Process for the production of compressed tablets

Abstract

The present patent application relates a process for the production of compressed tablets using specific coated particles, wherein the coating (system) comprises at least one wax and/or at least one fat. Furthermore it relates to compressed (compacted) tablets and as well as to specific coated particles.

Claims

1. A compressed tablet comprising: (a) 0.1-40 wt. %, based on the total weight of the compressed tablet, of a powder composition comprising coated particles compressed at a pressure of 5 kN to 40 kN, wherein each of the coated particles comprises: (a1) 40 wt-%-95 wt-%, based on the total weight of the coated particle, of a core comprising at least one active ingredient selected from the group consisting of fat-soluble vitamins, water-soluble vitamins and carotenoids, and (a2) 5 wt-%-60 wt-%, based on the total weight of the coated particle, of a coating on the core which comprises a coating system comprised of at least one wax and/or at least one fat selected from the group consisting of glycerine monostearate, carnauba wax, candelilla wax, sugarcane wax, palmitic acid, stearic acid, (fully) hydrogenated cottonseed oil, (fully) hydrogenated palm oil, and (fully) hydrogenated rapeseed oil, and (b) 60-99.9 wt. %, based on the total weight of the compressed tablet, of at least one additional ingredient, excipient and/or auxiliary agent selected from the group consisting of fillers, acidity regulators, anti-adherents, dyes, flavours and sweeteners, wherein the compressed tablet exhibits less initial loss after 35 days of the at least one active ingredient from the core as compared to an identical compressed tablet not comprising the coating on the core.

2. The compressed tablet according to claim 1, wherein the coated particles comprise, based on total weight of the coated particle, 50 wt. %-90 wt. % of the core and 10 wt. %-50 wt. % of the coating system.

3. The compressed tablet according to claim 1, wherein the at least one active ingredient in the core is selected from the group consisting of vitamins, carotenoids, minerals and plant extracts.

4. The compressed tablet according to claim 3, wherein the least one active ingredient is selected from the group consisting of fat-soluble vitamins, water-soluble vitamins; and carotenoids.

5. The compressed tablet according to claim 3, wherein the at least one active ingredient is selected chosen form the group consisting of vitamins A, D, E and K and derivatives thereof.

6. The compressed tablet according to claim 3, wherein the active ingredient core comprises vitamin A.

7. The compressed tablet according to claim 3, wherein the at least one active ingredient is a water-soluble vitamin selected from the group of consisting of B vitamins and vitamin C.

8. The compressed tablet according to claim 3, wherein the at least one active ingredient is a carotenoid selected from the group consisting of α-carotene, β-carotene, 8′-apo-β-carotenal, 8′-apo-β-carotenoic acid esters, canthaxanthin, astaxanthin, lycopene, lutein, zeaxanthin and crocetin.

9. A compressed tablet comprised of a plurality of coated particles compressed at a pressure of 5 kN to 40 kN, wherein each of the coated particles comprise: (i) 40 wt. %-95 wt. %, based on the total weight of the coated particle, of a core which comprises at least one active ingredient selected from the group consisting of vitamins A, D, E, and K, and (ii) 5 wt. %-60 wt. %, based on the total weight of the coated particle, of a coating system present as a coating on the core, wherein the coating system is includes at least one one wax and/or at least one fat selected from the group consisting of glycerine monostearate, carnauba wax, candelilla wax, sugarcane wax, palmitic acid, stearic acid, at least partially hydrogenated cottonseed oil, at least partially hydrogenated palm oil and at least partially hydrogenated rapeseed oil, wherein the compressed tablet exhibits less initial loss after 35 days of the at least one active ingredient from the core as compared to an identical compressed tablet not comprising the coating on the core.

10. A powder composition comprised of coated particles, wherein the coated particles consist of: (i) 40 wt. %-95 wt. %, based on the total weight of the coated particle, of a core which comprises at least one active ingredient selected from the group consisting of vitamins A, D, E, and K, and (ii) 5 wt. %-60 wt. %, based on the total weight of the coated particle, of a coating system present as a coating on the core, wherein the coating system is includes at least one one wax and/or at least one fat selected from the group consisting of glycerine monostearate, carnauba wax, candelilla wax, sugarcane wax, palmitic acid, stearic acid, at least partially hydrogenated cottonseed oil, at least partially hydrogenated palm oil and at least partially hydrogenated rapeseed oil, wherein a compressed tablet of the powder composition compressed at 5 kN to 40 kN exhibits less initial loss after 35 days of the at least one active ingredient from the core as compared to an identical compressed tablet not comprising the coating on the core.

Description

FIGURES

(1) FIG. 1: storage stability of the coated particles according to the present invention as well as the storage stability of an uncoated particle.

(2) The invention is illustrated by the following Example. All temperatures are given in ° C. and all parts and percentages are related to the weight.

EXAMPLES

Example 1

(3) A total of 300 g of particle containing vitamin A acetate having a particle size distribution between 150 μm and 600 μm were coated on a fluidized bed coating using bottom spray set up. The cores were introduced into the reactor at room temperature and conditioned at the desired temperature before spraying the wax material. Carnauba wax (128.6 g) was molten beforehand at 95° C. and sprayed at a rate of about 3 g.Math.min.sup.−1. The entire process was concluded after approximately 50 min. Then the product was cooled down to RT in the reactor and the collected product was sieved to isolate the fraction between 160 to 500 μm in size. The use of sugarcane wax led to an end product containing large quantity of agglomerates. In the case of microcrystalline wax, the product became too sticky to be processed to the end. The same procedure was followed for the fully hydrogenated palm oil (palm oil FH); in this case the material was also molten at 95° C.

(4) TABLE-US-00001 Carnauba wax Sugarcane wax Palm oil FH % % %   <160 μm 0.1 0.3 0.1 160-500 μm 84.4 54.9 98.7   >500 μm 15.5 44.8 1.2 Total 100 100 100

Example 2

(5) 100 g of powder consisting of 13.52 g of the coated vitamin A acetate particles (potency: 500′000 IU/g), 33.24 g microcrystalline cellulose, 49.86 g calcium phosphate and 0.2 g of magnesium stearate was mixed during 10 min. The amount of product form to be added to the mixture was calculated to get a tablet with 84′500 IU/g of vitamin A acetate. 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 1, 7 and 35 days of storage.

(6) The initial loss of the coated particles according to the present invention is far lower than those of the prior art particles. This can be seen in FIG. 1, where all values are listed.

Example 3

(7) The following table represents a typical multivitamin/multimineral tablet composition.

(8) The tablets are made by tableting machine (Korsch XL 100) in a 22×9 mm oblong form. The compression force was 17.5 kN.

(9) TABLE-US-00002 TABLE Typical multivitamin/Multimineral tablet composition content Ingredient mg or IU  1 Vitamin A (in the coated form of 3000 IU Example 1)  2 Beta Carotene 2000 IU  3 Zeaxanthin   1.0  4 Vitamin D.sub.3  400 IU  5 Vitamin C  60.0  6 Vitamin E  30 IU  7 Vitamin B.sub.1 (Thiamine)   1.5  8 Vitamin B.sub.2   1.7  9 Vitamin B.sub.3 (Niacinamide)  20.0 10 Vitamin B.sub.5 (Pantothenic Acid)  10.0 11 Vitamin B.sub.6 (Pyridoxol)   2.0 12 Vitamin B.sub.8 (Biotin)   0.03 13 Vitamin B.sub.9 (Folic Acid)   0.4 14 Vitamin B.sub.12   0.006 15 Vitamin K.sub.1   0.025 16 Iron  18.0 17 Copper   2.0 18 Manganese   2.0 19 Zinc  15.0 20 Iodine   0.15 21 Chrome   0.06 22 Selenium   0.05 23 Molybdene   0.075 24 Potassium Chloride  40.0 25 Magnesium  100.0 26 Calcium and Phosphorus  162.0 27 Crospovidone NF   7.0 28 Silicium   2.00 29 Stearic Acid.sup.5   4.0 30 Magnesium Stearate.sup.6   4.0 31 Cellulose, microcryst.  346.85