Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Reexamination Certificate
1998-04-13
2001-08-28
Dodson, Shelley (Department: 1616)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
C424S400000, C424S402000, C424S443000, C424S445000, C424S447000
Reexamination Certificate
active
06280765
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a patch which allows the controlled release into the epidermis of at least two pharmaceutically, cosmetically or dermo-pharmaceutically active compounds, in particular compounds having different solubilities. According to the invention, this relates, in particular, to a first group of liposoluble active agents and to a second group of water-soluble active agents.
In the description of the present invention hereinbelow, the term “patch” denotes an active-agent delivery system having a composite structure in the form of layers which, when applied to the skin, ensures release of the active product by transdermal action.
As regards the liposoluble active compound, this is, in particular, a compound capable of being dissolved in an apolar medium such as an oily medium.
As regards the water-soluble active compound, it is in solid form, in particular in the form of a particulate powder or in the form of granules.
2. Description of the Prior Art
It is known to use patches which allow, by transdermal action, the penetration of active compounds.
Such patches generally have a structure containing several successive layers in the following order: a first layer, known as the support layer, which is generally occlusive, i.e. consisting of a material which is impermeable to the active compound, so as to prevent evaporation of the latter and promote the transdermal action; a second layer, known as the polymer layer, bound to the support layer and containing the active compound, it being possible for this layer to come into direct contact with the skin; optionally, in order to promote binding of the patch to the skin, a layer of an adhesive material applied to the surface of the polymer layer and permeable to the active compound; lastly, a detachable protective layer hermetically covering the polymer layer, so as to protect it against any external contamination during the storage time prior to the patch being used.
A patch structure consisting of an occlusive support layer and comprising, bound to the latter, a polymer layer made of a matrix of a silicone polymer including, in the dispersed state, fatty substances and hydrophilic active compounds, is known, in particular according to U.S. Pat. No. 5,232,702. This form of patch is more particularly suitable for delivering water-soluble active compounds and the patent does not describe the delivery of additional active compounds of lipophilic nature.
Moreover, document WO 96/14822 describes an occlusive patch of a form adapted for the treatment of wrinkles, of the abovementioned type containing a water-soluble active compound in powder form in an anhydrous matrix wherein the matrix may contain an oil, used as a penetration agent.
Furthermore, document FR-A-2,738,744 describes a patch for the controlled release of at least one cosmetically or dermo-pharmaceutically active compound, this patch containing a reservoir layer, bound to a support layer wherein the reservoir layer consists of a hydrophobic polymer matrix in which are dispersed particles of the active compound (which may be unstable in oxidizing medium) and particles of at least one water-absorbing agent, the reservoir layer being anhydrous.
A patch consisting of a silicone matrix containing a liposoluble active agent, a water- soluble active agent and an oil for increasing the penetration of the liposoluble active agent, this water-soluble active agent being in particulate form dispersed in the matrix, is also known from document DE-A-4,210,165.
SUMMARY OF THE INVENTION
The present invention relates to a controlled-delivery system containing an anhydrous polymer matrix in which is dispersed an oil in the form of droplets, this matrix being intended to release simultaneously lipophilic active compounds and hydrophilic active compounds. The use of an anhydrous polymer matrix in which an oil is dispersed has the advantage of being able to give a particularly flexible patch, designed to adhere to non-planar skin surfaces, with a high radius of curvature, and of not being hampered by regions of skin folds.
Tests have shown that in patches of the prior art, adhesion to the skin was difficult particularly when a relatively large proportion of oil was incorporated.
It has been found surprisingly, that the addition of a water-absorbing agent to the matrix leads to a substantial improvement in the adhesive power of the patch of the invention.
Moreover, the Inventor has observed that by dispersing in a hydrophobic polymer matrix, an appropriate amount of oil, in which a first lipophilic active compound is dissolved, a patch is obtained containing an anhydrous polymer layer but nevertheless allowing excellent controlled release of a second pulverulent active compound of hydrophilic nature.
The patch of the invention allows, in particular, the packaging and controlled administration of an assembly of skin-nourishing and/or skin-repairing substances of lipophilic and hydrophilic nature, and in particular lipophilic and hydrophilic active agents which have a tendency to inactivate each other when they are found in combination.
It has also been observed, entirely surprisingly and unexpectedly, that it is possible to package one (or more) hydrophilic active compound(s), one (or more) lipophilic active compound(s) and one (or more) oil(s) in the same polymer matrix. Thus, it is possible to prepare, for example, a stable combination of particles of a water-soluble compound, which is unstable in aqueous medium or in the open air and/or of a liposoluble active compound, which is also unstable in aqueous medium or in the open air, with an unsaturated oil, which has a drying effect in the open air, without any risk of degradation of the active compounds and without any risk of hardening of the oil.
DETAILED DESCRIPTION OF THE INVENTION
The subject of the present invention is a pharmaceutical, cosmetic or dermo-pharmaceutical patch containing a hydrophobic polymer layer bound to a support layer and containing: a) first particles of at least one water-soluble active compound, b) second particles of oil, c) at least one liposoluble active compound, and d) third particles of a water-absorbing agent, dispersed homogeneously in the polymer layer.
According to a first embodiment, the liposoluble active compound is dissolved in the oil.
According to another embodiment, the liposoluble active compound is in particulate form, in the form of powder or granules, dispersed in the polymer layer.
The oil which can be used in accordance with the invention can be chosen from the following oils, alone or as a mixture, among which mention may be made of: oils of animal, plant or mineral origin, and in particular animal or plant oils formed by fatty acid esters of polyols, in particular liquid triglycerides, for example sunflower oil, corn oil, soybean oil, marrow oil, grapeseed oil, sesame oil, hazelnut oil, pistachio oil, apricot oil, almond oil or avocado oil; fish oils, glyceryl tricaprocaprylate, or plant or animal oils of formula R
1
COOR
2
in which R
1
represents a higher fatty acid residue containing from 7 to 19 carbon atoms and R
2
represents a branched hydrocarbon chain containing from 3 to 20 carbon atoms, for example purcellin oil, wheatgerm oil, beauty-leaf oil, sesame oil, coriander oil, safflower oil, passion flower oil, musk rose oil, macadamia oil, fruit (grape, blackcurrant, orange, kiwi) seed oil, rapeseed oil, coconut oil, groundnut oil, evening primrose oil, palm oil, castor oil, flax oil, jojoba oil, chia oil, olive oil or cereal germ oil such as wheatgerm oil, rice bran oil, karite butter; acetyl glycerides; alkyl or polyalkyl octanoates, decanoates or ricinoleates; fatty acid triglycerides; glycerides; liquid paraffin, liquid petroleum jelly, perhydrosqualene; fatty alcohols (stearyl alcohol, cetyl alcohol) and fatty acids (stearic acid) and esters thereof; poly(C
1
-C
20
) alkyl siloxanes and in particular those containing trimethyl silyl end groups, preferably those whose viscosity is less than 0.06 m
2
/s, among
Dodson Shelley
L'Oreal
Oblon & Spivak, McClelland, Maier & Neustadt P.C.
LandOfFree
Pharmaceutical, cosmetic or dermo-pharmaceutical patch for... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pharmaceutical, cosmetic or dermo-pharmaceutical patch for..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pharmaceutical, cosmetic or dermo-pharmaceutical patch for... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2480039