Formulation

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 in the form of a tablet having a weight of 100 to 1000 mg which comprises a compressed mixture of pellets (a) and particles (b), wherein each of the pellets (a) has a coating layer of a coating material and comprises 15-75 wt. %, based on total weight of the pellets (a), of riboflavin, and wherein each of the particles (b) comprise at least one aminosalicylate and/or at least a pharmaceutically acceptable salt and/or at least one prodrug thereof.

2. The multiple unit pellet system according to claim 1, which further comprises at least one auxiliary ingredient.

3. The multiple unit pellet system according to claim 2, wherein the at least one auxiliary ingredient is selected from the group consisting of binders, fillers, lubricants, proteins, dyes, flavours, sweeteners, minerals, and antioxidants.

4. The multiple unit pellet system according to claim 2, wherein the total amount of the auxiliary ingredients is up to 99 wt. %, based on the total weight of the tablet.

5. The multiple unit pellet system according to claim 1, wherein the particles (b) comprise at least one aminosalicylate and/or at least a pharmaceutically acceptable salt and/or at least one prodrug thereof which is selected from the group consisting of 4-aminosalicylic acid, Balsalazide, Olsalazine, Sulfasalazine and Mesalazine (5-Aminosalicylic acid).

6. The multiple unit pellet according to claim 1, wherein the coating material is selected from the group consisting of ogcellulose acetate phthalate (CAP), polyvinyl acetate phthalate (PVAP), hydroxypropyl methyl cellulose phthalate (HPMCP), methacrylic acid copolymers, shellac, fats, alginate, chitosan, pectin, cyclodextrin and gums.

7. The multiple unit pellet according to claim 6, wherein the coating layer of the coating material on the pellets (a) has a thickness of 50-70 μm.

8. The multiple unit pellet according to claim 7, wherein the coating material is present in an amount which is 5-60 wt. %, based on the total weight of the pellets (a).

9. A process for the production of the multiple unit pellet system according to claim 1, comprising the steps of: (i) providing the pellets (a) and the particles (b); (ii) coating at least the pellets (a) with a coating material; (iii) forming a compressible mixture by mixing the pellets (a) and the particles (b); (iv) optionally adding other ingredients to the compressible mixture formed according to step (iii); and (v) compressing the compressible mixture into the tablet form of the multiple unit pellet system.

Description

EXAMPLES

Example 1: Coating with Alginate/Shellac

(1) 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%.

(2) 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

(3) 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

(4) 80 g granulated Riboflavin was coated with 60 g Eudragit FS30D and 10 g PlasACRYL 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%.

(5) 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.