DE102007043776A1 - Use of microcapsules and microcapsules - Google Patents

Abstract

Microcapsules are disclosed comprising: 1) a core containing an odorant and / or flavoring and / or a biologically active agent optionally associated with a solid or liquid carrier, and 2) a wall, preferably semipermeable are and / or destructible by mechanical pressure, temperature or humidity. These constitute a single filler or filler material in conjunction with other filler materials for a hollow or porous molding or one or more parts thereof, the molding having an inlet and an outlet for air.

Description

The The invention relates to the use of microcapsules according to the The preamble of claim 1 and a microcapsule according to the The preamble of claim 9.

microcapsules have been known since 1954, when they first took shape were used by carbonless copy paper. Your use was then extended to countless areas. A comprehensive summary of the current state of microencapsulation technology is in the series: MML Volumes 1 to 8, Hrsg, Reza Arshady et al., Kenus Books, London, especially in Volume 1: Microspheres, Micorcapules & Liposomes: Preparation and Chemical Applications and in Volume 2: Microspheres, Microcapules & Liposomes: Medical & Biotechnology Applications, to find.

There are also known microcapsules whose relevant ingredients are present in the core of the capsule on a carrier; see, for. B. the WO 2006/038134 ,

Also Semipermeable walls for microcapsules are known. Often it is an alginate comprehensive Material used.

One The invention relates to the use of microcapsules as Filling material for hollow or porous moldings according to claim 1.

These Shaped bodies allow the ingredient the microcapsules, once released, can be inhaled. By the use of appropriate microcapsules is Among other things, no burning of material required to release the ingredients.

One Another object of the invention are certain microcapsules according to claim 9, particularly for use according to claim 1 are suitable.

advantageous Embodiments are subject of the dependent claims.

According to one first aspect of the invention are microcapsules which are a core, an odor and / or flavor and / or a pharmaceutical or biological agent with a solid or liquid Carrier associated, contains, and include a wall, the semipermeable or by mechanical pressure, temperature or Moisture is destructible, in a hollow or porous molding or one or more parts thereof, wherein the molded body has an inlet and an outlet opening having.

This With the aim of achieving the effective ingredients of the microcapsules with an air or humectant stream when inhaled into the To get airway. In the case of tobacco ingredients must no tobacco to be burned.

Under "Microcapsule" is understood as a structure that has a core completely from a - possibly semipermeable - thin wall is surrounded. The size of the microcapsules is generally 1-1500 μm, preferably 10 μm-300 μm, more preferably 30 to 150 microns, but in individual cases also more, z. B. to 2000, 3000, 4000, 5000 microns, amount.

The Shape of the molding is in many cases a cigarette, a cigarillos, a cigar, a pipe or a hookah or a pipe insert.

The Microcapsules can be used together with other substances, such as Fillers, non-encapsulated odor, taste or biological agents, optionally with inorganic or associated organic or even biological carriers or also present together with biological materials. these can all with water, an aqueous solution or a suitable organic liquids or mixtures thereof be moistened.

Of the or the active ingredient (s) of the microcapsules are released, by either destroying the wall of the microcapsule or their permeability is increased or by diffusing the ingredient through the wall, optionally in the form of a solution.

The Type of microcapsules used, in particular, the way in which the drug passes out of the capsule is partly in terms set in the type of molding.

So are suitable microcapsules by external pressure be destroyed, especially for pipe-like Application devices using a pipe stopper the capsules can be destroyed by mechanical pressure.

By Heat destructible microcapsules can heated in hookah-like application devices which are known to heat the pipe contents, but not burned.

Microcapsules which are destroyed by the action of moisture can also be used in these application devices, as well as in cigarette, cigarillo or cigar-like application devices. The moisture required to destroy the wall passes, for example, by sucking the generally humid ambient air or by admixing a moist filler in the molding, s that he can get into the environment of the wall of the microcapsules. There are many moisture-degradable wall materials whose hydrolyzed constituents are non-toxic. A well-suited one includes aliphatic polyesters.

It is also a chemical destruction of the capsule walls possible, the destruction accomplishing Chemicals initially protected in other microcapsules stored by one of the aforementioned Mechanisms can be opened, then what the chemical destruction mechanism becomes active.

A another class of microcapsules has semipermeable walls. Through this, the active ingredient can diffuse out of the capsule. optionally in a solvent such as water, ethanol, Polyalcohol and the like dissolved. In the latter case For example, the water or the like, the z. B. as a humectant is present in a filler in the device, from the outside penetrate through the capsule wall, dissolve the ingredient in the core and then along with the dissolved ingredient from the Diffuse capsule out. Semipermeable wall materials include often alginates, eg. B. alkaline earth alginates.

In MML, Volume 1: Microspheres, Micorcapules & Liposomes: Preparation and Chemical Applications and in the other volumes (top) can be found many examples of suitable wall materials.

Of the Core of the microcapsules contains an odor, flavor or biological or pharmaceutical active substance (hereinafter often collectively referred to as "ingredient").

Everyone such gaseous, liquid or solid matter, which has a noticeable vapor pressure and consequently in one Air, solvent or moisture flow into the respiratory tract can be sucked in as an ingredient of the microcapsules Question.

But also charged, usually present in salt form ingredients Can be used as these when removed from the microcapsule are dissolved out, mixed with existing moisture and be inhaled in this way.

Also Sugar, killed or living organisms such as killed Yeast, vitamins (such as vitamin C) and dietary supplements (such as organic and inorganic salts of metals) as ingredients possible, both as carrier material, which in the course of time after destruction of the capsule wall dissolves, as well as impregnation of a porous or adsorbent carrier material.

In In a particularly preferred embodiment, the Ingredients Ingredients of tobacco leaves, especially of tobacco leaf extracts or juices, such as. For example nicotine. By the use of the invention is a Enjoyment of tobacco leaf ingredients possible without a combustion process is needed and smoke is created.

Also other drugs, eg. As alcohol, can be used in the invention Be contained microcapsules.

Another preferred embodiment of the invention is the use of microcapsules containing an inhalable medicament, e.g. As an active ingredient in asthma drug. Such agents are for. B. the "Red List ^® ", latest vintage, Editio Cantor Verlag, Aulendorf, removable.

Of the Ingredient of the capsules may be associated with a carrier be, z. B. on or in such ad- or absorbed or by a chemical bond (ionic, covalent, hydrogen-bonding) or complex binding) to be bound thereto.

Of the The purpose of binding to a carrier is to provide the ingredient (better) to be able to bring in the capsule, z. B. at very volatile ingredients, as well as its effect a slow release associated with the carrier extend.

Of the Carrier can be solid or liquid. A solid Carrier will often consist of a polymer or include such organic, inorganic, inorganic-organic, of synthetic or natural origin. Example are Polyester, silica, silicones, starch and cellulose. But also metals, minerals (eg porous species of dolomite, Clays such as montmorillonite and silicas and silicates like kieselguhr) and salts are suitable as carriers.

at liquid carriers can be z. B. to polyethylene glycols act different molecular weights.

In A preferred embodiment is in the used microcapsules to those in the second aspect of the Invention be discussed.

If required, the hollow shaped body before use in an air-tight or moisture-proof envelope.

A second aspect of the invention relates to a Microcapsule which can be used particularly advantageously in the first aspect of the invention.

The microcapsule according to the invention preferably has one semipermeable, permeable to water molecules Wall on and contains a core that does not penetrate the wall can. The core comprises a carrier with which one or more Ingredients are associated. The association between carriers and ingredient can be repealed by solvolysis and the This released ingredient can penetrate the semipermeable wall.

Under The many known materials include a particularly suitable Material for semipermeable wall alginates, typically Erdalaklialginate, or consists thereof. The permeability of alginates can be tailor made for a special purpose become.

at The ingredients may be the ones mentioned above in the first aspect Invention mentioned act. The same applies the carriers.

The solvizable association between ingredient and carrier can take all conceivable forms. The ingredient can be added to the Carrier adsorbed, absorbed in this, with this in the form of a mixed crystal, ionic, covalent, by hydrogen bonding or by complex binding be connected to this.

The only condition is that the association by solvolysis can be lifted. Under "solvolysis" is here in the first place a solvolysis by water (ie a hydrolysis) understood, but a solvolysis by other polar compounds, e.g. For example, alcohols or amines, is also considered.

solvolysable or, in the narrower sense, hydrolyzable bonds between a carrier and an ingredient are quenched by a water or solvent molecule in the - as whatever - binding between ingredient and carrier pushes and destroys them. There are countless possibilities for solvatable or hydrolyzable bonds between Ingredient and carrier, and therefore only a few by way of example.

Z. B. can be a relatively less polar molecule on a support like silica gel adsorbed and from this adsorption bond be displaced by water. An example nitrogen-containing compound may be present as a complex with a transition element, from it by water or even an organic solvent as glycol or propylene glycol is displaced. An alkaloid may be via a hydrolyzable bond (eg ester bond, Diphosphate bridge, silylene group and many others) covalently to a solid starch carrier or a liquid polyethylene glycol molecule be bound with high molecular weight. Salts and generally ionic compounds For example, they can be adsorbed on a mineral or absorbed in a mineral, dissolved out by water and in dissolved form through the semipermeable wall and diffuse out of the capsule.

In In the preceding examples, the ingredient-released Vehicles generally do not use the semipermeable wall. It However, there are also carrier-ingredient pairs where this is the Case can be, for. For example, 2 large alkaloid molecules could be hydrolyzed connected, which would make them too big to to diffuse through the semipermeable wall. After the hydrolysis but this could be possible. In this case the carrier would be an ingredient at the same time. One member or both members of the pair of carrier ingredient, In the special case ingredient ingredient, can in free state also liquid (or even gaseous) be.

Of the Ingredient in the core is released slowly when water or another solvent, such as glycol, gradually penetrates into the microcapsule, resulting in appropriate selection of the wall and / or the concentration (amount) of the microcapsule surrounding Water / solvent can be achieved. This will prolongs the duration of action of the ingredient. The diffusion of the ingredient through the semipermeable wall, as long as a concentration gradient is present. As the ingredient is often transported away immediately from the capsule wall, In principle, the ingredient can be completely eliminated from the microcapsule diffuse out as long as there is enough solvent / water present to ensure the solvolysis / hydrolysis.

In Cases where for the microcapsules or a Part of the same a wall material is chosen, which for At least one of the ingredients is semipermeable, the finished moldings alone (or in groups) in envelopes packed, which is impermeable to all ingredients are.

QUOTES INCLUDE IN THE DESCRIPTION

This list The documents listed by the applicant have been automated generated and is solely for better information recorded by the reader. The list is not part of the German Patent or utility model application. The DPMA takes over no liability for any errors or omissions.

Cited patent literature

• - WO 2006/038134 [0003]

Claims (22)

Use of microcapsules comprising: - one Kernel, the odor and / or flavor and / or a contains biological or pharmaceutical active substance, the optionally with a solid or liquid carrier is associated, and - a wall that is semipermeable and / or by mechanical pressure and / or temperature and / or a Chemical undusable or moisture is destructible or in their permeability is controllable, as only Filling material or as filling material in conjunction with other fillers for a hollow or porous shaped body or one or more parts the same, wherein the shaped body an entrance and a Outlet for a gas flow, in particular air flow has. Use according to claim 1, characterized that the shaped body contains a cigarette, cigarillo, cigar, Whistle or water pipe-like shape. Use according to claim 1 or 2, characterized that the carrier is an organic, inorganic, organic-inorganic synthetic or natural polymer or comprises such. Use according to claim 1 or 2, characterized that the carrier is a metal, a mineral or a salt. Use according to one of the preceding claims, characterized in that the odor and / or Ge flavor and / or biological active ingredient derived from tobacco leaves and / or a drug like caffeine, alcohol or a pharmaceutical Drug includes. Use according to one of claims 1 to 5, characterized in that the odor and / or flavor and / or biological agent comprises an inhalable medicament. Use according to one of the preceding claims, characterized in that the wall is destructible by moisture Wall is. Use according to claim 7, characterized the wall comprises an aliphatic polyester. Microcapsule which is a preferably semipermeable, for solvent-permeable wall and includes a core that can not penetrate the wall and the an odor and / or flavor and / or a biological Active substance with a solid or liquid carrier contains, characterized in that the odor and / or flavoring and / or bioactive agent solvolyzable is associated with the wearer and in the free state the Wall can penetrate. Microcapsule according to claim 9, characterized in that that it is the solvysable association with the carrier a solvolyzable ionic, covalent, hydrogen-bonding or complex binding or an adsorption or absorption binding. Microcapsules according to claim 9 or 10, characterized that the solvolysis is a hydrolysis. Microcapsule according to one of claims 9 to 11, characterized in that the carrier is a solid Carrier is. Microcapsule according to claim 12, characterized in that that the solid carrier is an organic, inorganic, organic-inorganic synthetic or natural polymer or comprises such. Microcapsule according to claim 12, characterized in that that the solid carrier is a metal, a mineral or a Salt is. Microcapsule according to one of claims 9 to 11, characterized in that the carrier is a liquid Carrier is. Microcapsule according to claim 15, characterized in that that the liquid carrier after the solvolytic Cleavage of the odor and / or flavor and / or biological Active substance can not penetrate the wall. Microcapsule according to one of claims 9 to 16, characterized in that the wall comprises an alginate. Microcapsule according to one of claims 9 to 17, characterized in that the odor and / or flavor and / or biological active ingredient derived from tobacco leaves or a drug like nicotine, caffeine, alcohol or a pharmaceutical Drug includes. Microcapsule according to one of claims 9 to 18, characterized in that the odor and / or flavor and / or biological agent comprises an inhalable medicament. Use according to claim 1 or 2, characterized that the microcapsules microcapsules according to one of the claims 9 to 19 are. Use according to claim 20, wherein among the Microcapsules are those whose wall material passes through a chemical destroyed or in the permeability for at least one ingredient can be changed thereby in that the chemical is present in microcapsules whose Wall material by mechanical pressure and / or temperature and / or Moisture destructible or in permeability is controllable for the chemical. Use according to one of claims 19 to 21, wherein the wall material of the microcapsules semipermeable for at least one of the ingredients is characterized in that that the molded body in one for all ingredients impermeable cladding is included.