United States Patent:  6,060,078

Assignee:  Sae Han Pharm Co., Ltd. (Kyunggi-do, KR)

Filed:  September 28, 1998

The present invention relates to a chewable tablet containing a medicament in a core and a process for preparation thereof. In particular, the present invention relates to a chewable tablet comprising a core containing a medicament in the center of the tablet in a state of jelly or chewable base and an outer layer wrapping the core which is made up of chewable base such as a gum, a soft candy or a caramel. The chewable tablet is easy to take and has a good taste and nice chewing property due to the unique tablet form. In addition, the tablet has an advantage in bioavailability resulting from increased absorption rate and excellent stability due to unique preparation process. Therefore, the chewable tablet and the preparation process of the present invention can be used in pharmaceutical industry usefully.

DETAILED DESCRIPTION OF THE INVENTION

In the present invention, a chewable tablet containing a medicament in a core in a state of jelly or chewable base and a process for preparation thereof are provided.

In detail, the tablet of the present invention comprises a core containing a medicament in a state of jelly or chewable base; and an outer layer of chewable base wrapping the core.

Any kind of medicament may be contained in the core, preferably a medicament of bitter taste, a medicament which is unstable to heat, vitamins which are liable to transform, natural plant extracts or other organic compounds may be contained in the core.

More preferably, vitamins such as vitamin A, vitamin B, vitamin B₁, vitamin B₂, vitamin B₆, vitamin C, vitamin E and vitamin K; natural plant extracts such as Sohgunjung-tang extracts, Sipchundaebo-tang extracts and Eleutherococcus senticosus extracts; organic compounds such as dimenhydrinate, meclazine.HCl, acetaminophen, asprin, phenylpropanolamine.HCl and cetylpyridinium chloride; or gastrointestinal agents such as aluminum hydroxide gel dried, domperidone, soluble azulene, L-glutamine and hydrotalcite may be contained in the core.

These medicaments may be used alone or in combination.

The medicament contained in the tablet may be used in usual dose.

For example, Eleutherococcus senticosus extracts is used in the chewable tablet in a dose of 195-390 mg/day; dimenhydrinate in a dose of 20-200 mg/day; meclazine.HCl in a dose of 25-75 mg/day; aspirin in a dose of 1-4.5 mg/day; phenylpropanolamine-HCl in a dose of 75-100 mg/day; cetylpyridinium chloride in a dose of 6-8 mg/day; and domperidone in a dose of 30-60 mg/day.

The jelly base of the core, which contains the above medicament in a state of jelly, may be selected from the group consisting of pectin, sorbitol, maltitol, isomalt, liquid glucose, sugar, citric acid and a flavoring agent.

The chewable base of the core or the outer layer may be selected from the group of gum, soft gum, soft nougat, soft candy, hard candy and caramel, which are easy to take and tasty. In addition, the chewable base may additionally contain excipients selected from the group consisting of sugars; a protecting agent of adhesion to oral cavity and crystallization of sugars; an enhancing agent of chewing property; a keeping agent of hardness and extension property; a flavoring agent; a souring agent; a coloring agent; and combinations thereof, according to the kind of chewable base.

The sugar used in the present invention may be selected from the group consisting of white sugar, liquid glucose, sorbitol, dextrose, isomalt, liquid maltitol, aspartame and lactose, and this sugar may comprise 50-90 weight % by total weight of the ingredients.

Glycerin, lecithin, hydrogenated palm oil or glyceryl monostearate may be used as a protecting agent of crystallization of the sugars in 0.04-2.0 weight % by total weight of the ingredients, to prevent adhesion to oral cavity and improve the soft property of the products.

Isomalt or liquid maltitol may be used as an enhancing agent of chewing property, which can increase the chewing properties by controlling the composition ratio and it must be prepared at temperatures of 135-140^oC. under vapor pressure of 5.5 bar.

A gum such as gelatin or arabic gum may be used as a keeping agent of hardness and extension property in 0.1-2.0 weight % by total weight of the ingredients.

In addition, a flavoring agent such as a food flavor or a fruits extract; a souring agent such as citric acid may be added in adequate amount, and a coloring agent such as a food color may be optionally added in small amount.

The chewable tablet of the present invention is prepared by the process in which the medicament, an effective ingredient, is contained in the core in a state of jelly or chewable base separate from the outer layer, whereas the conventional chewable tablet was prepared by mixing a medicament and additives and then, melting them at high temperatures, therefore, forming soft candy or jelly, in which the medicament was dispersed on the whole tablet.

In detail, the chewable tablet of the present invention is prepared by the following process comprising the steps of:

(a) preparing an outer layer of chewable base and a core of jelly or chewable base, respectively;

(b) mixing a medicament with the jelly or chewable base of the core at room temperature (25^oC.);

(c) making candy rope containing fixed amount of medicament  through the process in which each of the prepared outer layer of chewable base and the core of jelly or chewable base containing medicament is put into two extruding machine, which is designed specially by the present inventors (Korean Patent application No. 98-30511), respectively, and then each of the outer layer and the core is extruded at the same time by using the above extruding machine, maintaining temperatures of 50-90^oC. on the outer layer and 5-8^oC. on the core; and

(d) forming a chewable tablet by cutting the above candy rope.

The chewable tablet prepared by the above process has an advantage in bioavailability resulting from increased absorption rate, because the tablet is dissolved or chewed in the mouth and then moved into gastrointestinal tract in a state of whole solution or granule, whereas the conventional solid tablet or capsule was absorbed through disintegration and dissolution.

Further, the conventional chewable tablet was prepared by mixing a medicament, an effective ingredient, and additives, then melting them at high temperatures as a whole, thus the medicament was liable to change in physico-chemical properties. On the contrary, the medicament contained in the chewable tablet of the present invention as an effective ingredient is not changed in physico-chemical properties and keeps the effect of medicament, therefore has a excellent stability, because the chewable tablet of the present invention is prepared by the process in which the medicament is mixed with a jelly or a chewable base at room temperature.

To confirm the stability of the chewable tablet of the present invention, an acceleration test was performed on the product prepared by the present process under certain condition ((1) room temperature, (2) 40^oC., relative humidity (RH) 75%) for certain period (for 6 months, tested every 0, 2, 4, 6 months) and the changes of physico-chemical properties were observed. As a result, the chewable tablet of the present invention did not change in properties, state and content of the effective medicament and it was suitable for both of microorganism limit test and heavy metal test. The chewable tablet, therefore, has been proved to have excellent stability.

In addition, the chewable tablet of the present invention provides taste mask effect to a bitter tasty medicament, which is contained in the medicament, and better chewing property and taste than the conventional tablets by means of an outer tasty chewable base.

Claim 1 of 11 Claims

1. A chewable tablet comprising a core containing a medicament in a state of jelly or chewable base; and an outer layer of chewable base wrapping the core, wherein the said chewable base contains an enhancing agent of chewing property selected from the group consisting of isomalt and liquid maltitol and a keeping agent of hardness and extension property being a gum including gelatin or arabic gum.

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