Oral administration of at least one pharmaceutical and/or antigenic active substance

Patent metadata

Field	Value
Publication number	US-10238737-B2
Application number	US-201515509284-A
Country	US
Kind code	B2
Filing date	Sep 7, 2015
Priority date	Sep 23, 2014
Publication date	Mar 26, 2019
Grant date	Mar 26, 2019

Abstract

Disclosed is a gastro-resistant vector for the oral administration of at least one pharmaceutical and/or antigenic active substance including an aqueous phase (W) and an oily phase (O) in the form of a water-in-oil (W/O)-type emulsion wherein the aqueous phase includes at least one active principle and between 2 and 40 wt. % of a hydrophilic polymer that is insoluble in an aqueous phase of pH<6.5.

First claim

The invention claimed is:

1. A gastroresistant vector suitable for oral administration of at least one pharmaceutical and/or antigenic active substance comprising:
an aqueous phase (W), and
an oily phase (O),

said vector being in the form of an emulsion of water-in-oil (W/O) type,
wherein the aqueous phase comprises at least one active ingredient and sodium polyacrylate, and
wherein said vector comprises at least 10% by weight water, 20% to 80% by weight of oil, and from 2% to 40% by weight of sodium polyacrylate.

2. The vector as claimed in claim 1 , wherein the oily phase comprises at least one surfactant and at least one oil chosen from fatty acid esters, a fluid mineral oil, a vegetable oil, and squalane.

3. The vector as claimed in claim 2 , wherein the oil chosen is ethyl oleate.

4. The vector as claimed in claim 1 , comprising an immunity adjuvant chosen from alginates, a microemulsion, and divalent salts.

5. The vector as claimed in claim 1 , wherein the active ingredient is a substance capable of being denatured or degraded during direct oral administration and is chosen from an antigen, a medicament, an antiparasitic and an antibiotic.

6. The vector as claimed in claim 1 , wherein the amount of said sodium polyacrylate added is greater than 4% by weight of the final composition and less than 20% by weight of the final composition.

7. A gastroresistant carrier comprising one or more vectors as claimed in claim 1 .

8. A composition comprising at least one vector as defined in claim 1 .

9. A medicament that is orally active in human or veterinary therapy and that has curative and/or preventive properties and/or properties enabling diagnosis, comprising the vector of claim 1 .

10. A pharmaceutical and/or veterinary product intended for oral vaccination, comprising the medicament of claim 9 .

11. A process for preparing a vector as defined in claim 1 , comprising the following steps:
a) preparing an oily phase comprising one or more oils, and an emulsifying system, comprising one or more emulsifying surfactants and sodium polyacrylate and optionally water for stabilizing the vector;
b) adding water containing the active ingredient to be made gastroresistant, with stirring, in order to form an emulsion of water-in-oil (W/O) type comprising at least 10% by weight of water.

12. The process as claimed in claim 11 , wherein the aqueous phase (W) of the emulsion of water-in-oil (W/O) type contains an active ingredient which is a substance capable of being denatured or degraded during direct oral administration and is chosen from an antigen, a medicament, an antiparasitic and an antibiotic.

13. The process as claimed in claim 11 , wherein the sodium polyacrylate is added in step a) in the form of oily reverse latex.

14. The process as claimed in claim 11 , wherein the sodium polyacrylate is added in step a) in the form of powder to be dispersed in the water.

15. The process as claimed in claim 11 , wherein the sodium polyacrylate is added in step a) in the form of a liquid aqueous dispersion or of an organic solution to be emulsified in the starting oily composition.

16. The process as claimed in claim 11 , wherein the steps take place at a temperature below 55° C.

17. The process of claim 16 , wherein the steps take place at a temperature between 5° C. and 35° C.

Assignees

• Soc Dexploitation De Produits Pour Les Industries Chimiques Seppic

Inventors

• Ben Arous Juliette
• Dupuis Laurent
• Gaucheron Jerome

Classifications

• A61P37/00

  Drugs for immunological or allergic disorders · CPC title

• A61P31/00

  Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics · CPC title

• A61K47/38

  Cellulose; Derivatives thereof · CPC title

• A61K47/36 Primary

  Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin · CPC title

• A61K47/34

  Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence) · CPC title