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. Process for the production of compressed tablets, wherein coated particles comprising (i) 40 wt-%-95 wt-%, based on the total weight of the coated particle, of a core, comprising at least one active ingredient and (ii) 5 wt-%-60 wt-%, based on the total weight of the coated particle, of a coating system, and said coating system comprises at least one wax and/or at least one fat, are compressed with a pressure of a least 5 kN.

2. Process according to claim 1 wherein a pressure of 5-40 kN is applied.

3. Process according to claim 1 or claim 1, wherein the coating system comprises at least one wax and/or fat, which has a dropping point of from 30 to 85 C., preferably 40 to 70 C.

4. Process according to claim 1, wherein the coating system comprises at least one wax and/or at least one fat chosen 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.

5. Process according to claim 1, wherein the coated particle comprises 50 wt-%-90 wt-%, based on the total weight of the coated particle, of core and 10 wt-%-50 wt-%, based on the total weight of the coated particle, of coating system.

6. Process according to claim 1, wherein the core comprises at least one active ingredient chosen form the group consisting of vitamins, carotenoids, minerals and plant extracts.

7. Process according to claim 6, wherein the core comprises at least one active ingredient chosen form the group consisting of fat-soluble vitamins, such a vitamin A, D, E, and K (as well as derivatives thereof); water-soluble vitamins such as B vitamins and vitamin C; and carotenoids such as -carotene, -carotene, 8-apo--carotenal, 8-apo--carotenoic acid esters, canthaxanthin, astaxanthin, lycopene, lutein, zeaxanthin and crocetin.

8. Process according to claim 6, wherein the core comprises at least one active ingredient chosen form the group consisting of vitamins A, D, E, and K (as well as derivatives of any of these vitamins).

9. Process according to claim 6, wherein the core comprises vitamin A and/or its derivatives.

10. Compressed tablets comprising (i) 0.1-40 wt-%, based on the total weight of the compressed tablets, of the coated particles, which comprise 40 wt-%-95 wt-%, based on the total weight of the coated particle, of a core, comprising at least one active ingredient and 5 wt-%-60 wt-%, based on the total weight of the coated particle, of a coating system, and said coating system comprises at least one wax and/or at least one fat, and (ii) 60-99.9 wt-%, based on the total weight of the compressed tablets, of at least one additional ingredient, excipient and/or auxiliary agent chosen from the group consisting of fillers (such as microcrystalline cellulose), acidity regulators (such as calcium phosphate), anti-adherent (such as magnesium stearate), dyes, flavours and sweeteners.

11. Compressed tablets according to claim 10 comprising coated particles which comprise (i) 40 wt-%-95 wt-%, based on the total weight of the coated particle, of a core, comprising at least one active ingredient chosen from the group consisting of vitamin A, D, E, and K (preferably is vitamin A and/or its derivative), and (ii) 5 wt-%-60 wt-%, based on the total weight of the coated particle, of a coating system which is chosen form the groups 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.

12. Coated particles comprising (i) 40 wt-%-95 wt-%, based on the total weight of the coated particle, of a core, comprising at least one active ingredient chosen from the group consisting of vitamin A, D, E, and K (preferably is vitamin A and/or its derivative), and (ii) 5 wt-%-60 wt-%, based on the total weight of the coated particle, of a coating system which is chosen form the groups 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.

13. Coated particles consisting of (i) 40 wt-%-95 wt-%, based on the total weight of the coated particle, of a core, comprising at least one active ingredient chosen from the group consisting of vitamin A, D, E, and K (preferably is vitamin A and/or its derivative), and (ii) 5 wt-%-60 wt-%, based on the total weight of the coated particle, of a coating system which is chosen form the groups 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.

Description

FIGURES

[0105] FIG. 1: storage stability of the coated particles according to the present invention as well as the storage stability of an uncoated particle.

[0106] 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

[0107] A total of 300 g of particle containing vitamin A acetate having a particle size distribution between 150 m and 600 m 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 m 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.

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

Example 2

[0108] 100 g of powder consisting of 13.52 g of the coated vitamin A acetate particles (potency: 500000 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 84500 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.

[0109] 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

[0110] The following table represents a typical multivitamin/multimineral tablet composition.

[0111] The tablets are made by a tableting machine (Korsch XL 100) in a 229 mm oblong form. The compression force was 17.5 kN.

TABLE-US-00002 TABLE Typical multivitamin/Multimineral tablet composition content Ingredient mg or IU 1 Vitamin A (in the coated form of Example 1) 3000 IU 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