Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules
Reexamination Certificate
2000-05-04
2002-06-11
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Capsules
C424S457000, C424S456000, C424S451000
Reexamination Certificate
active
06403119
ABSTRACT:
FIELD OF THE INVENTION
This application relates to an encapsulated vitamin composition, and is particularly applicable to a vitamin composition encapsulated in a soft gelatin capsule.
BACKGROUND OF THE INVENTION
Soft and hard shell capsules are widely used within the pharmaceutical and health food industry and have gained an acceptance as they present pharmaceutical and health products in a form that is readily consumed and digested by a user. These capsules are generally made up of a shell and an active filling material. The shell is formed of readily digested materials, for example a soft gelatin capsule may comprise a mixture of gelatin, glycerol and water. Hard shell capsules generally comprise gelatin and water. Generally soft and hard shell capsules are suitable for encapsulating a wide range of pharmaceutical and health products in the form of a suspension.
Water soluble vitamins such as the B group vitamins, and Ascorbic Acid are generally presented in the form of a suspension in edible oil when encapsulated in a soft gelatin or hard shell capsule. Oils such as Soya Bean Oil are generally used. The vitamins may be used on their own as the active ingredient, or in combination with herbal materials such as Bioflavanoids, Rutin etc; or with other vitamins. Ascorbic Acid for example, may be combined with other vitamins such as B groups, Betacarotene, Vitamin D and Vitamin E etc; or with minerals such as trace elements of iron, calcium, magnesium and zinc etc. Soft gelatin capsules containing vitamins such as Ascorbic Acid are used for a number of therapeutic and complementary medicine purposes, for example as a component in anti-oxidant therapy in conjunction with Betacarotene and Vitamin E.
Ascorbic Acid has been formulated in a soft gelatin capsule for some time. Generally, when such capsules are presented in the market place they are prepared with opaque shell coloring. Ascorbic Acid and other water-soluble vitamins, such as the B group vitamins, however have a finite solubility in the shell and can migrate from the filling material to the shell if not completely insolubilised. Over time, the water soluble vitamin in the shell may oxidise or may react with the shell causing the shell to darken. The amount needed to cause this darkening can be quite small. The darkening will not effect the overall assay of the capsule, however it can become unsightly. For this reason, generally dark, opaque shells are used to encapsulate Ascorbic Acid and B group vitamin compositions to hide the darkening of the shell. The darkening precludes the use of light colours such as citrus colours for the shell, such as yellow, orange or lime coloring.
SUMMARY OF THE INVENTION
The present invention overcomes, resists or at least alleviates one or more of the difficulties associated with the discoloration of vitamin-containing capsules.
Applicants have found that water soluble vitamin particles, such as Ascorbic Acid particle, that were coated with a material that did not dissolve in both the fill liquid excipients (such as oil based solutions or other encapsulatable liquid based systems) and the shell of the soft or hard shell capsule, but were still able to dissolve from the vitamin particle in the gastrointestinal tract, overcame the disadvantages of discoloration of the shell. Ascorbic Acid particles that are available for use in tablet form can be coated, but have a much larger particle size than what would be suitable for use as a filling material for a soft gelatin or hard shell capsule.
Accordingly, in a first aspect, the present invention resides in a vitamin composition encapsulated in a soft or hard shell capsule, said vitamin composition comprising water soluble vitamin particles suspended in a fill liquid, wherein;
said water soluble vitamin particles are coated with a material that is substantially insoluble in the fill liquid and the shell of the capsule, but soluble in the gastrointestinal tract of a mammal, and
the coated water soluble vitamin particles are of a size that are suitable for encapsulating as a suspension in said capsule; wherein said composition and capsule resist discoloration.
The present invention also resides in a process for manufacturing a soft or hard shell capsule containing a coated vitamin composition and which resists discoloration, including the steps of:
(i) providing water soluble vitamin particles which have been coated with a material that is insoluble in a fill liquid and the shell of a soft or hard shell capsule, but soluble in the gastrointestinal tract of a mammal, wherein the coated water soluble vitamin particles are of a size that are suitable for encapsulating as a suspension in the capsule;
(ii) suspending the coated vitamin particles in a compatible fill liquid; and
(iii) encapsulating the vitamin composition in a soft or hard shell capsule to produce the vitamin composition as hereinbefore described.
DETAILED DESCRIPTION OF THE INVENTION
Most preferably the capsule is a soft gelatin capsule comprising gelatin, a suitable polyol and water. The suitable polyol is preferably glycerol. Although soft gelatin capsules are preferred, the advantages of the invention are applicable to other soft shell capsules and hard shell capsules, and compositions encapsulated in hard shell capsules also form part of the invention.
Water soluble vitamins that have found to be suitable for use in this invention are the B group vitamins namely Thiamine, Riboflavin, Folic Acid, Biotin, Nicotinic Acid, Pantothenic Acid, Pyridoxine, Cyanocobalamine and Lipoic Acid and Vitamin C, namely Ascorbic Acid. The invention has been found to be particularly applicable for use with Ascorbic Acid.
The fill liquids of the invention may be any liquid based system that is encapsulatable in a soft or hard shell capsule. The coating material may be either hydrophobic or hydrophilic in nature. The selection of the fill liquid for encapsulation will depend upon the nature of the coating material used. For example, if the coating material is hydrophobic, a hydrophilic fill liquid, such as Macrogol 400 will preferably be used. If the coating material is hydrophilic, a hydrophobic fill liquid will preferably be used, such as Soya Bean Oil. This will ensure that the coating material will be insoluble in the fill liquid.
Preferred hydrophobic fill liquids include vegetable oil, vegetable oil derivatives or medium chain triglycerides or mixtures thereof. Suitable vegetable oils include Almond Oil; Arachis Oil; Borage Oil; Canola Oil; Evening Primrose Oil; Fractionated Coconut Oil; Lecithin; Linseed Oil; Maize Oil; Olive Oil; Rapeseed Oil; Rice Bran Oil; Safflower Oil; Soya Bean Oil; Spearmint Oil; Sunflower Oil or Wheatgerm Oil.
Preferred hydrophilic fill liquids include polyethylene glycols having a molecular weight of from 300 to 8,000 or mixtures of polyethylene glycol with other polyols. Most preferred hydrophilic fill liquids include Macrogol 400 and mixtures of Macrogol 400 and propylene glycol and/or glycerol.
The coating material may comprise any material having the requisite properties of insolubility in the fill liquid and the shell of the capsule, whilst being able to disassociate from the particle in the gastrointestinal tract.
The selection of the fill liquid is determined by the solubility of coating material in the fill liquid. Whereas this is largely determined by the hydrophobic/hydrophilic nature of the fill liquid, it has been found that some hydrophobic coating materials remain insoluble in hydrophobic fill liquids. For example, some hydrogenated vegetable oils remain insoluble in a hydrophobic fill liquid such as Soya Bean Oil. Similarly some hydrophilic coating materials will remain insoluble in polyethylene glycol fill liquids.
Whereas it is preferred to select the fill liquid by its hydrophobic/hydrophilic nature, the selection of the fill liquid is determined by the solubility of the coating material in the fill liquid.
Suitable hydrophilic coating materials include glycols and polyglycols having a molecular weight of from 1000-8000. Preferred hydrophilic coating m
Oppenheim Richard Charles
Truong Hung Cam
Bennett Rachel M.
Nickey Donald O.
Page Thurman K.
R. P. Scherer Technologies, Inc.
Rozycki Andrew G.
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