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WO2008080773A1 - Procédé de production de formes galéniques solides contenant des copolymères greffés - Google Patents

Procédé de production de formes galéniques solides contenant des copolymères greffés Download PDF

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Publication number
WO2008080773A1
WO2008080773A1 PCT/EP2007/063673 EP2007063673W WO2008080773A1 WO 2008080773 A1 WO2008080773 A1 WO 2008080773A1 EP 2007063673 W EP2007063673 W EP 2007063673W WO 2008080773 A1 WO2008080773 A1 WO 2008080773A1
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WO
WIPO (PCT)
Prior art keywords
dosage forms
polyethylene glycol
solid dosage
acid
mixing
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.)
Ceased
Application number
PCT/EP2007/063673
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German (de)
English (en)
Inventor
Karl Kolter
Angelika Maschke
Maximilian Angel
Simone Schillo
Franz-Josef Dietzen
Kathrin MEYER-BÖHM
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.)
BASF SE
Original Assignee
BASF SE
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 BASF SE filed Critical BASF SE
Publication of WO2008080773A1 publication Critical patent/WO2008080773A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers

Definitions

  • the invention relates to a process for the preparation of solid dosage forms by mixing at least one polymeric binder and optionally at least one active ingredient and optionally conventional additives to form a plastic mixture and shaping.
  • the invention relates to a process for the preparation of solid pharmaceutical forms.
  • Graft copolymers of polyvinyl alcohol and polyethylene glycol are known per se. Their use for pharmaceutical dosage forms is known, for example, from WO 00/18375 or EP-A 1125954.
  • the present invention is therefore a process for the preparation of solid dosage forms by mixing at least one polymeric binder, at least one active ingredient and optionally conventional additives under BiI- Phyg a plastic mixture and shaping, which is characterized in that the polymeric binder is a water-soluble Graft copolymer of polyvinyl alcohol-polyethylene glycol used.
  • the process according to the invention enables the production of solid dosage forms with very rapid release of the active ingredient ("instant release") in a simple and cost-effective manner.
  • Another surprising advantage of the method according to the invention is that even formulations of temperature-sensitive active substances can be prepared gently.
  • the dosage forms prepared according to the invention are very stable.
  • the active substance is often contained in the form of a supersaturated solution, it shows no or very slight crystallization phenomena or changes in the release of active ingredient.
  • the graft copolymer of polyvinyl alcohol-polyethylene glycol stabilizes the active ingredient.
  • the rate of release can be by blending with other polymers such as polyvinylpyrrolidone, crosslinked polyvinylpyrrolidone, copolymers of vinylpyrrolidone and vinyl acetate; Cellulose ethers such as hydroxypropyl cellulose,
  • Hydroxypropylmethylcellulose or hydroxyethylcellulose cross-linked sodium carbonate xymethylcellulose; cross-linked sodium carboxymethyl starch; Polyethylene glycols or ethylene oxide / propylene oxide block copolymers (eg, the Pluronic brands of BASF AG); polyvinyl alcohols; partially saponified polyvinyl alcohols or suitable low molecular weight substances, such as sugar alcohols, sugars, surfactants or salts in a wide range.
  • the substances mentioned can also be used to adjust the solubility of active ingredients in the dosage form.
  • polyoxyethylene fatty acid esters polyoxyethylene fatty alcohol ethers, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbitan fatty alcohol ethers, polyglycerol fatty acid esters, sugar esters, ethoxylated castor oil, hydrogenated ethoxylated castor oil, ethoxylated 12-hydroxystearic acid, sodium lauryl sulfate, sodium dioctylsulfosuccinate.
  • the active ingredient may be in the dosage form in the form of a solid solution or a solid dispersion.
  • the solid solution no particulate agent can be detected, whereas in the solid dispersion, the drug is contained in amorphous or crystalline form.
  • ethylcellulose polyvinyl acetate, acrylate-methacrylate copolymers, for example of Eudragit type (Eudragit RS, RL, NE), the release of delayed.
  • Eudragit RS, RL, NE Eudragit RS, RL, NE
  • Dosage forms are understood here to mean all forms which are suitable for use as medicaments, plant treatment agents, feedstuffs and foods and for the release of fragrances and perfume oils or other cosmetic active ingredients. These include, for example, tablets of any shape, pellets or granules.
  • the dosage forms obtainable according to the invention generally comprise: I 0.1 to 90% by weight, in particular 0.1 to 60% by weight (based on the total weight of the dosage form) of an active substance,
  • additives may also be included.
  • the polymers used according to the invention as binders are accessible in a manner known per se by free-radical polymerization.
  • the preparation is carried out, for example, by means of solution, precipitation, suspension or emulsion polymerization using compounds which form radicals under the polymerization conditions.
  • a graft copolymer which is obtainable by free-radically initiated polymerization of vinyl acetate in the presence of polyethylene glycol as the graft base with subsequent saponification of the ester groups is preferably used in the process according to the invention.
  • Suitable polyethylene glycols have molecular weights of 400 to 50,000, in particular 1500 to 20,000. Polyethylene glycols having molecular weights of 3,000 to 10,000 are particularly preferred as the graft base. Very particular preference is given to polyethylene glycol 6000.
  • the graft copolymers contain from 30 to 98% by weight of polyvinyl alcohol units and from 2 to 70% by weight of polyethylene glycol, preferably from 50 to 90% by weight of polyvinyl alcohol units and from 10 to 50% by weight of polyethylene glycol.
  • graft copolymer of 75% by weight of polyvinyl alcohol units and 25% by weight of polyethylene glycol.
  • the preparation of such graft copolymers is known per se, for example from WO 00/18375, to the disclosure of which reference is made expressly with respect to the preparation.
  • the graft copolymers may have average molecular weights of 5,000 to 500,000 daltons, especially 15,000 to 100,000 daltons.
  • binders such as polymers, copolymers, cellulose derivatives, starch and starch derivatives. Suitable examples are:
  • Polyvinylpyrrolidone PVP
  • copolymers of N-vinylpyrrolidone (NVP) and vinyl esters in particular vinyl acetate, copolymers of vinyl acetate and crotonic acid, partially saponified polyvinyl acetate, polyvinyl alcohol, polyhydroxyalkyl acrylates, polyhydroxyalkyl methacrylates, polyacrylates and polymethacrylates (Eudragit types), copolymers of methyl methacrylate and acrylic acid, polyacrylamides, polyethylene glycols, cellulose esters, cellulose ethers, in particular methylcellulose and ethylcellulose, hydroxyalkylcelluloses, in particular hydroxypropylcellulose, hydroxyalkyl-alkylcelluloses, in particular hydroxypropyl-ethylcellulose, cellulose phthalates, in particular cellulose acetate phthalate and hydroxypropylmethylcellulose phthalate, and mannans, especially galactomannans.
  • PVP Polyvinylpyr
  • polyvinylpyrrolidone copolymers of N-vinylpyrrolidone and vinyl esters
  • polyhydroxyalkyl acrylates polyhydroxyalkylmethacrylates
  • polyacrylates polymethacrylates
  • alkylcelluloses and hydroxyalkylcelluloses are particularly preferred.
  • the polymeric binder which can be used according to the invention is intended to soften under the processing conditions in the total mixture of all components in the range from 50 to 180 ° C., preferably from 60 to 130 ° C.
  • the glass transition temperature of the mixture should therefore be below 180 ° C., preferably below 130 ° C., in particular below 90 ° C. If necessary, it is reduced by conventional, pharmacologically acceptable plasticizing excipients.
  • the amount of plasticizer is at most 30 wt .-%, based on the total weight of binder and plasticizer, so that storage-stable drug forms are formed, which show no cold flow.
  • plasticizers examples include:
  • the concentration of plasticizer is generally 0.5 to 20, preferably 2 to 15 wt .-%, based on the total weight of the mixture.
  • Preferred plasticizers are water, polyethylene glycols, polyoxyethylene-polyoxypropylene block copolymers, propylene glycol, 2-pyrrolidone, N-methylpyrrolidone, triacetin, triethyl citrate, ethoxylated castor oil, hydrogenated ethoxylated castor oil, ethoxylated 12-hydroxystearic acid, polysorbates, polyoxyethylene fatty acid esters and fatty alcohol ethers.
  • Usual galenic auxiliaries whose total amount can be up to 100 wt .-%, based on the polymer, are, for.
  • extenders or fillers such as silicates or silica, magnesium oxide, alumina, titanium oxide, dicalcium phosphate, stearic acid or its salts, for.
  • magnesium or calcium salt methyl cellulose, sodium carboxymethyl cellulose, talc, sucrose, lactose, sugar alcohols such as sorbitol, XyNt, maltitol, isomalt, corn or corn starch, potato flour, polyvinyl alcohol, in particular in a concentration of 0.02 to 50, preferably 0.20 to 20% by weight, based on the total weight of the mixture.
  • Lubricants such as aluminum and calcium stearate, talc and silicones, in a concentration of 0.1 to 5, preferably 0.1 to 3 wt .-%, based on the total weight of the mixture.
  • Plasticizers such as animal or vegetable fats, in particular in hydrogenated form and those which are solid at room temperature. These fats preferably have a melting point of 5O 0 C or higher. Preferred are triglycerides of the C12, C14, C16 and Ci8 fatty acids. Even waxes, such as carnauba wax or beeswax, are useful. These fats and waxes may advantageously be admixed alone or together with mono- and / or diglycerides or phosphatides, in particular lecithin. The mono- and diglycerides are preferably derived from the fatty acids mentioned above. acid types. The total amount of fats, waxes, mono-, diglycerides and / or lecithins is 0.1 to 30, preferably 0.1 to 5 wt .-%, based on the total weight of the mass for each layer;
  • Dyes such as azo dyes, organic or inorganic pigments or dyes of natural origin, with inorganic pigments in a concentration of 0.001 to 10, preferably 0.5 to 3 wt .-%, based on the total weight of the mixture are preferred;
  • Stabilizers such as antioxidants, light stabilizers, hydroperoxide destroyers, radical scavengers, stabilizers against microbial attack.
  • wetting agents for example, H. Sucker et al., Pharmazeutician Technologie, Thieme-Verlag, Stuttgart 1978.
  • auxiliaries are also to be understood as meaning substances for producing a solid solution of the active substance.
  • auxiliaries are, for example, pentaerythritol and pentaerythritol tetraacetate, polymers such as. As polyethylene or polypropylene and their block copolymers (poloxamers), phosphatides such as lecithin, homo- and copolymers of vinylpyrrolidone, surfactants such as polyoxyethylene-40-stearate and citric and succinic acid, bile acids, sterols and others such. In J.L. Ford, Pharm. Acta HeIv. 61, 69-88 (1986).
  • Adjuvants also include additions of bases and acids for controlling the solubility of an active ingredient (see, for example, K. Thoma et al., Pharm. Ind. 5J [, 98-101 (1989)].
  • Active substances within the meaning of the invention are to be understood as meaning all substances having a physiological action, provided that they do not decompose under the processing conditions. These are, in particular, active pharmaceutical ingredients (for humans and animals), active ingredients for plant treatment, insecticides, feed and food ingredients, fragrances and perfume oils.
  • active pharmaceutical ingredients for humans and animals
  • active ingredients for plant treatment active ingredients for plant treatment
  • insecticides active ingredients for plant treatment
  • insecticides active ingredients for plant treatment
  • fragrances and perfume oils fragrances and perfume oils.
  • the amount of active ingredient per unit dose and the Concentration may vary widely depending on the efficacy and rate of release. The only condition is that they are sufficient to achieve the desired effect. Thus, the concentration of active ingredient in the range of 0.1 to 95, preferably from 20 to 80, in particular 30 to 70 wt .-% are. Also drug combinations can be used. Active substances within the meaning of the invention are also vitamins and minerals.
  • the vitamins include the vitamins of the A group, the B group, which in addition to Bi, B2, B ⁇ and B12 and nicotinic acid and nicotinamide and compounds with vitamin B properties are understood, such.
  • Active substances within the meaning of the invention also include peptide therapeutics.
  • For plant treatment agents include, for. Vinclozolin, epoxiconazole and quinmerac.
  • the process according to the invention is suitable, for example, for processing the following active substances:
  • a plastic mixture of the components is provided, which is then subjected to a shaping step.
  • the mixing of the components and the plasticization of the mixture can be done in different ways.
  • Plastification means softening the mixture by the action of pressure, shear forces, temperature and or softening. Softening preferably takes place by combined action of shear forces and temperature increase, in particular in combination with plasticizers.
  • the mixing can take place before, during and / or after the formation of the plastic mass.
  • the components may first be mixed and then plasticized or simultaneously mixed and melted. Often there is one more Homogenization of the plastic mixture to obtain a highly dispersed distribution of the active ingredient.
  • the sensitive active ingredient (s) may be used in solid form or as a solution or dispersion.
  • the components are used as such in the manufacturing process. However, they can also be in liquid form, i. H. as a solution, suspension or dispersion are used.
  • the solvent used for the liquid form of the components is primarily water or a water-miscible organic solvent or a mixture thereof with water.
  • useful solvents are also water-immiscible or miscible organic solvents.
  • Suitable water-miscible solvents are in particular C 1 -C 4 -alkanols, such as ethanol, isopropanol or n-propanol, polyols, such as ethylene glycol, glycerol and polyethylene glycols.
  • Suitable water-immiscible solvents are alkanes such as pentane or hexane, esters such as ethyl acetate or butyl acetate, chlorinated hydrocarbons such as methylene chloride and aromatic hydrocarbons such as toluene and xylene.
  • Another useful solvent is liquid CO2.
  • solvent which solvent is used in an individual case depends on the component to be absorbed and its properties.
  • pharmaceutical agents are often used in the form of a salt, which is generally water-soluble.
  • Water-soluble active substances can therefore be used as aqueous solution or, preferably, be taken up in the aqueous solution or dispersion of the binder. The same applies to active substances which are soluble in one of the solvents mentioned when the liquid form of the components used is based on an organic solvent.
  • plasticizing and / or mixing takes place in a device customary for this purpose.
  • mixing apparatus As a mixing apparatus in particular those devices are useful, which are used in the plastic technology for mixing. Suitable devices are described for example in "mixing in the production and processing of plastics", H. Pahl, VDI-Verlag, 1986. Particularly suitable mixing apparatuses are extruders and dynamic and static mixers, and stirred tank, single-shaft agitators with stripping devices, especially so-called paste agitators, multi-shaft Stirrers, in particular PDSM mixers, solid mixers and preferably mixed kneading reactors (eg ORP, CRP, AP, DTB from List or Reactotherm from Krauss-Maffei or Ko-Kneader from Buss), Doppelmüldenkneter (trough mixer) and Stamp mixer (internal mixer) or rotor / stator systems (eg Dispax from IKA).
  • mixed kneading reactors eg ORP, CRP, AP, DTB from List or Reactotherm from Kra
  • Powdered components may be in free feed, e.g. B. be introduced via a differential dosing.
  • Plastic compounds can be fed directly from an extruder or fed via a gear pump, which is particularly advantageous for high viscosities and high pressures.
  • Liquid media can be added via a suitable pump set.
  • the mixture obtained by mixing and / or softening the binder, the active ingredient and optionally the additive or the additives is doughy to viscous (thermoplastic) or liquid and therefore extrudable.
  • the glass transition temperature of the mixture is below the decomposition temperature of all components contained in the mixture.
  • the process steps of mixing and plasticizing can be carried out in the same apparatus or in two or more separately operating devices.
  • the preparation of a premix can be carried out in one of the usual mixing devices described above.
  • Such a premix can then be directly, z. B. in an extruder, fed and then optionally extruded with the addition of other components.
  • the process according to the invention makes it possible to use single-screw extruders, intermeshing screw extruders or even multi-screw extruders, in particular twin-screw extruders, rotating in the same direction or in opposite directions and optionally equipped with kneading disks as extruders.
  • the extruders are generally equipped with an evaporation section.
  • twin-screw extruders are particularly preferred.
  • the inventive method is usually carried out by plasticizing at elevated temperature, preferably at temperatures of 60 to 130 ° (internal temperature).
  • the nozzle design is carried out depending on the polymeric binder used and the desired pharmaceutical form.
  • the resulting extrudate is preferably solvent-free.
  • the plastic mixture is usually subjected to a final shaping.
  • a variety of shapes depending on the tool and type of molding, can be generated.
  • the extruded strand can be between a strip and a roll, between two strips or between two rolls, as described in EP-A-358 105, or by calendering in a calender with two forming rolls, See, for example, EP-A-240 904.
  • Hot granulation typically results in lenticular dosage forms (tablets) of 1 to 10 mm in diameter, while cold granulation is normally associated with cylindrical products of a length to length ratio
  • Diameter of 1 to 10 and a diameter of 0.5 to 10 mm leads.
  • multilayer dosage forms can be prepared, for example, oblong tablets, dragees, lozenges and pellets. The resulting granules can then - optionally after grinding - are compressed in the usual way to tablets.
  • Micropastils can be made by the Rotoform-Sandvik process. These Dosage forms can be rounded in a subsequent process step by conventional methods and / or provided with a coating. Suitable materials for film coatings are z.
  • polyacrylates such as the Eudragit types
  • cellulose esters such as the Hydroxypropylcellulosephthalate
  • cellulose ethers such as ethyl cellulose, hydroxypropylmethyl cellulose or hydroxypropyl cellulose.
  • multilayer pharmaceutical forms can also be produced by co-extrusion, in which case several mixtures of the components described above are combined during extrusion in a tool in such a way that the desired layer structure of the multilayered pharmaceutical form results.
  • different binders are used for different layers.
  • Multilayer dosage forms preferably comprise two or three layers. They may be in open or closed form, especially as open or closed multilayer tablets. At least one of the layers contains at least one pharmaceutical agent. It is also possible to incorporate another active ingredient in another layer. This has the advantage that two incompatible active ingredients can be processed or that the release characteristics of the active ingredient can be controlled.
  • the molding is carried out by coextrusion, wherein the mixtures are led out of the individual extruders or other aggregates in a common co-extrusion tool and discharged.
  • the shape of the coextrusion tools depends on the desired pharmaceutical form. For example, tools with a flat outlet gap, so-called slot dies, and tools with nikringspaltförmigem outlet cross section are suitable.
  • solid solutions is familiar to the expert, for example from the literature cited above.
  • the active ingredient is molecularly dispersed in the polymer.
  • the graft polymers were processed by the process according to the invention without crosslinking.
  • the skilled person would have expected due to the structure of the graft polymers under the stress of temperature and shear forces crosslinking with dehydration.
  • the following examples are intended to illustrate the process of the invention without, however, limiting it.
  • the extruder used was a co-rotating twin-screw extruder ZSK 25 with a screw diameter of 25 mm, consisting of 5 zones (wefts) and provided with a collection device, a deaeration device and a perforated nozzle plate. Each zone was individually heated or cooled. The temperature profile was kept constant throughout.
  • the plasticized mass was extruded through a 2-hole die with a hole diameter of 4 mm, at a screw speed of 100 rpm and a throughput of 2 kg / h.
  • the emerging strands were granulated by means of hot stripping, extended to a conveyor belt, cooled and then comminuted to a particle diameter of less than 0.8 mm.
  • the graft polymer used was a polymer composed of 75% by weight of polyvinyl alcohol and 25% by weight of polyethylene glycol units (PEG 6000) having a saponification degree of 94 mol%, MW 45,000 daltons.
  • PEG 6000 polyethylene glycol units
  • the granules according to Examples 1 to 9 were filled in quantities of 500 mg into hard gelatine capsules and the release was tested at pH 6.8 (phosphate buffer), 37 ° C. and 100 rpm in a paddle apparatus according to USP 28. In all cases, the drug was completely released after 45 min.

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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Abstract

L'invention concerne un procédé de production de formes galéniques solides par mélange d'au moins un liant polymère, d'au moins un agent actif et éventuellement d'additifs usuels pour obtenir un mélange plastique et le façonner. L'invention est caractérisée en ce que le liant polymère utilisé est un copolymère greffé aqueux à base de polyvinylalcool-polyéthylèneglycole.
PCT/EP2007/063673 2006-12-29 2007-12-11 Procédé de production de formes galéniques solides contenant des copolymères greffés Ceased WO2008080773A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06127335.5 2006-12-29
EP06127335 2006-12-29

Publications (1)

Publication Number Publication Date
WO2008080773A1 true WO2008080773A1 (fr) 2008-07-10

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009118356A3 (fr) * 2008-03-25 2010-02-18 Formac Pharmaceuticals N.V. Procédé de préparation de dispersions solides
US9439971B2 (en) 2008-09-25 2016-09-13 Basf Se Use of polyether-based and vinyl monomer-based copolymers as binders for dosing forms comprising solid active ingredients
US9789065B2 (en) 2008-10-07 2017-10-17 Basf Se Process for producing oral dosage forms with controlled release

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD99911A1 (fr) * 1972-11-07 1973-09-05
DE19814739A1 (de) * 1998-04-02 1999-10-07 Basf Ag Verwendung von Polyalkylenoxid-haltigen Pfropfpolymerisaten als Solubilisatoren
WO2000018375A1 (fr) * 1998-09-30 2000-04-06 Basf Aktiengesellschaft Utilisation de polymerisats hydromiscibles ou hydrodispersibles contenant des polyethers comme agent de recouvrement, liant et/ou substance auxiliaire filmogene dans des formes d'administration pharmaceutiques
WO2004060298A2 (fr) * 2002-12-30 2004-07-22 Sarnoff Corporation Films a dissolution rapide destines a l'administration de medicaments
WO2005009386A2 (fr) * 2003-07-24 2005-02-03 Smithkline Beecham Corporation Films a dissolution orale
WO2006029787A1 (fr) * 2004-09-13 2006-03-23 Basf Aktiengesellschaft Comprimes buccaux se desintegrant
WO2007065619A2 (fr) * 2005-12-08 2007-06-14 Lts Lohmann Therapie-Systeme Ag Cachet alveolaire constitue de copolymere greffe d'alcool polyvinylique et de polyethyleneglycol

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DD99911A1 (fr) * 1972-11-07 1973-09-05
DE19814739A1 (de) * 1998-04-02 1999-10-07 Basf Ag Verwendung von Polyalkylenoxid-haltigen Pfropfpolymerisaten als Solubilisatoren
WO2000018375A1 (fr) * 1998-09-30 2000-04-06 Basf Aktiengesellschaft Utilisation de polymerisats hydromiscibles ou hydrodispersibles contenant des polyethers comme agent de recouvrement, liant et/ou substance auxiliaire filmogene dans des formes d'administration pharmaceutiques
WO2004060298A2 (fr) * 2002-12-30 2004-07-22 Sarnoff Corporation Films a dissolution rapide destines a l'administration de medicaments
WO2005009386A2 (fr) * 2003-07-24 2005-02-03 Smithkline Beecham Corporation Films a dissolution orale
WO2006029787A1 (fr) * 2004-09-13 2006-03-23 Basf Aktiengesellschaft Comprimes buccaux se desintegrant
WO2007065619A2 (fr) * 2005-12-08 2007-06-14 Lts Lohmann Therapie-Systeme Ag Cachet alveolaire constitue de copolymere greffe d'alcool polyvinylique et de polyethyleneglycol

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ANONYMOUS: "Kollicoat IR", TECHNICAL INFORMATION BASF, XX, XX, July 2006 (2006-07-01), pages 1 - 12, XP002429201 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009118356A3 (fr) * 2008-03-25 2010-02-18 Formac Pharmaceuticals N.V. Procédé de préparation de dispersions solides
US8216495B2 (en) 2008-03-25 2012-07-10 Formac Pharmaceuticals N.V. Preparation method for solid dispersions
US9439971B2 (en) 2008-09-25 2016-09-13 Basf Se Use of polyether-based and vinyl monomer-based copolymers as binders for dosing forms comprising solid active ingredients
US9789065B2 (en) 2008-10-07 2017-10-17 Basf Se Process for producing oral dosage forms with controlled release

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