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Claims for Patent: 6,039,974

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Claims for Patent: 6,039,974

Title: Pharmaceutical composition for combination of piperidinoalkanol-decongestant
Abstract:The present invention provides a pharmaceutical composition in the form of a bilayer tablet comprising, (a) a first discrete zone made with Formulation (A) which comprises, a therapeutically effective decongestant amount of a sympathomimetic drug, or a pharmaceutically acceptable salt thereof, in an amount of about 18% to about 39% by weight of Formulation (A), and a first carrier base material, the first carrier base material comprising a mixture of; (I) carnauba wax in an amount of about 59% to about 81% by weight of Formulation (A); and (ii) a suitable antiadherent in an amount of about 0.25% to about 2.00% by weight of Formulation (A); wherein said first carrier base material provides a sustained release of the sympathomimetic drug; and (b) a second discrete zone made with Formulation (B) which comprises a therapeutically effective antihistaminic amount of a piperidinoalkanol, or a pharmaceutically acceptable salt thereof, in an amount of about 15% to about 30% by weight of Formulation (B) and a second carrier base material, the second carrier base comprising a mixture of; (I) a cellulose diluent in an amount of about 27% to about 73% by weight of Formulation (B); (ii) pregelatinized starch in an amount of about 15% to about 30% by weight of Formulation (B); (iii) a suitable disintegrant in an amount of about 0.25% to about 6.00% by weight of Formulation (B); and (iv) a suitable lubricant in an amount of about 0.25% to about 2.00% by weight of Formulation (B); wherein said second carrier base material provides an immediate release of the piperidinoalkanol or the pharmaceutically acceptable salt thereof.
Inventor(s): MacLaren; David D. (Overland Park, KS), Lefler; John R. (Overland Park, KS), Minish; Sharon K. (Independence, MO)
Assignee: Hoechst Marion Roussel, Inc. (Bridgewater, NJ)
Application Number:09/127,478
Patent Claims: 1. A pharmaceutical composition in the form of a bilayer tablet comprising,

(a) a first discrete zone made with Formulation (A) which comprises, a therapeutically effective decongestant amount of a sympathomimetic drug, or a pharmaceutically acceptable salt thereof, in an amount of about 18% to about 39% by weight of Formulation (A), and a first carrier base material, the first carrier base material comprising a mixture of;

(I) carnauba wax in an amount of about 59% to about 81% by weight of Formulation (A); and

(ii) a suitable antiadherent in an amount of about 0.25% to about 2.00% by weight of Formulation (A);

wherein said first carrier base material provides a sustained release of the sympathomimetic drug; and

(b) a second discrete zone made with Formulation (B) which comprises a therapeutically effective antihistaminic amount of a piperidinoalkanol, or a pharmaceutically acceptable salt thereof, in an amount of about 15% to about 30% by weight of Formulation (B) and a second carrier base material, the second carrier base comprising a mixture of;

(I) a cellulose diluent in an amount of about 27% to about 73% by weight of Formulation (B);

(ii) pregelatinized starch in an amount of about 15% to about 30% by weight of Formulation (B);

(iii) a suitable disintegrant in an amount of about 0.25% to about 6.00% by weight of Formulation (B); and

(iv) a suitable lubricant in an amount of about 0.25% to about 2.00% by weight of Formulation (B);

wherein said second carrier base material provides an immediate release of the piperidinoalkanol or the pharmaceutically acceptable salt thereof.

2. The pharmaceutical composition of claim 1 wherein the piperidinoalkanol is of the formula; ##STR8## wherein X is a number ranging from about zero to about 5, and the individual optical isomers thereof.

3. A pharmaceutical composition in the form of a bilayer tablet comprising,

(a) a first discrete zone made with Formulation (A) which comprises, a therapeutically effective decongestant amount of a sympathomimetic drug, or a pharmaceutically acceptable salt thereof in an amount of about 25% to about 33% by weight of Formulation (A), and a first carrier base material, the first carrier base material comprising a mixture of;

(I) carnauba wax in an amount of about 66% to about 74% by weight of Formulation (A); and

(ii) a suitable antiadherent in an amount of about 0.50% to about 1.50% by weight of Formulation (A);

wherein said first carrier base material provides a sustained release of the sympathomimetic drug; and

(b) a second discrete zone made with Formulation (B) which comprises a therapeutically effective antihistaminic amount of a piperidinoalkanol of the formula; ##STR9## wherein X is a number ranging from about zero to about 5, and the individual optical isomers thereof, in an amount of about 15% to about 24% by weight of Formulation (B) and a second carrier base material, the second carrier base comprising a mixture of;

(I) a cellulose diluent in an amount of about 43% to about 67% by weight of Formulation (B);

(ii) pregelatinized starch in an amount of about 15% to about 24% by weight of Formulation (B);

(iii) a suitable disintegrant in an amount of about 3.20% to about 4.80% by weight of Formulation (B); and

(iv) a suitable lubricant in an amount of about 0.50% to about 1.00% by weight of Formulation (B);

wherein said second carrier base material provides an immediate release of the piperidinoalkanol or the pharmaceutically acceptable salt thereof.

4. A pharmaceutical composition according to claim 1 wherein a suitable glidant is included in the first carrier base material of Formulation (A) in an amount of 0.00% to about 3.00% by weight of Formulation (A).

5. A pharmaceutical composition according to claim 1 wherein a suitable glidant is included in the first carrier base material of Formulation (A) in an amount of 0.00% to about 0.75% by weight of Formulation (A).

6. A pharmaceutical composition according to claim 5 wherein the suitable glidant is colloidal silicon dioxide.

7. A pharmaceutical composition according to either claim 3 or claim 6 wherein the sympathomimetic drug is pseudoephedrine hydrochloride.

8. A pharmaceutical composition according to claim 7 wherein the suitable antiadherent of Formulation (A) is stearic acid, and in Formulation (B), the suitable disintegrant is croscarmellose sodium and the suitable lubricant is magnesium stearate.

9. A pharmaceutical composition according to claim 8 wherein the pseudoephedrine hydrochloride, carnauba wax, stearic acid and colloidal silicon dioxide of Formulation (A) are combined in amounts of about 28.17%, about 70.42%, about 1.15% and about 0.25% respectively, by weight of the composition of Formulation (A), and the piperidinoalkanol, cellulose diluent, pregelatinized starch, croscarmellose sodium and magnesium stearate of Formulation (B) are combined in amounts of about 17.09%, about 61.67%, about 17.09%, about 3.42% and about 0.75% respectively, by weight of the composition of Formulation (B).

10. The pharmaceutical composition according to claim 9 wherein the piperidinoalkanol is 4-[4-[4-(hydroxydiphenylmethyl)-1-piperdinyl]-1-hydroxybutyl]-.alpha., .alpha.-dimethylbenzeneacetic acid hydrochloride.

11. The pharmaceutical composition according to claim 10 wherein the 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl-.alpha.,.alp ha.-dimethylbenzeneacetic acid hydrochloride is present in an amount of about 60 mg and the pseudoephedrine hydrochloride is present in an amount of about 120 mg.

12. A pharmaceutical composition according to claim 11 wherein the bilayer tablet is coated with a suitable coating agent.

13. A pharmaceutical composition according to claim 11 wherein the bilayer tablet has a hardness of about 15 kp to about 25 kp.
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