JPH1160503A - Solid preparation excellent in feeling when taken - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject preparation by including Teprenone and a medicinal agent with unpleasant taste to mask the unpleasant taste. SOLUTION: This solid preparation in the form of e.g. tablets, capsules, is obtained, through a conventional pharmaceutical manufacturing process, by including (A) Teprenone [6,10,14,18-tetramethyl-5,9,13,17-nonadecatetraen-2-one(geranylgeranyl acetone)] of the formula and (B) a medicinal agent with unpleasant taste such as bitter taste (e.g. ibuprofen, aspirin, chloramphenicol, diphenhydramine hydrochloride, magnoliae cortex, Atractylodes lancea rhizome); wherein the weight ratio B/A is pref. <=10.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a solid preparation excellent in ingestibility, in which unpleasant sensation during taking is reduced in a pharmaceutical preparation having irritation such as bitterness.

[0002]

2. Description of the Related Art Many of the active ingredients of pharmaceuticals have a stimulus such as bitterness, and various methods for masking bitterness have been used. In recent years, it has been a natural mission for drug providers to provide medicines that are easy to take without discomfort, especially in consideration of the benefits and compliance of patients and consumers. Conventionally, a method of masking stimuli such as bitterness has been a method of suppressing the dissolution of bitter components by applying a coating to the preparation in many cases. For example,
-27423 discloses a method of masking bitterness by coating a preparation with a film coating. However, film coating is not suitable for dosage forms other than tablets,
Further, in the case of granules and the like, there was a problem that the ingestibility was rather deteriorated due to roughness and the like.

[0003] As a coating method that can be used relatively widely without being limited to a specific dosage form, a method of masking bitterness by applying a coating with wax or the like to a preparation is often used. For example, JP-A-4-300821 discloses a method of coating a preparation with a wax-like substance such as a higher alcohol or a higher fatty acid, and JP-A-5-201855 discloses a method in which a water-soluble polymer such as a binder and a saccharide are dispersed. A method of providing an outer layer on a granule is disclosed. However, when such a coating with a wax or the like is applied, since the components of these coating agents are solid components that are insoluble in water, it is not possible to avoid deterioration of ingestibility such as roughness.
Furthermore, there was a problem that the preparation process was complicated.

As another method, for example, Japanese Patent Laid-Open No.
No. 327528 discloses a method of masking bitterness by supporting a bitter component in pores of a substance having a pore structure such as cellulose, and sealing the bitter component.In this method, a component having a stimulus such as bitterness is used. Since it cannot be completely enclosed and enclosed, the masking effect is weak, and the preparation process is complicated, so that it cannot be said to be an effective method.

[0005]

As a method which does not rely on coating with a coating agent, Japanese Patent Application Laid-Open No. 9-143100 discloses a method of masking bitterness by combining mannitol and lactose in combination. According to this method, it does not worsen the mouthfeel of the grain, etc., and it is said that there is an improvement in the ingestibility, but there is a disadvantage that the bitter taste masking effect is weak for a drug having a bitter taste, and it is more effective. A bitterness masking method is required. Accordingly, an object of the present invention is to find a general method that has a stronger bitter masking effect than before and furthermore is not limited by the target drug and dosage form, thereby allowing the contained active ingredient to be contained. An object of the present invention is to provide a pharmaceutical preparation excellent in ingestibility in which discomfort due to irritation such as bitterness is alleviated while maintaining stability.

[0006]

SUMMARY OF THE INVENTION Teprenone is an isoprenoid derivative widely used as a therapeutic agent for gastritis and gastric ulcer. The present inventors have conducted intensive studies in order to solve the above-mentioned problems, and as a result, by blending the above-mentioned teprenone in a drug having an unpleasant taste such as bitterness and irritation, the conventional ingestion deteriorates. The present inventors have found that the discomfort caused by the stimulation such as bitterness can be alleviated more strongly without any problem, and have completed the present invention.

[0007] That is, the present invention is a solid preparation containing teprenone and a drug having an unpleasant taste, in which the unpleasant taste is concealed, and can be easily produced without any complicated steps. It is possible.

[0008] Teprenone in the present invention has a structural formula

Embedded image 6,10,14,18-tetramethyl-5 represented by
9,13,17-nonadecatetraen-2-one (geranylgeranylacetone). Drugs having irritation such as bitterness in the present invention are not particularly limited, ibuprofen,
Caffeine, aspirin, acetaminophen, chloramphenicol, erythromycin, indomethacin,
Diphenhydramine hydrochloride, or a crude drug such as carrot, aloe, oak, koboku, engosaku, sojutsu, akamegawiwa, or an extract thereof. In short, the present invention can be applied to any ingredient that causes discomfort due to stimulation such as bitterness when taken. The solid preparation according to the present invention is a solid preparation containing 10 parts by weight or less, more preferably 5 parts by weight or less, still more preferably 3.5 parts by weight or less of a drug having an unpleasant taste with respect to 1 part by weight of teprenone.

The solid preparation in the present invention is not particularly limited, such as powders, granules, fine granules, capsules, pills and tablets. In short, the bitterness masking method of the present invention can be applied to any solid preparation.

[0010] The solid preparation of the present invention can be easily produced by a usual preparation method without going through any complicated steps. First, for example, since teprenone is an oily substance at normal temperature and normal pressure, teprenone is adsorbed to silicic anhydride, hydrated silicon dioxide, a porous substance, and the like. Next, a drug having an unpleasant taste, and if necessary, lactose, mannitol and the like, mixed with an excipient, and added with a binder such as polyvinylpyrrolidone and hydroxypropylcellulose, and granulated,
It can be dried and sieved to obtain granules. This can be further made into capsules and tablets by a usual method. As another granulation method, a usual method such as extrusion granulation, fluidized bed granulation or spray drying granulation can be used.

Hereinafter, the present invention will be described in detail with reference to Examples and Test Examples, but the present invention is not limited thereto.

[0012]

[Example 1] [Example] Mixer (Super mixer SMV-20 manufactured by Kawata)
50 g of hydrated silicon dioxide (Fuji Silysia) and 660 g of lactose (DMV) in a mold), and mix with stirring.
7.5 g was charged and adsorbed. After the adsorption treatment, 224.7 g of D-mannitol (Towa Kasei Kogyo Co., Ltd.) and 27.5 g of Kokuboku extract (333.6 g in terms of crude drug) were added and mixed by stirring to obtain a powdery solid preparation. This powdery solid preparation was packaged in 1 g portions, and used as a sample for the ingestion test in the examples. [ Comparative Example] A powder prepared from the above example except that teprenone was omitted was used as a comparative example. That is, after mixing 50 g of hydrated silicon dioxide (Fuji Silysia) and 660 g of lactose (DMV) into a mixer (Super Mixer SMV-20 manufactured by Kawata) and mixing with stirring, 262.2 g of D-mannitol (Towa Kasei Kogyo) was added. 27.5 g of Koboku extract (333.6 g of crude drug equivalent) was added and further mixed by stirring to obtain a powdery solid preparation. This powdery solid preparation was packaged in 1 g portions, and used as a sample for a compliance test of Comparative Example.

[0013]

Test Example 1 Each of the samples for the ingestion test of the examples and the control produced in Example 1 was handed over to volunteers.
A comparative test on bitterness and discomfort was conducted. Table 1 shows the results.

[0014]

[Table 1]

[0015]

[Example 2] [Example] Mixer (Kawata Super Mixer SMV-20)
50 g of hydrated silicon dioxide (Fuji Silysia) and 890 g of lactose (DMV) in a mold, and mix with stirring.
0 g was charged and adsorbed. After adsorption treatment, caffeine 10g
And mixed by stirring to obtain a powdery solid preparation. This powdery solid preparation was packaged in 0.5 g portions, and used as a sample for a test of the ingestibility in the examples. [ Comparative Example] A powder prepared from the above example except that teprenone was omitted was used as a comparative example. That is, 50 g of hydrated silicon dioxide (Fuji Silysia), 940 g of lactose (DMV) and 10 g of caffeine were added to a mixer (Kawata Super Mixer SMV-20).
And mixed by stirring to obtain a powdery solid preparation. This powdery solid preparation was packaged in 0.5 g portions, and used as a sample for a compliance test of Comparative Example.

[0016]

Test Example 2 Each of the samples prepared in Example 2 and the control example for the ingestion test was handed to volunteers.
A comparative test on bitterness and discomfort was conducted. Table 2 shows the results.

[0017]

[Table 2]

[0018]

[Example 3] [Example] Mixer (Super mixer SMV-20 manufactured by Kawata)
50 g of hydrated silicon dioxide (Fuji Silysia) and 870 g of lactose (DMV) in a mold), and stir and mix.
0 g was charged and adsorbed. After the adsorption treatment, 30 g of Engosaku extract (300 g of crude drug equivalent) was added and stirred and mixed to obtain a powdery solid preparation. This powdery solid preparation was packaged in 0.5 g portions, and used as a sample for a test of the ingestibility in the examples. [ Comparative Example] A powder prepared from the above example except that teprenone was omitted was used as a comparative example. That is, 50 g of hydrated silicon dioxide (Fuji Silysia), 920 g of lactose (DMV) and 30 g of Engosaku extract (300 g of crude drug equivalent) were put into a mixer (Super Mixer SMV-20, manufactured by Kawata), and mixed by stirring. A solid preparation was obtained. This powdery solid preparation was packaged in 0.5 g portions, and used as a sample for a compliance test of Comparative Example.

[0019]

Test Example 3 Each of the samples for the test of the ingestibility of the example and the control prepared in Example 3 was handed to volunteers.
A comparative test on bitterness and discomfort was conducted. Table 3 shows the results.

[0020]

[Table 3]

[0021]

From Tables 1, 2 and 3, it is clear that the solid preparation of the present invention masks unpleasant tastes such as bitterness. Conventional masking of bitterness has a weak effect on components having bitterness, and even if masking of bitterness is possible, the feeling of taking the drug is worsened, such as roughening of the preparation surface. INDUSTRIAL APPLICABILITY The present invention is effective for a component having a bitter taste, and can be formulated by simply passing through a generally known simple formulation process. ADVANTAGE OF THE INVENTION By this invention, the discomfort of bitterness etc. was relieved and the solid dosage form excellent in ingestibility was able to be provided.

Claims (3)

[Claims] (1) A solid preparation comprising teprenone and a drug having an unpleasant taste, wherein the solid preparation conceals an unpleasant taste. 2. The solid preparation according to claim 1, wherein the drug having an unpleasant taste is a crude drug. 3. The solid preparation according to claim 1, wherein the drug having an unpleasant taste is Kokuboku or Soujutsu.