomachache, abdominal pain and soreness by relieving excessive tension and spasm of the gastrointestinal tract, and has been widely used as a gastrointestinal analgesia and spasm in OTC medicines.

  By the way, butylscopolamine bromide has a problem that it gives a feeling of discomfort when taken because it is very bitter and is very easily soluble in water. Therefore, as a method of concealing this bitter taste and improving the feeling of taking it, it has been used as a sugar-coated tablet or capsule, and a dosage form in which the drug does not start dissolving directly in the oral cavity.

  In addition, as a method of concealing the bitter taste in combination, butyl scopolamine bromide, stevia (patent document 1), specific flavor and sweetening agent (patent document 2), stomach-soluble polymer and nonionic disintegrant (patent document 3) The method of adding acid mucopolysaccharide, a refreshing agent, a sweetening agent (patent document 4), etc. is disclosed. Furthermore, a method of dissolving or suspending butylscopolamine bromide in a liquid excipient containing sucralose while maintaining the pH at about 2 to about 5 (Patent Document 5), or using double particles of butylscopolamine bromide as core particles. Also disclosed is a method (US Pat. No. 5,648,859) of applying a water-insoluble polymer as its outer layer coating agent.

  However, any of these methods is insufficient in effect, and in the technique of producing core particles and then coating it, it is a costly method in the production process, so it is expensive to adopt. Also had the problem of being difficult.

JP-A-9-52838 JP 10-273435 A JP-A-11-228393 JP, 2008-106048, A Japanese Patent Publication No. 2004-538309 JP 2008-37863 A

  Therefore, an object of the present invention is to provide an oral composition which effectively reduces the bitter taste of butylscopolamine bromide and which does not give discomfort when taken, more simply than the prior art.

  In order to develop a method for preventing the bitter taste of butylscopolamine bromide, the present inventors searched for masking effects of various materials, and formulated butylscopolamine bromide in combination with a thickener and an emulsifier to obtain butylscopolamine bromide. By dissolving or suspending in water, it has been found that an unpleasant bitter taste is suppressed and an oral composition excellent in feeling of taking can be obtained, and the present invention has been completed.

  That is, the present invention is an oral composition containing butyl scopolamine bromide, a thickener and an emulsifier, and dissolving or suspending butyl scopolamine bromide in an aqueous solution.

  The present invention is also the above oral composition further comprising a sweetening agent and / or an acidulant.

  The oral composition of the present invention can prevent or reduce the strong bitterness due to butylscopolamine bromide even in water by blending butylscopolamine bromide with a thickener and an emulsifier. Therefore, according to the present invention, it is possible to provide a patient with a drug which is excellent in taking properties.

As described above, butylscopolamine bromide, which is an active ingredient of the oral composition of the present invention (hereinafter referred to as "the present composition"), relieves excessive gastrointestinal tension and spasm, thereby causing stomachache, abdominal pain and depression. It has a soothing effect, and its molecular formula is C ₂₁ H ₃₀ BrNO ₄ , its molecular weight is 440.37.

  In the composition of the present invention, the content of butylscopolamine bromide is, for example, preferably 0.01 to 1.0% by mass (hereinafter, simply referred to as "%") in an oral composition, and 0.095 to 0.1%. Is more preferred. Moreover, as a ratio of solid content with respect to components other than water contained in this invention composition, content of butylscopolamine bromide is preferably 2.0 to 85%, and more preferably 7.5 to 80%. .

  The thickener used in the composition of the present invention is a polysaccharide thickener, and examples thereof include xanthan gum and carrageenan, which may be used alone or in combination of two or more. it can. Although the content of the thickener varies depending on the type of the thickener, for example, 10 to 80 parts by mass of the thickener is preferable to 10 parts by mass of butyl scopolamine bromide, and 10 to 40 parts by mass is more preferable. Also, 10 to 20 parts by mass is particularly preferable.

  Furthermore, as the emulsifier used in the composition of the present invention, for example, lecithin, soybean lecithin, purified soybean lecithin and purified egg yolk lecithin etc. may be mentioned, and one or more of them may be used in combination. it can. The content of the emulsifier is preferably 10 to 100 parts by mass, more preferably 10 to 40 parts by mass, and particularly preferably 10 to 20 parts by mass with respect to 10 parts by mass of butylscopolamine bromide.

  The composition of the present invention can be prepared by appropriately blending the above-mentioned components and forming a solution or a suspension, but it is possible to further blend a sweetening agent, and it is preferable to do so. This can further suppress the bitterness of butylscopolamine bromide. Examples of sweetening agents used herein include sucralose, acesulfame potassium, saccharin, saccharin sodium, aspartame, stevia extract, purified extract of stevia, thaumatin, disodium glycyrrhizinate, trisodium glycyrrhizinate, dipotassium glycyrrhizinate, etc. Be These sweeteners can be used alone or in combination of two or more.

  The content of the above-mentioned sweetener is preferably 2 to 15 parts by mass, more preferably 2.5 to 15 parts by mass, and still more preferably 3 to 10 parts by mass with respect to 10 parts by mass of butylscopolamine bromide. Preferably, 3 to 7.5 parts by mass is particularly preferable, and 3 to 5 parts by mass is more particularly preferable.

  An acidulant can be further incorporated into the composition of the present invention, and it is preferable to do so. This can further suppress the bitterness of butylscopolamine bromide. Examples of the acidulant used here include citric acid, malic acid, tartaric acid, lactic acid, ascorbic acid, erythorbic acid, succinic acid, fumaric acid and the like. These acidulants can be used alone or in combination of two or more.

  The content of the acidulant is preferably 2 to 30 parts by mass, more preferably 2.5 to 15 parts by mass, and still more preferably 3 to 10 parts by mass with respect to 10 parts by mass of butylscopolamine bromide. , 3 to 7.5 parts by mass is particularly preferable, and 3 to 5 parts by mass is more particularly preferable

As a particularly preferred embodiment of the composition of the present invention, the composition shown below can be mentioned.
10 parts by mass of butyl scopolamine bromide
Thickener 10 to 20 parts by mass
Emulsifier 10 to 20 parts by mass
Sweetener 2.5 to 15 parts by mass
Acidulant 2.5 to 15 parts by mass

  The composition of the present invention is prepared by adding each of the above-mentioned components and optional components used for ordinary oral pharmaceuticals formulated according to the purpose to water to form a solution or a suspension.

  Ingredients used for ordinary oral pharmaceutical products include preservatives, excipients, binders, disintegrants, perfumes, dyes and the like.

  Among these, as the preservative, benzoic acid, sodium benzoate, ethanol, glycerin, sorbitol, propylene glycol, phosphoric acid, potassium glutamate and the like are preferable.

  In addition, as the excipient, lactose, sucrose, glucose, crystalline cellulose, corn starch, mannitol, dextrin, trehalose and the like are preferable.

  Furthermore, as the binder, for example, crystalline cellulose, carmellose, carmellose sodium, hydroxypropyl cellulose, hypromellose, gelatin, pullulan, povidone and the like are preferable.

  Furthermore, as a disintegrant, for example, carboxymethyl starch sodium, carmellose calcium, croscarmellose sodium, hydroxypropyl cellulose, partially pregelatinized starch, crospovidone and the like are preferable.

  The composition of the present invention can be prepared using a conventional method used for internal use liquid preparations and the like. Each component is prepared by dissolving or suspending in purified water. At that time, as necessary, a part or all of each component is dissolved or suspended in a part of purified water in advance, a part or all of a purified water is heated or cooled, or filtered with a membrane filter or the like Or sterilization may be performed, or nitrogen substitution may be performed.

  The composition of the present invention prepared in this manner is excellent in the feeling of taking, despite containing butylscopolamine bromide, the bitterness of butylscopolamine bromide is suppressed by the action of a thickener, an emulsifier, etc. It is. Therefore, the composition of the present invention can be used as it is as a liquid preparation such as an oral liquid preparation, a syrup preparation or a jelly preparation, or as a semisolid preparation.

  In addition, by removing water from the composition of the present invention, it can be used as a solid preparation such as an orally disintegrating tablet, a film preparation, a troche tablet, granules, fine granules, dry syrup and the like. The solid preparation thus obtained, even when in contact with water or the like at the time of taking, can suppress the bitter taste of butylscopolamine bromide in that state, so it is easy to take.

  The dose of the composition of the present invention obtained as described above is 10 mg as butyl scopolamine bromide per dose up to three times a day for an OTC pharmaceutical. Moreover, if it is a medical drug, 10-20 mg can be administered per dose 3 to 5 times a day, and the dose may be appropriately adjusted depending on the age and symptoms.

  EXAMPLES The present invention will next be described in more detail by way of Examples and Comparative Examples, which should not be construed as limiting the invention in any way.

Example 1
Each ingredient is weighed according to the prescription shown in the following Table 1, and each prescription is put into a glass container. Next, 10 mL of purified water was added to each glass container, and an oral composition was manufactured using a magnetic stirrer by sufficiently stirring each component until it was dissolved or uniformly dispersed. By this, the oral composition of inventions 1 to 10 and comparisons 1 to 4 was obtained.

  About each obtained oral composition, the masking sensory test of bitterness was done in accordance with the following evaluation criteria about the taste and aftertaste at the time of dosing using five subjects. The respective average results are shown in Table 2.

<Masking evaluation criteria>
(Rating) (content)
4 points: very masking effect 3 points: masking effect 2 points: slight masking effect 1 point: slight masking effect 0 point: no masking effect

  From Inventive Product 1 and Inventive Product 2 in Table 2, the bitter taste of butylscopolamine bromide can be suppressed by blending a thickener and an emulsion in both the taste and aftertaste when taken. I understood. Moreover, it turned out that the masking effect of an after taste and aftertaste becomes high by mix | blending a sweetener and an acidulant further from the invention goods 3-the invention goods 10. FIG.

  On the other hand, Comparative Product 1 containing no emulsifier and Comparative Product 2 containing no thickener had almost no masking effect on the taste. In addition, Comparative Product 3 and Comparative Product 4 that did not contain both an emulsifier and a thickener had almost no masking effect in any of the taste and aftertaste even when a sweetener and an acidulant were blended. .

Comparative example 1
Each component was weighed according to the prescription of comparative products 5 to 8 shown in Table 3 below. Comparative products 5 to 8 were obtained in the same manner as in Example 1 above.

  A sensory test of bitter taste was conducted on the comparative products 5 to 8 in accordance with the same evaluation criteria as described above. The respective average results are shown in Table 4.

  From Comparative Product 5 to Comparative Product 8 in Table 4, when the sweetening agent, the acidulant or the thickening agent was individually blended, particularly, the aftertaste of butylscopolamine bromide had almost no masking effect at all.

The oral composition of the present invention prevents the bitter taste of butylscopolamine bromide and has an excellent feeling upon taking, so that it can be suitably used for various drugs and the like containing butylscopolamine bromide as an active ingredient.

Claims (11)

An oral composition comprising butyl scopolamine bromide, xanthan gum and lecithin , wherein butyl scopolamine bromide is dissolved or suspended in an aqueous solution. The oral composition according to claim 1, comprising 10 to 80 parts by mass of xanthan gum based on 10 parts by mass of butyl scopolamine bromide. The oral composition according to claim 1 or 2 , wherein 10 to 100 parts by mass of lecithin is contained with respect to 10 parts by mass of butylscopolamine bromide. The oral composition according to any one of claims 1 to 3 , further comprising a sweetening agent and / or an acidulant. The sweetening agent is one or more selected from sucralose, acesulfame potassium, saccharin, saccharin sodium, aspartame, stevia extract, stevia extract, stevia extract, thaumatin, disodium glycyrrhizinate, trisodium glycyrrhizinate and dipotassium glycyrrhizinate An oral composition according to claim 4 . The oral composition according to claim 4 or 5, which contains 2 to 15 parts by mass of the sweetening agent based on 10 parts by mass of butylscopolamine bromide. The oral composition according to any one of claims 4 to 6 , wherein the acidulant is one or more selected from citric acid, malic acid, tartaric acid, lactic acid, ascorbic acid, erythorbic acid, succinic acid and fumaric acid. object. The oral composition according to any one of claims 4 to 7 , which contains 2 to 430 parts by mass of the acidulant based on 10 parts by mass of butylscopolamine bromide. 10 to 20 parts by weight of xanthan gum , 10 to 20 parts by weight of lecithin , 2.5 to 15 parts by weight of a sweetening agent and 2.5 to 15 parts by weight of an acidulant based on 10 parts by weight of butylscopolamine bromide Item 9. An oral composition according to any one of Items 4 to 8 . A solid preparation obtained by removing water from the oral composition according to any one of claims 1 to 9 . The solid preparation according to claim 10 , which is an orally disintegrating tablet, a film preparation, a troche tablet, a granule, a fine granule or a dry syrup.