JPH1045628A - Agar for tablet and preparation of tablet - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain agar useful as a tablet base or assistant capable of imparting a tablet with excellent disintegrability, especially high disintegration rate by adding water to solid or powdery agar to effect the absorption of water and dehydrating and drying the swollen agar. SOLUTION: An agar (A) useful as a tablet base or assistant to form a tablet mixed with a drug and having a definite shape is produced by adding water to a solid or powdery agar (B) to effect the absorption of water and again dehydrating and drying the swollen agar by hot-air drying, freeze-drying, vacuum drying, etc. The agar (A) is produced preferably by adding water to an agar obtained by filtering an extract of seaweed or to the component B, dissolving the agar by heating, cooling the obtained agar sol to form an agar gel (C), freeze-drying the product C as it is or after pulverization and crushing the freeze-dried product. The agar (A) capable of imparting a tablet with excellent disintegrability as well as sufficient tablet strength can be produced by the process.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a method for producing agar which is used as a base or auxiliary for mixing tablets with a medicine to form tablets of a uniform shape, and a method for producing tablets using agar produced by the method. About.

[0002]

2. Description of the Related Art Tablets are obtained by molding a medicine into a certain shape, and are molded as they are, or in many cases, by mixing other additives. Depending on the production method, tablets are classified into wet tablets in which a drug or other mixture is simply put into a mold and dried, and compressed tablets in which the mixture is compression-molded. Compressed tablets also include those that directly compress raw materials (direct method) and those that once produce granules and compress them without directly compressing the raw materials (indirect method).

[0003] Conventionally, various types of bases for tablets have been used, and solid agar and agar powder are one of them. Agar is used not only as a base for tablets, but also as an excipient to gain weight and size when the main drug is small, a binder to strengthen the binding of powder, to accelerate disintegration in water and gastric juice. It is also used as an auxiliary such as a disintegrant.

[0004] Tablets are required to have a certain tablet strength and excellent disintegration properties. Particularly, in the case of compressed tablets, generally, compared to wet tablets, tablet strength is high, but disintegration is poor. Therefore, in order to obtain excellent disintegration properties, crystalline cellulose, synthetic silicate, etc. should be added. Is performed.

[0005]

The base for tablets is as follows:
It is desirable to have a property that, when molded, sufficient tablet strength is obtained and also excellent disintegration is obtained. This is because a tablet having such properties can be made into a tablet without combining many other auxiliary agents such as a binder and a disintegrant. From this viewpoint, conventional agar can be used as a base for disintegration, but has not been able to say that it has a sufficient function in disintegration, particularly in disintegration rate.

[0006] An object of the present invention is to provide a method for producing agar as a base or adjuvant for tablets, which makes it possible to obtain tablets exhibiting excellent disintegration properties. Another object of the present invention is to provide a method for producing a tablet showing excellent disintegration properties using agar as a base or adjuvant for tablets.

[0007]

The present invention firstly relates to a method for producing agar as a base or adjuvant for tablets for mixing tablets with a medicine to form tablets of a fixed shape, comprising the steps of: And a step of again dehydrating and drying the agar that has been swollen by water in this step. Secondly, the present invention relates to a method for producing agar as a tablet base or an adjuvant for mixing tablets with a medicine to form a tablet having a predetermined shape, which is obtained through extraction and filtration steps from seaweed, or A step of cooling an agar sol obtained by adding and heating and dissolving solid or powder agar to form an agar gel; and a step of lyophilizing and then crushing the agar gel obtained in this step. It is characterized by. Thirdly, the present invention relates to a method for producing agar as a tablet base or an auxiliary agent for mixing tablets with a drug to form a tablet having a predetermined shape, which is obtained through extraction and filtration steps from seaweed, or A process of cooling an agar sol obtained by adding and heating and dissolving solid or powdered agar to form an agar gel, a process of micronizing the agar gel obtained in this process, and a process of micronizing in this process. Freeze-drying the obtained agar gel and then pulverizing it.

The present invention also relates to a method for producing a tablet, comprising mixing the tablet agar obtained by any of the above first to third methods with a drug as a tablet base or an adjuvant to form a tablet. It is characterized by molding. The invention further provides
A method for producing tablets using solid or powdered agar as a base or adjuvant for tablets, wherein at least one of excipients, binders, disintegrants, and lubricants is added in addition to solid or powdered agar. A step of adding water to the primary raw material to cause water absorption and swelling, a step of again dehydrating and drying the primary raw material having absorbed water and swelling in this step to obtain a solid or powdery secondary raw material, and converting the secondary raw material obtained in this step to And forming a tablet by mixing.

[0009] The reason why the disintegration of tablets using the agar treated according to the present invention is improved is as follows. Ordinary powder agar is obtained by drying agar dehydrated by squeezing or freezing, and then physically pulverizing it with a pulverizer to form a powder.Even if powdered, each particle is still a hard layer of agar It seems to be. On the other hand, in the first method of the present invention, the agar particles are softened by absorbing water and swelling, and then dehydrated and dried and pulverized in this state to obtain fine agar particles for tablets. Voids are created. In this case, hot air drying, freeze drying (freeze drying), vacuum drying, or the like is used as a dehydration drying method. In the case of hot-air drying, the surface of the agar particles is partially melted by heat to form a film, and this film formation slightly reduces the bonding property by tableting. However, according to the first method, fine pores of the agar particles are formed. Increases the water absorption, and thus the tablets using the obtained agar have a high disintegration rate.

When the gelled agar without swelling due to water absorption in the second method is freeze-dried and pulverized, agar particles having a porous structure with many voids are obtained. Further, when the agar gelled by the third method is micronized and freeze-dried, a more homogeneous and porous agar particle structure can be obtained. The powdered agar for tablets obtained by these methods not only exhibits excellent disintegration as a result of the porous nature of each particle when the tablet is molded, but also has high tablet strength.
According to the present invention, the primary raw material to which at least one of excipients, binders, disintegrants, and lubricants is added in addition to solid or powdered agar is added to cause water absorption and swelling. Alternatively, a powdery secondary raw material is obtained, and the secondary raw material is mixed with a drug to form a tablet, whereby a tablet exhibiting excellent disintegration properties can be obtained. In particular, when the tablet agar obtained by the present invention is used as a tablet base, an advantage of exhibiting excellent disintegratability can be obtained without adding a disintegrant.

[0011]

Embodiments of the present invention will be described below. After 100 parts of water was kneaded with 100 parts of powder agar as a primary raw material to absorb and swell the agar, it was dried with hot air.
The dried agar was pulverized into powder agar as a secondary raw material (sample 1). 100 parts of water was kneaded with 100 parts of powder agar as a primary raw material to absorb and swell the agar, and then freeze-dried. The dried agar was pulverized into powder agar as a secondary raw material (sample 2). An agar sol obtained by heating and dissolving 5 parts of powder agar as a primary material in 100 parts of water was cooled and solidified to form an agar gel, which was freeze-dried and pulverized to obtain powder agar as a secondary material (sample 3). An agar gel is prepared by cooling and coagulating an agar sol obtained by heating and dissolving 5 parts of powder agar as a primary material in 100 parts of water. Then, it was ground to obtain powder agar as a secondary material (sample 4).

The powdered agar as a secondary material obtained by the above-described method is used as a base and compression-molded without adding chemicals and other auxiliaries to form a stone-like pseudo tablet (φ12-16R).
made. As a comparative example, a pseudo tablet was compression-molded under the same conditions using the primary raw material as a base, and a characteristic comparison test of both was performed. The comparative test data is summarized in the table below. Disintegration time is the time to disintegration when the simulated tablet is soaked in water.

[0013]

[Table 1]

As is apparent from Table 1, the agar powders of Samples 1 to 4, which are secondary raw materials obtained by applying a certain treatment to the primary raw materials, are compared with the disintegration time of the pseudo-tablet using the primary raw material powder agar. The disintegration time of the pseudo-tablet used is greatly reduced. Further, those using samples 3 and 4 have not only a shorter disintegration time but also a higher hardness than those using the primary raw materials.

In addition to solid or powdered agar, excipients,
A primary raw material is prepared by adding at least one of a binder, a disintegrant, and a lubricant. The primary raw material is added, hydrated and swelled with water, and dehydrated and dried to obtain a solid or powdery secondary raw material. It was also confirmed that the molding of the compound obtained tablet properties excellent in disintegration.

[0016]

As described above, according to the present invention,
(1) Solid or powdered agar is hydrated by water absorption,
This is dehydrated and dried. (2) Agar sol obtained by adding and heating and dissolving agar is cooled to form an agar gel, which is freeze-dried and then crushed. (3) Addition of agar and heating and melting The agar sol obtained is cooled to form an agar gel,
A tablet agar exhibiting excellent disintegration properties can be obtained by a method of forming fine particles, freeze-drying and pulverizing them.

Claims (5)

[Claims] 1. A method for producing agar as a tablet base or adjuvant for mixing tablets with a drug to form a tablet having a uniform shape, comprising the steps of adding solid or powdered agar to water and swelling it. And a step of dehydrating and drying the agar that has been swollen by water in this step again. 2. A method for producing agar as a base or adjuvant for tablets for mixing tablets with a medicine to produce tablets of a fixed shape, which is obtained from seaweed through extraction and filtration steps, or solid or powdery. Cooling the agar sol obtained by adding and heating and dissolving the agar to form an agar gel; and freeze-drying and then pulverizing the agar gel obtained in this step. To produce agar for tablets. 3. A method for producing agar as a tablet base or adjuvant for mixing tablets with a drug to form tablets of a fixed shape, which is obtained from seaweed through extraction and filtration steps, or solid or powdery. Agar gel formed by cooling the agar sol obtained by adding and heating and dissolving the agar of the agar gel obtained in the above step, and micronizing the agar gel obtained in this step; agar gel micronized in this step Freeze-drying and then pulverizing the agar for tablet. 4. A tablet production method comprising mixing the tablet agar obtained by the method according to any one of claims 1 to 3 with a medicine as a tablet base or an adjuvant to form a tablet. Method. 5. A method for producing a tablet using solid or powdered agar as a base or adjuvant for tablets, comprising, in addition to solid or powdered agar, excipients, binders, disintegrants,
A step of adding water to at least one of the lubricating agents to add water and swelling the primary material, a step of again dehydrating and drying the primary material swollen by water absorption to obtain a solid or powdery secondary material, Mixing the secondary raw material obtained in (1) with a drug to form a tablet.