Emisphere Technologies, Inc.

Usv Pharmaceutical Corporation

Clinical Technologies Associates, Inc.

Martin L Kantor

Sam J Milstein

Evgueni N Barantsevitch

Solomon S Steiner

Joseph Auerbach

Howard M Pack

This invention provides an encapsulated fragrance in which the fragrance is controlled can be released by exposing the encapsulated fragrance to a solution of a predetermined pH. The invention also contemplates a process for preparing encapsulated fragrances.

Microencapsulated fragrances and method for preparation

Methods for preparing microspheres containing imidazole derivatives are provided. Also provided is the use of imidazole derivatives containing microspheres for treating fungal infections. Oral dosage forms for oral administration are also provided.

Method of solubilizing and encapsulating itraconazole

Improved proteinoid carriers and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described. The proteinoid carriers are soluble within selected pH ranges within the gastrointestinal tract and display enhanced stability towards at least one of photolysis or decomposition over time. The proteinoid carriers are prepared from proteinoids having between 2 and 20 amino acids and having a molecular weight of between about 250 and 2400 daltons.

Proteinoid carriers and methods for preparation and use thereof

Solutions comprising itraconazole solubilized in a solvent comprising at least one volatile organic acid are provided. Methods for preparing microspheres containing imidazole derivatives are provided. Also provided is the use of imidazole derivatives containing microspheres for treating fungal infections. Oral dosage forms for oral administration are also provided.

Method of solubilizing itraconazole

The present invention provides emulsions, and a method for preparing emulsions, comprising (A) an aqueous phase, (B) an non-aqueous phase, and (C) (i) a proteinoid emulsifier, (ii) a modified hydrolyzed vegetable protein emulsifier wherein said modified hydrolyzed vegetable protein is modified with an amine reactive modifying agent, (iii) an acylated non-.alpha.-amino acid emulsifier, (iv) an acylated poly amino acid emulsifier, (v) an acylated peptide emulsifier, (vi) a sulfonated non-.alpha.-amino acid emulsifier, (vii) a sulfonated poly amino acid emulsifier, (viii) a sulfonated peptide emulsifier, or (ix) any combination of any of (i), (ii), (iii), (iv), (v), (vi), (vii), and (viii). The proteinoids, modified hydrolyzed vegetable proteins, modified non-.alpha.-amino acids, modified poly amino acids, and modified peptides used in the present invention provide emulsions having improved stability against degradation and/or decomposition.

Proteinoid emulsions and methods for preparation and use thereof

Methods for preparing microspheres are provided. A carrier vehicle and a precipitator are nebulized and contacted. Alternatively, a carrier is nebulized in an aqueous acid and the concentration of the acid is decreased. Apparatus are also provided.

Spray drying method and apparatus

Improved proteinoid micropheres and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described. The proteinoid microspheres are soluble within selected pH ranges within the gastrointestinal tract and display enhanced stability towards least one of photolysis or decomposition over time. The proteinoid microspheres are prepared from proteinoids having between 2 and 8 amino acids and having a molecular weight of about 1000 daltons.

Proteinoid microspheres and methods for preparation and use thereof

Improved proteinoid microspheres and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described. The proteinoid microspheres are soluble within selected pH ranges within the gastrointestinal tract and display enhanced stability towards at least one of photolysis or decomposition over time. The proteinoid microspheres are prepared from proteinoids having between 2 and 8 amino acids and having a molecular weight of about 1000 daltons.

Microcapsules containing oil-based biologically active compounds which are stable over extended time periods for release of the encapsulated compound in the intestine. There are a number of biologically active compounds having an oil base which must be orally ingested in order to have a beneficial effect. An example of one such biologically active oil-based compound is a fish oil having a high content of polyunsaturated omega-3 fatty acids which has been demonstrated to reduce plasma levels of triglycerides, very low density lipoprotein, low density lipoproteins and cholesterol in normal and hyperlipidemic subjects. The disclosed microcapsules eliminate the unfortunate problems of the unpleasant taste and smell of the fish oil, as well as the aftertaste, particularly when ingested in large quantities, and provide a palatable and practical means of ingesting efficacious quantities of fish oil. In addition, the normal oxidation of polyunsaturated fatty acids is inhibited.

Microencapsulation of fish oil

Acylated amino acids having the general formula ##STR1## are prepared by reacting a compound of formula II ##STR2## with a compound of formula III

Direct n-acylation of amino acids

Disclosed is a method of preparing N-amino compounds from corresponding secondary amines by reacting a secondary amine with nitrous acid and zinc in a neutral pH reaction media to form the corresponding N-amine.

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Mamaroneck, NY, United States of America

Martin L Kantor