Abstract
The present invention relates to a nutraceutical delivery system, particularly for a controlled administration of one or more active nutraceutical ingredients to a body, and further particularly for oral administration of one or more active nutraceutical ingredients to a body. The system may thus comprise a base component soluble in body fluids and also a separate first component. The base component and the separate first component may be soluble in body fluids. The first component may furthermore comprise an effective amount of a first active nutraceutical ingredient.
Claims
1. A nutraceutical delivery system, comprising: a base component soluble in body fluids; and a separate first component soluble in body fluids, wherein the first component comprises a first active nutraceutical ingredient, and the first component is inhomogeneously arranged in the base component.
2. The system according to claim 1, wherein the base component is provided as a three-dimensional body, and wherein the separate first component is inhomogeneously arranged throughout and/or within a portion of the base component.
3. The system according to claim 1, wherein a concentration of the first active nutraceutical ingredient varies throughout or within a portion of the system.
4. The system according to claim 3, wherein the concentration of the first active nutraceutical ingredient is highest at a center, at an edge or at an intermediate region of the system.
5. The system according to claim 3, wherein the concentration of the first active nutraceutical ingredient increases towards or increases away from a center of the nutraceutical delivery system.
6. The system according to claim 3, wherein a concentration profile of the first active nutraceutical ingredient throughout and/or within a portion of the system comprises a smooth transition to an area of increased and/or relatively high concentration and/or the concentration profile of the first active nutraceutical ingredient throughout the system comprises more than one area of increased and/or relatively high concentration.
7. (canceled)
8. The system according to claim 3, wherein the variation of the concentration of the first active nutraceutical ingredient throughout the system is at least 5%.
9. (canceled)
10. The system according to claim 1, wherein the first active nutraceutical ingredient has a concentration profile within the system such that the first nutraceutical ingredient is released from the system at a predetermined release profile comprising a section with a release at a constant rate.
11. The system according to claim 1, wherein the first active nutraceutical ingredient has a concentration profile within the system such that the first nutraceutical ingredient is released from the system at two or more dosages, wherein release of the first active nutraceutical ingredient at one of the dosages starts within 1 second to 24 hours of application of the system, before release of the first active nutraceutical ingredient at another one of the two or more dosages.
12. The system according to claim 1, wherein an exterior surface of the system is free of the first component.
13. The system according to claim 1, further comprising a separate second component soluble in body fluids, said second component comprising a second active nutraceutical ingredient.
14. The system according to claim 13, wherein the second component is inhomogenously arranged in the base component.
15. (canceled)
16. The system according to claim 13, wherein the first component and the second component are arranged in the system such that upon application of the system, release of the first active nutraceutical ingredient starts before release of the second active nutraceutical ingredient.
17. The system according to claim 13, wherein the first component and the second component are arranged in the system such that upon application of the system, a time release characteristic of the first active nutraceutical ingredient differs from a time release characteristic of the second active nutraceutical ingredient.
18. The system according to claim 1, wherein the total amount of the first active nutraceutical ingredient in the system is between 1 g and 100 g.
19. (canceled)
20. (canceled)
21. (canceled)
22. (canceled)
23. The system according to claim 1, further comprising a marking component optically different from the base component, the marking component arranged such that it forms a two-dimensional pattern on a surface of the system and/or is visible from an exterior view of the system.
24. The system according to claim 1, wherein the first component is optically different from the base component and/or in that the first component is arranged such that it forms a two-dimensional pattern on a surface of the system and/or the first component is visible from an exterior view of the system.
25. The system according to claim 23, wherein the two-dimensional pattern is a discontinuous pattern.
26. (canceled)
27. The system according to claim 1, wherein the first active nutraceutical ingredient is selected from vitamins, minerals, herbs, botanicals, amino acids, or dietary substances for use by man to supplement the diet by increasing the total dietary intake.
28. (canceled)
29. (canceled)
30. (canceled)
31. (canceled)
32. A method of using the nutraceutical delivery system of claim 1, comprising applying the nutraceutical delivery system to a body for controlled administration of the first nutraceutical ingredient to the body.
Description
[0081] The present invention will, in the following, be described with reference to the enclosed figures.
[0082] FIGS. 1a to 1i show several designs of nutraceutical delivery systems according preferred embodiments of the present invention;
[0083] FIG. 2a shows a further design of a nutraceutical delivery system according to a further embodiment;
[0084] FIG. 2b shows a concentration profile corresponding to the embodiment in FIG. 2a;
[0085] FIG. 3a shows an active nutraceutical ingredient release profiles of a common nutraceutical delivery system;
[0086] FIGS. 3b to 3c show active nutraceutical ingredient release profiles of nutraceutical delivery systems according to embodiments of the present invention;
[0087] FIGS. 4a to 4d show further designs of nutraceutical delivery systems according to embodiments of the present invention;
[0088] FIGS. 5a to 5d show further designs of nutraceutical delivery systems according to embodiments of the present invention;
[0089] FIG. 6 shows a further design of a nutraceutical delivery system according to an embodiment of the present invention; and
[0090] FIG. 7 shows a structured nutraceutical delivery system according to an embodiment the present invention.
[0091] FIGS. 1a to 1i illustrate a total of nine design options for a nutraceutical delivery systems according to embodiments of the present invention. It may be seen that all the designs in FIGS. 1a to 1i comprise a base component, which may form the overall body of the respective nutraceutical delivery system. The base component may be considered as a matrix. Within said matrix further components may be arranged. These further components are marked as component A, component B, component C, and component D. Each component may comprise an effective amount of a separate active nutraceutical ingredient. Accordingly, any of the components A-D may be considered as a first component within the meaning of the present invention. The base component as well as any one of the components A-D may be soluble in body fluids, such as, for example, in gastric acid or the like.
[0092] The design of nutraceutical delivery system according to the embodiment shown in FIG. 1a may have a round shape. The Nutraceutical delivery system in FIG. 1a may have the form of a tablet, a disc or the like. Such Nutraceutical delivery system may have a particular diameter D. The diameter D may be, for example, 15 mm. Also Nutraceutical delivery systems with other diameters may be provided.
[0093] Within the base component of the nutraceutical delivery system according to the embodiment in FIG. 1a, a first component A with a first active nutraceutical ingredient, a second component B with a second active nutraceutical ingredient and a third component C with a third active nutraceutical ingredient may be provided. It may be comprehended from FIG. 1a that the respective active nutraceutical ingredients are not distributed homogeneously throughout the nutraceutical delivery system. Instead the active nutraceutical ingredients are arranged inhomogeneously within the base component. In particular, the components A, B, C may be provided at particular positions within the nutraceutical delivery system. The components A, B, C may, for example, be provided in a polygonal shape, and preferably with a hexagonal cross section.
[0094] Upon application of nutraceutical delivery system in accordance with the embodiment shown in FIG. 1a, the base component may dissolve first, as the dissolution of the entire system may begin at the edge of the system. After a certain and/or predetermined period of time, component C and then component B may start to dissolve. Thereby the respective active nutraceutical ingredients may be released, particularly in a controlled and/or adjusted manner. Subsequently, component A may start to dissolve. Thereby the respective first active nutraceutical ingredient provided therein may be released. Due to the particular arrangement of the components in the nutraceutical delivery system, the different active nutraceutical ingredients may be released at different stages and/or at different dosages after application of the nutraceutical delivery system. Due to the particular arrangement of the different components within and/or throughout the nutraceutical delivery system according to the embodiment in FIG. 1a, each active nutraceutical ingredient may be released at a particular time after application of the nutraceutical delivery system. Such release may have a particular and/or individual profile. In particular, an active nutraceutical ingredient-specific release profile may be obtained.
[0095] The nutraceutical delivery system in accordance with the embodiment in FIG. 1b may be formed as a tablet. Such a tablet may have a height of, for example, 2.5 mm. Furthermore, such a tablet may have a diameter of 15 mm. The components B and C, each having an active nutraceutical ingredient, may be provided within the base component in an inhomogeneous manner. Upon application of the system according to the embodiment of FIG. 1b, particular release profiles of the active nutraceutical ingredients within components B and C may be obtained. Smooth transitions between phases of increased release may thereby be obtained.
[0096] The nutraceutical delivery system in accordance with the embodiment in FIG. 1c may be similar to that of nutraceutical delivery system in accordance with FIG. 1a, however comprising, beside the base component, merely two components B and C. Components B and C may each comprise an active nutraceutical ingredient. With application of such system, particular release profiles of the active nutraceutical ingredients contained in components B and C may be obtained. Smooth transitions between phases of increased release may be achieved in this manner.
[0097] In the nutraceutical delivery system in accordance with the embodiment in FIG. 1d, two components with active nutraceutical ingredients may be provided in a tube-like shape. Alternatively, the components may be provided in form of stacked plates or the like.
[0098] The nutraceutical delivery system in accordance with the embodiment in FIG. 7e has a design where the components with active nutraceutical ingredients may be provided as spots within or throughout the base component. By applying such system, particular and/or specifically adjusted release profiles of the active nutraceutical ingredients within components B and C may be obtained. Smooth transitions between phases of increased release may be achieved in this manner.
[0099] The nutraceutical delivery system in accordance with the embodiment in FIG. 1f has a design of a particular height H, for example, a height H of 25 mm. Only one component with an active nutraceutical ingredient may be arranged inhomogeneously within the respective base component. The component with the active nutraceutical ingredient may be provided in a tube-like manner, particular by the arrangement of a plurality of tube shaped elements. Alternatively, the component may be provided in form of plates or the like.
[0100] The nutraceutical delivery system in accordance with the embodiment in FIG. 1g may be similar to nutraceutical delivery system in accordance with the embodiment in FIG. 1e, However the components with active nutraceutical ingredients may be arranged in a more random manner. With application of the system, particular release profiles of the active nutraceutical ingredients within components B and C may be obtained. Smooth transitions between phases of increased release may be achieved.
[0101] The nutraceutical delivery system in accordance with the embodiment in FIG. 1h has a design, where the components with the active nutraceutical ingredients may be provided and/or arranged in the form of circles within and/or throughout the base component. By applying such nutraceutical delivery system, the base component and the first component may dissolve in an alternating manner. That is, the first active nutraceutical ingredient may be released intermittently, particularly in a periodic manner. Subsequent to the complete release of the first active nutraceutical ingredient, the second component may start dissolving. Thereby the second active nutraceutical ingredient may be released. It may be comprehended that the circles of component A are not necessarily concentric. The circles may also not have any uniform thickness. A particular and/or specifically adjusted release profile may be obtained due to this particularly inhomogeneous arrangement. Smooth transitions between phases of increased release may be achieved in this manner.
[0102] The nutraceutical delivery system in accordance with the embodiment in FIG. 1i has a design where a component with an active nutraceutical ingredient may be provided in a particular pattern within a matrix of additives. The matrix of additives may be arranged within the base component.
[0103] Each of the embodiments described above with regard to FIGS. 1a to 1i may provide a particular release characteristics with regard to the active nutraceutical ingredient or the plurality of ingredients provided therein, respectively. In accordance with the present invention, it is possible to choose design suitable for a given application, said design having an inhomogeneous arrangement of the active nutraceutical ingredient in the base component, therewith particularly achieving a desired release profile or characteristic.
[0104] FIG. 2a shows a design of a nutraceutical delivery system according to a further embodiment of the present invention. According to this embodiment, the component 10 with the active nutraceutical ingredient and the base component 12 may be arranged on a grid-like structure. Each pixel of the grid-like structure may be defined by the active nutraceutical ingredient component or the base component. It may be comprehended that the two components 10 and 12 are arranged such that the density of pixels provided by the active nutraceutical ingredient component 10 may be higher at a central part or central portion of the nutraceutical delivery system. This may also become apparent from the concentration profile of the active nutraceutical ingredient component 10, as shown in FIG. 2b. Said concentration profile has a peak of high active nutraceutical ingredient concentration at a center of the system. Furthermore, a rather low concentration of the active nutraceutical ingredient is provided at the edges of the system. There may, in turn, be a rather smooth transition from the low concentration of the active nutraceutical ingredient at the edges to the high concentration of the active nutraceutical ingredient at the center. Thus, the transition may be free of any abrupt steps or the like. The release profile of such nutraceutical delivery system upon dissolution of the two components may be adjusted or configured in a desired and/or specifically chosen manner.
[0105] FIG. 3a shows the release profile of a common nutraceutical delivery system comprising a homogeneously distributed active nutraceutical ingredient. FIGS. 3b and 3c show release profiles of a nutraceutical delivery systems according to the present invention. In FIGS. 3a to 3c, the design of the respective nutraceutical delivery system is shown next to the graphs. The nutraceutical delivery systems may be provided in a round shape. More particular, the nutraceutical delivery systems may, for example, be provided in form a tablet dissolving upon oral administration. The respective graphs in FIGS. 3a to 3c each show the release of the respective active nutraceutical ingredient of the respective nutraceutical delivery system over a given period of time.
[0106] According to the graph in FIG. 3a, the respective nutraceutical delivery system is designed in a manner such that the active nutraceutical ingredient is homogeneously distributed throughout the system. This homogeneous distribution may be considered as key feature of common prior art nutraceutical delivery systems. The homogeneous distribution is due to the corresponding manufacturing processes. With application and dissolution of a classical nutraceutical delivery systems, the respective active nutraceutical ingredient may be released. In view of the dissolution characteristics of such homogeneous system and the shape of such a system, a particular and fixed release profile may be obtained. It may be comprehended from the graph in FIG. 3a that the release of the active nutraceutical ingredient increases gradually over time, subsequently reaches a maximum, and then decreases gradually again.
[0107] In view of the inhomogeneous arrangement of the active nutraceutical ingredient in accordance with the present invention, different release profiles may be achieved. The design corresponding with the graph in FIG. 3b is different from that corresponding to the graph in FIG. 3a, specifically concerning the active nutraceutical ingredient being arranged at an edge of the nutraceutical delivery system. Therefore, the homogeneous distribution of the active nutraceutical ingredient, as provided in common systems, may be suspended. The active nutraceutical ingredient may accordingly be inhomogeneously arranged in the system. In this case a high concentration at the edge of the system may be provided. Furthermore, the concentration of the active nutraceutical ingredient may smoothly decrease towards the center of the system. By applying such nutraceutical delivery system corresponding to the graph in FIG. 3b, the release of the active nutraceutical ingredient may be rather high in the beginning and may subsequently decrease in a gradual manner. A high initial release of an active nutraceutical ingredient may be beneficial for certain applications.
[0108] According to the design corresponding with the graph in FIG. 3c, the active nutraceutical ingredient may be accumulated at a central part of the nutraceutical delivery system. In this case, the concentration of the active nutraceutical ingredient may be relatively high or highest at the center of the system. Thus, a gradient of concentration may point from the edge of the system to its center. It may be comprehended from the respective graph in FIG. 3c that the release increases approximately gradually over a prolonged period of time. Accordingly, the maximum release rate may be delayed in time in comparison to a common design with a homogenous distribution of the respective nutraceutical ingredient. The release of the active nutraceutical ingredient can be considered to be more constant for an extended period of time, as compared to a common design. A release profile in accordance with the graph in FIG. 3c may be beneficial for certain applications. FIGS. 4a to 4d show further embodiments of a nutraceutical delivery system according to the present invention. The overall shape of the systems may be that of a round disk, for example, with a diameter of 5-25 mm, preferably 20 mm or 15 mm, and, for example, with a thickness of 0.5-15 mm, preferably 2 mm or 6 mm. The tablets in FIGS. 4a to 4c are depicted with a cut 14 to allow for a view into the tablets and therewith on the arrangement of the components in the tablets.
[0109] The design of nutraceutical delivery system according to the embodiment in FIG. 4a has a first component 16 with a first active nutraceutical ingredient. The first active nutraceutical ingredient may be provided at the central part of the tablet, and furthermore surrounded by a base component 18. The entire tablet may be coated with a coating 20. Said coating 20 may, for example, be a hydrophilic coating. The coating 20 may also provide entericcoated properties, for example. The concentration of the active nutraceutical ingredient within the tablet may be relatively high or highest at the center of the tablet. The concentration profile of the active nutraceutical ingredient may be adjusted in a manner such that a smooth transition from the edge of the tablet towards the center of the tablet is achieved. The transition is indicated by different cross hatches in FIG. 4a.
[0110] The design of nutraceutical delivery system according to the embodiment in FIG. 4b has a first component 22 with a first active nutraceutical ingredient and a second component 24 with a second active nutraceutical ingredient. The components may be provided within a base component 18, as may be comprehended from FIG. 4b. A coating 20 may again be provided. The second component 24 may be arranged in the form or a sphere. A concentration of the second active nutraceutical ingredient may be relatively high or highest on the surface 26 of such sphere. The concentration may furthermore smoothly decrease towards the center of the sphere. The first component 22 may be provided within and/or throughout the sphere formed of the second component 24. By applying the tablet and with dissolution of the components 22 and 24 of the tablet, the second active nutraceutical ingredient may be released prior to the first active nutraceutical ingredient. Both active nutraceutical ingredients may be released within a transition period.
[0111] In the design of nutraceutical delivery system according to the embodiment in FIG. 4c two different active nutraceutical ingredients 28 and 30 may be provided.
[0112] The second active nutraceutical ingredient 30 may be provided at a central part of the tablet. The first active nutraceutical ingredient 28 may be provided around the second active nutraceutical ingredient 30. There may furthermore be provided an interface region 32 between both active nutraceutical ingredients. In this interface region, an overlap of the active nutraceutical ingredients 28 and 30 may be present. Thus, in this interface region 32, both active nutraceutical ingredients 28 and 30 may be arranged. A smooth crossover may thereby be achieved. Finally, also layers 34 may be provided in this embodiment, said layers 34 extending through the system. The layers 34 may be hydrophobic layers. The layers 34 may particular have dissolution resistant and/or dissolution delaying properties, as mentioned above.
[0113] The design of nutraceutical delivery system according to the embodiment in FIG. 4d may be free of any coating. An active nutraceutical ingredient 36 may again be inhomogeneously arranged in the tablet. Thus, areas or regions with different concentrations of the active nutraceutical ingredient may be provided in this embodiment, as indicated with different hatch types in FIG. 4d.
[0114] FIGS. 5a to 5d show further embodiments of a nutraceutical delivery system according to the present invention. The overall shape of the systems shown in FIGS. 5a to 5d may be that of a round disk with a particular thickness. As may be comprehended, the systems may comprise one or more markings. The markings may, in turn, be arranged at least partially on the surface of the tablets. Accordingly, the markings may form a visible and/or two-dimensional pattern on the surface of the tablets. As may be comprehended from FIG. 5, the pattern of the marking may be a discontinuous pattern. Said pattern may also comprise smooth curves and/or sharp edges. The pattern may therefore be arranged in an inhomogeneous manner. The markings may, for example, be formed by a particular marking component. The markings may also be provided by a component with an active nutraceutical ingredient. Nutraceutical delivery systems with such markings may be considered to comprise a particular security feature. That is, with such markings, security features may be created. Such security features may allow authenticating the origin of the nutraceutical delivery system by a user or consumer of the system.
[0115] FIG. 6 shows a further embodiment of a nutraceutical delivery system according to the present invention. The system according to FIG. 6 may be provided in a spherical shape. The system may furthermore be provided with a coating 20, particularly a hydrophobic coating. Such a coating may comprise hydrophilic pores 36. The pores 36 may have sizes in the range of 1 m to 500 m, for example. There may be provided a base component 20 and also three different active nutraceutical ingredients inside the nutraceutical delivery system. The three different active nutraceutical ingredients may be active nutraceutical ingredient A, active nutraceutical ingredient B, and active nutraceutical ingredient C. Active nutraceutical ingredient C may, for example, be provided at a central part of the system with a peripheral pattern. The further two active nutraceutical ingredients A and B may, for example, surround active nutraceutical ingredient C. Active nutraceutical ingredient B may be provided as a hollow sphere and/or with a homogeneous distribution of the respective active nutraceutical ingredient. Further to this, there may be provided an inhomogeneous distribution of active nutraceutical ingredient A, surrounding the active nutraceutical ingredient C. The concentration of active nutraceutical ingredient A may thereby diminish towards an edge of the nutraceutical delivery system shown in FIG. 6. The diminishing concentration of active nutraceutical ingredient A is indicated by different hatch types. The concentration may diminish smoothly towards the edge of the nutraceutical delivery system.
[0116] FIG. 7 shows a cross-section of a nutraceutical delivery system according to an embodiment of the present invention. As may be comprehended, the surface of the nutraceutical delivery system is structured. The structuring may be formed by protrusions and/or recesses. The protrusions and/or recesses may be formed on one side thereof of the system. Thereby the surface may be enlarged or increased, and due to this enlarged and/or increase surface, the dissolution of the nutraceutical delivery system can be enhanced. As a consequence, the release of the active nutraceutical ingredient may be enhanced and/or facilitated. It is possible that the entire surface of the nutraceutical delivery system may be structured in such a manner. It is likewise possible that only one or several parts or portions thereof may be structured in such a manner.
[0117] The nutraceutical delivery system according to the present invention allows to provide a particular inhomogeneous distribution of one or more active nutraceutical ingredients within the system. As a consequence, a desired release of the active nutraceutical ingredient(s) may be achieved. Possibly a prompt release or also a delayed release of an active nutraceutical ingredient may thereby be obtained. It is furthermore possible to release a particular single active nutraceutical ingredient at different dosages over a prolonged period of time. As an example, an intermittent release of an active nutraceutical ingredient may be provided. The release of the respective active nutraceutical ingredient(s) may accordingly occur phases.
[0118] It is likewise possible to obtain a release of different active nutraceutical ingredients in distinct phases with a single nutraceutical delivery system according to the present invention. The system may, for example, be designed in a manner such that a first active nutraceutical ingredient is released before a second active nutraceutical ingredient.
[0119] Possible design options based on the general concept of inhomogeneously arranging of one or more active nutraceutical ingredients in a nutraceutical delivery system are manifold. Accordingly, the examples and embodiments described above or shown in the figures can be combined to obtain further elaborate designs and/or embodiments with release profiles optimized to a particular application.
