JPH1160504A - Tablet composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a tablet composition by including sodium bicarbonate to improve medicinal ingredient leaching tendency. SOLUTION: This tablet composition is obtained by formulating sodium bicarbonate in the original tablet composition (e.g. >=5 min in disintegration time in the disintegration test listed in the Japanese pharmacopeia) to improve the leaching tendency of the medicinal ingredient contained therein (e.g. derived from natural products, such as senna extract, licorice extract, Kakkon-tou, Hachimi-jio-gan, Kikyo-tou); wherein the amount of the sodium bicarbonate to be formulated is pref. 3 wt.% based on the above medicinal ingredient.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a tablet composition having improved dissolution of a medicinal ingredient.

[0002]

2. Description of the Related Art Among drugs, for example, chloramphenicol, phenacetin, prednisolone, spironolactone, diazepam, phenytoin, dicumarol and digoxin have been known as poorly dissolving and water-soluble in water.

[0003] Conventionally, as a countermeasure for a drug having poor dissolution as described above, a method of improving the dissolution by chemically modifying the active ingredient itself, an additive to be added to a pharmaceutical formulation, for example, a type of disintegrant In addition, a method has been adopted in which the dissolution property is improved by examining the amount and the amount of the mixture or adding a surfactant or the like.

[0004]

However, methods for improving the dissolution property by chemically modifying the active ingredient itself include:
Not only does the cost increase due to an increase in the number of steps, but also there are problems such as labor and yield. Particularly when the active ingredient is a component derived from a natural product, the cost of the active ingredient is relatively high, and chemical This problem is often serious due to the low yield of the desired product depending on the modification reaction.

[0005] In addition, the method of adding a disintegrant or the like to a pharmaceutical formulation also requires that disintegrants such as carboxymethylcellulose, croscarmellose sodium and partially pregelatinized starch used in the formulation are expensive, leading to an increase in cost. There is a problem and an adverse effect on the formulation process (granulation and tableting properties are reduced).

[0006] As described above, in spite of a desire for improvement in dissolution properties, it has not been easy in practice.

[0007] The present invention has been made to solve the above-mentioned disadvantages of the prior art and to provide a tablet composition having improved dissolution of a medicinal ingredient.

[0008]

Means for Solving the Problems To achieve the above object, the composition of the tablet composition employed in the present invention is, for example, a tablet composition having a disintegration time of 5 minutes or more in a disintegration test described in the Japanese Pharmacopoeia. On the other hand, the compound is characterized in that the dissolution property of a medicinal component is improved by blending sodium hydrogen carbonate.

[0009]

DESCRIPTION OF THE PREFERRED EMBODIMENTS The present invention will be described below in detail.

[0010] The present invention is a tablet composition in which the dissolution property of a medicinal component is improved by blending sodium hydrogen carbonate as described above. This sodium hydrogen carbonate is used as an antacid or an acidosis inhibitor. It is known that it is contained in the composition of a drug and is also used as a raw material for a drug, but it is generally contained in the base of an effervescent drug.

The present invention is particularly applicable to tablet compositions having a disintegration time of 5 minutes or more in the disintegration test described in the Japanese Pharmacopoeia, in particular, not applicable or difficult to comply with the rules of this disintegration test (within 30 minutes for uncoated tablets). It is effective when applied to various tablet compositions.

The medicinal component in the tablet composition of the present invention is not particularly limited, and examples thereof include components derived from natural products such as plant extracts and Chinese herbal extracts. In addition, the natural product-derived component may be of one type or two or more types.

Examples of the plant extract include, but are not limited to, senna extract, carrot extract, licorice extract, peony extract, sycin extract, juniper extract, shin yi extract, ginger extract, and ogi extract. .

[0014] Examples of the Kampo extract include Kakkonto, Kakkonyu Kagawa Kyuhoshii, Otoji-yu, Annakasan, Jumi-toxin-to, Hachimi-jio-maru, Dai-saiko-to, Sho-saiko-to, Saiko-keishi Hot water,
Saiko-ka-ryukotsuboreito, Hangeshashinto, Oren-dokuto, Hangesatsu-koboku-to, Gorei-san, Shosei-ryu-to, Koki-ki-go-to, Shofu-san, Tokishakuyaku-san, Kami-shoyo-san, Keishi-sho Bukuryo-gan, Keishika-ryukotsuboreito, Mao-to, Bakumondoto, Shigyakusan, Ryokei-jutsu-kanto, Hochu-ekki-to,
Keishi-to, Shichimono-descent-yu, Juzen-taiho-to, Jingaku-ryo-to, Seiki-kami-hofu-to, Bofu-tsu-sei-san, Megami-san, Shakuyaku-kanzo-to, Hira-gasan-san, Dai-o-kanzo-to, Toki-in-ko, Rokumi-maru On the other hand, Shokenchuto, Daikenchuto, Shinseiseito, Gyusha-Nekikimaru, Saireito, Bukuryo-chonai-kokakuto, Orento, Tokikenchuto, Keishibukuryomaru In addition, there may be mentioned, for example, but not limited to, okuinin, asojinmaru, mao-bushi-saishin-to, keishi-ka-shakuyaku-dai-o-to, seika-ekki-to, kikyo-to.

The Kampo extract is obtained by extracting, concentrating and drying a crude drug. Generally, it has a high binding ability and easily absorbs moisture. It is difficult. In addition, the daily dose is as high as 6000 mg, which is much higher than the dose of the active ingredient of the new drug. That is, when preparing such a Kampo extract, it is necessary to reduce the amount of excipients in order to improve the feeling of taking as much as possible. Therefore, in the disintegration test listed in the Japanese Pharmacopoeia, the disintegration time is 5 minutes or more. Is often recognized.

In the present invention, the amount of sodium bicarbonate used together with the above-mentioned active ingredient is preferably 3% or more, particularly preferably 7%, based on the weight of the active ingredient.
% To 70%. When the amount of sodium hydrogencarbonate is less than 3%, the effect of the addition is not so noticeable.

Excipients and lubricants can be appropriately added to the tablet composition of the present invention, if necessary, such as sugars such as lactose, candy powder and sucrose; corn starch. , Dextrin, PCS and the like; starches such as crystalline cellulose and hydroxypropyl cellulose; and inorganic substances such as magnesium aluminate metasilicate, magnesium stearate, nylon and titanium oxide.

The method for preparing the tablet composition of the present invention is not particularly limited, and a general tableting machine can be used.

[0019]

Next, the present invention will be described in detail with reference to examples.

Example 1-1 Windproof Tsushosan Extract Powder Windproof Tsushosan Extract Powder 78.12% by weight Sodium bicarbonate 10.44% by weight (about 13.36% based on Windproof Tsushosan Extract powder) Cellulose 10.74% by weight Magnesium stearate 0.70% by weight Each of the above-mentioned raw materials was sieved using a sieve, weighed based on the above blending ratio, and the mixture was used as a mixed powder for tableting.
This was tableted using a tableting machine.

The tablets obtained as described above were subjected to a dissolution test by the second method (paddle method) of the dissolution test published in the Japanese Pharmacopoeia under the following conditions. Figure 1 shows the results
It was shown to. Test solution: Purified water (37 ° C ± 0.5 ° C) Test solution volume: 900 mL Paddle rotation speed: 50 rpm Detector: UV

Examples 1-2 to 1-4 and Comparative Example 1 Tablets were obtained and dissolved in the same manner as in Example 1-1 except that the weights of sodium hydrogen carbonate and crystalline cellulose were changed as shown in Table 1 below. The test was performed. The results are shown in FIG.

[0023]

[Table 1]

Example 2-1 Gorei-san extract tablets Gorei-san extract powder 68.63% by weight Sodium bicarbonate 20.57% by weight (about 29.97% based on Gorei-san extract powder) Cellulose 10.30% by weight Magnesium stearate 0.50% by weight Using the above raw materials, tablets were obtained in the same manner as in Example 1-1.
A dissolution test was performed. The results are shown in FIG.

Examples 2-2 to 2-4 and Comparative Example 2 Tablets were obtained and dissolved in the same manner as in Example 1-1 except that the weights of sodium hydrogen carbonate and crystalline cellulose were changed as shown in Table 2 below. The test was performed. The results are shown in FIG.

[0026]

[Table 2]

Example 3-1 Tokishakuyakusan extract tablet Tokishakuyakusan extract powder 83.33% by weight 14.17% by weight of sodium bicarbonate (about 17.00% based on Tokishakuyakusan extract powder) Cellulose 2.00% by weight Magnesium stearate 0.50% by weight Using the above raw materials, tablets were obtained in the same manner as in Example 1-1.
A dissolution test was performed. The results are shown in FIG.

Examples 3-2 to 3-8 and Comparative Example 3 Tablets were obtained and dissolved in the same manner as in Example 1-1 except that the weights of sodium hydrogen carbonate and crystalline cellulose were changed as shown in Table 3 below. The test was performed. The results are shown in FIG.

[0029]

[Table 3]

Example 4 Homi-kogi-to extract powder 74.00% by weight of antimi-gogi-to extract powder 25.00% by weight of sodium hydrogen carbonate (approximately 33.78% with respect to the anti-mi-gogi-to extract powder) 1.00% by weight of magnesium stearate Using the above raw materials, a tablet was obtained in the same manner as in Example 1-1,
A dissolution test was performed. The results are shown in FIG.

Comparative Example 4 A tablet was obtained and a dissolution test was carried out in the same manner as in Example 1-1 except that crystalline cellulose was used instead of sodium hydrogen carbonate. The results are shown in FIG.

Example 5-1 Gushi-Carne Ki-Gan Extract Powder 72.50% by weight of Gushi-Carne Ki-Gan Extract Powder 10.00% by weight of sodium bicarbonate (about 13.79% based on Gushi-Carne Ki-Gan Extract Powder) Cellulose 17.00% by weight Magnesium stearate 0.50% by weight Using the above raw materials, a tablet was obtained in the same manner as in Example 1-1.
A dissolution test was performed. The results are shown in FIG.

Examples 5-2, 3 and Comparative Example 5 Tablets were obtained in the same manner as in Example 1-1 except that the weights of sodium hydrogen carbonate and crystalline cellulose were changed as shown in Table 4 below, and a dissolution test was performed. Carried out. The results are shown in FIG.

[0034]

[Table 4]

Example 6 Keishi-bukuryo pill extract powder Keishi-buku-ryo pill extract powder 56.00% sodium bicarbonate 10.00% crystalline cellulose 33.50% magnesium stearate 0.50% And a tablet was obtained in the same manner as in Example 1-1.

Example 7 Shoseiryuto extract powder Shoseiryuto extract powder 75.00% Sodium bicarbonate 12.00% Crystalline cellulose 12.50% Magnesium stearate 0.50% In the same manner as in -1, a tablet was obtained.

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[Procedure amendment]

[Submission date] November 7, 1997

[Procedure amendment 1]

[Document name to be amended] Statement

[Correction target item name] Brief description of drawings

[Correction method] Added

[Correction contents]

[Brief description of the drawings]

FIG. 1 is a graph showing the results of a dissolution test of Examples 1-1 to 1-4 and Comparative Example 1.

FIG. 2 is a graph showing the results of dissolution tests of Examples 2-1 to 2-4 and Comparative Example 2.

FIG. 3 is a graph showing the results of a dissolution test of Examples 3-1 to 3-8 and Comparative Example 3.

FIG. 4 is a graph showing the results of a dissolution test of Example 4 and Comparative Example 4.

FIG. 5 is a graph showing the results of a dissolution test of Examples 5-1 to 5-3 and Comparative Example 5.

Continued on the front page (72) Inventor Hideyuki Maruyama 3586 Yoshiwara, Ami-cho, Inashiki-gun, Ibaraki Pref.

Claims (7)

[Claims] Claims: 1. A tablet composition characterized in that the dissolution of a pharmaceutically active ingredient is improved by blending sodium bicarbonate. 2. In the disintegration test described in the Japanese Pharmacopoeia, the dissolution property of a medicinal component is improved by adding sodium hydrogen carbonate to a tablet composition having a disintegration time of 5 minutes or more. Tablet composition. 3. The medicinal component is one or two of natural component-derived components.
The tablet composition according to claim 1 or 2, which is at least one species. 4. The tablet composition according to claim 3, wherein the component derived from a natural product is a plant extract. 5. The tablet composition according to claim 3, wherein the component derived from a natural product is a Kampo extract. 6. The herbal extract is Kakkon-to, Kakkon-to-Kagawa Kyu-Shin-i, Oji-ji-to, Annaka-san, Jumi-toxin-to, Hachimi-jio-gan, Dai-saiko-to, Sho-saiko-to, Saiko-keishi-to, Saiko-to Karyukotsuboreito, Hangeshashinto, Oren-dokuto, Hangesatsu-koboku, Goreisan, Shoseiryuto, Boku-ki-goto, Shofu-san, Toki-Shakuyaku-san, Kami-shoyo-san, Keishi-bukuryo-maru , Keishi-ka-ryukotsuboreito, Mao-to, Bakumondo-to, Shigyakusan, Ryokei-jutsu-kan-yu, Hochu-ekki-to, Keishi-to, Shichimono-descent-to, Juzen-taiho-to, Jingaku-ren-yo , Seikatsu Hofuyu, Hofutsu Seisho, Meishan, Shakuyaku kanzoto, Hiragansan, Daiokanzoto, Toki Yoko, Rokumimaru, Jiji-Hatsu, Shokenchuto, Daikenchuto, Shinyaku Hot water, beef cart Nekkiki-maru, Saireito, Bukuryo-drinking Hankato, Oren-to, Tokikenchu-to, Keishi-bukuryo-maru-ka-yokujin, Asako-inmaru, Mao-bushi-saishin-to, Keishi-ka-shakuyaku 6. The method according to claim 5, which is Taikyo-to, Seishatsu-ekki-to, Kikyo-to, etc. Tablet composition. 7. The tablet composition according to claim 1, wherein the amount of sodium hydrogencarbonate is 3% or more based on the weight of the active ingredient.