MULTIPLE UNIT PELLET SYSTEM TABLET COMPRISING RIBOFLAVIN

Abstract

The present invention relates to a new formulation of specific nutritional ingredients (nutraceuticals) and/or pharmaceutical compounds.

Claims

1. A multiple unit pellet system, which comprises at least two different pellets (a) pellets (pellets (a)) comprising 10-90 wt-%, based on the total weight of the pellet (a), of riboflavin and (b) particles (particles (b)) comprising at least one thiopurine and/or at least a pharmaceutically acceptable salt and/or at least one prodrug thereof, wherein the pellets (a) are coated.

2. Multiple unit pellet system according to claim 1, wherein the least one thiopurine and/or at least a pharmaceutically acceptable salt and/or at least one prodrug thereof is chosen from the group consisting of 6-mercaptopurine, azathioprine and thioguanine.

3. Multiple unit pellet system according to claim 1, which is in the form of a tablet.

4. Multiple unit pellet system according to claim 1, which comprises at least one auxiliary ingredient.

5. Multiple unit pellet system according to claim 4, wherein the at least one auxiliary ingredient is chosen from the group consisting of binders, fillers, lubricants, proteins, dyes, flavours, sweeteners, minerals, and antioxidants without being limited thereto

6. Multiple unit pellet system according to claim 4, wherein the total amount of the auxiliary ingredients is up to 99 wt-%, based on the total weight of the MUPS tablet.

7. Multiple unit pellet system according to claim 1, wherein the coating material is chosen from the group consisting ogcellulose acetate phthalate (CAP) (Aquateric®), poly vinyl acetate phthalate(PVAP) (Coateric®), hydroxypropyl methyl cellulose phthalate(HPMCP), and methacrylic acid copolymers, shellac, fats alginate, chitosan, pectin, cyclodextrin and other gums.

8. Process for the production of the multiple unit pellet system according to claim 1, comprising the following step: (i) the pellets (a) and the particles (b) are produced, and (ii) the pellets (a) and optionally the particles (b) are coated, and (iii) the pellets and the particles are mixed, and (iv) optionally other ingredients, which are useful or desired to form the tablet are added, and (v) compressing the mixture obtained in step (iii) or step (iv) into a tablet.

Description

EXAMPLES

Example 1: Coating with Alginate/Shellac

[0104] 80 g granulated Riboflavin was successively coated with 9% Na-alginate, 1% Ca-Chloride and 25% shellac using a WFP-mini fluid bed processor (DMR) in Wurster configuration. 89 g coated product with particle size between 250 and 1000 μm was obtained. Coating material was 35% of the particle mass, riboflavin content 50%. 20 mg of coated powder (containing 10 mg of Riboflavin) was dissolved in 1000 ml water for 15 min. Absorption of the solution was measured at 545 nm using a spectrophotometer (Genesys 20, thermo Scientific). Absorption of the solution was 0.065.

Comparison Example 2: Solution of Uncoated Riboflavin

[0105] 10 mg of riboflavin powder was dissolved in 1000 ml water for 15 min. Absorption of the solution was measured at 545 nm using a spectrophotometer (Genesys 20, thermo Scientific). Absorption of the solution was 0.386.

Example 3: Coating with Eudragit FS30D

[0106] 80 g granulated Riboflavin was coated with 60 g Eudragit FS30D and 10 g PIasACRYL T20 using a WFP-mini fluid bed processor (DMR) in Wurster configuration. 71 g coated product with particle size between 250 and 1000 μm was obtained. Coating material was ca. 20% of the particle mass, riboflavin content was 60%. 16.6 mg of coated powder (containing 10 mg of Riboflavin) was dissolved in 1000 ml water for 15 min. Absorption of the solution was measured at 545 nm using a spectrophotometer (Genesys 20, thermo Scientific). Absorption of the solution was 0.087.