# US 2008/0187587 A1 · Controlled release formulations containing an active ingredient, preferably melatonin and the method of preparation

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- Number: US 2008/0187587 A1
- Document ID: US20080187587A1
- Status: Published application
- Kind: A1
- Application number: 11/983,958
- Filed: 2007-11-13
- Published: 2008-08-07
- Earliest claimed: 2000-05-17
- Assignees: Ambros Pharma S.R.L.
- Inventors: Bojidar M. Stankov
- Web page: https://patentgrep.com/patent/US20080187587A1

## CPC

- A61K 31/4045: Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
- A61K 9/209: {containing drug in at least two layers or in the core and in at least one outer layer}
- A61P 5/00: Drugs for disorders of the endocrine system
- A61P 25/00: Drugs for disorders of the nervous system
- A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A controlled release melatonin tablet having: (a) a slow release nucleus of melatonin, hydroxypropyl methylcellulose, a lubricant, a volume excipient and a glidant, wherein 95% of the melatonin is released within 5 hours in an oscillating tray containing gastric/intestinal juice at 37° C.; (b) a fast release cortex coating on said nucleus of melatonin, hydroxypropyl methylcellulose, a lubricant, a volume excipient and a glidant, wherein at least 95% of the melatonin is released within 10 minutes in an oscillating tray containing gastric/intestinal juice at 37° C.

## Claims

### Claim at position 1

1-15. (canceled)

### Claim 16

A controlled release melatonin tablet which consists of:
(a) a slow release nucleus consisting of melatonin, hydroxypropyl methylcellulose, a lubricant, a volume excipient and a glidant, wherein 95% of the melatonin is released within 5 hours in an oscillating tray containing gastric/intestinal juice at 37° C.;
(b) a fast release cortex coating on said nucleus which consist of melatonin, hydroxypropyl methylcellulose, a lubricant, a volume excipient and a glidant, wherein at least 95% of the melatonin is released within 10 minutes in an oscillating tray containing gastric/intestinal juice at 37° C.

### Claim 17 (depends on 16)

The melatonin tablet as defined in claim 16 which consist of:
(a) a slow release nucleus consisting of 1-3 mg of melatonin, hydroxypropyl methylcellulose, a volume excipient and a glidant;
(b) a fast release cortex coating on said nucleus which consists of 0.5-1.5 mg of melatonin with hydroxypropyl methylcellulose, a volume excipient and a glidant.

### Claim 18 (depends on 16)

The melatonin tablet as defined in claim 16 wherein the content of melatonin is between 0.1 and 100 mg in the slow release nucleus and between 0.1 and 100 mg in the fast release cortex.

### Claim 19

A controlled release melatonin tablet which consists of:
(a) a slow release nucleus consisting of melatonin, hydroxypropyl methylcellulose, a volume excipient and a glidant which releases the melatonin over a 5 to 7 hour period in vivo;
(b) a fast release cortex coating on said nucleus consisting of melatonin, hydroxypropyl methylcellulose, a volume excipient and a glidant which releases the melatonin in 5-10 minutes in vivo.

### Claim 20 (depends on 19)

A method of inducing and maintaining sleep which consists of the administration of the formulation of claim 19 to one who suffers from a sleep disorder.

### Claim 21

(canceled)