Galenical system for active transport, method for preparation and use

• US 9,192,679 B2
• Filed: 10/27/2014
• Issued: 11/24/2015
• Est. Priority Date: 03/24/2003
• Status: Active Grant

• Current Assignee: Capsugel France SAS (Lonza Group AG)
• Original Assignee: Capsugel France SAS (Lonza Group AG)
• Inventors: Ioualalen, Karim, Raynal, Rosanne
• Primary Examiner(s): Palenik, Jeffrey T
• Application Number:
  US14/523,999
• Publication Number:
  US 20150044297A1
• Time in Patent Office: 393 Days
• Field of Search: None
• US Class Current: 1/1
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/65 Tetracyclines
• CPC Class Codes: A61K 31/7048 having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin , digitoxin or digoxin
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/0095 Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006
• CPC Class Codes: A61K 9/14 Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51
• CPC Class Codes: A61K 9/1617 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 23/02 Local anaesthetics
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system

Abstract

The invention relates to a novel galenical system for taste masking, protecting an active substance, in particular in an acid medium, modulating releasing properties, masking mucous irritability and toxicity of certain active substances, for preparing aqueous forms which have a masked taste, are stable and pH independent. Said invention also relates, in particular to a galenical system which is embodied in the form of lipidic solid particles and strictly hydrophobic and devoid of water, surface active agents, emulsifiers, solvent traces and which is characterized in that it comprises at least one type of hydrophobic wax and at least one type of fatty non-neutralised acid.

Claims

1. A galenic system for oral administration in the form of strictly hydrophobic solid lipidic particles containing no water, surfactants, emulsifying agents or traces of solvents, characterised in that it comprises at least one hydrophobic wax, an active constituent, and additionally at least one non-neutralised fatty acid;

wherein the hydrophobic solid lipidic particles have a melting temperature between 30°

C. and 45°

C. after incorporation of the active constituent.

2. The galenic system according to claim 1 characterised in that the lipidic particles are in a spherical form.

3. The galenic system according to claim 1, characterised in that the hydrophobic wax is a vegetable, animal or mineral wax, or a mix of at least one wax and at least one non-amphiphilic oil.

4. The galenic system according to claim 1, characterised in that quantity of the hydrophobic wax is between 0.5% and 99%.

5. The galenic system according to claim 1, characterised in that it also comprises at least one additional hydrophobic compound capable of adjusting the melting point and physicochemical properties of the galenic system.

6. The galenic system according to claim 1, characterised in that the melting point of the hydrophobic wax may be between 15 and 75°

C.

7. The galenic system according to claim 1, characterised in that the hydrophobic wax is chosen from among triglycerides and derivatives, palm oil, Camauba wax, Candellila wax, Alfa wax, cocoa butter, ozokerite, vegetable waxes, beeswaxes and modified beeswaxes.

8. The galenic system according to claim 1, characterised in that the non-neutralised fatty acid is chosen from among fatty acids with linear chains with between 4 and 18 carbon atoms and has a content by mass of between 0.5% and 75%.

9. The galenic system according to claim 1, characterised in that it is in the form of lipidic particles with a size of between 0.5 microns and 1500 microns.

10. The galenic system according to claim 1, characterised in that the capacity of particles for holding the active constituent ranges from 0.02% to 75% by weight of the particles.

11. A galenic system for oral administration in the form of strictly hydrophobic solid lipidic particles containing no water, surfactants, emulsifying agents or traces of solvents, characterised in that it comprises at least one hydrophobic wax having a melting point between 30°

C. and 45°

C. and additionally at least one non-neutralised fatty acid.

13. The galenic system according to claim 11, characterised in that the lipidic particles are in a spherical form.

14. The galenic system according to claim 11, characterised in that the hydrophobic wax is a vegetable, animal or mineral wax, or a mix of at least one wax and at least one non-amphiphilic oil.

15. The galenic system according to claim 14, characterised in that the hydrophobic wax is chosen from among triglycerides and derivatives, palm oil, Camauba wax, Candellila wax, Alfa wax, cocoa butter, ozokerite, vegetable waxes, beeswaxes and modified beeswaxes.

16. The galenic system according to claim 11, characterised in that quantity of the hydrophobic wax is between 0.5% and 99%.

17. The galenic system according to claim 11, characterised in that it also comprises at least one additional hydrophobic compound capable of adjusting the melting point and physicochemical properties of the galenic system.

18. The galenic system according to claim 11, characterised in that the non-neutralised fatty acid is chosen from among fatty acids with linear chains with between 4 and 18 carbon atoms and has a content by mass of between 0.5% and 75%.

19. The galenic system according to claim 11, characterised in that it is in the form of lipidic particles with a size of between 0.5 microns and 1500 microns.

12. A galenic system for oral administration in the form of strictly hydrophobic solid lipidic particles containing no water, surfactants, emulsifying agents or traces of solvents, characterised in that it comprises at least one vegetable wax selected from olive wax, rice wax, hydrogenated jojoba wax or absolute flower waxes;

and additionally at least one non-neutralised fatty acid.