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Claims for Patent: 5,948,437

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Claims for Patent: 5,948,437

Title: Pharmaceutical compositions using thiazepine
Abstract:The invention relates to sustained release formulations comprising 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f] [1,4]thiazepine or a pharmaceutically acceptable salt thereof, to methods of treating psychotic states and hyperactivity utilizing the sustained release formulations and to a process for preparing the sustained release formulations.
Inventor(s): Parikh; Bhavnish Vinod (Hockessin, DE), Timko; Robert Joseph (West Chester, PA), Addicks; William Joseph (Morgantown, WV)
Assignee: Zeneca Limited (GB)
Application Number:08/864,306
Patent Claims: 1. A sustained release formulation comprising a gelling agent and 11 -[4-[2-(2-hydroxyethoxy)ethyl]- 1 -piperazinyl]dibenzo-[b,f] [1,4]thiazepine or a pharmaceutically acceptable salt thereof, together with one or more pharmaceutically acceptable excipients.

2. A sustained release formulation according to claim 1 wherein the gelling agent is hydroxypropyl methylcellulose.

3. A sustained release formulation according to claim 2 comprising about 5 to 50% by weight of a hydroxypropyl methylcellulose selected from the group consisting of (a) a hydroxypropyl methylcellulose having a viscosity of about 40 to 60 cps, a methoxy content of about 28 to 30% by weight and a hydroxypropoxy content of from about 7 to less than 9% by weight, (b) a hydroxypropyl methylcellulose having a viscosity of about 3,500 to 5,600 cps, a methoxy content of about 28 to 30% by weight and a hydroxypropoxy content of about 7 to 12% by weight, (c) a hydroxypropyl methylcellulose having a viscosity of about 80 to 120 cps, a methoxy content of about 19 to 24% by weight and a hydroxypropoxy content of from about 7 to less than 9% by weight and (d) a hydroxypropyl methylcellulose having a viscosity of about 3,500 to 5,600 cps, a methoxy content of about 19 to 24% by weight and a hydroxypropoxy content of about 7 to 12% by weight, or mixtures thereof; with the proviso that if the formulation contains a hydroxypropyl methylcellulose described under (d) above the total amount of hydroxypropyl methylcellulose present in the formulation must be greater than 25.8% by weight.

4. A sustained release formulation according to claim 3 comprising about 5 to 40% by weight of a hydroxypropyl methylcellulose selected from the group consisting of (a)-(d) or mixtures thereof.

5. A sustained release formulation according to claim 4 comprising about 8 to 35% by weight of a hydroxypropyl methylcellulose selected from the group consisting of (a)-(d) or mixtures thereof.

6. A formulation according to claim 5 comprising about 10 to 30% by weight of a hydroxypropyl methylcellulose selected from the groups (a)-(d) or mixtures thereof.

7. A formulation according to claim 6 comprising about 15 to 30% by weight of a hydroxypropyl methylcellulose selected from the groups (a)-(d) or mixtures thereof.

8. A formulation according to claim 7 wherein the one or more pharmaceutically acceptable excipients are selected from the group consisting of microcrystalline cellulose, lactose, magnesium stearate, sodium citrate and povidone.

9. A formulation according to claim 8 wherein the one or more pharmaceutically acceptable excipients are selected from the group consisting of (a) about 4 to 20% by weight of microcrystalline cellulose, (b) about 5 to 20% by weight of lactose, (c) about I to 3% by weight of magnesium stearate, (d) about 10 to 30% by weight of sodium citrate and (e) about 1 to 15% by weight of povidone.

10. A formulation according to claim 1 wherein 11 -[4-[2-(2hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine is in the form of a hemifumarate salt.

11. A formulation according to claim 1 wherein one of the one or more pharmaceutically acceptable excipients is a pH modifier.

12. A formulation according to claim 11 wherein the pH modifier is sodium citrate.

13. A method of treating psychotic states or hyperactivity in a warm-blooded animal which comprises administering to said warm-blooded animal an effective amount of a formulation according to anyone of claims 1-12.

14. A process for preparing a formulation according to anyone of claims 1 or 2 which comprises mixing 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[[b,f][1,4]thiazepin e, or a pharmaceutically acceptable salt thereof, a gelling agent and other excipients.

15. A process for preparing a formulation according to anyone of claims 1 or 2 which comprises:

(a) mixing 11-[4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine , or a pharmaceutically acceptable salt thereof, a gelling agent and other excipients;

(b) wet granulating the mixed components;

(c) drying the mixture;

(d) milling the dried mixture;

(e) blending the mixture with a lubricant; and

(f) compressing the blended mixture to form tablets.
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