Tablet comprising cetirizine and pseudoephedrine
AssigneeUCB Farchim S.A.
InventorsDomenico Fanara, Anthony Guichaux, Monique Berwaer, Michel Deleers
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Abstract
The present invention concerns a tablet comprising two distinct segments. More particularly the invention relates to combinations of two pharmaceutical substances and methods of treatment of allergic disorders.
Claims49
A tablet comprising at least two distinct segments, one segment of which comprises as active ingredient predominantly cetirizine and a second segment of which comprises as active ingredient predominantly pseudoephedrine, said segments being composed and formed In such a way that the resulting tablet is substantially free of impurities formed by reaction of cetirizine with pseudoephedrine, and with the proviso that the tablet comprises less than 5% by weight, relative to the total weight of the tablet, of an alkalinizing agent.
A tablet comprising at least two distinct segments one segment of which comprises as active ingredient predominantly cetirizine and a second segment of which comprises as active ingredient predominantly pseudoephedrine, said segments being composed and formed in such a way that the pharmacokinetic profiles of the cetirizine and pseudoephedrine are substantially the same as in a dosage form containing each as sole active ingredient in the same amount.
A tablet according to any one of the preceding claims wherein the interfacial surface area of the pseudoephedrine segment and cetirizine segment is less than 180 mm2.
A tablet according to any one of the preceding claims wherein the tablet further comprises a barrier segment wherein said barrier segment separates the cetirizine segment and the pseudoephedrine segment.
A tablet according to any one of the preceding claims wherein the pseudoephedrine segment comprises less than 5% by weight, relative to the total weight of the pseudoephedrine segment, of an allying agent.
A tablet according to any one of the preceding claims wherein the tablet comprises a plurality of pseudoephedrine segments.
A tablet according to any one of the preceding claims wherein said cetirizine segment is in the form of a compression coating.
A tablet according to any one of the preceding claims wherein said cetirizine segment is in the form of a spray coating.
A tablet according to any one of the preceding claims wherein the pseudoephedrine segment contains inert pharmaceutical excipients in an amount of 0.75 to 4.5 times that of the pseudoephedrine itself by weight.
A tablet according to any one of the preceding claims wherein the cetirizine segment contains inert pharmaceutical excipients in an amount of 5 to 30 times that of the cetirizine itself by weight.
A tablet according to any one of the preceding claims wherein the ratio of the total amount of inert pharmaceutical excipients present to the total aggregate amount of all active ingredients is between 2 and 6 by weight.
A tablet according to any one of the preceding claims wherein the weight ratio of pseudoephedrine to cetirizine is between 12 and 30.
A tablet according to any one of the preceding claims wherein the pseudoephedrine segment comprises between about 108 and 132 mg of pseudoephedrine and the cetirizine segment comprises between about 4.5 and 5.5 mg of cetirizine.
A tablet according to any one of the preceding claims wherein the pseudoephedrine segment is in a slow release form.
A tablet according to any one of the preceding claims wherein the cetirizine is in an immediate release form.
A tablet according to any one of the preceding claims wherein the tablet weight is between 200 to 800 mg.
A tablet according to any one of the preceding claims wherein the tablet comprises an amount of cetirizine which when dosed to a human subject gives a cetirizine area under the plasma cetirizine concentration versus time curve which is between 80% and 125% of the area under the plasma cetirizine concentration versus time curve observed when a dihydrochloride cetirizine immediate release tablet comprising said amount of cetirizine is dosed to same human subject at the same cetirizine dose.
A tablet according to any one of the preceding claims wherein the tablet comprises an amount of pseudoephedrine which when dosed to a human subject gives a pseudoephedrine area under the pseudoephedrine plasma concentration versus time curve which is between 80% and 125% of the area under the plasma pseudoephedrine concentration versus time curve observed when a pseudoephedrine sustained release tablet comprising said amount of pseudoephedrine is dosed to same human subject.
A tablet according to any one of the preceding claims wherein the particle size of the pseudoephedrine present is chosen such that it has a flow index less than 25.
A tablet according to any one of the preceding claims wherein the particle size of the pseudoephedrine present is chosen such that it has an ability to settle of less than 30 ml.
A tablet according to any one of the preceding claims wherein not more than 10% of the pseudoephedrine present therein has a particle size of less than 100 μm.
A tablet according to any one of the preceding claims wherein the pseudoephedrine containing segment also contains a methyl cellulose ether derivative having a viscosity of about 11,000 to 21,000 mPa.
A tablet according to any one of the preceding claims wherein the cetirizine containing segment also contains a disintegrant.
A tablet according to any one of the preceding claims wherein the cetirizine segment contains excipients including a polyhydroxyl compound having a molecular weight of less than 400.
A tablet according to any one of the preceding claims wherein the tablet is a bi-layer tablet, the cetirizine segment being a layer and the pseudoephedrine segment being a layer.
A tablet according to anyone of the preceding claims which comprises an additional coating layer.
A tablet according to anyone of the preceding claims wherein the tablet is packaged in a moisture protective packaging material.
A tablet according to anyone of the preceding claims wherein the tablet is packaged in an oxygen protective packaging material.
A tablet according to anyone of the preceding claims wherein the cetirizine segment comprises cetirizine dihydrochloride.
A tablet according to anyone of the preceding claims wherein the cetirizine segment comprises levocetirizine.
Use of a tablet according to anyone of the preceding claims, for the manufacture of a medicament for preventing or treating disorders or conditions associated with rhinitis, cold, flu, cold-like and flu-like symptoms, and allergic rhinitis, relief of nasal congestion, seasonal rhinitis, sneezing, rhinorrhea, nasal and ocular pruritus, redness of the eyes, tearing, sneezing.
Dependencies are inferred from the claim text.