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Claims for Patent: 9,265,720

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Claims for Patent: 9,265,720

Title:Pharmaceutical formulations useful in the treatment of insomnia
Abstract: There is provided a formulation suitable for transmucosal administration comprising a short acting hypnotic drug, which formulation provides a measurable plasma concentration of drug within 10 minutes of administration. The formulation is capable of providing sleep on demand, and preferably comprises particles of drug, for example zolpidem or a pharmaceutically-acceptable salt thereof and a mucoadhesion promoting agent, such as sodium carboxymethylcellulose, which particles of drug and mucoadhesive are presented upon the surface of larger carrier particles.
Inventor(s): Pettersson; Anders (Kode, SE), Nystrom; Christer (Stockholm, SE), Bredenberg; Susanne (Uppsala, SE)
Assignee: Orexo AB (Uppsala, SE)
Application Number:11/666,361
Patent Claims: 1. A method of treating insomnia in an individual by sublingual administration of a pharmaceutical composition, the method comprising: providing the pharmaceutical composition in a dosage form comprising a tablet sized for placement under a tongue, wherein the pharmaceutical composition comprises (a) carrier particles having exterior surfaces, (b) particles of zolpidem or a pharmaceutically acceptable salt thereof sized smaller than the carrier particles and presented, at least in part, upon the exterior surfaces of the carrier particles and said particles of zolpidem or salt thereof cover at least 90% of the exterior surfaces of said carrier particles; and (c) particles of a mucoadhesion promoting agent sized smaller than the carrier particles and presented, at least in part, upon the exterior surfaces of the carrier particles, wherein both the particles of zolpidem or a pharmaceutically acceptable salt thereof and the particles of the mucoadhesion promoting agent are presented, at least in part, upon the exterior surfaces of the carrier particles; and sublingually administering the pharmaceutical composition to the individual to treat the insomnia by placing the tablet under the tongue of the individual, wherein sublingual administration of the pharmaceutical composition provides a therapeutic outcome comprising (i) a measurable plasma concentration of zolpidem within 10 minutes of sublingual administration; and (ii) a time difference following sublingual administration between a first measurable plasma concentration of zolpidem and a maximum measured plasma concentration of zolpidem that is within a range of about 80 minutes to about 160 minutes; and (iii) a plasma concentration of zolpidem that is capable of maintaining sleep for at least about 6 hours after sublingual administration; wherein said individual is thereby treated for insomnia.

2. A method according to claim 1 wherein the insomnia comprises transient insomnia.

3. A method of providing sleep on demand to an individual by sublingual administration of a pharmaceutical composition, the method comprising providing the pharmaceutical composition in a dosage form comprising a tablet sized for placement under a tongue, wherein the pharmaceutical composition comprises (a) carrier particles having exterior surfaces, (b) particles of zolpidem or a pharmaceutically acceptable salt thereof sized smaller than the carrier particles and presented, at least in part, upon the exterior surfaces of the carrier particles and said particles of zolpidem or salt thereof cover at least 90% of the exterior surfaces of said carrier particles; and (c) particles of a mucoadhesion promoting agent sized smaller than the carrier particles and presented, at least in part, upon the exterior surfaces of the carrier particles, wherein both the particles of zolpidem or a pharmaceutically acceptable salt thereof and the particles of the mucoadhesion promoting agent are presented, at least in part, upon the exterior surfaces of the carrier particles; and sublingually administering the pharmaceutical composition to the individual to treat the insomnia by placing the tablet under the tongue of the individual, wherein sublingual administration of the pharmaceutical composition provides a therapeutic outcome comprising (i) a measurable plasma concentration of zolpidem within 10 minutes of sublingual administration; and (ii) a time difference following sublingual administration between a first measurable plasma concentration of zolpidem and a maximum measured plasma concentration of zolpidem that is within a range of about 80 minutes to about 160 minutes; and (iii) a plasma concentration of zolpidem that is capable of maintaining sleep for at least about 6 hours after sublingual administration; wherein said individual is thereby provided with sleep on demand.

4. A method according to claim 1 or 3 wherein at least 50% of the zolpidem that is present in the pharmaceutical composition upon sublingual administration is released within 5 minutes, as tested and measured in a standard in vitro paddle apparatus according to the United States Pharmacopoeia, using a phosphate buffer at pH 6.8 (USP) as dissolution medium.

5. A method according to claim 4 wherein at least 50% of the zolpidem that is present in the pharmaceutical composition upon administration is released within 3 minutes.

6. A method according to claim 1 or 3 wherein the therapeutic outcome further provides (iv) a plasma concentration of zolpidem that does not result in decreased alertness and/or impairment of psychomotor function in a patient following sleep at least about 7 hours after sublingual administration.

7. A method according to claim 1 or 3 wherein the salt of zolpidem is zolpidem hemitartrate.

8. A method according to claim 1 or 3 wherein the particles of zolpidem or pharmaceutically-acceptable salt thereof are microparticles.

9. A method according to claim 8 wherein the microparticles have a weight based mean diameter of between about 1 .mu.m and about 10 .mu.m.

10. A method according to claim 1 or 3 wherein the zolpidem or a pharmaceutically acceptable salt thereof comprises between about 5 to about 15 weight percent of the pharmaceutical composition.

11. A method according to claim 1 or 3 wherein the pharmaceutical composition comprises about 5 mg to about 12 mg of zolpidem or a pharmaceutically acceptable salt thereof in a dose unit of the pharmaceutical composition.

12. A method according to claim 1 or 3 wherein the mucoadhesion promoting agent is sodium carboxymethylcellulose.

13. A method according to claim 12 wherein the sodium carboxymethylcellulose is internally crosslinked sodium carboxymethylcellulose (croscarmellose sodium).

14. A method according to claim 1 or 3 wherein the mucoadhesion promoting agent comprises between about 3.5 to about 6.5 weight percent of the pharmaceutical composition.

15. A method according to claim 1 or 3 wherein the pharmaceutical composition further comprises a binder or disintegrating agent.

16. A method according to claim 15 wherein the binder is microcrystalline cellulose.

17. A method according to claim 16 wherein the microcrystalline cellulose is silicified microcrystalline cellulose.

18. A method according to claim 15 wherein the binder comprises between about 2.0 to about 3.0 weight percent of the pharmaceutical composition.

19. A method according to claim 1 or 3 wherein the carrier particles have a weight based mean diameter of between about 150 .mu.m to about 400 .mu.m.

20. A method according to claim 1 or 3 wherein the carrier particles comprise mannitol.

21. A method according to claim 20 wherein the mannitol is spray-dried mannitol.

22. A method according to claim 1 or 3 wherein the carrier particles comprise between about 70 to about 85 weight percent of the pharmaceutical composition.

23. A method according to claim 1 or 3 wherein the coverage is between about 130% and about 180%.

24. A method according to claim 1 or 3 wherein the pharmaceutical composition further comprises a lubricant.

25. A method according to claim 24 wherein the lubricant is magnesium stearate.

26. A method according to claim 1 or 3 wherein the tablet has a weight of about 80 mg and a diameter of about 6 mm.
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