Preparation of emulsions and concentrates thereof

• US 20040043043A1
• Filed: 08/15/2003
• Published: 03/04/2004
• Est. Priority Date: 09/20/2000
• Status: Abandoned Application

• Current Assignee: Nycomed Pharma AS (Takeda Pharmaceutical Company Limited)
• Original Assignee: Nycomed Pharma AS (Takeda Pharmaceutical Company Limited)
• Inventors: Pienne, Jan Yngvar, Schlyter, Jimmy Hirschsprung
• Application Number:
  US10/380,544
• Publication Number:
  US 20040043043A1
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A23L 27/80 Emulsions
• CPC Class Codes: A23L 33/15 Vitamins
• CPC Class Codes: A23V 2002/00 Food compositions, function of food ingredients or processes for food or foodstuffs
• CPC Class Codes: A23V 2250/032 Citric acid
• CPC Class Codes: A23V 2250/054 Sorbic acid
• CPC Class Codes: A23V 2250/156 Mineral combination undefined extract A23V2250/1638
• CPC Class Codes: A23V 2250/1592 Iron
• CPC Class Codes: A23V 2250/1598 Iodine
• CPC Class Codes: A23V 2250/16 Potassium
• CPC Class Codes: A23V 2250/1614 Sodium
• CPC Class Codes: A23V 2250/1642 Zinc
• CPC Class Codes: A23V 2250/1842 Lecithin
• CPC Class Codes: A23V 2250/1944 Medium-chain triglycerides
• CPC Class Codes: A23V 2250/211 Carotene, carotenoids
• CPC Class Codes: A23V 2250/5024 Agar
• CPC Class Codes: A23V 2250/505 Galactomannan
• CPC Class Codes: A23V 2250/506 Guar
• CPC Class Codes: A23V 2250/507 Locust bean, carob
• CPC Class Codes: A23V 2250/606 Fructose
• CPC Class Codes: A23V 2250/61 Glucose, Dextrose
• CPC Class Codes: A23V 2250/642 : Sorbitol
• CPC Class Codes: A23V 2250/70 : Vitamins
• CPC Class Codes: A23V 2250/702 : Vitamin A
• CPC Class Codes: A23V 2250/704 : Vitamin B
• CPC Class Codes: A23V 2250/708 : Vitamin C
• CPC Class Codes: A23V 2250/71 : Vitamin D
• CPC Class Codes: A23V 2250/712 : Vitamin E
• CPC Class Codes: A23V 2250/714 : Vitamin K
• CPC Class Codes: A61K 47/14 : Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• 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 9/107 : Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00
• CPC Class Codes: A61P 3/02 : Nutrients, e.g. vitamins, minerals

Abstract

The invention provides a process for the preparation of a liquid emulsion composition having a continuous aqueous phase containing a gelling agent and a thickener and optionally a physiologically tolerable amount of at least one water soluble vitamin and/or non-vitamin drug, and a discontinuous oil phase, optionally comprising at least one lipophilic vitamin and/or non-vitamin lipophilic drug and optionally an edible triglyceride, said emulsion composition further containing at least one emulsifying agent, said process comprising: forming an aqueous composition comprising an aqueous solution of a gelling agent and a thickener and optionally at least one water soluble vitamin and/or non-vitamin drug; forming a water-immiscible liquid composition comprising at least one emulsifying agent and optionally at least one lipophilic vitamin and/or non-vitamin drug; mixing said water-immiscible composition with at least part of said aqueous composition whereby to form an oil-in-water emulsion; and if required mixing further components with said emulsion whereby to form said liquid emulsion composition.

Claims

1. A process for the preparation of a liquid emulsion composition having a continuous aqueous phase containing a gelling agent and a thickener and optionally a physiologically tolerable amount of at least one water soluble vitamin and/or non-vitamin drug, and a discontinuous oil phase, optionally comprising at least one lipophilic vitamin and/or non-vitamin drug and optionally an edible triglyceride, said emulsion composition further containing at least one emulsifying agent, said process comprising:

forming an aqueous composition comprising an aqueous solution of a gelling agent and a thickener and is optionally at least one water soluble vitamin and/or non-vitamin drug;

forming a water-immiscible liquid composition comprising at least one emulsifying agent and optionally at least one lipophilic vitamin and/or non-vitamin drug;

mixing said water-immiscible composition with at least part of said aqueous composition whereby to form an oil-in-water emulsion; and

if required mixing further components with said emulsion whereby to form said liquid emulsion composition.

2. A process for the preparation of an emulsion concentrate comprising forming a liquid emulsion composition by a process as claimed in claim 1 and then drying said liquid emulsion composition.

4. A process as claimed in claim 2 or claim 3 wherein drying is effected by spray drying.

5. A process as claimed in claim 4 further comprising the step of adding particulate sucrose or sorbitol into the atomisation zone of the spray dryer.

6. A process as claimed in any one of claims 1 to 5 wherein said liquid emulsion further comprises a solid carrier.

7. A process as claimed in claim 6 wherein said solid carrier comprises sucrose, sorbitol, lactose or maltodextrin.

8. A process as claimed in any preceding claim wherein said gelling agent is selected from agar agar, alginates, carrageenans, gellan gum and pectin.

9. A process as claimed in any preceding claim wherein said thickener is an edible gum or a mixture of edible gums.

10. A process as claimed in any preceding claim wherein said liquid emulsion contains in the discontinuous oil phase thereof a non-vitamin drug compound.

11. A process as claimed in claim 10 wherein said drug compound is a lipophilic drug selected from Probucol, Diazepam, Danazol, Halofantrine and Cyclosporin A.

12. A process as claimed in any one of claims 1 to 10 wherein said liquid emulsion comprises a cough suppressant together with one or more analgesics.

3. A process for the preparation of an emulsion concentrate comprising spray drying or freeze drying a liquid emulsion having a continuous aqueous phase containing a gelling agent and a thickener and a discontinuous edible oil phase, said emulsion further containing at least one emulsifying agent.

13. A pharmaceutical composition in emulsion form comprising a discontinuous oil phase containing an edible oil with dissolved or dispersed therein a non-vitamin drug compound or compound mixture, and a continuous aqueous phase containing a gelling agent and a thickener, together with an emulsifying agent.

25. A method of treatment of a human or non-human mammal subject to combat conditions associated with vitamin deficiency (e.g. beri-beri, nyctalopia, megaloblastic haemopoiesis, pernicious anemia, hypoprothrombis anemia, pellegra, sprue, scurvy, rickets), said method comprising orally admininstering to said subject a composition or emulsion concentrate as claimed in any one of claims 13 to 19, 21 and 22, optionally following dilution thereof in a physiologically tolerable aqueous liquid.

14. A spray dried emulsion concentrate comprising at least one lipophilic vitamin and/or non-vitamin drug, a gelling agent and a thickener, and optionally an edible triglyceride, further containing at least one emulsifying agent.

16. An emulsion concentrate as claimed in claims 14 or 15 wherein said lipophilic vitamin and/or non-vitamin drug is present in the discontinuous phase.

18. An emulsion concentrate as claimed in claims 14 or 15 wherein said water-soluble vitamin and/or non-vitamin drug is present in the aqueous phase.

20. A kit comprising a first container containing a physiologically tolerable aqueous liquid, and a second container containing an emulsion concentrate as claimed in any one of claims 14 to 19.

15. A freeze dried emulsion concentrate comprising at least one lipophilic vitamin and/or non-vitamin drug, a gelling agent and a thickener, and optionally an edible triglyceride, further containing at least one emulsifying agent.

17. A freeze-dried or spray dried emulsion concentrate comprising at least one water-soluble vitamin and/or non-vitamin drug, a gelling agent and a thickener, and optionally an edible triglyceride, further containing at least one emulsifying agent.

19. An emulsion concentrate comprising droplets of an edible oil dispersed in a gelling agent, a thickener and an emulsifying agent, said emulsion concentrate containing at least one lipophilic vitamin.

21. An emulsion composition comprising a continuous aqueous phase and a discontinuous oil phase which contains a particulate solid at a concentration such that said phases are isodense.

22. A liquid emulsion composition having a continuous aqueous phase containing a gelling agent and a thickener and optionally a physiologically tolerable amount of at least one water soluble vitamin and/or non-vitamin drug, and a discontinuous oil phase optionally comprising at least one lipophilic vitamin and/or non-vitamin drug and optionally an edible triglyceride, said emulsion composition further containing at least one emulsifying agent, said oil phase comprising at least one of (i) droplets of a discontinuous aqueous phase containing a physiologically active or beneficial compound dissolved therein, (ii) an inorganic particulate, and (iii) a non-vitamin lipophilic drug compound.

23. An emulsion composition as claimed in claim 22 wherein said non-vitamin lipophilic drug compound is selected from Probucol, Diazepam, Danazol, Halofantrine and Cyclosporin A.

24. An emulsion composition as claimed in claim 22 which comprises a cough suppressant together with one or more analgesics.