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BR-112019023437-B1 - SOLID PARTICLES, USE AND COMPACTED TABLETS COMPRISING THE SAME

BR112019023437B1BR 112019023437 B1BR112019023437 B1BR 112019023437B1BR-112019023437-B1

Abstract

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

Inventors

  • Jihane Achkar
  • Bernd Schlegel
  • Loni Schweikert
  • OLIVIA BRIGITTE VIDONI

Assignees

  • DSM IP ASSETS B.V

Dates

Publication Date
20260310
Application Date
20180517
Priority Date
20170519

Claims (5)

  1. 1. Solid particles, characterized by comprising: i) 22% to 75% by weight, based on the total weight of the solid particles, of vitamin A and/or its derivatives, ii) 20% to 70% by weight, based on the total weight of the solid particles, of at least one emulsifier, and iii) 5% to 55% by weight, based on the total weight of the solid particles, of at least one non-reducing sugar, wherein the solid particles are free of antioxidants and wherein the at least one emulsifier is not derived from an animal source, wherein the non-reducing sugar is trehalose, wherein the vitamin A derivative is chosen from the group consisting of vitamin A acetate or vitamin A palmitate, and wherein the at least one 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, methylcellulose, hydroxypropylmethylcellulose), lignosulfonate, polysaccharide gums (such as acacia gum (gum arabic), modified acacia gum, TIC gum, linseed gum, ghatti gum, tamarind gum, and arabinogalactan), gelatin (bovine, fish, porcine, poultry), vegetable proteins (such as, for example, peas, soybeans, castor beans, cottonseed, potatoes, sweet potatoes, cassava, rapeseed, sunflowers, sesame, flaxseed, safflower, lentils, oilseeds, wheat, rice, corn, barley, rye, oats, lupin, and sorghum), animal proteins including milk or whey proteins, lecithin, polyglycerol esters of fatty acids, monoglycerides of fatty acids, fatty acid diglycerides, sorbitan ester, and sugar ester (as well as derivatives thereof).
  2. 2. Solid particles, according to claim 1, characterized by comprising: 10% to 50% by weight, based on the total weight of the solid particle, of at least one non-reducing sugar.
  3. 3. Solid particles, according to claim 1 or 2, characterized by comprising 25% to 65% by weight, based on the total weight of the solid particle, of vitamin A and/or its derivatives.
  4. 4. Use, characterized by being of solid particles, as defined in any one of claims 1 to 3, in the production of compacted tablets.
  5. 5. Compacted tablets, characterized by comprising at least one solid particle, as defined in any one of claims 1 to 3.

Description

[0001] This patent application relates to innovative solid particles comprising a high quantity of vitamin A and/or its derivatives (such as vitamin A acetate and vitamin A palmitate) and which do not comprise any antioxidant. The innovative particles are very stable (against oxidation). [0002] Packed tablets are a very useful way to administer fat-soluble vitamins. They are easy to consume, easy to store, and easy to handle. [0003] When compacted tablets are produced, adverse conditions must be applied. Clearly, a certain amount of pressure must be used to compress any formulation into a tablet. Therefore, there is usually a problem: the ingredients that are part of the formulation, which are usually compacted, are squeezed out and therefore no longer form part of the tablet. In other words, the tablet typically contains less fat-soluble vitamin in the compacted tablet than in the formulation that was compacted. Typically, the content of fat-soluble vitamins decreases during the storage of compacted tablets. [0004] Gelatin, which is often used to formulate fat-soluble vitamins, is usually derived from an animal source and is therefore not suitable for vegetarians. [0005] In addition, it is very usual and common to add at least one antioxidant to the solid particle to improve particle stability. [0006] Due to the importance of compressed tablets, comprising vitamin A and/or its derivatives (such as vitamin A acetate and vitamin A palmitate), there is always a need for improved compressible formulations. [0007] Surprisingly, it was found that such an improvement was achieved by adding one or more non-reducing sugars and not adding antioxidants to the solid formulation, which is used to produce compacted tablets. [0008] Therefore, the present invention relates to solid particles (SP) comprising: (i) at least 20 percent by weight (% by weight), 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, [0009] in which the solid particles do not comprise any antioxidant. [0010] Therefore, the present invention relates to solid particles (SP’) comprising: (i) at least 20 percent by weight (% by weight), based on the total weight of the solid particles, of vitamin A acetate and/or vitamin A palmitate, (ii) at least one emulsifier and (iii) at least one non-reducing sugar, [0011] in which the solid particles do not comprise any antioxidant. [0012] These solid particles show better storage stability (of vitamin A and/or its derivatives (such as vitamin A acetate and vitamin A palmitate)) per se also when compacted into tablets. [0013] Antioxidants are a class of preservatives, which includes natural antioxidants (such as ascorbic acid and tocopherols) as well as synthetic antioxidants (such as propyl gallate, tertiary butylhydroquinone, butylated hydroxyanisole, and butylated hydroxytoluene). [0014] It is surprising that even without the use of antioxidants the solid particles are equally stable. [0015] It is also possible to produce solid particles with only these three types of ingredients. [0016] Therefore, the present invention relates to solid particles (SP1) consisting of: (i) at least 22 percent by weight (% by weight), 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. [0017] Therefore, the present invention relates to solid particles (SP1’) consisting of: (i) at least 22 percent by weight (% by weight), based on the total weight of the solid particles, of vitamin A acetate and vitamin A palmitate, (ii) at least one emulsifier and (iii) at least one non-reducing sugar. [0018] Preferred non-reducing sugars are non-reducing disaccharides; most preferred are sucrose and/or trehalose, with maximum preference given to trehalose. [0019] Sucrose is a disaccharide combination of the monosaccharides glucose and fructose with the formula C12H22O11. It is commercially available from many suppliers. [0020] Sucrose is typically extracted and refined from cane or beet sugar for human use. [0021] Trehalose, also known as micose or tremalose, is a natural alpha-linked disaccharide formed by an α,α-1,1-glycoside linkage between two α-glucose units. [0022] There is an industrial process in which trehalose is derived from corn starch. There are known biological pathways for the biosynthesis of trehalose. [0023] Trehalose is commercially available from a variety of suppliers. [0024] The amount of non-reducing sugar in the solid particles is 5 to 55 percent by weight (% by weight), based on the total weight of the solid particles. Preferably 10 to 50 percent by weight, based on the total weight of the solid particles; more preferably 15 to 45 percent by weight, based on the total weight of the solid particles. [0025] Therefore, the present invention relates to solid particles (SP2), which are solid particles (SP), (SP'), (S