CA2028733A1 - Antacid tablets - Google Patents

Abstract

- 6 - O.Z. 0650/01017 Abstract of the Disclosure: A biconvex tablet whose height and diameter are approximately equal and are from 1.5 to 4 mm and which, besides conventional pharmaceuti-cal auxiliaries, contains an antacid as active substance is described.

Description

3 ~
o.z. 0~5(~/01017 The present invention relate~ to small antacid tablets, 50 to 1000 of which are swallowed with liquid per dose. This avoids the unpleasantness associated with S taking conventional antacid forms.
Drugs which have to be tak~n in high doses and are unpleasant to take in that they cause deposits on and between the teeth and in the mouth meet with resistance from patients (low patient compliance).
Antacids are examples of this, it often being necessary to take from 1 to 3 g, and are commercially available in the form of chewable tablets or gels.
Chewable tablets cause long-lastins depo3its on the teeth when chewed, and these persist in an unpleasan~ manner for a long period because of the sandy texture of the insoluble active substance. Gels involve tiresome pre~
paration by tearing open and Xneading a sachet to expel the gel, possibly with stirring in water and/or applica-tion to the mouth. Once again, the insoluble substances are deposited between the teeth and in the mouth.
It is an object of the present invention to develop a form for antacids which avoids the unpleasant-ness of taking them.
We have found that this ob~ect is achieved by biconvex tablets whose height and diameter are approxi-mately the same and are from 1.5 to 4 mm and which, besides con~entional pharmaceutical auxiliaries, contain an antacid as active substance. These small ~ablets are easy to swallow and do not remain adherent in the mouth.
Antacid~ are substances which counter hyper-acidity of ga~tric juice (heartburn). Example~ of suit-able compounds are magnesium hydroxide, oxide, carbonate and silicate, aluminum hydroxide and phosphate, and magnesium aluminum silicates. ~he former use of sodium bicarbonate ha~ been abandoned. Antacids are generally employed in amounts of from 60 to 95 % by weight, prefer-ably 65 to 90 ~ by weight, ba~ed on the tablet (without - 2 - O.Z. 0650/0~017 coating).
The tablets are produced with conventional pharmaceutical auxiliaries in proportions of from 2 to 20 ~ with a diameter of from 1.5 to 4 mm in biconvex S form, with the height being approximately equal to the diameter (~ max. 25 %, preferably max. 10 ~). It is not necessary for all surfaces to be convex, on the contrary they can be manufactured with a narrow flat rim.
Examples of conventional pharmaceutical auxiliar-ies are binders such as lactose, starch, gelatin, micro-crystalline cellulose or polyvinylpyrrolidone (PVP)~
disintegrants such as crosslinked PVP, corn starch, starch glycolate or alginic acid, lubricants such as magnesium stearate or talc, and flow regulators such as highly disperse silica.
In order to avoid an unpleasant taste and to Lmprove the ease of swallowing, the tablets can be provided by conventional processes with coatings of water-soluble polymers or sugar. The polymers which are preferably employed are water-soluble cellulose deriva-tives such as methylcellulose or hydroxypropylmethyl-cellulose, and PVP.
From 50 to 500 such tablets of appropriate size and the desired do~age can be used a~ granules with conventional measuring appliances such as measuring spoons or dose dispensers, or else packed in single-dose sachets. No re~idue is left in the mouth after intake with a reasonable amount of liquid.
Inclusion of disintegrants in the tablet formula-tion can be used to ensure that each tablet rapidly disintegrates in the stomach 50 that, in con~unction with the large surface area and the distribution of the tablets in the volume of the stomach, rapid availability of the active substance is ensured.
The small tablets can be produced, for example, as described in US 4,797,287 and US 4,828,843.

- 3 - O.~. 06S0/01017 Composition Dose unit Batch 1. ~luminum hydroxide (dried g~l) 600 mg 1.20 kg 2. Magnesium hydroxide (powder) 210 mg 0.42 kg 3. Lactose 50 mg 0.10 kg 4. Polyvinylpyrrolidone35 mg O.n7 kg 5. Crosslinked polyvinylpyrrolidone 40 mg 0O08 kg 6. Highly disperse silica 5 mg 0.01 kg 7. Magnesium stearate 20 mg 0.04 kg Production of 2000 dose units Ingredients 1. to 3. were mixed in a high-performance laboratory mixer tStephan UMC 12) and granu-lated with an 8 % aqueous solution of 4. The granules were passed through a 1.0 mm screen and then dried in a circulating air oven at 60 to 70C. The dry granules were passed through a 0.63 mm screen and then initially mixed with 5. and 6. an~ finally mixed with added 7.
The composition ready for tableting was com-pressed in an eccentric press with 205 mm concave dies to20 give microtablets which were 2.5 mm high and weighed 12.0 mg each.
80 of these microtablets comprise a dose unit.
The disintegration time (Ph. Eur. method) of the micro-tablets is 9 min, and they can easily be swallowed with 5 a glass of water without unpleasan~ sensations.

Composition Dose unit Batch 1. Aluminum hydroxide (dried gel) 500 mg 1.00 kg 2. Calcium carbonate (heavy, powder) 100 my 0.20 kg 3. Magnesium hydroxide (powder) 200 mg 0.40 kg 4. Polyvinylpyrrolidone30 mg 0.06 kg 5. Lactose, directly tabletable 130 mg 0.26 kg 6. Microcrystalline cellulose 100 my 0.20 kg 7. Corn starch 100 mg 0.20 kg 8. Highly disperse silica10 mg 0.02 Xg 9. Magnesium stearate 30 mg 0.06 kg lO.Hydroxypropylmethylcellulose 20 mg 0.04 kg ~8~3 - 4 - O.Z. 0650/01017 Production of ~000 dose units Ingredients l. to 3. were mixed in a high-performance laboratory mixer (Stephan UMC 12) and granu-lated with an B ~ aqueous solution of 4. The granules were passed through a 1.2 mm screen and then dried in an oven at 60C. The dry granules were passed through a 0.8 mm screen and then initially mixed with 5. to 8. and finally mixed with added 9.
The composition ready for tableting was com-pressed in an eccentric press with 3 mm concave dies togive microtablets which were 3 mm high and weighed 20 mg each.
A 5 % aqueous solution of lO. was sprayed onto the microtablets in a fluidized bed ~Glatt WSG 5) with the inlet air at 50C.
60 of these microtablets comprise a dose unit.
The disintegration time (Ph. Eur. method) of the micro-tablets is 8 min. They can easily be swallowed with a glass of water without unplea ant sensations.

Claims (2)

1. A biconvex tablet whose height and diameter are approximately equal and are from 1.5 to 4 mm and which, besides conventional pharmaceutical auxiliaries, contains an antacid as active substance.

2. A tablet as claimed in claim 1 with a diameter of from 2 to 3 mm.