Title:  Multiple unit effervescent dosage forms comprising proton pump inhibitor

United States Patent:  6,132,770

Assignee:  AstraZeneca AB (Sodertalje, SE)

Filed:  February 13, 1997

PCT NO:  PCT/SE96/01738

102(e) Date:  February 13, 1997

PCT PUB. Date:  July 17, 1997

Foreign Application Priority Data:  Jan 08, 1996[SE] (9600073)

A new tableted multiple unit effervescent dosage form containing an acid susceptible proton pump inhibitor in the form of the racemate, an alkaline salt thereof or one of its single enantiomers or an alkaline salt thereof, and effervescent tablet constituents. The proton pump inhibitor is preferably omeprazole or an alkaline salt thereof, or S-omeprazole or an alkaline salt thereof. Further the invention refers to a method for the manufacture of such a formulation, and the use of such a formulation in medicine.

SUMMARY OF THE INVENTION

The Applicant has now surprisingly found that effervescent tablets according to the present invention comprising enteric coated units of an acidic susceptible proton pump inhibitor can be manufactured by compressing said units into tablets without significantly affecting the properties of the enteric coating. As explained above, if the enteric coating is damaged during compression of the enteric coated units the acid resistance of said enteric coating in the manufactured tablets will not be sufficient and the manufactured tablets will not fulfil standard requirements on enteric coated articles, such as those defined in the United States Pharmacopeia USP. Furthermore, the active substance may be destroyed by the acidic solution/dispersion obtained by the effervescence, if such requirements not are fulfilled.

One object of the present invention is to provide a tableted multiple unit effervescent dosage form comprising an acid susceptible proton pump inhibitor, or an alkaline salt thereof or one of its single enantiomers or an alkaline salt thereof, in which the active substance is in the form of enteric coating layered units compressed together with effervescent tablet excipients into such an effervescent tablet. The enteric coating layer(s) covering the individual units of active substance has properties such that the compression of the units into a tablet does not significantly affect the acid resistance of the enteric coated units. The active substance is prevented from degradation and dissolution in acidic media and the dosage form has a good stability during long-term storage. The enteric coating covering the individual units disintegrates/dissolves rapidly in near neutral or alkaline media.

The tableted multiple unit effervescent dosage form is especially suitable for patients with swallowing disorders and in pediatrics.

Claim 1 of 27 Claims

What is claimed is:

1. An oral pharmaceutical composition in the form of a multiple unit effervescent tablet comprising, as a first component, a core material comprising an acid susceptible proton pump inhibitor, and as a separate second component, at least one effervescent tablet constituent, wherein the core material is in the form of pellets covered with an enteric coating layer having mechanical properties such that the acid resistance of the enteric coated pellets is not significantly affected by compression of the pellets with the other tablet components during tableting.

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