Abstract: The present disclosure relates to an apparatus and method for combining a solid particulate with a solvent prior to an injection protocol within an injector device. The solid particulate may be a pharmaceutical compound and the microcapsules contain a solvent for such particulate. Upon application of pressure, the microcapsules may be configured to burst and release the solvent, thereby dispersing and/or partially dissolving the particulate. The injector therefore allows for the use of relatively unstable pharmaceutically active compounds in a device that requires relatively long storage times and the use of pharmaceutical compounds that are relatively stable in the dry state.

Abstract: Enantomerically purified phenothiazines are provided as active ingredients of medicaments to limit activity of bone resorbing cells so as to reduce bone loss. Novel phenothiazine derivatives are provided. A method of synthesizing enantiomerically pure phenothiazine derivatives is provided that avoids post-synthetic enantiomeric resolution.

Abstract: This invention is directed to an apparatus and method for producing microparticles comprising pharmacologically active agents and biodegradable polymers. The apparatus includes a spinning disk containing a reservoir in the center thereof and a flat inclined surface. The apparatus optionally includes serrations and/or a flat surface beneath the periphery of the disk that is parallel to the rotational axis of the disk. The invention is also directed to a method for producing microparticles containing pharmacologically active agents, using the spinning disk apparatus. Formulations containing ophthalmically active agents are provided. Formulations exhibiting zero order release rates are also described.

Abstract: The present disclosure relates to a method of melt processing an active agent. The method may include encapsulating an active agent in a first polymer material exhibiting a first processing temperature T1 and forming capsules including the active agent. The method may also include melt processing the capsules with a second polymer material exhibiting a second processing temperature T2, wherein T1>T2.

Abstract: The present disclosure relates to non-aggregating nanoparticles and their associated methods of preparation. The nanoparticles may have a surface and a size range of 1 nm to 999 nm, along with a zeta potential of ?50 to 50 millivolts. A polycation and/or polyanion may be disposed on the nanoparticle surface. In addition, an active ingredient may be encapsulated within the nanoparticles or associated with the polycation or polyanion on the nanoparticle surface.

Abstract: The present invention relates to two-phase systems of a bioactive ingredient in particle form that has limited or no solubility in a liquid medium, which provides stability to the active ingredient that is similar to the active ingredient when in the solid state. The active ingredient may be capable of therapeutically treating for the presence of a cholinesterase inhibitor.

Abstract: Bis-quaternary pyridinium-aldoxime salts are disclosed, and their associated polymorphic character, along with their methods of preparation. Such polymorphic salts may then be used for treatment of exposure to cholinesterase inhibitors, such as a phosphorous containing cholinesterase inhibitor type compound.

Abstract: The present disclosure is directed at a pharmaceutically active nanoparticle suspension that may be optically clear. Such suspensions may be formed by selective dissolution of a pharmaceutically active compound in a first solvent followed by introduction into a second solvent, such as an aqueous medium, without substantial use of surfactants and/or mechanical shear.

Abstract: A respiratory volume/flow monitoring system, including a pneumotach that measures micromovements of a membrane in a MRI environment, gates (triggers) a MRI machine to start image acquisition at specific lung volumes or airflow rates during the breathing cycle or other breathing maneuvers of a patient. The system provides breathing motion artifact suppression for any imaging test susceptible to breathing motion artifact, allows respiratory monitoring of the subject during an MRI procedure, and provides the capability to perform spirometric testing while the subject is in the MRI environment. Embodiments of the invention are also applicable for patients undergoing CT imaging or any other imaging modality that allows external triggering.

Abstract: This invention is directed to an apparatus and method for producing microparticles comprising pharmacologically active agents and biodegradable polymers. The apparatus includes a spinning disk containing a reservoir in the center thereof and a flat inclined surface. The apparatus optionally includes serrations and/or a flat surface beneath the periphery of the disk that is parallel to the rotational axis of the disk. The invention is also directed to a method for producing microparticles containing pharmacologically active agents, using the spinning disk apparatus. Formulations containing ophthalmically active agents are provided. Formulations exhibiting zero order release rates are also described.

Abstract: This invention is directed to an apparatus and method for producing microparticles comprising pharmacologically active agents and biodegradable polymers. The apparatus includes a spinning disk containing a reservoir in the center thereof and a flat inclined surface. The apparatus optionally includes serrations and/or a flat surface beneath the periphery of the disk that is parallel to the rotational axis of the disk. The invention is also directed to a method for producing microparticles containing pharmacologically active agents, using the spinning disk apparatus. Formulations containing ophthalmically active agents are provided. Formulations exhibiting zero order release rates are also described.

Abstract: This invention is directed to an apparatus and method for producing microparticles comprising pharmacologically active agents and biodegradable polymers. The apparatus includes a spinning disk containing a reservoir in the center thereof and a flat inclined surface. The apparatus optionally includes serrations and/or a flat surface beneath the periphery of the disk that is parallel to the rotational axis of the disk. The invention is also directed to a method for producing microparticles containing pharmacologically active agents, using the spinning disk apparatus. Formulations containing ophthalmically active agents are provided. Formulations exhibiting zero order release rates are also described.

Abstract: This invention is directed to an apparatus and method for producing microparticles comprising pharmacologically active agents and biodegradable polymers. The apparatus includes a spinning disk containing a reservoir in the center thereof and a flat inclined surface. The apparatus optionally includes serrations and/or a flat surface beneath the periphery of the disk that is parallel to the rotational axis of the disk. The invention is also directed to a method for producing microparticles containing pharmacologically active agents, using the spinning disk apparatus. Formulations containing ophthalmically active agents are provided. Formulations exhibiting zero order release rates are also described.

Abstract: The present invention provides processes which are flexible, cost effective, and commercially viable methods of manufacturing or producing products from 2-hydroxyacetophenone (2-HAP).Of particular interest of the available products are 4-hydroxycoumarin, warfarin-alkali salt, preferably warfarin sodium and warfarin-alkali salt-isopropyl alcohol (2-propanol) complex, more preferably warfarin-sodium-isopropyl alcohol complex.As is known, these compounds are useful as vitamin K dependent anticoagulants in the treatment of humans and animals. In different doses, they are also useful as rodenticide.The inventive process involves contacting 2-HAP, carbonate ester and effective base followed by treatment with an unsaturated ketone and phase transfer catalyst to ultimately yield product.

Abstract: The present invention provides novel substituted pyrazines or pyrazine derivatives ("NPD") which are functional and have useful application as a monomer for a variety of high performance polymers such as polyester, polyarylate, polycarbonate, polyetherketones, epoxides, polyimides, polyamides, and polyamides-imides. These NPD have the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are defined herein.

Abstract: An arylisonitrosoalkanone is hydrogenated in the presence of a noble metal catalyst and a weak carboxylic acid to form an arylalkanolamine which is then hydrogenated in the presence of a strong mineral acid and the transition metal catalyst to form an arylalkylamine. When the arylisonitrosoalkanone is an isonitrosoacetophenone, the isonitrosoacetophenone is prepared by one of two methods.In the first method, a substituted or an unsubstituted isonitrosoacetophenone is prepared from a corresponding substituted or unsubstituted acetophenone by oxidizing the acetophenone to form a substituted or an unsubstituted phenylglyoxalacetal in a reactor, hydrolyzing the phenylglyoxal acetal in the same reactor to form a corresponding substituted or unsubstituted phenylglyoxal, and condensing the phenylglyoxal with hydroxylamine or a salt thereof in the same reactor to form the substituted or unsubstituted isonitrosoacetophenone.

Abstract: An arylisonitrosoalkanone is hydrogenated in the presence of a noble metal catalyst and a weak carboxylic acid to form an arylalkanolamine which is then hydrogenated in the presence of a strong mineral acid and the transition metal catalyst to form an arylalkylamine. When the arylisonitrosoalkanone is an isonitrosoacetophenone, the isonitrosoacetophenone is prepared by one of two methods.In the first method, a substituted or an unsubstituted isonitrosoacetophenone is prepared from a corresponding substituted or unsubstituted acetophenone by oxidizing the acetophenone to form a substituted or an unsubstituted phenylglyoxalacetal in a reactor, hydrolyzing the phenylglyoxal acetal in the same reactor to form a corresponding substituted or unsubstituted phenylglyoxal, and condensing the phenylglyoxal with hydroxylamine or a salt thereof in the same reactor to form the substituted or unsubstituted isonitrosoacetophenone.

Abstract: This invention provides a process for directly preparing hydrohalide salts of arylethylamines from (.alpha.-chloro-.alpha.-oximino)acetophenones. The process involves hydrogenation in presence of a transition metal catalyst in an organic acid in substantial absence of moisture. The process is illustrated by conversion of 4-hydroxy (.alpha.-chloro-.alpha.

Abstract: This invention provides a process for directly preparing arylethylamines and their salts from (.alpha.-halo-.alpha.-oximino)acetophenones. The process involves hydrogenation in presence of a transition metal catalyst. The process is illustrated by conversion of 4-hydroxy-(.alpha.-chloro-.alpha.

Abstract: Arylalkylamines (as the hydrochloride salt), e.g. tyramine hydrochloride, are prepared by hydrogenating substituted or unsubstituted aryl-.alpha.-oximinoalkyl ketones, e.g. p-hydroxyisonitroacetophenone, in either in an aqueous reaction medium comprising hydrochloric acid, essentially without the presence of a lower alkyl alcohol in said reaction medium, or in an aqueous reaction medium comprising water, hydrochloric acid, and a lower alkyl alcohol, wherein the alcohol comprises less than about 90% by volume of the reaction medium. A substituent on the aryl portion of the aryl-.alpha.-oximinoalkyl ketone must be on a position which activates the aromatic ring.