# US 7,611,729 B2 · Dosage forms having prolonged active ingredient release

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- Number: US 7,611,729 B2
- Document ID: US7611729B2
- Status: Granted
- Kind: B2
- Application number: 10/488,276
- Filed: 2002-09-04
- Published: 2004-09-16
- Granted: 2009-11-03
- Earliest claimed: 2001-09-10
- Assignees: Lunamed AG
- Inventors: Peter Truog
- Web page: https://patentgrep.com/patent/US7611729B2

## CPC

- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 3/12: for electrolyte homeostasis
- A61P 7/06: Antianaemics
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 13/08: of the prostate
- A61P 13/12: of the kidneys
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 37/04: Immunostimulants
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2846: {Poly(meth)acrylates}
- 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 relates to prolonged-release oral dosage forms of 4-phenylbutyric acid salts, such as sodium 4-phenylbutyrate. The prolonged release oral dosage forms are preferably tablets. The prolonged release is achieved by formulating 4-phenylbutyric acid with a delaying matrix material, such as hydroxypropylmethyl cellulose. The prolonged release oral dosage forms of the present invention may be administered once or twice a day to a patient suffering from a disease such as cancer or a urea cycle disorder.

## Claims

### Claim 1

A prolonged release oral pharmaceutical dosage form of a 4-phenylbutyric acid salt comprising:
250 mg of a 4-phenylbutyric acid salt;
wherein the dosage form comprises 146 mg of hydroxypropylmethylcellulose, 261 mg of lactose, 30 to 60 mg of microcrystalline cellulose, 10 mg of hardened vegetable oil or talcum, 1.5 mg of magnesium stearate, and optionally about 1 mg of highly dispersed silicon dioxide, that permits a rate of release of 4-phenylbutyric acid during a period of about 6 to 24 hours.

### Claim 2 (depends on 1)

The prolonged release oral pharmaceutical dosage form of claim 1, wherein the tablet weighs 0.7 g.

### Claim 3 (depends on 1)

The prolonged release oral pharmaceutical dosage form of claim 1, wherein the tablet further comprises a film coating.

### Claim 4 (depends on 1)

A method to treat a patient suffering from adenocarcinoma of the prostate comprising administering the prolonged release oral pharmaceutical dosage form of claim 1 twice a day.

### Claim 5 (depends on 4)

The method of claim 4, wherein the effective dose upon twice daily administration to a patient is about 250 to about 2000 mg per day.

### Claim 6 (depends on 1)

The prolonged release oral pharmaceutical dosage form of claim 1, wherein the 4-phenylbutyric acid salt is sodium 4-phenylbutryate.