Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Reexamination Certificate
2001-03-20
2003-01-21
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
C424S401000, C424S456000, C424S464000, C424S489000
Reexamination Certificate
active
06509029
ABSTRACT:
The invention relates to carotenoid formulations comprising a mixture of &bgr;-carotene, lycopene and lutein.
Carotenoids form a group of pigments which have a yellow or red color, are widespread in nature and confer the characteristic colors on many foodstuffs.
Epidemiological studies have moreover shown that frequent and regular consumption of carotenoid-containing fruit and vegetables reduces the risk of chronic disorders, including cardiovascular disorders, and has a beneficial effect on cancer prevention.
This protective function of the carotenoids is seen both in their action as antioxidants and, as in the case of &bgr;-carotene, in their provitamin A activity.
There is particular interest in this connection in the three carotenoids &bgr;-carotene, lycopene and lutein, which occur widely in foodstuffs such as, for example, tomatoes, carrots, spinach, paprika and broccoli [see Journal of the American Dietetic Association, 97(9), 991-996 (1997)]. In particular, the mixture of these three carotenoids represents a system with particular antioxidant properties.
This is why nutritionists recommend additional, preventive intake of antioxidant vitamins and carotenoids. The food and drugs market therefore offers consumers a large number of such “cytoprotective products”.
Formulations for food products or food supplements which specifically comprise a combination of &bgr;-carotene, lycopene and lutein in high concentrations and high purity have, however, not been disclosed to date.
Thus, lycopene is obtainable, for example, under the name Lyc-O-Mato® (from LycoRed, Israel) as a 6% strength oily dispersion. According to WO 97/48287 it is extracted as natural carotenoid from tomatoes. Because of the high phospholipid content in Lyc-O-Mato®, together with a high viscosity of the oily dispersion, the use properties of this formulation are not always satisfactory. In particular, the use of Lyc-O-Mato® is unsatisfactory for producing high-concentration carotenoid-containing gelatin capsules.
U.S. Pat. No. 5,382,714 and U.S. Pat. No. 5,648,564 describe processes for isolating lutein from the oily extract from marigolds, and the use of the lutein obtained in this way as food color and as antioxidant in cancer prophylaxis. These patents provide no pointers to combinations of &bgr;-carotene, lycopene and lutein.
It is an object of the present invention to provide stable formulations of a ternary combination of carotenoids consisting of &bgr;-carotene, lycopene and lutein which do not have the abovementioned prior art disadvantages.
We have found that this object is achieved by carotenoid formulations comprising a mixture of &bgr;-carotene, lycopene and lutein.
The term “carotenoid formulations” means for the purpose of this invention both solutions, solubilizates and dispersions, such as emulsions and suspensions, and dry carotenoid powders produced therefrom. Preferred formulations are dispersions, such as emulsions and suspensions, in particular oil-containing suspensions.
The ratio of the amounts of the carotenoids present in the mixture is 1 part of &bgr;-carotene, 0.05 to 20 parts of lycopene and 0.05 to 20 parts of lutein, preferably 1 part of &bgr;-carotene, 0.1 to 5 parts of lycopene and 0.1 to 5 parts of lutein, particularly preferably 1 part of &bgr;-carotene, 0.2 to 2 parts of lycopene and 0.1 to 2 parts of lutein, very particularly preferably 1 part of &bgr;-carotene, 0.3 to 1.2 parts of lycopene and 0.1 to 0.5 part of lutein.
The content of &bgr;-carotene, lycopene and lutein in the form of the combination according to the invention in the formulations is generally between 0.1 and 40% by weight, preferably between 5 and 35% by weight, particularly preferably between 10 and 33% by weight, very particularly preferably between 15 and 32% by weight, based on the total amount of the formulation.
The carotenoid formulations are further distinguished by having a phosphorus content of less than 2.0% by weight, advantageously less than 1.0% by weight, preferably less than 0.5% by weight, particularly preferably less than 0.1% by weight, very particularly preferably less than 0.02% by weight, based on the total amount of the mixture of &bgr;-carotene, lycopene and lutein.
The low phosphorus content is at the same time associated with a low content of phospholipids, which improves the use properties of the formulations, such as, for example, the flowability of oil-containing dispersions, especially at low temperatures. The dispersants according to the invention have such a low viscosity even at temperatures between 5° C. and 40° C. that it is possible to dispense with heating the carotenoid dispersion (to reduce the viscosity) during further processing, e.g. during filling into gelatin capsules. This means that it is possible to avoid unwanted losses of activity through chemical or thermal breakdown of the carotenoids.
The carotenoids used to produce the formulations are preferably employed in the form of their crystals with a purity exceeding 75%, preferably exceeding 90%, particularly preferably exceeding 95%, very particularly preferably exceeding 98%. It is moreover possible to employ &bgr;-carotene, lycopene and lutein from natural sources as well as, preferably, synthetically prepared carotenoids, in particular synthetically prepared &bgr;-carotene and lycopene. Thus, for example, the &bgr;-carotene or lycopene used can be obtained by one of the processes disclosed in EP-A-382067 or EP-A-000140.
Besides the abovementioned mixture of &bgr;-carotene, lycopene and lutein, the carotenoid formulations according to the invention can contain at least one other active substance in concentrations of 0.01 to 40% by weight, preferably 0.1 to 30% by weight, particularly preferably in concentrations of 0.5 to 20% by weight.
Possible examples of these active substances are the following:
Other carotenoids such as for example bixin, zeaxanthin, cryptoxanthin, citranaxanthin, canthaxanthin, &bgr;-apo-4-carotenal, 8-apo-8-carotenal, &bgr;-apo-8-carotenoic esters, astaxanthin, singly or as mixture.
Vitamins, e.g. vitamin A, vitamin A acetate, vitamin A palmitate, riboflavin, vitamin B
12
, ascorbic acid, ascorbyl palmitate, nicotinic acid, nicotinamide, pyridoxine hydrochloride, vitamin D
3
, tocopherol, tocopherol acetate, tocopherol palmitate, tocotrienol, vitamin K, thiamine, calcium pantothenate, biotin, lipoic acid, folic acid, folic acid derivatives such as tetrahydrofolic acid, 5-methyltetrahydrofolic acid, 10-formyltetrahydrofolic acid or 5-formyltetrahydrofolic acid.
Compounds with vitamin or coenzyme characteristics, e.g. choline chloride, carnitine, taurine, creatine, ubiquinones, S-methylmethionine, S-adenosylmethionine.
Polyunsaturated fatty acids, e.g. linoleic acid, linolenic acid, arachidonic acid, eicosapentaenoic acid, docosahexaenoic acid.
Garlic constituents, e.g. diallyl thiosulfinate, S-allylcysteine sulfoxide, vinyldithiines, ajoene.
Allithiamines such as benfotiamine, fursultiamine, octotiamine or bentiamine.
Glutathione and its esters such as, for example GSH monomethyl ester, GSH dimethyl ester, GSH monoethyl ester, GSH diethyl ester.
Depending on the nature of the formulation, it may contain, besides the carotenoids, at least one other ancillary substance or additive such as, for example, oils, protective colloids, plasticizers, antioxidants and/or emulsifiers.
In the case of a dispersion, especially in the case of a suspension or an emulsion, it is advantageous to use in addition a physiologically acceptable oil such as, for example, sesame oil, corn oil, cottonseed oil, soybean oil or peanut oil, esters of medium chain-lengths vegetable fatty acids and, in addition, fish oils such as, for example, mackerel, sprat or salmon oil.
Examples of protective colloids used are gelatin, fish gelatin, starch, dextrin, plant proteins, pectin, gum arabics, casein, caseinate or mixtures thereof. However, it is also possible to employ polyvinyl alcohol, polyvinylpyrrolidone, methylcellulose, carboxymethylcellulose, hydroxypropylcellulose and alginates. For further details, re
Holm-Hansen Jan
Michelsen Birgit
Runge Frank
BASF - Aktiengesellschaft
Keil & Weinkauf
Page Thurman K.
Tran S.
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