HK1074793A1 - Daily melatonin dosing units - Google Patents

Abstract

The invention relates to a composition containing a combination of melatonin , ginkgo biloba, and biotin as active substances. Said composition is particularly suitable for producing formulations used for topical application in hair.

Description

The present invention relates to a single-use container for a medicinal product or cosmetic product for topical application containing a single dose of melatonin or a melatonin derivative equivalent to a locally effective dose but not producing a systemic effect.

Melatonin-containing products can be used for a variety of medical and cosmetic purposes.

EP 0 867 181 A1 reveals a nasal formula containing melatonin and a selected additive of glycerin, cyclodextrin or mixtures thereof, used for induction of sleep.

US 6.281.241 B1 concerns the use of melatonin and melatonin-containing compounds for the treatment of female androgenetic alopecia. The compound is supplied in light-protected aluminium bottles containing 33 ml of 0.1% melatonin solution in an ethanol/water mixture.

US 4.746.674 describes a procedure for topical treatment of the skin and/or scalp which involves the administration of a melatonin-containing compound, with melatonin in a range of 10-4 to about 1% by weight.

US 5,985,293 concerns a topical cosmetic composition to improve or maintain the appearance of the skin and/or scalp, containing melatonin or a melatonin analogue in a quantity of less than 10-4% by weight of the total weight of the composition.

EP 0 150 751 A1 reveals a disposable topical application container for a preparation comprising a body of container with flat, transverse and opposite flange-like parts and an axially extending neck, the neck having a point of attachment for the delivery of the preparation contained in the disposable container.

GB 2 079 238 A concerns a dispenser or container for the topical application of a medicinal product, which is made of plastic and contains a single dose of, for example, 0.5 to 5.0 g of the medicinal product.

AT 367 634 B reveals a multipack consisting of individual containers for liquids and/or solids, closed on all sides, arranged side by side and connected in a plane, each container being connected on a narrow side by a step in or parallel to the container plane, the cross-section of which is rejuvenated at the points of connection with the containers.

DE 200 19 365 U1 discloses disposable containers for the reception of liquid or gel-like pharmaceutical preparations containing a single dose of the pharmaceutical preparation and comprising a formwork, a rotatable and/or detachable and/or breakable closure cap and a flag at the bottom of the formwork for the application of imprints and/or labels.

The present invention relates to a disposable container for a medicinal product or cosmetic product for topical application containing a single dose of melatonin or a melatonin derivative equivalent to a locally effective dose but not producing a systemic effect, the single dose being 0.01 to 0.2 mg of melatonin or melatonin derivative and the single dose being a daily dose.

The single-use container according to the invention allows the application of a dose of melatonin or a melatonin derivative that is locally effective but does not cause an undesirable change in normal melatonin plasma levels.

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The single dose according to the invention is a dose which provides a positive cosmetic and/or therapeutic effect without significant changes in plasma levels. The single dose according to the invention is approximately 0.01 to approximately 0.2 mg melatonin. The single dose corresponds to a daily dose, preferably a daily dose to be administered in the evening.

The product or cosmetic product is preferably in liquid formulation. For topical application of the product, solutions, suspensions, emulsions, microemulsions, nano-systems, creams, gels, lotions, sprays, foams or ointments, and any other formulation that can be applied topically, are suitable.

The medicinal product or cosmetic contained in the disposable container of the invention may have different concentrations of melatonin or a melatonin derivative depending on its intended use, preferably containing a concentration of about 0.001 to about 0.01 % (w), more preferably about 0.003 to 0.004% (w) of melatonin or a melatonin derivative, and a particularly preferred concentration of about 0.0033 % (w).

In one embodiment, the therapeutic or cosmetic product contains melatonin or a melatonin derivative as the only active substance, but may also contain one or more additional active substances, such as vitamin A, vitamin A acid or other vitamin A derivatives, biotin and/or gingko biloba.

In a preferred embodiment, the medicinal product or cosmetic product contains a combination of the active substances melatonin or a derivative of melatonin with biotin and/or gingko biloba. The active substances in this embodiment may be available in different dosages. A particularly preferred dosage of this combination is from about 0.05 to about 0.2 mg, particularly preferably about 0.1 mg of melatonin or a derivative of melatonin, from about 0.2 to about 0.4 mg, particularly preferably about 0.3 mg of biotin, and from about 1.3 to 1.7 mg, particularly preferably about 1.5 mg of gingko biloba.

In another preferred embodiment, the product contains a combination of the active substances melatonin or a melatonin derivative and vitamin A, vitamin A acid or another vitamin A derivative. In this preferred combination, the dosage of melatonin or melatonin derivative is preferably around 0,05 to 0,2 mg, and preferably around 0,1 mg melatonin.

In addition, the medicinal product or cosmetic product may contain one or more cosmetic and/or pharmaceutical excipients or additives, such as thickeners, minerals or fragrances.

The composition of the invention may be used to promote hair growth, in particular for the prevention and/or treatment of alopecia in men or women, and the indications of particular preference are androgenetic alopecia of the male type, androgenetic alopecia of the female type, diffuse alopecia of the male type and diffuse alopecia of the female type.

The disposable container of the invention may contain different volumes of the medicinal product or cosmetic product, depending on the intended application or use. In a preferred embodiment, the disposable container contains approximately 2,5 to 3,5 ml, preferably 2,9 to 3,2 ml of the product. A particularly preferred volume is approximately 3,0 ml.

The therapeutic or cosmetic product can be packaged by any suitable method known to the state of the art, preferably under GMP conditions, to ensure that the product is sterile and that no problems arise, such as bacterial contamination, when the product is applied.

The container of the invention can be made of virtually any material, in particular a material approved for the packaging of foodstuffs and pharmaceutical products. Preferred materials are, for example, plastics or mixtures of plastics. Particularly suitable plastics are, for example, polyethylene, polyvinyl chloride, polystyrene, polypropylene, polycycloolefins or mixtures or copolymers thereof, with particular preference being polyethylene or polycycloolefins.

The disposable container may be transparent, opaque, colourless or coloured, depending on the desired optical appearance. For example, any colourants may be added to the plastic to obtain a coloured container. A non-transparent container is preferably used if the product contains photosensitive substances, as a non-transparent container can also provide protection from light.

The container of the invention may be of virtually any shape; examples of preferred containers are shown in Figures 1 and 2. preferably, a suitable container shall consist of a part containing the product and a single-use closure connected to the bottom by a breakpoint.

The advantage of using the container is that it has a one-way lock on its head that can be opened by turning, which makes it easy to open. In addition, the container can only be released after opening by applying pressure. This pressure can be applied, for example, when applying by hand. This property allows the user to place the product in a targeted manner and to administer the product well. When applying the product to the scalp or hair, the opened container can be carried directly through the hair like a comb. This allows easy and safe handling of the container and proper dosing of the product.

Depending on the purpose, the disposable container shall be marked and/or labelled by stamping or printing.

Two or more single-use containers may still be connected separately, preferably 5 or 10 containers connected together to form an arrangement, and one or more containers may be packed, preferably in a light-tight package, especially preferably in an aluminium bag.

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Packaging, especially light-tight packaging, allows storage for a longer period without loss of efficacy and may also provide protection against gas loss.

Depending on the purpose, an aluminium bag containing one or more disposable containers may be printed and/or labelled.

In another embodiment of the invention, a packaging unit comprising several arrangements of disposable containers is provided.

The invention is further explained by the accompanying Figures 1 and 2 and examples. Fig. 1 shows an arrangement of 5 detachable containers with a preferred design.1 A shows a front view, 1 B a side view, 1 C a side view and 1 D a perspective view from above.Fig. 2 shows a front view of a single disposable container with a preferred design.

Examples Example 1: Composition of a formulation according to the invention containing the active substances melatonin, ginkgo biloba and biotin

The composition contains 0.05% by weight of Ginkgo Biloba dry extract, 0.01% by weight of biotin, 0.0033% by weight of melatonin and other additives, water and ethanol.

Example 2: Clinical trial

The composition described in example 1 was tested in a randomized, double-blind, placebo-controlled, crossover design study in 8 healthy female patients at a daily dose of 0.1 mg melatonin (3 ml composition) applied to the scalp daily for 14 days before bedtime.

Urine and blood were collected and measured for melatonin and the metabolite 6-hydroxymelatonin sulphate.

Plasma melatonin profiles of the melatonin or placebo treated patients were found to match the concentration-time profiles for endogenous melatonin described in the literature, demonstrating that topical application of the melatonin-containing compound for 14 days did not alter endogenous melatonin secretion.

Administration of the compound for 14 days did not result in an increase in plasma melatonin concentration or urine 6-hydroxymelatonin sulphate concentration beyond physiological levels. Topical application of the melatonin-containing compound was not associated with adverse reactions.

Overall, no systemic effects are induced by the administration of the composition.

Claims (26)

1. A disposable container for a medicament or cosmetic agent for topical application, containing a single dose of melatonin or of a melatonin derivative which corresponds to a locally effective dose but which does not cause any systemic effect, wherein the single dose is 0.01 to 0.2 mg of melatonin or melatonin derivative, and wherein the single dose corresponds to a daily dose.
2. The container as claimed in claim 1, characterized in that the agent is present as a liquid formulation.
3. The container as claimed in claim 2, characterized in that the liquid formulation has a concentration of 0.001 to 0.01 % (by weight) of melatonin.
4. The container as claimed in claim 3, characterized in that the liquid formulation has a concentration of 0.003 to 0.004% (by weight) of melatonin.
5. The container as claimed in any one of the preceding claims, characterized in that the agent contains, as sole active substance, melatonin or a melatonin derivative.
6. The container as claimed in any one of claims 1 to 4, characterized in that the agent contains, as active substances, a combination of melatonin or a melatonin derivative together with biotin and/or gingko biloba.
7. The container as claimed in any one of claims 1 to 4, characterized in that the agent contains, as active substance, a combination of melatonin or a melatonin derivative and vitamin A, vitamin A acid, or another derivative of vitamin A.
8. The container as claimed in any one of the preceding claims, characterized in that it contains 2.5 to 3.5 ml of the agent.
9. The container as claimed in claim 8, characterized in that it contains 2.9 to 3.2 ml of the agent.
10. The container as claimed in any one of the preceding claims, characterized in that the agent is filled into the container under GMP conditions.
11. The container as claimed in any one of the preceding claims, characterized in that it is made of a plastic.
12. The container as claimed in claim 11, characterized in that it is made of polyethylene, polypropylene, polyvinyl chloride, polystyrene or a mixture of these.
13. The container as claimed in any one of claims 1 to 12, characterized in that it is colorless.
14. The container as claimed in any one of claims 1 to 12, characterized in that it is colored.
15. The container as claimed in any one of claims 1 to 14, characterized in that it is transparent.
16. The container as claimed in any one of claims 1 to 14, characterized in that it is non-transparent.
17. The container as claimed in any one of the preceding claims, characterized in that it has, on its head, a disposable closure piece which is opened by turning it.
18. The container as claimed in any one of the preceding claims, characterized in that, after opening, the agent emerges only when pressure is applied.
19. The container as claimed in any one of the preceding claims, characterized in that it carries lettering either printed on or embossed and/or is provided with a label.
20. An arrangement of several containers, as claimed in any one of claims 1 to 19, which are connected to one another in a detachable manner.
21. The arrangement as claimed in claim 20, characterized in that 5 containers are connected to one another in a detachable manner.
22. The arrangement as claimed in claim 20, characterized in that 10 containers are connected to one another in a detachable manner.
23. The arrangement as claimed in any one of claims 20 to 22, characterized in that it is packed into an aluminum bag.
24. The arrangement as claimed in claim 23, characterized in that the bag consists of an aluminum-containing laminated foil and additionally includes polyethylene, polyester and/or paper.
25. The arrangement as claimed in claim 23 or 24, characterized in that the aluminum bag is printed on and/or is provided with a label.
26. A package unit comprising several arrangements as claimed in any one of claims 20 to 25.