Abstract:
The present invention features solid pharmaceutical dosage formulations comprising ritonavir. As a non-limiting example, a dosage form of the present invention comprises a solid dispersion or solid solution of ritonavir in a matrix, where the matrix comprises at least one water-soluble polymer, such as copovidone, and at least one surfactant, such as polyoxyl 40 hydrogenated castor oil or macrogolglycerol hydroxystearate. Preferably, the solid dispersion or solution does not include, or includes only an insignificant amount of, PEG.
Abstract:
The invention relates to a method for producing water dispersible dry powders from hardly soluble compounds, whereby a dispersion is provided, containing the poorly soluble compound in a microdispersed form in a dispersion agent. The dispersion of the poorly soluble compound is concentrated by tangential-filtration and the dispersion agent is removed. The invention also relates to preparations based on said water dispersible dry powders.
Abstract:
The invention concerns a method of producing medicaments in solid form by mixing at least one pharmacologically acceptable polymer binder, at least one pharmaceutical active substance and optionally conventional pharmaceutical additives, extruding the mixture and shaping the medicament, a pre-mixture being prepared from the components and fed into the extruder. The method according to the invention enables high-quality medicaments to be produced in a simple and careful manner.
Abstract:
Solid medicaments obtainable by the extrusion of a melt, containing a mixture of homo and/or copolymers of N-vinyl pyrrolidone and degraded starches besides one or more active agents.
Abstract:
Disclosed are sustained-release matrix pellets of spherical to lenticular shape and uniform maximum diameter in the range of 0-5 to 4 mm, consisting of a) 0.1 to 87 wt % of at least one biologically active compound, b) 5 to 50 wt % of at least one water-insoluble polymer, c) 5-45 wt % of at least one lipophilic component as plasticizer for the b) polymer, d) 3 to 40 wt % of a natural or semisynthetic gelling agent, e) 0 to 50 wt% of one or more common formulation auxiliaries.
Abstract:
A method for forming a solution of only slightly soluble active substances is described, comprising the following steps: a) the active substance is dissolved, together with a phospholipid and a water-soluble lipid, in an organic solvent; 2) the solution thus obtained is reduced in volume; 3) the residue is taken up in a strongly acid buffer solution and stirred at elevated temperature until a colloidal solution forms; 4) the colloidal solution is cooled, its pH adjusted to a value of 6 to 7 and the solution sterilized. Particularly suitable for use in this method are lipids of formula (I) In which m, a, b, x and y are as defined in the description.
Abstract:
A process is disclosed for processing hardly soluble active substances together with phospholipids into a homogeneous solution. The process is characterized in that a) the active substance is mixed with a phospholipid, b) and acid aqueous solution of a carbohydrate is added to the residue at an increased temperature and the mixture is stirred at an increased temperature until a homogeneous colloidal solution is obtained, and c) this solution is cooled, set at a pH value from 4 to 5 and sterilized.
Abstract:
The preferred exemplary embodiments in the present application provide formulations and methods for the delivery of drugs, particularly drugs of abuse, having an abuse-relevant drug substantially confined in the core and a non-abuse relevant drug in a non-core region. These formulations have reduced potential for abuse. In the formulation, preferably the abuse relevant drug is an opioid and the non-abuse relevant drug is acetaminophen or ibuprofen. More preferably, the opioid is hydrocodone, and the non-abuse relevant analgesic is acetaminophen. In certain preferred embodiments, the dosage forms are characterized by resistance to solvent extraction; tampering, crushing or grinding. Certain embodiments of the inventions provide dosage forms that provide an initial burst of release of drug followed by a prolonged period of controllable drug release.
Abstract:
A process for producing a solid dispersion of an active ingredient which comprises feeding the active ingredient and a matrix-forming agent to an extruder and forming a uniform extrudate, wherein the extruder comprises at least two rotating shafts (2), each of the shafts (2) carrying a plurality of processing elements disposed axially one behind the other, the processing elements defining (i) a feeding and conveying section (A), (ii) at least one mixing section (B), and (iii) a discharging section (E), wherein the processing element(s) defining the mixing section (B) comprise(s) a mixing element (11, 12, 13) that is derived from a screw type element (figure 2).
Abstract:
Disclosed is a method for producing dosage forms comprising a solid dispersion of a microcrystalline agent. According to said method, a thermoplastic polymer having a minimum glass transition temperature Tg of 40 o C is melted, and an agent is homogeneously dissolved in the melt; crystallization of the agent is initiated in the obtained mass; and the mass is cooled. Crystallization of the agent can be initiated by adding a nonsolvent, seed crystals of the agent, or a derivatization reagent. Crystallization can also be initiated by maintaining the mass at a certain temperature for a sufficient amount of time, said temperature being lower than the temperature at which the agent can be fully dissolved in the mass.