Solid pharmaceutical compositions containing benzofuran derivatives

• US 8,318,800 B2
• Filed: 12/13/2007
• Issued: 11/27/2012
• Est. Priority Date: 06/23/1997
• Status: Expired due to Fees

• Current Assignee: Sanofi-Aventis (Sanofi-Synthélabo SA)
• Original Assignee: Sanofi
• Inventors: Abramovici, Bernard, Gautier, Jean-Claude, Gromenil, Jean-Claude, Marrier, Jean-Marie
• Primary Examiner(s): Lundgren, Jeffrey S.
• Assistant Examiner(s): FINN, MEGHAN R
• Application Number:
  US11/955,565
• Publication Number:
  US 20080139645A1
• Time in Patent Office: 1,811 Days
• Field of Search: 514/469, 514/467, 514/975, 514/960
• US Class Current: 514/469
• CPC Class Codes: A61K 31/343 condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/06 Antiarrhythmics
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The present invention relates to a solid pharmaceutical composition for oral administration characterized in that it comprises a benzofuran derivative with antiarrhythmic activity, or one of the pharmaceutically acceptable salts thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients.

Claims

1. A solid pharmaceutical composition for oral administration comprising dronedarone, or a pharmaceutically acceptable salt thereof, as an active principle, and a pharmaceutically acceptable nonionic hydrophilic surfactant optionally in combination with one or more pharmaceutical excipients wherein the nonionic hydrophilic surfactant is present in a proportion of from 1% to 50% by weight of the active principle in base form.

2. The pharmaceutical composition according to claim 1, wherein the active principle is dronedarone hydrochloride.

3. The pharmaceutical composition according to claim 1 wherein the nonionic hydrophilic surfactant is selected from the group consisting of poloxamers, polyethoxylated castor oils, and polyethylene hydroxystearates.

4. The pharmaceutical composition according to claim 3, wherein the nonionic hydrophilic surfactant is selected from the group consisting of poloxamer 124, poloxamer 188, poloxamer 237, poloxamer 338, poloxamer 407, and polyethylene hydroxystearate 660.

5. The pharmaceutical composition according to claim 4 wherein the nonionic hydrophilic surfactant is poloxamer 407.

6. The pharmaceutical composition according to claim 1, which is in a tablet or a gelatin capsule form, wherein the nonionic hydrophilic surfactant is present in a proportion of from 1% to 20% by weight of the active principle in base form.

7. The pharmaceutical composition according to claim 6, which is in a tablet or a gelatin capsule form, wherein the nonionic hydrophilic surfactant is present in a proportion of from 5% to 15% by weight of the active principle in base form.

8. The pharmaceutical composition according to claim 1 containing from 50 to 500 mg of active principle.

9. The pharmaceutical composition according to claim 8, which is in a tablet or a gelatin capsule form, containing from 200 to 400 mg of active principle.

10. The pharmaceutical composition according to claim 9, which is in a tablet or a gelatin capsule form, containing from 200 to 400 mg of active principle, calculated in base form, and 10% by weight of nonionic hydrophilic surfactant relative to the active principle in base form.

11. The pharmaceutical composition according to claim 10 wherein the nonionic hydrophilic surfactant is poloxamer 407.

12. The pharmaceutical composition according to claim 1 comprising one or more pharmaceutical excipients selected from the group consisting of a binder, a flow agent, a vinylpyrrolidone polymer or copolymer, a diluent, a starch and a lubricant.

13. The pharmaceutical composition according to claim 12, wherein the one or more pharmaceutical excipients is selected from the group consisting of methylcellulose, hydroxyethylcellulose, methylhydroxypropylcellulose, a macrogol, colloidal silica, polyvinylpyrrolidone, lactose, mannitol, wheat starch, corn starch, magnesium stearate, and sodium stearyl fumarate.

14. A solid pharmaceutical composition in tablet form for oral administration consisting essentially of dronedarone or a pharmaceutically acceptable salt thereof, as an active principle;

a pharmaceutically acceptable nonionic hydrophilic surfactant, wherein said nonionic hydrophilic surfactant is a poloxamer; and

one or more pharmaceutical excipients;

said nonionic hydrophilic surfactant being present in a proportion of from 5% to 15% by weight of the active principle in base form.

15. The pharmaceutical composition according to claim 14 wherein the one or more pharmaceutical excipients are selected from the group consisting of a binder, a flow agent, a vinylpyrrolidone polymer or copolymer, a diluent, a starch and a lubricant.