SOLID PARTICLES

Abstract

The present patent application relates to solid particles comprising vitamin A and/or its derivatives, which are more stable when compressed into tablets.

Claims

1. Solid particles comprising (i) at least 20 wt-%, based on the total weight of the solid particles, of vitamin A and/or its derivatives, (ii) at least one emulsifier, and (iii) at least one non-reducing sugar, wherein the solid particles do not comprise any antioxidants.

2. Solid particles according to claim 1 comprising 5-55 weight-% (wt-%), based on the total weight of the solid particle, of at least one non-reducing sugar (preferably trehalose).

3. Solid particles according to claim 1 comprising 10-50 weight-% (wt-%), based on the total weight of the solid particle, of at least one non-reducing sugar.

4. Solid particles according to claim 1, wherein the vitamin a derivative is chosen from the group consisting of vitamin A acetate or vitamin A palmitate.

5. Solid particles according to claim 1 comprising 22-75 wt-%, based on the total weight of the solid particle, of vitamin A and/or its derivatives.

6. Solid particles according to claim 1 comprising 25-65 wt-%, based on the total weight of the solid particle, of vitamin A and/or its derivatives.

7. Solid particles according to claim 1 comprising 20-70 wt-%, based on the total weight of the solid particles, of at least one emulsifier.

8. Solid particles according to claim 1, wherein the at least emulsifier is chosen from the group consisting of modified (food) starches, ascorbyl palmitate, pectin, alginate, carrageenan, furcellaran, dextrin derivatives, celluloses and cellulose derivatives (e.g. cellulose acetate, methyl cellulose, hydroxypropyl methyl cellulose), lignosulfonate, polysaccharide gums (such as gum acacia (=gum arabic), modified gum acacia, TIC gum, flaxseed gum, ghatti gum, tamarind gum and arabinogalactan), gelatine (bovine, fish, pork, poultry), plant proteins (such as are for example peas, soybeans, castor beans, cotton, potatoes, sweet potatoes, manioc, rapeseed, sunflowers, sesame, linseed, safflower, lentils, nuts, wheat, rice, maize, barley, rye, oats, lupin and sorghum), animal proteins including milk or whey proteins, lecithin, polyglycerol ester of fatty acids, monoglycerides of fatty acids, diglycerides of fatty acids, sorbitan ester, and sugar ester (as well as derivatives thereof).

9. Use of the solid particles according claim 1 in the production of compressed tablets.

10. Compressed tablets comprising at least one solid particle according to claim 1.

Description

EXAMPLES

Example 1

[0081] 370.6 g of deionized water were heated up to 60 C.-65 C. in a vessel. 324.00 g of food modified starch and 121.2 g of trehalose were added and the mixture was brought into solution while stirring at 60-65 C. The obtained solution was cooled to 50-55 C. and degassed for 1 hour. Thereupon, 188.78 g vitamin A acetate) were added to the matrix system and emulsified. The temperature of the process was always kept below 65 C. After emulsification the inner phase of the emulsion had an average particle size of about 272 nm (Dv(0.1)=100 nm, Dv(0.5)=272 nm, Dv(0.9)=559 nm), measurement realized by laser diffraction (Malvern 3000). After emulsification the moisture of the emulsion, determined by a halogen moisture analyzer (Mettler Toledo, Type HR73-P), was checked and adapted if necessary. Afterwards 150 g of the emulsion were sprayed into a spray pan containing 1500 g of corn starch using a rotating spray nozzle. The obtained particles were sieved off (150 to 600 m) from the excess of corn starch and dried at room temperature using a stream off air. The final product particle size after drying was in average 246 m (Dv(0.1)=198 m, Dv(0.5)=246 m, Dv(0.9)=303 m) measured by laser diffraction (Malvern 3000).

[0082] Solid particles with the composition as listed in the table 1 have been obtained.

TABLE-US-00001 TABLE 1 The solid particle according to the present invention Ingredient Amount [wt %] Vitamin A Acetate (2.8 Mio I.U/g) 27.00 Food modified starch 48.39 Trehalose 18.61 Corn Starch 4.00 Water 2.00

Example 2: Composition with an Antioxidant (Comparison Example)

[0083] The same procedure as described hereinbefore was followed using 190.82 g of an oil mixture (188.78 g vitamin A acetate, 1.04 g BHT) and using less modified food starch (316.75 g))

TABLE-US-00002 TABLE 2 The solid particle comprising an antioxidant (BHT) Ingredient Amount [wt %] Vitamin A Acetate (2.8 Mio I.U/g) 27.00 BHT 1.5 Food modified starch 47.31 Trehalose 18.19 Corn Starch 4.00 Water 2.00

Example 3

[0084] This example was done in analogy to example 1, but sucrose was used instead of trehalose.

Example 4 (Comparison Example)

[0085] This example was done in analogy to example 2, but sucrose was used instead of trehalose.

[0086] All solid particles (from Example 1, 2 3 and 4) were tested. The results are summarised in the following tables.

TABLE-US-00003 TABLE 3 Per se stability of the solid particles (stored for 12 months) Solid Content of Vitamin A acetate Content of Vitamin A particles stored at 25 C. [%] acetate stored at 30 C. [%] Exp. 1 90 82 Exp. 2 90 83 Exp. 3 90 81 Exp. 4 84 81

Example 5: Stability in Stress Tablets

[0087] 100 g of powder consisting of 27 g of vitamin A acetate particles (as obtained in Example 1 and 2), 33.24 g microcrystalline cellulose, 49.86 g calcium phosphate and 0.2 g of magnesium stearate was mixed during 10 min. This end preparation was then compressed with a pressure of 35 KN. The tablets (common disk-shaped; 0.2 g) were stored at room temperature in a closed brown-glass bottle and the vitamin A acetate content determined after 24 months of storage.

[0088] It was found that after that period of storage time, surprisingly the amount of Vitamin A acetate was for both tablets at 64%. It could be seen that the solid particles without antioxidant are as stable as the ones with an antioxidant.