JPS6133122A - Preparation of tablet having improved disintegrating property - Google Patents

Abstract

PURPOSE:To obtain simply the titled tablet to be easily administrated, by blending an aqueous extracted solution of crude drug with cellulose glycolate or calcium cellulose glycolate to give powder, compression molding it together with an excipient, etc. CONSTITUTION:An aqueous extracted solution of crude drug or its concentrated solution is blended with cellulose glycolate or calcium cellulose glycolate as an adsorbent. The blend is dried to give powder, which is compression molded directly or optionally together with an excipient and a lubricant, to give tablets of crude drug having high hardness and improved disintegrating properties. The adsorbent is water-insoluble but has properties to absorb three times as much water as its own weight, it can be compression molded alone, and the adsorbent containing dried crude drug has improved compression molding properties and is tableted easily.

Description

DETAILED DESCRIPTION OF THE INVENTION (a) Object of the invention [Field of industrial application] This invention relates to a method for manufacturing tablets with good disintegration, and particularly to a method for manufacturing tablets of crude drugs.

[Prior art]

Herbal medicines have few side effects, exhibit a variety of pharmacological actions, and have a variety of uses. One of the methods of utilizing the medicinal components of crude drugs is to treat pulverized crude drugs with hot water and take the immersion liquid or hot liquid as it is. It is also made into tablets to make it easier to take. That is, the extract containing the soaking liquid and hot liquid is concentrated as much as possible, mixed with appropriate excipients, powdered, and added with additives necessary for tabletting (e.g., lubricants, disintegrants, etc.). ) is added and then compressed into tablets.

[Problem that the invention seeks to solve]

In the above-mentioned conventional technology, when taking the immersion liquid or hot liquid as is, there are problems in that the volume is large and it is difficult to take it due to unpleasant odor and taste, and it is easy to spoil and has poor storage stability. Furthermore, in the case of tabletting, the extract is generally concentrated as much as possible and then tabletted, but this concentration requires time and effort.

The present invention solves these problems and provides a simple method for producing crude drug tablets that are easy to take, have high hardness, and have good disintegration properties.

(B) Structure of the Invention This invention involves adding and mixing cellulose glycolic acid or its calcium salt to an aqueous extract of a herbal medicine or its concentrate, and drying the resulting powder, which can be used as it is or optionally with excipients.
The present invention provides a method for producing tablets with good disintegration, which is characterized by compression molding together with a lubricant.

When the drug is in the form of an oil or an aqueous solution, it has conventionally been adsorbed onto a powder and compression-molded as a powder. For example, fine particles of silicon oxide have been used as the adsorbent.

This invention uses cellulose glycolic acid or its calcium salt as an adsorbent for crude drugs. All of these are listed in the Japanese Pharmacopoeia as tablet disintegrants, and although they are water-insoluble, they have the property of absorbing about three times their own weight in water, and can be compressed into tablets even when used alone. can.

When an aqueous extract of a crude drug or its concentrate is mixed with powdered cellulose glycolic acid or its calcium salt, it is rapidly adsorbed. These can be easily dried to a moisture content of 1 to 10% using a ventilation dryer commonly used in the pharmaceutical industry. Therefore, even in the case of a concentrated solution, a slight concentration is sufficient.

It is generally said that compression molding of powder requires the presence of an appropriate amount of moisture, but in the case of 1asi glycolic acid or its calcium salt, it is normal drying conditions to overdry to less than the above moisture content m. Even if it is overdried, it will easily recover to the above moisture content if left under normal climatic conditions. The adsorbent of the present invention containing the dried crude drug has excellent compression moldability and is easy to tablet. For example, by adding a crude drug lubricant, compression molding is possible, and tablets containing the active ingredients of the crude drug at a high concentration can be obtained.

Although it is optional to add other excipients to the formulation, tablets with high hardness and high disintegration can be obtained. The good physical properties of these formulations are superior to conventional adsorbents such as silicon oxide.

Examples 1 and 2 and Comparative Example 1 Licorice extract was produced by the following method.

(1) 300 g of dried licorice was immersed in 1500 cc of water, left to stand for 2 days, and then separated into solid content and extract liquid (1) using fine gauze.

(2) 1000 cc of water was further added to the solid content, left to stand for one day, and extract liquid (2) was separated in the same manner.

(3) Combine extract (1) and extract ('2J) and heat.
Concentrate to approximately 60 CC and extract licorice extract (solid content, approximately 4
6%).

In contrast to the above licorice extract, approximately the same ship's cellulose calcium glycolate (ECG505 manufactured by Nichirin Kagaku Kogyo) (
Example 1), cellulose glycolic acid (NS300, manufactured by Nichirin Kagaku Kogyo) (Example 2), and microcrystalline cellulose (Avicel PHIOI manufactured by Asahi Kasei) (Comparative Example 1) were mixed, and each was completely absorbed. These were dried with ventilation at 70° C. for about 12 hours to obtain a powder in which medicinal ingredients were adsorbed. To these powders, 0.5% of a lubricant (calcium stearate) was added, and in the case of microcrystalline cellulose, 5% of a disintegrant (EC0505) was added. It was compressed into tablets and molded at the same pressure.

The hardness of the obtained tablet (Monsanto hardness tester), artificial gastric fluid (
Table 1 shows the time required for disintegration at a temperature of 36-31°C. In addition, the moisture content when the obtained tablets were left at 65% RH 120°C for one day and night is also listed, but compared to Comparative Example 1, Examples 1 and 2 are equivalent even though the moisture content is about twice as much. It has high hardness and extremely good disintegration properties.

The licorice extract in Table 1 deteriorated in quality after being left for 3 days, but no change in quality was observed in the tablets even after 1 month.

Example 3 A ginseng extract-containing powder was prepared using the following procedure.

(1) 18 g of dried ginseng root was immersed in 600 cc of water and gently boiled for 5 hours. Thereafter, the heating was increased and the volume was concentrated to about 300 cc.

(2J centrifuge to remove solids, add S to the extract
Fibrin calcium glycolate (E CG 505) 2
0Q was added, and the water/ethanol was distilled off under reduced pressure at 80° C. while adding ethanol.

(3) Finally, ethanol was distilled off from the ethanol slurry, and the resulting powder was dried with ventilation at 70° C. for about 12 hours. The yield was 21.5g.

The obtained extract-containing powder was tableted in the same manner as in Example 1 to obtain tablets with a hardness of 30k or more and a disintegration time of 7 to 8 minutes.

It should be noted that the above extract-containing powder could be taken as a powder, and had good storage stability.

(C) Effects of the Invention According to the present invention, it is possible to produce crude drug tablets that are easy to take, have high hardness, and have good disintegration properties without requiring much labor and time.

Claims (1)

[Claims] 1. Compression molding of the powder obtained by adding and mixing cellulose glycolic acid or its calcium salt to an aqueous extract of a crude drug or its concentrate and drying it as it is or with excipients and lubricants as desired. A method for producing tablets with good disintegration characteristics.