Abstract:
The present inventions relates to a pharmaceutical composition comprising, in one dosage form, metamizole, drotaverine, and caffeine, in which metamizole in the said composition is present in the form of a granulate comprising metamizole, and drotaverine and caffeine are present outside the said granulate. The present inventions relates also to a granulate comprising metamizole and a granulate comprising drotaverine, as well as their use.
Abstract:
Embodiments of the disclosure relate generally to formulations, methods, kits, and dosage forms for improved stability of an active pharmaceutical ingredient, wherein the active ingredient comprises a compound of the formula:(I) wherein X is N, Y is H or optionally substituted C 1 -C 6 alkyl; R 4 is morpholine optionally substituted with by C 1 -C 6 alkyl; R 7 is C 1 -C 6 alkyl optionally substituted by one or more F; R 8' is halogen; and R 6 is (II),, wherein R 10 is H, C 1 ,-C 6 alkyl, halogen, CN or CF 3 ; R 12 is H or halogen; R 13 is H, halogen or C1-C 6 alkyl; and R 17 is H, C 1 -C 6 alkyl, (C 1 -C 6 alkyl)-NH 2 ; and, pharmaceutically acceptable salts and free bases thereof, wherein the active ingredient remains in substantially amorphous form after storage of the pharmaceutical formulation for a predetermined time and conditions. In one embodiment the formulations, methods, kits and dosage forms comprising the active pharmaceutical ingredient with improved stability can be used in the treatment of a condition characterized by the dysregulation of one of both of the RAS/RAF/MEK/ERK and PI3 K/AKT/PTEN/mTOR pathways.
Abstract:
The present invention provides a process for manufacturing a co-processed directly compressible excipient for sustained/extended release formulation based on pharmaceutically acceptable inert diluent, hydrophilic swellable polymer and a binder.
Abstract:
The present invention relates to a process to prepare solid pharmaceutical forms comprising a quantity of mesalazine comprised between 75 and 95%, i.e. between 1000 and 1600 mg of drug per dosage unit. Furthermore, the present invention relates to a granulate and/or tablets obtained/obtainable with the process according to the invention, preferably coated to allow the controlled release of the drug. Finally, the present invention relates to the use of the granulate and/or the tablets as a medicament, preferably for the treatment of chronic inflammatory pathologies that preferably affect the intestinal tract.
Abstract:
Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung eines pharmazeutischen Granulats, enthaltend als Wirkstoff Apixaban oder ein Salz davon. Um ein Verfahren bereitzustellen, in welchem der Wirkstoff weitgehend unabhängig von seiner Partikelgrößenverteilung eingesetzt werden kann, wobei mittels des resultierenden Granulats aber dennoch Darreichungsformen hergestellt werden können, die ausreichend konsistente Wirkstoff-Auflösungsraten für eine unverzögerte Wirkstofffreisetzung zeigen, wird vorgeschlagen ein Verfahren der gattungsgemäßen Art umfassend die Schritte des a) Bereitstellens eines Lösungsmittels; b) Zusammenführens des Lösungsmittels mit dem Wirkstoff unter Erhalt einer Granulierflüssigkeit; c) Feuchtgranulierens eines pulverförmigen Materials mittels der Granulierflüssigkeit.
Abstract:
The invention relates to self-assembling microparticles comprising a solid matrix and probiotic bacteria, wherein the solid matrix comprises soybean protein and a divalent or trivalent metal, and wherein the probiotic bacteria are distributed throughout the solid matrix; said matrix protects said probiotic bacteria during processing, storage, as well as during transit through the gastrointestinal tract, thus prolonging their lifetime and facilitating release into the intestine and improving their probiotic effect. The present invention also relates to the method for obtaining the self-assembling microparticles and to the products and compositions incorporating them.
Abstract:
A method of preparing a pharmaceutical formulation which is suitable for inhalation, the method comprising: providing a solution comprising a first solvent or mixture of solvents and a poorly water soluble active agent; providing a second solution comprising a second solvent or mixture of solvents and an excipient. The first and second solvents or mixture of solvents are removed by simultaneously drying both solutions in a spray dryer equipped with a three-fluid nozzle to produce particles comprising an active agent and an excipient.
Abstract:
L'invention a pour objet un procédé d'encapsulation d'une ou plusieurs substances par une matrice, ledit procédé comprenant la préparation d'un mélange de ladite matrice à l'état liquide avec ladite ou lesdites substances, puis la solidification du mélange obtenu, ladite matrice étant constituée de vanilline ou d'éthylvanilline ou d'un mélange vanilline/éthylvanilline. Le composé solide ainsi obtenu est particulièrement intéressant dans le domaine de l'alimentation humaine et animale, de la pharmacie, en tant que parfum dans l'industrie des cosmétiques, de la parfumerie et de la détergence, ou en tant que principe actif encapsulé dans le domaine de la pharmacie. L'utilisation d'un composé choisi parmi la vanilline, l'éthylvanilline et les mélanges vanilline/éthylvanilline comme encapsulant est également un objet de la présente invention.
Abstract:
Granules de mannitol pour compression directe La présente invention a pour objet des granules de mannitol utiles pour la préparation de comprimés par compression directe, qui ne requièrent qu'une faible quantité de lubrifiant pour être mis en œuvre. La présente invention a également pour objet un procédé pour la préparation de tels granules. La présente invention englobe également des compositions pulvérulentes comprenant ces granules, ainsi que des procédés de compression directe mettant en œuvre ces compositions pulvérulentes. La présente invention porte enfin sur des comprimés composés de ces compositions pulvérulentes.
Abstract:
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 copolvmerized 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.