FR2840221A1 - System for releasing active agents, e.g. , drugs, fertilizers, foods or cosmetics, into a liquid comprises an agent containing polymer film produced by application onto a disposable support - Google Patents

Abstract

System for releasing active agents (I) into a liquid comprises a (I)-containing polymer film produced by application onto a disposable support.

Description

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 The subject of the present invention is a polymeric film containing active agents or substances (designated by the term "active agents"), obtained by spreading on a disposable support and intended to release the "active agents" in a liquid.

PRIOR ART AND TECHNICAL CHALLENGE TO BE TAKEN A large number of systems have been described for conveying and delivering active agents or substances (designated by the term "active agents") in fields as diverse as phytosanitary, cosmetology, pharmacy, food, household products (cleaning products, DIY products, etc.).

The "active ingredients" concerned can be in various forms: A) powders (detergents, medicines, etc.) B) agglomerated or compressed powders:
1) granules for fertilizers, phytosanitary antiparasitics, bath salts, soluble coffees ...

 2) tablets for detergents, medicines, cubes of spices or flavorings, sweeteners, sugars ...

C) more or less viscous liquids (medicines, hygiene products, flavors, detergents, edible liquids, cosmetic creams and lotions ...).

D) gels, pasta, ointments ...

 The drawbacks of these presentations are in particular the following: - bulk, - difficult dosing for non-unit systems, - difficult transport for liquids and powders, - rarity of unit systems for liquids and low-dose active ingredients, - risk of breakage or bursting of the packaging of liquids or powders, - limitation of the number of active release profiles achievable for powders and liquids type presentations, - stability during storage.

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 Polymeric films have also been proposed for conveying pharmaceutical or oral hygiene active agents, but they are designed to be applied to surfaces such as the skin or a mucous membrane and not for release into a liquid.

 The system according to the invention overcomes most of the drawbacks mentioned for current presentations of "assets". It appeared, in fact, that the polymer film technology, a well-established industrial technology commonly used in the packaging trades, could, surprisingly and in a new way, be advantageously used to convey various "active ingredients" in order to release into a liquid.

 This liquid can be a biological liquid (in the case of medicines for example), hot or cold water in the case of a drink for example, or water intended for washing objects or for household hygiene or body, or rainwater for phytosanitary uses in particular. It can also be liquids of a different nature than water such as for example ethanol or an oily solvent, or mixtures of liquids of different nature.

 The polymer film system described is surprisingly capable of carrying "active ingredients" of very different nature (hydrophilic, lipophilic, pulverulent or liquid ...), of very varied uses (phytosanitary, food, medicinal, cosmetic , coloring ...), and to release them in a liquid according to very varied programs (immediate, delayed, prolonged, pulsed release ...) and this using a single and same process: spreading on a disposable support.

DESCRIPTION OF THE INVENTION
The present invention relates to a new system for the release of active agents or substances (designated by the term "active agents"), consisting of a polymeric film obtained by spreading on a disposable support, containing the active agent (s), and releasing the "active" by swelling and / or disintegration and / or dissolution and / or diffusion in a liquid.

 Thanks to this technology, it is possible to convey very different "active ingredients", dispersed (suspensions, emulsions) or dissolved in the film.

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 According to a first characteristic, the system comprises at least one monolayer film containing the "active" (s), the film-forming polymer (s) (or copolymers) and possibly the excipients or adjuvants necessary for the formulation (for manufacturing, presentation, release , stability ...) of the system.

 Depending on the nature of the polymers (or copolymers) and excipients (or adjuvants) used, a large number of formulations with variable "active" release profiles can be produced: immediate, prolonged release over several hours or days, delayed release, pulsed release (several successive releases with a delay between each).

 For the production of the films, the following polymers or copolymers (obtained by reaction of the polymers mentioned in different proportions) can be used (in dispersion in the appropriate solvents), alone or mixed to produce films which are soluble or insoluble in liquids, and without that this list is not exhaustive: of polyvinyl, acrylics and derivatives, polyvinyl alcohol, cellulose and derivatives (cellulose acetophthalate, sodium carboxymethylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, methylcellulose, methylhydroxyethylcellulose, methylhydroxypropylcellulose), polyvinyl acetate, polyvinyl chloride fluorocarbons, glycerol, polyesters, polyolefins, polyethers, polyethylenes, polyamides, polyethylene glycols, polyimides, natural polymers (gelatin, gum arabic, alginates, starches and derivatives, gum tragacanth, carrageenans, chitosans), polysiloxanes, polypropylene, polyurethanes , polyvinylpyrrolidone and derivatives such as copolymers of vinyl pyrrolidone and vinyl acetate, propylene glycol, copolymer of poly (methyl vinyl ether / maleic anhydride). The various excipients, polymers or copolymers are mixed and then according to conventional film manufacturing technologies, put into films with a thickness of 5 m to 3 cm. The films are dried by heat (preferably between 30 ° C. and 100 ° C.) and / or by means of infrared ramps and / or by the use of microwaves.

 In addition to the film-forming polymers, excipients or adjuvants can be added. They are absorption promoting agents, emulsifiers, texturing agents, flavorings, sweeteners, colors, adhesives; the following excipients, without this list being exhaustive: fatty acids and derivatives, fatty alcohols and derivatives, polyglycolized saturated or unsaturated glycerides, N-methyl-2-pyrrolidone, emulsifying agents (such as polyoxyethylenated esters and esters of sorbitan, oleates , lecithins of animal or vegetable origin,

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 polyoxyethylenated castor oil, sucro esters, fatty acid esters of polyethylene glycol, fatty acid esters of glycerol, fatty acid esters of propylene glycol, bile acids and their salts), diethylene glycol monoethyl ether, dimethylisosorbide , terpenes, phospholipids, polycarbophils (such as in particular those sold under the names of "CARBOPOL" by BFGoodrich), vegetable or mineral oils, carbohydrates, cyclodextrins and derivatives, silica and derivatives, acids and bases for pH adjustment.

 According to a second characteristic of the invention, it is possible to superimpose different films of identical or different formulations so as to produce complex films.

According to this characteristic, it is possible to formulate incompatible "active ingredients" and / or programmed release systems.

 According to a third characteristic of the invention, the systems are cut out so as to obtain units. Before cutting, the systems may have undergone an operation such as folding, winding, etc. without this list of operations being limiting, so as to produce systems adapted to the need. It can thus, by way of illustration, be produced disks (or other shapes such as: ovals, squares or rectangles of variable dimensions), or systems wound and then cut into units, or folded systems for example parallelepipedic or cubic.

 According to the invention it is also possible to seal the films, according to the state of the art, in particular hot, or by applying an adhesive to all or part of the film.

According to a fourth characteristic of the invention, the units obtained according to the methods described in the third characteristic can be placed as such in a primary packaging, such as sachet, blister, bottle, cup, alone or in the presence of other identical or different products. They can also be placed: A) In the case of medicinal active ingredients: in a capsule, or a tablet or soft capsule ..., alone or in the presence of one or more other galenical forms and / or powdered excipients , liquids or semi-solids; more, several different units or of the same formulation can be placed in the same capsule or soft capsule or tablet.

B) In the case of "active ingredients" for cosmetic or hygienic use, or for phytosanitary purposes, or for food use, or for household use: in a capsule, a tablet, a soft capsule,

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 a filter paper, a woven pocket ..., without this list being exhaustive, alone or in the presence of other identical or different products.

The types of “active ingredients” which can be transported in the system which is the subject of the present invention are the following, without this list being limiting or exhaustive: medicaments for human or veterinary use, food products (flavors, spices, colorings, coffee , concentrates for sauces or other preparations ...), domestic (detergents, descalers, deodorants, dyes ......), phytosanitary products (insecticides, fertilizers, weedkillers, seeds ...).

 The following EXAMPLES illustrate the invention but do not limit it in any way.

EXAMPLE 1
Medication film Shake 2 g of polyoxyethylene 400,0,5 g of polysorbate 80, 10 g of sodium diclofenac in 50 g of water and 50 g of ethanol until a clear solution is obtained. Slowly add 3 g of hydroxypropylcellulose to the solution, keeping stirring until a clear solution is obtained.

Spread the solution on a sheet of plasticized Kraft paper so as to obtain a film with a thickness of 100 m. Dry under a current of hot air at 60 C until the solvents have evaporated.

 Remove the film obtained from Kraft paper, roll it up and cut it into units. Divide the units into capsules so as to have 20 mg of sodium diclofenac per capsule.

EXAMPLE 2
Film for instant coffee Add slowly and with stirring to 100 ml of concentrated coffee extract, 2.5 g of sodium carboxymethylcellulose, continuing to stir until a clear solution is obtained.

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Spread the solution on a sheet of plasticized Kraft paper so as to obtain a film with a thickness of 300 m. Dry under a current of hot air at 60 C until the solvents have evaporated.

 Remove the film obtained from Kraft paper, cut with a cookie cutter in units. Divide the units into individual sachets.

EXAMPLE 3
Film for concentrated detergent for dishwashers.

Shake 2 g of polyoxyethylene 400,0,5 g of polysorbate 80,50 g of concentrated liquid detergent in 50 g of water until a clear solution is obtained. Slowly add 3 g of sodium carboxymethylcellulose to the solution, keeping stirring until a clear solution is obtained.

Spread the solution on a sheet of plasticized Kraft paper so as to obtain a film with a thickness of 200 m. Dry under a current of hot air at 60 C until the solvents have evaporated.

Remove the film obtained from Kraft paper, fold it and cut it into units. Divide the units into blisters.

The polymeric film system for the release of "active ingredients" in liquids, according to the invention, is used on the one hand for the formulation of new drugs for the pharmaceutical industry, on the other hand to facilitate the use of " active "by the consumer (easy and non-fragile transport even for liquids, unit dosages, improved conservation ...) both in the food industry, phytosanitary, cosmetic, or DIY sectors, by its new concept: release of the "active ingredients" from a film placed in a liquid.

Claims (11)

 CLAIMS 1. System for the release of active agents or substances (designated by the term "active agents") in a liquid, characterized in that the "active agents" are contained in at least one polymeric film obtained by spreading on a disposable support and are released into a liquid. 2. System according to claim 1 characterized in that the film consists of polymers and / or copolymers of film-forming type more or less soluble or insoluble in the liquid. 3. System according to claim 1 characterized in that excipients or adjuvants can be added to (x) or copolymer (s) to obtain a film consisting of a gelled formulation of solution, suspension, emulsion, pre-emulsion, micro- type. emulsion, pre-micro-emulsion. 4. System according to claim 1 characterized in that excipients or adjuvants can be added to (x) or copolymer (s) so that the active agent (s) are dispersed, in suspension or in emulsion, or dissolved in the film. 5. System according to claim 1 characterized in that the film consists of excipients and / or polymers and / or copolymers allowing programmed release of the "active" (s): immediate, prolonged release, delayed release, pulsed release. 6. System according to claim 1 characterized in that the film may contain an adhesive or be coated partially or completely with an adhesive. 7. System characterized by the superposition of several systems each characterized by any one of claims 1 to 6, leading to the superposition of films of identical or different formulations. <Desc / Clms Page number 8> 8. System according to claims 1 to 7 characterized in that the system is in the form of units of various geometric shapes after any one or more of the following operations: folding, winding, cutting, without there being any notion of order in these operations. 9. System according to claim 8 characterized in that it can be placed, as is in a primary packaging system. 10. System according to claim 9 characterized in that the primary packaging system is a: sachet, blister, ampoule, bottle, bottle, pill box, jar, bucket, case, woven or non-woven pocket, pouch, paper, filter, " wafer ", box, tin can. 11. System according to claim 8 characterized in that it can be introduced in another form of presentation such as: powder, granule, more or less viscous or semi-solid liquid, gel, tablet, capsule, soft capsule, cachet.