Formulation and method for the release of paroxetine in the large intestine

1. A formulation comprising paroxetine or a pharmaceutically acceptable salt thereof, in a controlled or delayed release swallow pharmaceutical formulation, and an enteric coating surrounding the core wherein the enteric coating consists of about 75% by weight methacrylic acid copolymer, about 12.5% by weight talc, about 11.25% by weight softener, about 1% by weight polysorbate, and about 0.25% by weight sodium hydroxide, wherein after about 5 to about 12 hours post administration, releases more than 65% of the paroxetine or a pharmaceutically acceptable salt thereof in a large intestine of a mammal, and is substantially insoluble in a stomach and a small intestine of the mammal.

2. The formulation of claim 1 , wherein the formulation releases more than 70% of the paroxetine or a pharmaceutically acceptable salt thereof in the large intestine.

3. The formulation of claim 1 , wherein a substantial portion of the paroxetine or a pharmaceutically acceptable salt thereof is released after at least about 5 hours following administration.

4. The formulation of claim 1 , wherein a substantial portion of the paroxetine or pharmaceutically acceptable salt thereof is released after at least about 7 hours following administration.

5. The formulation of claim 1 , wherein less than 35% of the paroxetine or pharmaceutically acceptable salt thereof is released in the stomach, small intestine, or a combination thereof.

6. The formulation of claim 1 , wherein the formulation comprises a caplet, tablet, particle, granule, or powder form.

7. A method of treating or preventing any one or more of alcoholism, anxiety, depression, obsessive compulsive disorder, panic disorder, chronic pain, obesity, senile dementia, migraine, bulimia, anorexia, social phobia, Pre-Menstrual Syndrome (PMS), adolescent depression, major depressive disorders, panic disorders, social anxiety disorders, premenstrual dysphoric disorders, and substance abuse comprising administering a therapeutically effective amount of the formulation of claim 1 .

8. The formulation of claim 1 , wherein the formulation is a controlled and delayed release formulation.

9. A formulation comprising paroxetine or a pharmaceutically acceptable salt thereof, in a delayed release swallow pharmaceutical formulation, and an enteric coating wherein the enteric coating consists of about 75% by weight methacrylic acid copolymer, about 12.5% by weight talc, about 11.25% by weight softener, about 1% by weight polysorbate, and about 0.25% by weight sodium hydroxide.

10. A method of treating and/or prophylaxis of one or more psychiatric disorders comprising the steps of:

administering a therapeutically effective amount of the formulation of claim 1 to a mammal in need thereof.

11. The method of claim 10 , wherein the amount of paroxetine or a pharmaceutically acceptable salt thereof in the formulation is between 1 and 100 mgs per unit.

12. The method of claim 10 , further comprising the step of administering the formulation to a mammal in order to treat one or more of the following disorders: alcoholism, anxiety, depression, obsessive, compulsive disorder, panic disorder, chronic pain, obesity, senile dementia, migraine, bulimia, anorexia, social phobia, Pre-Menstrual Syndrome (PMS), adolescent depression, trichotillomania dysthymia, major depressive disorders, panic disorders, social anxiety disorders, premenstrual dysphoric disorders and substance abuse.

13. The method of claim 10 , wherein about greater than 65% of the paroxetine or a pharmaceutically acceptable salt thereof is released after about 5 hours following ingestion.

14. The method of claim 10 , wherein about 70% or more of the paroxetine or a pharmaceutically acceptable salt thereof released after about 5 hours following ingestion.

15. A delayed release paroxetine composition comprising:

a core containing paroxetine or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier; and

an enteric coating surrounding the core wherein the enteric coating consists of about 75% by weight methacrylic acid copolymer, about 12.5% by weight talc, about 11.25% by weight softener, about 1% by weight polysorbate, and about 0.25% by weight sodium hydroxide.

16. The composition of claim 15 , wherein the paroxetine or a pharmaceutically acceptable salt thereof is selected from the group consisting of paroxetine hydrochloride, paroxetine hydrobromide, paroxetine acetate, paroxetine maleate, and paroxetine hydrochloride hemi-hydrate.

17. The composition of claim 15 , wherein the carrier comprises one or more of magnesium stearate, starch, glucose, lactose, sucrose, rice flour and chalk.

18. The composition of claim 15 , wherein the carrier comprises colloidal silicon dioxide and magnesium stearate.

19. A controlled release paroxetine composition comprising:

a core comprising

paroxetine hydrochloride hemihydrate;

microcrystalline cellulose;

magnesium stearate;

colloidal silicon dioxide;

hypromellose;

hydroxypropyl cellulose; and

lactose monohydrate; and

an enteric coating surrounding the core wherein the enteric coating consists of about 75% by weight methacrylic acid copolymer, about 12.5% by weight talc, about 11.25% by weight softener, about 1% by weight polysorbate, and about 0.25% by weight sodium hydroxide,

and wherein the methacrylic acid copolymer is chosen such that the composition is soluble at a pH of 6.8 in a large intestine of a mammal and is substantially insoluble in a stomach and a small intestine of the mammal.

20. The formulation of claim 1 , wherein the softener comprises at least one of dibutyl sebacate, a citric acid ester, a tartaric acid ester, a glycerin, a glycerin ester, and a phthalic acid ester.

21. The composition of claim 19 , wherein the softener comprises triethyl citrate.