WO1996003980A1

WO1996003980A1 - Improved effervescent delivery system

Info

Publication number: WO1996003980A1
Application number: PCT/US1995/009540
Authority: WO
Inventors: Stefanos A. Daskalakis
Original assignee: Bayer Corporation
Priority date: 1994-07-29
Filing date: 1995-07-28
Publication date: 1996-02-15
Also published as: AU3152495A

Abstract

An improved effervescent tablet is provided. The tablet contains acetylisylic acid, a critical ratio of bicarbonate to acid, flavors, sweeteners, tableting aids, and optionally other medicinals. The tablet has improved hardness and stability and can be readily compressed into a relatively small (by weight and diameter) effervescent tablet.

Description

IMPROVED EFFERVESCENT DELIVERY SYSTEM

FIELD OF THE INVENTION

The invention relates in general to effervescent compositions and in particular to effervescent compositions containing acelylsalicylic acid provided in tablet form.

BACKGROUND OF THE INVENTION

Effervescent tablets containing medicinal or nutritional supplements are marketed worldwide as over-the-counter products. These tablets are added to water and dissolved with a characteristic effervescence, prior to ingestion. Although these formulations have the advantage of delivering medication in solution, they have the additional problem of requiring a high degree of flavoring to mask the taste of the incorporated medications or supplements. In addition, because of the high reactivity of the effervescent components the tablet is prone to stability problems and can also be very difficult to compress into a suitably hard tablet for packaging and sale. This invention provides a formulation which solves the latter problem.

SUMMARY OF THE INVENTION

Disclosed herein is a composition containing between 0 lo 13 % (by weight) of acelylsalicylic acid and an effervescent component. In order to provide suitable tablet compressibility, it has been found that the ratio of bicarbonate component to acid, should be in the range between 1.5 and 1.0. The bicarbonate component is composed of 80 to 90% bicarbonate and 10 to 20% carbonate. The remainder of the tablet composition is composed of sweetener, flavors, and tableting aids. Additional medications may be added.

DESCRIPTION OF THE INVENTION

The invention disclosed herein provides an improved effervescent tablet containing acetylsalicylic acid and optionally other medicinals. The acetylsallcylic acid is present in a range between about 8 and 13 percent of the tablet and is generally sufficient to provide good lablet lubrication. The weight percentages given are based on a tablet weight range of from about 2000 to about 2400 mg for an effervescent tablet having a tablet diameter of about 19 millimeters (mm) to 22.5 mm. The weight range is preferably from about 2950 to about 3200 mg.

The effervescent component of the formulation is composed of an alkali metal bicarbonate component and an organic acid useful for consumption in medicinals. The alkali metal or alkaline earth metal bicarbonate component (referred to herein as the "bicarbonate component") is actually a combination of 80 to 90% by weight of bicarbonate and 10 - 20% by weight carbonate salt. It has been found that the ratio of bicarbonate component to organic acid is critical to provide suitable tablet hardness The ratio of bicaibonate component to acid is critical to provide improved tablet compressibility wiiile maintaining a low tablet weight and is between about 1.5 to about 1.8.

Sodium bicarbonate and sodium carbonate are the preferred ingredients of the bicarbonate component. But other alkali metal or alkaline earth metal salts, may be used as is well known in the art. Although any of a number of organic acids, including citric, malic, lartaric and succinic acids may be used, citric acid is preferred.

The preferred particle size of the acetylsalicylic acid is such that not more than 5% passes through a 40 mesh screen and not more than 20% passes through a 100 mesh screen, ie a normal distribution of particles between about 100 and 450 microns.

Flavors are an important component of effervescent formulations. It has been found that high intensity flavors, containing tocopherol as a stabilizing agent provide better and more prolonged flavor stability in the composition of the invention. Such flavors are available from Firmenich Incorporated, Princeton, NJ. Preferably such flavors are incorporated at levels between 0.156 to about 0.5% of the tablet weight.

Sweeteners are generally used in effervescent formulations. The preferred range for a sweetener in this composition is from about 0.4 lo 1.0 percent of the tablet weight. Any sweetener which imparts the necessary flavor may be used. Among the suggested sweeteners are sugar, aspartame and saccharin. Aspartame is a preferred sweetener.

It has been found that the composition described above allows the delivery of suitable amounts of acetylsalicylic acid, and optionally other medical components sometimes used in combination with acetylsalicylic acid.

The composition of the invention is further illustrated by the following example. Example: FLAVORED EFFERVESCENT TABLET bicarbonate component 1700. mg critic acid 1000. mg aspirin 330. mg aspartame 20 mg flavor (lemon lime) 8 mg tableting aids 1.5 mg

The bicarbonate component is composed of sodium bicarbonate and carbonate as described previously and prepared in a Huhn dryer. The acetylsalicylic acid is preferably in a particle size range from about 100 to about 450 microns. All components are weighed and mixed for about 10 to 20 minutes. The mixture is pan blended through a sifter using a suitable screen. The preferred particle size of acetylsalicylic acid is achieved by a distribution of particles not greater than 5% above 400 microns and not greater than 20% below 100 microns. After sifting the mixlure is returned to the mixer from from about 5 to 10 minutes. Finally the mixture is compress by standard methods in a tablet press.

It should be understood that many modifications and variations may be made in the proportions and components used herein without departing from the spirit and scope of the invention, which is solely defined by the claims.

Claims

WHAT IS CLAIMED IS:

1. An effervescent tablet composition, comprising: a. an effervescent couple, composed of an alkali metal bicarbonate and an organic acid chosen from the group consisling of citric, malic, succinc and lartaric acid wherein the ratio of bicarbonate component lo acid is in the range between about 1.5 to about 1.8; b. from aboul 8 to about 13% by weighl of acelylisalicyiic acid; c. from about 0.156 to about 0.5% by weight of a flavor component; d. from about 0.4% to about 1 % by weight of a sweetener; and e. tableting aids.

2. The composition of claim 1 , wherein the total tablet weight is in the range between 2,000 to 3,400 milligrams .

3. The composition of claim 2, wherein the tablet diameter is between about 19 and about 22.5 mm.

4. The composition of claim 1 wherein the bicarbonate component is composed of between about 80 to 90% by weight of bicarbonate and 10 to 20 % by weighl of carbonate.

5. The composition of claim 4 wherein the bicarbonate and carbonate both sodium salts.

6. The composition of claim 2 in which the particle size of acetylsalicylic acid is between aboul 100 and about 450 microns.

7. The composition of claim 1 in which the sweetener is selected from the group consisting of sugar, asparlame and saccharin.

8. The composilion of claim 1 in which the flavors are high intensity flavors containing tocopherol as a stabilizer.