# US 8,771,735 B2 · Immediate release dosage forms of sodium oxybate

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- Number: US 8,771,735 B2
- Document ID: US8771735B2
- Status: Granted
- Kind: B2
- Application number: 12/264,709
- Filed: 2008-11-04
- Published: 2010-05-06
- Granted: 2014-07-08
- Earliest claimed: 2008-11-04
- Assignees: Jazz Pharmaceuticals, Inc.
- Applicants: Andrea Rourke; Clark Allphin; Maura Murphy
- Inventors: Andrea Rourke; Clark Allphin; Maura Murphy
- Web page: https://patentgrep.com/patent/US8771735B2

## CPC

- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/282: {Organic compounds, e.g. fats}
- A61K 9/284: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone}
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- 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

The present invention provides a pharmaceutical composition, presented as a solid unit dosage form adapted for oral administration of sodium oxybate. The preferred unit dosage form is a tablet comprising a relatively high weight-percentage of sodium oxybate, in combination with a relatively small weight-percentage of total excipients. This permits the tablets to contain/deliver a pharmaceutically effective amount, e.g., about 0.5-1.5 g of sodium oxybate in each tablet with a delivery profile similar to that of the liquid form. The tablets are bioequivalent to the liquid form.

## Claims

### Claim 1

A compressed tablet of sodium oxybate for oral delivery of 0.5-1.25 g of sodium oxybate comprising 80-95 wt % sodium oxybate; 5-10 wt % compression aid; and 1-50% binder; wherein the tablet is bioequivalent to sodium oxybate oral solution.

### Claim 2 (depends on 1)

The compressed tablet of claim 1, wherein the tablet is coated to 1-10 wt % gain with a film coating.

### Claim 3 (depends on 1)

The compressed tablet of claim 1, wherein the tablet comprises 80-90 wt % sodium oxybate.

### Claim 4 (depends on 1)

The compressed tablet of claim 1, wherein the tablet does not contain a super-disintegrant.

### Claim 5 (depends on 1)

The compressed tablet of claim 1, wherein the tablet further comprises 0.1-10 wt % of a surfactant.

### Claim 6

An immediate release unit dosage form comprising an about 0.5-1.5 g compressed tablet comprising 80-95 wt-% sodium oxybate; about 2.5-7.5 wt-% microcrystalline cellulose and about 0.25-2.5 wt-% surfactant, wherein at least 90% of the sodium oxybate is released from the tablet within one hour from exposure of the tablet to an aqueous medium.

### Claim 7 (depends on 6)

The unit dosage form of claim 6, wherein the tablet is coated with a water resistant coating.

### Claim 8 (depends on 6)

The unit dosage form of claim 6, wherein the surfactant is an ionic surfactant.

### Claim 9 (depends on 6)

The unit dosage form of claim 6, further comprising a minor but effective amount of at least one of a second binder, a disintegrant, a glidant and a lubricant.

### Claim 10 (depends on 9)

The unit dosage form of claim 9, further comprising about 0.5-5 wt-% polyvinylpyrrolidone.

### Claim 11 (depends on 9)

The unit dosage form of claim 9, further comprising about 2.5-7.5 wt-% pregelatinized starch.

### Claim 12 (depends on 9)

The unit dosage form of claim 9, further comprising about 0.1-0.75 wt-% silicon dioxide.

### Claim 13 (depends on 9)

The unit dosage form of claim 9, further comprising magnesium stearate.

### Claim 14 (depends on 6)

A therapeutic method for treating a human afflicted with narcolepsy, restless leg syndrome, essential tremor, fibromyalgia, or chronic fatigue syndrome by orally administering to said human an effective amount of a unit dosage form of claim 6.

### Claim 15 (depends on 1)

A method for preparing the tablet of claim 1 by granulating a water-free composition comprising the sodium oxybate, the compression and the binder; and compressing the granulated composition to yield said tablet.

### Claim 16 (depends on 15)

The method of claim 15 further comprising coating said tablet with a water resistant coating.

### Claim 17 (depends on 16)

The method of claim 16 wherein the coating comprises PVA and lecithin.

### Claim 18

A compressed tablet of an oxybate salt for oral delivery of 0.5-1.25 g of oxybate salt comprising 80-95 wt % oxybate salt; 5-10 wt % compression aid; and 1-50% binder; wherein the tablet is bioequivalent to sodium oxybate oral solution.

### Claim 19 (depends on 18)

The tablet of claim 18 wherein the oxybate salt is selected from the group consisting of potassium oxybate, calcium oxybate, lithium oxybate and magnesium oxybate.