Beta-lactam antibiotic-containing tablet and production thereof

Abstract

This invention provides beta-lactam antibiotic-containing tablets capable of being orally taken either as such owing to their being small-sized, hence still easily swallowable, or, in the case of administration to the aged encountering some difficulty in swallowing, in the form of dispersions resulting from easy self-disintegration upon being dropped into water in a glass as well as a method of producing the same. The tablets of this invention comprise, on the per-tablet basis, 60-85% by weight of a beta-lactam antibiotic, 1-10% by weight of low-substituted hydroxypropylcellulose and / or crosslinked polyvinylpyrrolidone as a disintegrator, and 0.5-2% by weight of a binder. Granules to be compressed for tableting are prepared using water or an aqueous solution of ethanol or the like.

Description

[0001] This invention relates to .beta.-lactam antibiotic-containing tablets and a method of producing the same. More particularly, it relates to tablets of the above variety which can be orally taken either as such or, for taking by, for example, the aged who have difficulties in swallowing, as a dispersion available upon dropping the same into water in a glass for self-disintegration, and to a method of producing the same.BACKGROUND TECHNOLOGY[0002] Particularly in Europe and America, where .beta.-lactam antibiotics such as cefixime and cefdinir are administered generally in single doses of as great as 200 mg to 400 mg potency, unit dosage forms, whether they are capsules or tablets, have to be considerably large in size. When 400 mg potency capsules are prepared, for instance, the capsule size reaches approximately No. 0, so that not only patients having difficulties in swallowing but also ordinary adult patients become reluctant to take them or get a repulsive sensation in takin...

AI Technical Summary

Problems solved by technology

Such capsules are indeed difficult to take.

The problems encountered in taking such large dosage forms give an unnecessary sensation of oppression to patients on the occasion of taking them.

However, when such tablets are orally taken, they give off bubbles in the oral cavity, so that patients feel a discomfort or an unnecessary sensation of anxiety.

For securing a good shelf-life in a humid environment, it is necessary to use a moisture-proof packaging material, which increases the production cost.

However, said first disintegrator, which is used in a large amount, increases the tablet size.

This is because the use of a binder renders tablets extremely poor in self-disintegrating properties.

It is a problem that these steps are very inefficient.

Said tablets each contains 500 mg potency (about 570 mg) of amoxicillin and weighs about 970 mg, hence is very large and not entirely suited for oral administration.

However, when a commercial synthetic sweetener is incorporated, a problem arises, namely the self-disintegrating properties of tablets become poor, since synthetic sweeteners are soluble in water and become viscous and sticky.

The addition of a binder has an adverse effect on the self-disintegrating properties of tablets, hence is not desirable from the self-disintegration viewpoint.

However, the production of tablets without adding any binder give such inconveniences as mentioned hereinbefore.

However, incorporation of a large amount of such excipient according to said method results in an increase in tablet size, thereby making the tablets difficult to take with ease.

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