Schering Aktiengesellschaft

Alrise Biosystems Gmbh

Inhale Therapeutic Systems, Inc.

Actipac Biosystems Gmbh

Nektar Therapeutics

Ferring B.v.

Albayrak, Celal

Celal Albayrak

Johannes Wilhelm Tack

Georg R&ouml;ssling

Matthias Rothe

Georg Rossling

Reinhard Schmitz

Joachim Siegert

Georg R{haeck Over (o)}ssling

Georg Ro/ Ssling

Provided is a process for the production of nano- and/or microparticles containing a therapeutically active agent embedded in a polymer matrix or encapsulated by a polymer shell, and nano- and/or microparticles obtainable by the process, said process comprising the steps of:

Process for the preparation of drug loaded microparticles

Provided is a process for the production of nano- and/or microparticles containing a therapeutically active agent embedded in a polymer matrix or encapsulated by a polymer shell, and nano- and/or microparticles obtainable by the process, said process comprising the steps of: a) providing a solution of a polymer selected from polylactide, polyglycolide, and polyester copolymers comprising copolymerized units of lactic acid and/or glycolic acid in an organic solvent SI having limited water solubility: b) providing a solution or dispersion of a therapeutically active agent in as solvent or mixture of organic solvents S2 comprising at least 50 vol. % benzyl alcohol, c) combining the solution or the solution and suspension provided in step a) and step b) to provide an organic phase which comprises dissolved polymer and dissolved therapeutically active agent in a mixture of the organic solvents S I and S2; d) agitating the organic phase provided in step c) in a vessel and adding an aqueous surfactant solution to the agitated organic phase in a volume ratio of at least 2:1 in terms of the total volume of the aqueous surfactant solution to the total volume of the organic phase as provided in step c), thus causing the formation of a dispersion containing a continuous aqueous phase and a discontinuous organic phase; and e) allowing the spontaneous formation of the nano- and/or microparticles via transfer of organic solvent from the discontinuous organic phase into the continuous aqueous phase directly after the dispersion has been formed.

The invention relates to nano- or microparticles containing an active substance embedded in a polymer matrix and to a method for their production, comprising the steps of: a) effecting precipitation of an active substance in a solution which comprises a polymer dissolved in an organic solvent to obtain a suspension of the active substance, b) mixing the obtained suspension with an aqueous surfactant solution and solidifying the polymer to obtain a suspension of nano- or microparticles which contain an active substance.

Microparticles and method for their production

Microparticles and a method for their production is described. The process of the present invention provides a simple, quick, and efficient one-pot process for the production of microparticles containing a hydrophilic active agent of various and uniform morphologies, including microcapsules, microspheres, and microsponges. The microparticles are preferably used for pharmaceutical applications.

Induced phase transition method for the production of microparticles containing hydrophilic active agents

Microparticles and a method for their production is described. The process of the present invention provides a simple, quick, and efficient one-pot process for the production of microparticles containing a non-water soluble active agent. The microparticles are preferably used for pharmaceutical applications and comprise at least 80 wt % microspheres.

Induced phase transition method for the production of microparticles containing hydrophobic active agents

The invention relates to a process for the production of morphologically uniform microcapsules that contain peptides, proteins or other water-soluble biologically active substances as active ingredients as well as microcapsules that are produced according to this process with a degree of concentration of between 3 to 30% by weight and a diameter &lE;8 &mgr;m. According to the invention, biodegradable polymers are dissolved in a halogen-free solvent or solvent mixture, and the buffered active ingredient solution, which has a pH of between 6.0 to 8.0, is dispersed into this solution. Then, an aqueous solution that contains a surfactant (W/O/W-emulsion) is added to this W/O-emulsion, and the solvent is removed. The microcapsules that are produced with this process do not show any tendency toward agglomeration. The encapsulation efficiency of the process is approximately 90 to 95%.

Process for the production of morphologically uniform microcapsules and microcapsules that are produced according to this process

The invention relates to a process for the production of gaseous microparticles for ultrasonic diagnosis, whose wall material is built up from polyesters of &agr;-, &bgr;- or &ggr;- hydroxycarboxylic acids, particles that are produced according to this process, as well as their use in medical diagnosis.

Process for producing polymeric microparticles, microparticles produced by said process and the use of such particles in medical diagnostics

Method of producing morphologically uniform microcapsules and microcapsules produced by this method

The invention relates to gaseous microparticles for ultrasonic diagnosis, whose wall material is built up from block copolymers of polyesters of &agr;-, &bgr;- or &ggr;-hydroxycarboxylic acids with linear or star-shaped polyethylene glycols and optionally liquid crystals or whose wall material is built up from polyesters of &agr;-, &bgr;- or &ggr;-hydroxycarboxylic acids and liquid crystals, media that contain these particles for ultrasonic diagnosis, as well as a process for the production of the media and particles.

Gaseous microparticles for ultrasonic diagnosis and process for their production

Use of methylenemalondiester derivatives for the production of

A method of using cavitate- or clathrate-forming host/guest complexes for the preparation of contrast media in ultrasonic examination is provided. The host/guest complexes have a host which dissolves in a liquid carrier, releasing the guest (inert gas). With such contrast media, it is possible to diagnose blood and its flow conditions in the heart, and other organs, such as the myocardium, liver, spleen, and kidneys. Other internal systems such as the urinary ducts, the gastrointestinal tract, joints, and eyes can also be imaged.

Preparation comprising cavitate-  or clathrate-forming host/guest

Microparticles comprising biodegradable polymers, characterized in that they are synthesized from polymerizable aldehydes, which optionally contain additives and/or crosslinkers capable of copolymerization, optionally surfactants or surfactant mixtures, gases and/or highly volatile liquids in free or bound form, coupling agents, optionally biomolecules or macromolecules bound by these coupling agents as well as optionally diagnostically or therapeutically effective components, are suitable as ultrasonic contrast media.

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Berlin, Germany

Celal Albayrak