EP1411893A1 - Formes pharmaceutiques plates pour administration orale comprenant des particules contenant des substances actives - Google Patents

Formes pharmaceutiques plates pour administration orale comprenant des particules contenant des substances actives

Info

Publication number
EP1411893A1
EP1411893A1 EP02791449A EP02791449A EP1411893A1 EP 1411893 A1 EP1411893 A1 EP 1411893A1 EP 02791449 A EP02791449 A EP 02791449A EP 02791449 A EP02791449 A EP 02791449A EP 1411893 A1 EP1411893 A1 EP 1411893A1
Authority
EP
European Patent Office
Prior art keywords
particles
liquid
active substance
dosage form
active ingredient
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP02791449A
Other languages
German (de)
English (en)
Inventor
Frank Becher
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
LTS Lohmann Therapie Systeme AG
Original Assignee
LTS Lohmann Therapie Systeme AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by LTS Lohmann Therapie Systeme AG filed Critical LTS Lohmann Therapie Systeme AG
Publication of EP1411893A1 publication Critical patent/EP1411893A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1611—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient

Definitions

  • the invention relates to dosage forms for oral administration of active substances, comprising a carrier matrix and at least one active substance contained in particles. It relates in particular to flat oral dosage forms of small thickness.
  • the procedure is often such that the active ingredient is mixed in liquid form, with suitable carriers and auxiliaries, incorporated into the base or matrix material of the pharmaceutical form and then the desired dosage form is produced by further process steps.
  • wafer-like dosage forms also called “wafers”
  • the procedure is such that an active substance in liquid form is incorporated into the material of the carrier layer of the wafer, this can have the consequence that only relatively small amounts of active ingredient can be incorporated. Because of the small thickness of these systems, the mechanical properties of the carrier material, in particular the coherence and flexibility, would be impaired by an excessively high active substance loading.
  • the present invention was therefore based on the object of listing oral dosage forms or pharmaceutical preparations. gene, in the production of liquid active substance preparations can be assumed, but without the disadvantages mentioned above appear.
  • the invention provides that the carrier matrix of a dosage form mentioned in the preamble of claim 1 has a multiplicity of open-porous or capillary-containing particles, these particles serving as the active substance reservoir.
  • a particular advantage of this type of dosage form is that the active substance in question does not have to be uniformly distributed or dissolved in the carrier matrix, but rather is located in many small reservoir particles. This can significantly reduce the total amount of the active ingredient, since it is not necessary to distribute it homogeneously. It is sufficient if it is present in sufficient concentration in many small particles, and only in these, in order to be effective. Another advantage is that the strength of the dosage form or the carrier matrix is not impaired by the active substance in particle form, since the liquid active substance components are bound in the particles.
  • the particles according to the invention can be open-porous or capillary-containing particles with a large inner surface. 2. They can also be particles containing active ingredients which are obtained by the process described in WO 99/17868.
  • the first of these is the shape of the particles.
  • These particles serve as an active substance reservoir and contain at least one active substance, preferably in liquid form.
  • liquid form it is meant that the active ingredient itself is in the liquid state, or that it is present as a solution, dispersion, suspension, emulsion or as a liquid active ingredient preparation.
  • a main advantage of these medicinal preparations is that the particles containing the active substance are first loaded with liquid active substance or a liquid active substance preparation in a form known to the person skilled in the art.
  • this can be done in that the porous or capillary particles have a vacuum (preferably in the
  • This has the particular advantage that air, which is mostly in the capillaries, is removed; as a result, the specific weight of the particles is greater and they no longer float on the surface of the active substance liquid.
  • the particles are effectively washed around with the active ingredient liquid in a vacuum, which can be achieved, for example, by stirring with high-speed stirrers, shaking or in some other suitable manner. If normal pressure ratios are then established, the active substance liquid is pressed into the capillaries or pores by the air pressure.
  • the particles are introduced into the active substance liquid, and this is then placed under elevated pressure (preferably in the range from 2 to 300 bar, more preferably 10 to 200 bar, most preferably 10 to 100 bar), so that the Active substance is pressed into the air-filled pores. During the subsequent relaxation, the air in the pores escapes because the adhesive forces of the liquid are greater.
  • elevated pressure preferably in the range from 2 to 300 bar, more preferably 10 to 200 bar, most preferably 10 to 100 bar
  • the particles are brought to high temperatures (preferably in the range from 40 to 200 ° C., particularly preferably 50 to 150 ° C.), so that the pressure of the air in the pores is low; These hot particles are washed around with cold active ingredient liquid so that they can penetrate into the cavities. "Cold” means that the temperature is lower than that of the particles.
  • the loading of the particles can take place in such a way that the particles are suspended and mixed in the liquid active substance or the liquid active substance preparation under normal pressure and at room temperature (about 20-30 ° C.), preferably with stirring.
  • the loaded particles are separated from the excess active substance liquid, for example by sedimentation or filtration.
  • Particles in solid form are incorporated into the carrier matrix of the respective pharmaceutical preparation. Apart from the active substance liquid enclosed in the particles, no liquid, or only insignificant amounts, are introduced into the carrier matrix mass, so that the structure, consistency, stickiness, elasticity and other properties of the matrix material are not adversely affected. In any case, it is possible in this way to incorporate larger amounts of an active substance present in liquid form into a pharmaceutical preparation than would be the case with conventional production methods. In the manufacture of the Pharmaceutical forms according to the invention can therefore be used essentially the same methods and apparatus that are used for the processing of solid active pharmaceutical ingredients. In particular, the invention enables the production of flat, thin dosage forms based on liquid active substance preparations.
  • the different particles can also be loaded with different active substances, so that combination preparations can be produced in a simple manner.
  • Plasticizers or enhancers can be selected from the following substances or groups of substances:
  • Different particle types and sizes can advantageously be used in order to achieve differentiated release behavior.
  • Another advantage is that the use of liquid-filled particles of active ingredient ensures safety in the Drug production can be improved. This applies in particular if the personnel is at risk of contamination with active substances, in particular with toxic substances.
  • Active ingredient solutions can be loaded, especially those selected from the group consisting of activated carbon particles, particles from porous minerals, in particular diatomaceous earth particles, diatomaceous earth, pumice, lava, bentonite, ceramic or clay particles, silica gel particles, Siliciu - includes monoxide particles, zeolites and particles from natural or synthetic sponges or from solidified foams. Porous particles are also understood to mean those which have a capillary structure.
  • synthetic sponges or foams can be both biodegradable materials (e.g. solidified gelatin or collagen foams) and non-degradable materials (e.g. polyurethane foams, microcellular polyester or polyether foams).
  • superabsorbents such as swellable polymers, as described, for example, in PCT / EP 95/02120.
  • the average particle size of the porous particles is preferably 2 2 mm, more preferably 0,5 0.5 mm, even more preferably 200 200 ⁇ m, in particular ⁇ 50 ⁇ m.
  • the particle size can be adjusted, for example, by grinding and / or sieving, but also by growing suitable crystals or using suitable precipitation processes known to the person skilled in the art.
  • the particles used according to the invention are generally fine-pored, the average pore or capillary diameter preferably being 0,1 0.1 mm, more preferably 20 20 ⁇ m and particularly preferably 1 1 ⁇ m.
  • the proportion of particles loaded with the active ingredient, based on the carrier matrix can be varied within a wide range.
  • the active substance-loaded particles can be contained in a dosage form in a dosage form of up to 95%, depending on the carrier matrix selected in each case.
  • the proportion of particles is therefore preferably 0.1 to 95% by weight, more preferably 5 to 60% by weight, particularly preferably 5 to 25% by weight, in each case based on the overall dosage form. Due to the large range in terms of the particle content and also in terms of the amount or concentration of active substance in the individual particles, the dosage forms according to the invention can cover a wide range in terms of dosage.
  • the loading of these porous or capillary particles with active substance (s) can preferably be carried out in this way. conditions that the liquid active ingredient, an active ingredient solution, dispersion, suspension or emulsion, or a liquid active ingredient preparation, is mixed with a suitable amount of particles, whereby the pore or capillary spaces are filled with active ingredient liquid or solution.
  • the loaded particles can then be separated from the excess active substance liquid or solution by methods known to the person skilled in the art. Optionally, this can be followed by a drying process to remove any remaining liquid or solvent residues.
  • an active ingredient-containing solution which contains at least one solid active ingredient in dissolved form in a suitable solvent.
  • a suitable solvent This can also be a saturated drug solution.
  • CPF particles containing active ingredient which can be obtained by the process described in WO 99/17868 and which are referred to as "Concentrated Powder Form” (CPF) particles.
  • CPF particles are powdery, liquid-laden particles or agglomerates of particles which arise when an inert gas or gas mixture in a liquid active substance, an active substance-containing solution or suspension or other liquid active substance preparation under pressure (preferably about 5 to 500 bar, particularly preferably) in the range of 10 to 250 bar) is dissolved in this liquid, and this solution is then quickly expanded (for example through a nozzle), a powdery solid carrier material (carrier particles) being admixed at the same time.
  • carrier particles carrier particles
  • the powders so obtained are essentially dry and free-flowing and can contain up to 80% by weight of an active ingredient liquid. They have the advantage that they can be processed like solid particles despite a high liquid content.
  • the liquid contained is either in the capillary spaces of the aggregated carrier particles and / or in the pores of the carrier particles if open-pore carrier particles are used.
  • Starch types such as corn, potato, wheat starch
  • silicic acid or silicon dioxide celluloses (e.g. microcrystalline celluloses, cellulose derivatives such as carboxymethyl cellulose, cellulose fibers) can be used, for example, as powdery carriers or particles.
  • porous particles of the type mentioned at the outset can also be used as carrier particles, such as e.g. Activated carbon, zeolites, silica, or swellable polymers (especially so-called super absorber polymers).
  • Swellable polymers are preferably understood to mean water-swellable polymers, e.g. Polyvinyl alcohol with a high degree of hydrolysis or high molecular weight hydroxypropylmethyl cellulose.
  • the powdered carrier particles preferably have a particle size of less than 100 ⁇ m.
  • auxiliaries in the production of the powdery liquid-filled particles are: table salt, sugar, dextrin, proteins, titanium dioxide, fats, polyglycols, magnesium stearate, highly disperse silicon dioxide, glutate, lime, kaolin, polylactic acid, fats, waxes, verdik - kungs ittel.
  • emulsifiers such as phospholipids, in particular lecithin, or partial glycerides can also be added during the production.
  • the inert gases are primarily carbon dioxide, gaseous
  • Hydrocarbons e.g. methane, ethane, propane, butane
  • Ether nitrogen, nitrous oxide, ammonia or noble gases.
  • the particles loaded by the described process are also separated from the excess active substance liquid, for example by sedimentation or filtration.
  • the further processing and use of these particles, in particular the production of the dosage forms according to the invention, can be carried out in a corresponding manner as described above for the former form of the particles.
  • the particles, or at least a partial amount thereof are provided with a coating of fat and / or water-soluble substances after the active substance loading.
  • a coating of fat and / or water-soluble substances after the active substance loading.
  • Coats come among other things Considerable: film formers (e.g. polyacrylates, polymethacrylates), polyethylene glycols, vegetable or animal oils, liquid paraffin, polyvinylpyrrolidone, cellulose derivatives.
  • film formers e.g. polyacrylates, polymethacrylates
  • polyethylene glycols e.g. polyethylene glycols
  • vegetable or animal oils e.g. polyethylene glycols
  • liquid paraffin e.g., polyvinylpyrrolidone, cellulose derivatives.
  • the particles can be provided with an enteric coating which is soluble in the small intestine after being loaded with active ingredient. This is particularly recommended for active ingredients that Irritating mucous membrane or would be decomposed under the influence of gastric juice.
  • Suitable enteric coatings which are soluble in the small intestine are, in particular, cellulose derivatives such as cellulose acetate phthalate, cellulose acetate succinate and hydroxyethyl cellulose, methacrylic acid / ethyl acrylate copolymers and certain copolymers of acrylic acid, methacrylic acid and their esters, which are known to the person skilled in the art.
  • the present invention particularly relates to flat, orally administered dosage forms, e.g. wafer-like shapes; this is the most preferred embodiment.
  • the thickness of these flat pharmaceutical forms is preferably in the size range from 0.1 to 5 mm, particularly preferably in the range from 0.1 to 1 mm.
  • the proportion of the liquid active ingredient can be up to 60 wt. -5s, depending on the thickness and the type of carrier matrix, even up to 80 wt.? S.
  • the materials for the carrier matrix are in particular water-soluble and in particular film-forming polymers, or mixtures of such polymers, which may be synthetic or partially synthetic polymers or biopolymers of natural origin.
  • Particularly suitable are polymers which are preferably selected from the group comprising cellulose derivatives, polyvinyl alcohol, polyacrylate and polyvinyl pyrrolidone.
  • cellulose derivatives hydroxypropyl methyl cellulose, carboxymethyl cellulose, hydroxypropyl cellulose and methyl cellulose are particularly preferred.
  • water-soluble polysaccharides that are of vegetable or microbial origin. especially pullulan, xanthan, alginates, starch, dextrans and pectins. Proteins, preferably gelatin or other gel-forming proteins, are also suitable.
  • the principle according to the invention can also be used advantageously in the production of other flat oral dosage forms such as tablets, dragées, chewable tablets, lozenges, lozenges or sublingual tablets.
  • the basic substances, binders and other auxiliaries which are suitable for the production of these pharmaceutical forms and which in these cases are used to produce the carrier matrix are known to the person skilled in the art (for example starch, starch hydrolysates, cellulose, cellulose derivatives, sugar, gelatin, synthetic polymers such as Polyethylene glycols, polyvinyl alcohols, polyvinyl pyrrolidones, poly (meth) acrylates).
  • the invention also includes pharmaceutical forms in which the active substance-loaded particles are applied to at least one surface of a pharmaceutical form. This can be done by providing the surface of the carrier matrix with pressure-sensitive adhesive properties.
  • a further preferred embodiment of the invention relates to oral dosage forms which have mucoadhesive properties and which enable transmucosal administration of active substances.
  • these can be dosage forms to be applied buccally or sublingually.
  • the carrier matrix itself has mucoadhesive properties, or that at least one surface of the dosage form is equipped with mucoadhesive properties, for example a mucoadhesive coating.
  • Mucoadhesive properties can be achieved, for example, by using or adding substances such as starch, carboxymethyl cellulose sodium, carboxymethyl cellulose, hydroxypropyl cellulose, polyacrylic acid, polyvinyl pyrrolidones, polyethylene. Lenoxide polymers, ethyl or propyl cellulose, alginates, pecine or natural gums can be achieved.
  • the oral preparations according to the invention in particular flat pharmaceutical forms such as "wafers", can be formulated as preparations which can disintegrate in aqueous media (e.g. saliva).
  • aqueous media e.g. saliva
  • disintegrants e.g. Starch, cross-linked polyvinyl pyrrolidones.
  • the carrier matrix in which the active ingredient-containing particles are embedded can optionally contain auxiliary substances in addition to the matrix-forming base materials.
  • Fillers are used for this (eg SiO 2); Thickeners (eg alginates, pectin); Dyes (eg quinoline yellow or Ti ⁇ ) disintegrants, in particular disintegrants which draw water into the matrix and detonate the matrix from the inside (eg Aerosil); Emulsifiers (eg polyethoxylated sorbitan fatty acid esters such as TWEEN ® or polyethoxylated fatty alcohols such as BRIJ ® ); Plasticizers (eg polyethylene glycol, glycerin); Sweeteners (eg aspartame, saccharin); Preservatives (e.g. sorbic acid and its salts) and flavorings are also considered.
  • Fillers are used for this (eg SiO 2); Thickeners (eg alginates, pectin); Dyes (eg quinoline yellow or Ti
  • the carrier matrix can be, for example, hydrophilic swelling agents such as polyhydroxyalkyl methacrylates with a molecular weight of 5,000 to 5,000,000, mixtures of agar and carboxymethyl cellulose, swellable agents consisting of methyl cellulose mixed with weakly cross-linked agar, tragacanth , Gelatin or swellable ion exchange resins can be added.
  • hydrophilic swelling agents such as polyhydroxyalkyl methacrylates with a molecular weight of 5,000 to 5,000,000
  • mixtures of agar and carboxymethyl cellulose mixtures of agar and carboxymethyl cellulose
  • swellable agents consisting of methyl cellulose mixed with weakly cross-linked agar, tragacanth , Gelatin or swellable ion exchange resins can be added.
  • Active substances are understood to mean all medicinal substances used in the field of human or veterinary medicine, including vitamins, enzymes and hormones, as well as active substances for free metallic treatments and flavors or aromas.
  • the invention relates to active pharmaceutical ingredients that can be absorbed by the oral mucosa or that can be absorbed via the gastrointestinal tract. Active ingredients that are in the liquid state are particularly preferred; in addition, the invention is applicable to a large number of further active ingredients which can be brought into a liquid form, for example as a solution, dispersion, suspension or emulsion.
  • the active ingredient (s) contained in the pharmaceutical forms according to the invention can be released in various ways. After oral administration or application to a mucosal surface, the active ingredient can diffuse out of the particles and subsequently be absorbed. If the dosage form is designed to be disintegrable, the particles can first be released as such, and then the active ingredient contained in the particles can be released. If the particles are made from biodegradable material, the release can be influenced or accelerated by breaking down the particle material. In this way, the invention opens up many possibilities for controlling the release of active substance.
  • the invention further comprises methods for the production of oral pharmaceutical forms, starting from liquid active substances, active substance solutions or preparations.
  • the dosage forms according to the invention can preferably be obtained by first providing a carrier matrix material suitable for the desired pharmaceutical form, as described above, preferably in liquid or semi-solid form (for example as a solution or melt), or as a gel. Furthermore, a liquid active substance, an active substance solution or a liquid active substance preparation is provided. If the active substance is not itself liquid. it is dissolved, dispersed or suspended in a pharmaceutically acceptable solvent or solvent mixture suitable for the active ingredient.
  • the liquid active substance preparations can also contain combinations of active substances.
  • the liquid active substance or the active substance solution is mixed with particles which are open-porous or have capillary spaces (as described above), as a result of which the pore or capillary spaces are filled with active substance liquid or solution.
  • This process can be supported by adding surfactants or emulsifiers.
  • the particles loaded with active substance liquid are introduced into the carrier material mentioned in the first step and incorporated and mixed therein so that the particles are homogeneous are distributed in the carrier matrix.
  • wetting agents surfactants, e.g. SDS
  • emulsifiers e.g. lecithin
  • auxiliaries as mentioned above can be added and incorporated, and further drying can be carried out in order to produce the desired consistency of the carrier matrix by removing solvent.
  • dosage forms can be carried out using conventional methods, e.g. Pressing, punching or coating.
  • wafer-like dosage forms can be obtained by pouring or pouring out the still liquid carrier matrix mass with the porous particles dispersed therein in a thin layer onto a suitable foil-like base (eg polyester foil, PET) is coated. After drying, individual wafers can be produced by cutting or punching.
  • a suitable foil-like base eg polyester foil, PET
  • the porous particles loaded with active ingredient can be provided with a coating before embedding in the carrier matrix, which prevents diffusion of the active ingredient into the matrix (or into the solvent) as long as it has not yet dried or solidified.
  • the particles can be provided with a fat and / or water-soluble coating or with an enteric coating before embedding.
  • This active ingredient-containing powder is then embedded in the carrier material, which is in liquid or semi-solid form; further processing takes place as described above.
  • this manufacturing method can also be modified in various ways, for example by applying coatings or coatings to the particles before embedding.
  • the present invention thus advantageously makes it possible to produce oral dosage forms, in particular flat dosage forms, which can have a high content of an active ingredient in liquid form.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Zoology (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une forme pharmaceutique pour l'administration orale de substances actives, comprenant une matrice support et au moins une substance active. L'invention se caractérise en ce que la forme pharmaceutique présente une matrice support comprenant une pluralité de particules à pores ouverts ou à espaces capillaires, lesdites particules servant de réservoir de substances actives et contenant au moins une substance active.
EP02791449A 2001-07-27 2002-07-11 Formes pharmaceutiques plates pour administration orale comprenant des particules contenant des substances actives Withdrawn EP1411893A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10136781 2001-07-27
DE10136781A DE10136781B4 (de) 2001-07-27 2001-07-27 Flache orale Darreichungsformen mit wirkstoffhaltigen Partikeln
PCT/EP2002/007717 WO2003011248A1 (fr) 2001-07-27 2002-07-11 Formes pharmaceutiques plates pour administration orale comprenant des particules contenant des substances actives

Publications (1)

Publication Number Publication Date
EP1411893A1 true EP1411893A1 (fr) 2004-04-28

Family

ID=7693389

Family Applications (1)

Application Number Title Priority Date Filing Date
EP02791449A Withdrawn EP1411893A1 (fr) 2001-07-27 2002-07-11 Formes pharmaceutiques plates pour administration orale comprenant des particules contenant des substances actives

Country Status (6)

Country Link
US (1) US20040241231A1 (fr)
EP (1) EP1411893A1 (fr)
JP (1) JP2005526688A (fr)
KR (1) KR20040025704A (fr)
DE (1) DE10136781B4 (fr)
WO (1) WO2003011248A1 (fr)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008023999A1 (fr) * 2006-08-22 2008-02-28 Encoate Holdings Limited Composition permettant d'améliorer la libération d'un agent actif
US20120090539A1 (en) * 2010-10-15 2012-04-19 Wildcat Discovery Technologies Liquid infusion device and method
DE102017107468B4 (de) * 2017-04-06 2019-02-21 Lts Lohmann Therapie-Systeme Ag Verfahren zur herstellung eines, insbesondere oralen, wirkstofflaminats und wirkstofflaminat, insbesondere orales wirkstofflaminat

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3972995A (en) * 1975-04-14 1976-08-03 American Home Products Corporation Dosage form
US4175326A (en) * 1977-10-26 1979-11-27 Forsyth Dental Infirmary For Children Hollow-fiber devices for and a method of the treament and diagnosis of oral diseases
US4597959A (en) * 1982-04-30 1986-07-01 Arthur Barr Sustained release breath freshener, mouth and palate coolant wafer composition and method of use
EP0205336B1 (fr) * 1985-06-11 1991-09-11 Teijin Limited Préparation pharmaceutique orale à effet entretenn
JP2702953B2 (ja) * 1988-01-30 1998-01-26 オリンパス光学工業株式会社 薬液含浸セラミックス
US5139787A (en) * 1989-01-19 1992-08-18 Wm. Wrigley Jr. Company Gum composition containing dispersed porous beads containing active chewing gum ingredients and method
US6066337A (en) * 1994-01-27 2000-05-23 The Board Of Regents Of The University Of Oklahoma And Janssen Pharmaceutica, Inc. Method for producing a rapidly dissolving dosage form
US5595761A (en) * 1994-01-27 1997-01-21 The Board Of Regents Of The University Of Oklahoma Particulate support matrix for making a rapidly dissolving tablet
US5516522A (en) * 1994-03-14 1996-05-14 Board Of Supervisors Of Louisiana State University Biodegradable porous device for long-term drug delivery with constant rate release and method of making the same
EP0685164A1 (fr) * 1994-06-03 1995-12-06 Asama Chemical Co., Ltd. Additif alimentaire
US5660848A (en) * 1994-11-02 1997-08-26 The Population Council, Center For Biomedical Research Subdermally implantable device
US6949264B1 (en) * 1996-11-27 2005-09-27 Wm. Wrigley Jr. Company Nutraceuticals or nutritional supplements and method of making
ES2163138T3 (es) * 1997-10-06 2002-01-16 Adalbert Raps Stiftung Procedimiento para fabricar un producto en forma de polvo a partir de una sustancia liquida o de una mezcla de sustancias.
US6635281B2 (en) * 1998-12-23 2003-10-21 Alza Corporation Gastric retaining oral liquid dosage form
US6180682B1 (en) * 1999-01-26 2001-01-30 Virgil A. Place Buccal drug delivery system for use in male contraception
WO2001039836A1 (fr) * 1999-12-01 2001-06-07 Natco Pharma Limited Composition pharmaceutique lyophilisee a action rapide s'administrant par voie orale utilisee pour traiter la migraine
US20030015687A1 (en) * 2001-01-08 2003-01-23 Sud-Chemie Ag Plate-shaped pressed bodies

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO03011248A1 *

Also Published As

Publication number Publication date
US20040241231A1 (en) 2004-12-02
DE10136781A1 (de) 2003-02-20
KR20040025704A (ko) 2004-03-24
JP2005526688A (ja) 2005-09-08
DE10136781B4 (de) 2008-03-06
WO2003011248A1 (fr) 2003-02-13

Similar Documents

Publication Publication Date Title
DE69022876T2 (de) Arzneimittelformulierungen mit verzögerter Wirkstoffabgabe.
DE3586600T2 (de) Dosierungsform eine vielzahl mit einer diffusionshuelle ueberzogener einheiten enthaltend.
EP1110544B1 (fr) Méthode pour fabriquer une préparation orale masquant le goût
AT392901B (de) Verfahren zur herstellung einer granulaeren form mit verzoegerter freisetzung von pharmazeutisch wirksamen substanzen
DE3587274T2 (de) Dosierungsform eine vielzahl mit einer diffusionshuelle ueberzogener einheiten enthaltend.
DE60020343T2 (de) Cilostazol enthaltende zubereitung
DE3872739T2 (de) Arzneimittel mit langsamer freisetzung.
EP0917463A2 (fr) Formulations de tramadol a unites multiples
EP1509200B1 (fr) Preparations pouvant etre dissoutes sous forme de film pour la liberation de substances actives et procede de production desdites preparations
DE4200821A1 (de) Geschmacksmaskierte pharmazeutische mittel
DE19940944A1 (de) Retardierte, orale, pharmazeutische Darreichungsformen
DE102017112527B4 (de) Schnell zerfallende Schaumwafer mit hohem Flächengewicht
DE10107659A1 (de) Mucoadhäsive zerfallsfähige Arzneizubereitung zur Wirkstoffverabreichung in der Veterinär- und Humanmedizin
EP2415460A1 (fr) Formulations pour l'administration orale de prégabaline
EP0469328B1 (fr) Procédé pour la préparation de particules de petites dimensions à forte teneur en Etofibrate et à libération contrôlée, utilisation et formes administrables oralement desdites particules
DE60017361T2 (de) Direktverpressbare matrix zur kontrollierten abgabe von einmaltäglichen dosen von clarithromycin
DE60204125T2 (de) Verfahren zur herstellung von metoprolol enthaltenden mikropartikeln
DD235829A5 (de) Verfahren zur herstellung einer poroesen galenischen form
EP1414407B1 (fr) Formes posologiques renfermant des particules contenant un principe actif, destinees a etre utilisees sur la peau ou les muqueuses
DE10136781B4 (de) Flache orale Darreichungsformen mit wirkstoffhaltigen Partikeln
DE69113976T2 (de) Verfahren zur galenischen herstellung eines therapeutischen mittels, insbesondere auf aspirinbasis.
EP2632443B1 (fr) Préparation de films orodispersibles
DE102017127434A1 (de) Taschenförmige oral auflösende Filme mit hoher Wirkstoffbeladung
DE69209083T2 (de) System zur peroralen arzneimittelabgabe
WO2007079758A1 (fr) Granulés contenant un noyau avec un support soluble dans l'eau

Legal Events

Date Code Title Description
PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

17P Request for examination filed

Effective date: 20040101

AK Designated contracting states

Kind code of ref document: A1

Designated state(s): AT BE BG CH CY CZ DE DK EE ES FI FR GB GR IE IT LI LU MC NL PT SE SK TR

17Q First examination report despatched

Effective date: 20040928

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE APPLICATION HAS BEEN WITHDRAWN

18W Application withdrawn

Effective date: 20110907