Solid dispersions of Coenzyme Q10

Patent metadata

Field	Value
Publication number	US-10905657-B2
Application number	US-201615579975-A
Country	US
Kind code	B2
Filing date	Jun 10, 2016
Priority date	Jun 12, 2015
Publication date	Feb 2, 2021
Grant date	Feb 2, 2021

Abstract

The invention relates to a solid dispersion comprising Coenzyme Q 10 and a phospholipid, in the presence of a cellulosic derivative and/or a polymeric material selected from the group consisting of polyvinylpyrrolidone, polyvinyl acetate, poly (methacrylic acid, methyl methacrylate), poloxamers, chitosan, alginates, hyaluronic acid, pectin, pullulan, cyclodextrins, starch polymers, D-alpha-tocopheryl polyethylene glycol 1000 succinate.

First claim

The invention claimed is:

1. A solid dispersion comprising:
a) Coenzyme Q10
b) a phospholipid,
c) one or more a cellulosic derivative selected from the group consisting of carboxymethyl cellulose, methylcellulose, ethyl cellulose, hydroxypropylcellulose, hydroxyethyl cellulose, hydroxypropylmethyl cellulose, microcrystalline cellulose, cellulose acetate phthalate and hydroxypropylmethyl cellulose phthalate;
wherein the Coenzyme Q10 to phospholipid ratio is 0.5 to 1, and the phospholipid is the only surfactant,
said solid dispersion being obtained by a method comprising the steps of:
i) preparing a suspension of the one or more cellulosic derivative, the phospholipid in an organic solvent;
ii) preparing a solution of coenzyme Q10 in an organic solvent;
iii) mixing the solution obtained in step ii) with the suspension obtained in step i);
iv) stirring the suspension obtained in step iii) at a temperature between 40° C. and 70° C.;
v) removing the solvent from the suspension obtained in step iv).

2. A pharmaceutical or nutraceutical formulation for oral administration containing the solid dispersion according to claim 1 and a pharmaceutically or food acceptable excipient.

3. The solid dispersion according to claim 1 wherein the phospholipid is selected from the group consisting of lecithins from soy, sunflower or egg, phosphatidyl choline, phosphatidyl serine and phosphatidyl ethanolamine.

4. The solid dispersion according to claim 1 wherein the Coenzyme Q10 to cellulosic derivative ratio is 0.2 to 2.

5. The solid dispersion according to claim 4 wherein the Coenzyme Q10 to cellulosic derivative ratio is 0.5 to 1.

6. The solid dispersion according to claim 1 comprising Coenzyme Q10, a phospholipid and one or more a cellulosic derivative selected from microcrystalline cellulose, hydroxypropylmethyl cellulose, methylcellulose.

7. The solid dispersion according to claim 6 wherein the phospholipid is a lecithin from soy, sunflower or egg.

8. The solid dispersion according to claim 1 wherein the organic solvent is selected from the group consisting of ethanol, acetone and ethyl acetate.

9. The solid dispersion according to claim 8 wherein the organic solvent is ethyl acetate.

Assignees

• Indena Spa

Inventors

• Ciceri Daniele
• Peterlongo Federico
• Ronchi Massimo

Classifications

• A61P3/02

  Nutrients, e.g. vitamins, minerals · CPC title

• A61K31/122 Primary

  having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin · CPC title

• A61K9/14

  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 title

• A61K9/146 Primary

  with organic macromolecular compounds · CPC title

• A61P37/02

  Immunomodulators · CPC title