JPH11302200A - L-glutamine and magnesium methasilicate aluminate-containing preparation having improved disintegration - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a L-glutamine and magnesium mehasilicate aluminate- containing preparation having fine disintegration. SOLUTION: The L-glutamine and magnesium methasilicate aluminate- containing preparation contains (a) carmellose calcium or croscarmellose sodium as a disintegrant and (B) a binder contained in an amount of 3 wt.% or less based on the preparation. In this case, carmellose calcium or croscarmellose sodium is contained in a preparation of 3-10 wt.% based on the preparation.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to the improvement of the disintegration of a preparation containing L-glutamine and magnesium aluminate metasilicate.

[0002]

2. Description of the Related Art L-glutamine is used as a gastric mucosa repair agent.
On the other hand, magnesium aluminate metasilicate is widely used as an antacid and as active ingredients for gastrointestinal drugs.

[0003]

However, it has been clarified that the simultaneous disintegration of L-glutamine and magnesium aluminate metasilicate causes a disintegration delay, and in order to obtain a gastrointestinal drug having a rapid effect, the disintegration is improved. It is suggested that a device to do this is necessary. As a method for improving disintegration, a method of adding a disintegrant or a surfactant is known, but rapid disintegration cannot be obtained only by adding these, and development of a new method is required.

[0004]

Means for Solving the Problems The present inventors have made intensive studies on a method for improving the disintegration of a preparation containing L-glutamine and magnesium aluminate metasilicate, and as a result, have found that the amount of the binder and the disintegrant can be reduced. By devising it, they found that more rapid disintegration was obtained, and completed the present invention.

That is, the present invention provides a disintegrating agent characterized in that (a) the disintegrant is carmellose calcium or croscarmellose sodium, and (b) the amount of the binder is 3% by weight or less based on the preparation. It relates to a formulation containing improved L-glutamine and magnesium metasilicate aluminate. Hereinafter, the present invention will be described in detail. In the present invention, the amount of carmellose calcium and croscarmellose sodium used as disintegrants is not particularly limited, but is preferably 3 to 10% by weight based on the preparation. Further, as the binder used in the present invention, conventionally known binders can be used and are not particularly limited. For example, water-soluble polymers such as methyl cellulose and hydroxypropyl cellulose are exemplified. The amount of the binder used is not particularly limited as long as it is 3% by weight or less, but is preferably 2 to 3% by weight. Water (0-50% by weight) as a solvent for the binding solution:
It is preferable to use a solution of ethanol (50 to 100% by weight).

[0006] The preparation of the present invention is prepared by adding excipients such as corn starch, lactose and crystalline cellulose, lubricating agents such as magnesium stearate, and, if necessary, coloring agents and flavoring agents. Preparations, by further adding pharmaceutically active ingredients and the like generally blended in gastrointestinal drugs and the like, and performing ordinary operations according to the dosage form to obtain powders, fine granules,
Solid preparations containing L-glutamine and magnesium aluminate metasilicate such as granules, tablets (including sugar-coated tablets and film-coated tablets), capsules and the like can be provided.

[0007]

The preparation containing L-glutamine and magnesium aluminate metasilicate obtained by the method of the present invention has a good disintegration property, and a preparation which does not usually disintegrate easily can be easily disintegrated. Enables rapid release of the active ingredient.

[0008]

Next, the present invention will be described in detail with reference to examples and comparative examples, but the present invention is not limited to these examples. Example 1 (mixed powder) L-glutamine 400 g magnesium aluminate metasilicate 1134 g lactose 666 g carmellose calcium 70 g (binding solution) methylcellulose 70 g ethanol 980 g purified water 420 g total 3740 g The binding solution was mixed well in the above mixed components. Was added and kneaded, then granulated and dried to produce granules.

Example 2 (mixed powder) L-glutamine 400 g magnesium aluminate metasilicate 1134 g lactose 666 g croscarmellose sodium 70 g (binding solution) methylcellulose 70 g ethanol 980 g purified water 420 g total 3740 g While the above mixed powder components are well mixed. After adding a binding solution to the mixture and kneading the mixture, the mixture was granulated and dried to produce granules.

Comparative Example 1 A target preparation was prepared in the same manner as in Example 1 except that the following components were used as disintegrants. A: Low-substituted hydroxypropylcellulose B: Carboxymethyl starch sodium C: Corn starch D: Polysorbate 80 E: Not added Comparative Example 2 117 g of methylcellulose added in Example 1
(5% by weight based on the formulation), and the desired formulation was prepared in the same manner.

Test Example 1 The disintegration time of the preparations obtained in Example 1 and Comparative Examples 1 and 2 was measured in accordance with the Japanese Pharmacopoeia disintegration test method. Table 1 shows the results.
(Results) In Comparative Example 1, the disintegration was much slower than in Examples 1 and 2, and the most suitable disintegrant was carmellose calcium used in Example 1 or croscarmellose sodium used in Example 2. It became clear that there was. Also, in Comparative Example 2, the disintegration was considerably slower than in Examples 1 and 2, and it became clear that the addition amount of the binder was essential to be 3% or less.

[0012]

[Table 1]

Claims (2)

[Claims] The improved disintegration is characterized in that (a) the disintegrant is carmellose calcium or croscarmellose sodium, and (b) the amount of the binder is 3% by weight or less based on the preparation. A preparation containing L-glutamine and magnesium aluminate metasilicate. 2. The preparation according to claim 1, wherein carmellose calcium or croscarmellose sodium is 3 to 10% by weight based on the preparation.