Abstract: The present invention provides BZPA products with improved flowability and two methods of producing such BZPA products. Both methods successfully produce BZPA products that are not prone to agglomerate upon storage, and thus the flowability of such BZPA products does not degrade over time. The first method includes mechanically forming the BZPA crystals into large compacted pellets or briquettes without the introduction of any additives or binders. The compacted pellets are large enough that the physical and chemical effects that occur on the surface of small crystal particles are eliminated or minimized, but small enough that the BZPA can be easily handled and used in commercial applications. The second method includes adding a substantially inert anti-caking agent to the BZPA crystals to minimize or retard their tendency to agglomerate. The preferred anti-caking agent is silicon dioxide (SiO2), which is blended with the BZPA crystals in small amounts.

Abstract: Herein are disclosed a process for increasing in purity, or purifying, an N-protected-?-aminoalcohol which process comprises (i) adding water to a polar organic solvent in which an N-protected-?-aminoalcohol such as a (2R,3S)- or (2S,3R)-3-tert-butoxycarbonylamino-1-halo-2-hydroxy-4-phenylbutane or the like, or (ii) crystallizing such an N-protected-?-aminoalcohol from a diol or a diol-based mixed solvent, and a process for producing the corresponding N-protected-?-aminoepoxide which process comprises treating, with a base, the thus purity-enhanced N-protected-?-aminoalcohol. Such N-protected-?-aminoalcohols and N-protected-?-aminoepoxides are both useful as synthetic intermediates for medicine compounds, such as, e.g., HIV protease inhibitor and the like.

Abstract: Antimicrobially active 4-methyl-4-aryl-2-pentanols of the Formula 1 below, methods for the preparation of these compounds and their use as antimicrobial active compounds are described. Surprisingly, compounds of the Formula 1 for which: R=hydrogen, hydroxyl, alkoxy group with up to 10 C atoms, straight-chain or branched, saturated or unsaturated alkyl with up to 10 C atoms, alkylthioether group with up to 10 C atoms, the alkylthioether group being bonded to the aromatic ring via a thioether bridge, fluorine, chlorine, bromine, iodine, or alkyl with up to 10 C atoms that is interrupted by one or more oxygen and/or sulphur atoms, have proved to be antimicrobially active.

Abstract: In a process for liquid phase carbonylation of alcohols by carbon monoxide, the carbonylation reaction is carried out in a reaction zone at a temperature of 50° C. to 150° C. at a pressure in the range 0.5 MPa to 20 MPa in the presence of at least one catalyst comprising at least one rhodium and/or iridium complex and a halogenated promoter in at least one non-aqueous ionic liquid comprising at least one salt with general formula Q+A?, in which Q+ represents a quaternary ammonium and/or a quaternary phosphonium cation, said salt having a melting point of less than 90° C.; the non-aqueous ionic liquid containing at least the major portion of the catalyst is separated; and the separated non-aqueous ionic liquid containing at least the major portion of the catalyst is returned to the reaction zone.

Abstract: The present invention is directed to a process for stabilizing antioxidant compounds comprising the step of adding to said compound, in an aqueous mean, at least an oxygen-removing compound, at least a metallic ion sequestering compound and at least an oxidation reaction reversing compound. The invention is particularly useful to stabilize antioxidant compounds such as levogyrous ascorbic acid (LAA), popularly known as “Vitamin C”, and the LAA associated with proantocianidines (OPC) for the preparation of pharmaceutical and cosmetic compositions.

Abstract: The invention relates to a method for the coupled production of two esters by reacting a mixture of aliphatic alcohols with an aliphatic carboxylic acid and then treating the resulting mixture by distillation. During the distillation process, a side flow that is taken from the distillation column that is connected downstream of the esterification reactor is fed back into said esterification reactor. The pure ester compounds are obtained from the bottom of the distillation columns that are connected downstream of the esterification reactor.

Abstract: The present invention discloses a composition of a stable suspension of a poorly water soluble pharmaceutical agent or cosmetic in the form of particles of the pharmaceutical agent or cosmetic suspended in a frozen aqueous matrix and method for its preparation. The composition is stable for a prolonged period of time, preferably six months or longer and is suitable for parenteral, oral, or non-oral routes such as pulmonary (inhalation), ophthalmic, or topical administration.

Abstract: A pharmaceutically acceptable alendronate salt in an amorphous form.

Abstract: A process for preparing sulfonated arylphosphines by reaction of arylphosphines with oleum, wherein, after reaction of the arylphosphines with oleum, the sulfonation mixture is firstly diluted with water, an inert gas stream is then passed through the diluted sulfonation mixture until SO2 is no longer liberated from the diluted sulfonation mixture and the latter is then worked up further in a customary manner and its use.

Abstract: The invention includes a nonformulated, low-dose hypocholesterolemic composition comprising soya proteins and ?-sitosterol, wherein the soya proteins and the ?-sitosterol are present in a weight ratio of about 6±1.5 of the soya proteins to about 1±0.2 of the ?-sitosterol; and wherein the composition is made up as an optimal daily dose of only the two components for adults or for children.

Abstract: Method and system of producing microparticles loaded with biologically active drugs, including proteins such as ICAM-1, for controlled release of the drugs in a nasal passageway. The method includes introducing a drug/polymer feed solution and an emulsifier into a first mixing chamber to create an emulsion, then mixing a cross-linking agent together with the emulsion under controlled conditions to create microparticles loaded with the drug. The system includes a first mixing chamber, in which the emulsion is created, having a first port for introducing the drug/polymer solution, and a second port angled substantially perpendicular to the first port for introducing the emulsifier. A second mixing chamber adjacent to the first mixing chamber receives the emulsion and either contains a cross-linking agent or receives a stream of a cross-linking agent to solidify the microparticles.

Abstract: Devices and methods for treatment of erectile dysfunction and methods of manufacture and of use are provided. The devices include filmogenic material, a therapeutic agent, a permeation enhancer, and other ingredients. An embodiment of the device includes a backing and a release liner.

Abstract: A simulated capsule-like medicament comprising a subcoating of a mixture of a water-soluble, film-forming polymer, e.g. hydroxypropylmethyl cellulose and a hydrophobic plasticizer, e.g. castor oil, which promotes a smooth uniform and substantially bubble free outer coating, e.g. gelatin, for the capsule-like medicament; capsule-like medicaments which are slightly bowed in shape; and a process of making such medicaments.

Abstract: The use of an effective amount of at least one nitric oxide synthase inhibitor in a cosmetic composition or for making a pharmaceutical composition is disclosed, said inhibitor or pharmaceutical composition being intended to reduce the skin irritant effect of topically applied cosmetic or pharmaceutical substances. A cosmetic or pharmaceutical composition containing an effective amount of at least one nitric oxide synthase inhibitor, and a cosmetic treatment method using said cosmetic composition, are also disclosed.

Abstract: A hydroalcoholic lotion is disclosed which comprises (a) a lower alcohol and water in a weight ratio of about 35:65 to 100:0, and (b) between at least 0.5% and 8% by weight thickener system comprised of at least one emulsifier present in at least 0.05% by weight wherein the composition in a polymer free state has a viscosity of at least 4,000 centipoise at 23 degrees C. and wherein the emulsifier is comprised of at least one hydrophobic group and at least one hydrophilic group. The hydroalcoholic composition is useful as a hand preparation such as a lotion or as a presurgical scrub replacement.

Abstract: A topical sustained release delivery system for delivery of antifungal agents to the finger or toenails achieving high penetration through the nails by combining the antifingal agent with a keratolytic agent and a humectant. The pharmaceutical sustained release topical preparation is provided in a varnish or spray form for treating the nail and surrounding tissues, where the active ingredient is an antifungal agent, a keratolytic agent, or preferably a combination of an antifuingal and a keratolytic agent. The composition may further comprise an antibacterial, an antiviral, an antipsoriatic agents, or combinations thereof.

Abstract: The present invention provides methods and compositions involving resorbable hemostatic agents that have the essential absence of microfibrillar collagen. Resorbable hemostatic agents of the present invention comprise polyethylene glycol, which controls bleeding in tissue and does not delay or interfere with healing. The resorbable hemostatic agents of the present invention are biodegradable and biocompatible agents that effectively control bleeding in bone and other tissue without interfering with the subsequent healing of the tissue.

Abstract: A mixed micellar pharmaceutical formulation includes a micellar proteinic pharmaceutical agent, an alkali metal C8 to C22 alkyl sulfate, alkali metal salicylate, a pharmaceutically acceptable edetate and at least one absorption enhancing compounds. The absorption enhancing compounds are selected from the group consisting of lecithin, hyaluronic acid, pharmaceutically acceptable salts of hyaluronic acid, octylphenoxypolyethoxyethanol, glycolic acid, lactic acid, chamomile extract, cucumber extract, oleic acid, linolenic acid, borage oil, evening primrose oil, trihydroxy oxo cholanylglycine, glycerin, polyglycerin, lysine, polylysine, triolein and mixtures thereof. Each absorption enhancing compound is present in a concentration of from 1 to 10 wt./wt. % of the total formulation, and the total concentration of absorption enhancing compounds are less than 50 wt./wt. % of the formulation. Methods for administering insulin to the buccal region are also disclosed.

Abstract: Stable solutions of lipophilic drugs, such as cyclosporin, forming a polar lipid self-emulsifying drug delivery system. The solutions can include lipophilic drugs, such as cyclosporin, dissolved in a polar lipid, such as having a C6-C12 fatty acid monoglyceride content of at least about 50%, surfactants and triglycerides. The composition forms a fine emulsion on exposure to water. The encapsulated dosage form of this composition needs neither a hydrophilic component nor air-tight blister packaging, and is particularly suitable for oral administration.

Abstract: The present invention is concerned with physicochemically stable aqueous solutions of risperidone for oral and parenteral administration; processes for preparing such formulations.