Idemitsu Kosan Company, Limited

Cibus Pharmaceutical, Inc.

University of California

Sri International

Eurand America, Inc.

Venture Lending, a Division of Cupertino National Bank

Venture Lending

David R Friend

David Wong

Jagdish Parasrampuria

Francis J Martin

Eric Hauser Kuhrts

Peter J Dehlinger

Mauro Ferrari

Paul G Catz

Rafael E Sarabia

Steve Ng

Carl F Grove

Mark S Gebert

Jean-Marie Geoffroy

Harold W Nolen, Iii

Thomas P Weber

Karen Yu

Microfabricated, asymmetrical, reservoir-containing particles for use in the oral delivery of biopolymer therapeutic agents such as peptides, proteins and oligonucleotides are disclosed. The particles are encapsulated in enteric-coated capsules or tablets to provide passage through the stomach and release of a suspension of the particles in the intestinal lumen. The particles have a selected shape, and uniform dimensions preferably in the 100 &mgr;m to 1 mm range. The reservoirs open to the face of the particle and are filled with a therapeutic agent and selected excipients. The excipients are selected to delay the dissolution/release of the agent from the particle reservoirs for 5-60 minutes after the particle is released in the intestinal lumen. Alternatively, the pore is plugged with an erodable material. The face of the particle is grafted with a layer of muco-adhesive ligands designed to quickly bind the particle to the intestinal mucosa for several minutes to several hours after release of the particles from the enteric-coated carrier.

Particles for oral delivery of peptides and proteins

A taste-masked microcapsule composition for administration of a drug is provided. The composition comprises microcapsules of drug and a substantially water-insoluble polymeric material, typically a cellulosic polymer. The microcapsule composition may be incorporated into any number of pharmaceutical formulations, including chewable tablets, effervescent tablets, powders, liquid dispersions, and the like. A method for masking the taste of drugs is also provided, involving a phase separation coacervation technique in which drug is coated with relatively high levels of a polymeric material. These high coating levels give rise to effective taste masking, while nevertheless allowing targeted release of drug, so that the drug is released shortly after passage through the mouth.

Taste-masked microcapsule compositions and methods of manufacture

Disclosed is a substantially anhydrous, powdered, galactomannan composition consisting essentially of a galactomannan hydrocolloid exhibiting about 50% to about 90% by weight of anhydromannose residues and about 10% to about 50% by weight anhydrogalactose residues; less than about 1% by weight of protein material and less than about 3% of other nonaqueous impurities. This material is useful for preparing pharmaceutical compositions both in the substantially anhydrous form but preferably in an anhydrated form which includes about 5-15% by weight water. The pharmaceutical compositions comprise a therapeutically effective amount of a drug, the hydrated powered gallactomannan composition and optionally other pharmaceutically-acceptable excipients. When the hydrated powdered purified glactomannan of the invention is used to form a tablet, one sees improved hardness in the tablet formed. The pharmaceutical composition of the invention is particularly valuable for delivering a therapeutically effective drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition. Unique means to prepare the purified galactomannan in large quantities is provided.

Purified galactomannan as an improved pharmaceutical excipient

An oral-delivery pharmaceutical composition for reducing the gastric irritation effect of an NSAID in the upper GI tract of a mammal. The composition includes (a) a mucosal protective amount of a pharmaceutically-acceptable hydrocolloid gum obtainable from higher plants, (b) a dispersion-enhancing amount of another excipient and (c) a therapeutically-effective amount of an NSAID. Also disclosed is a process for preparing the composition and a method for reducing the gastric irritation effect of the NSAID by administering the composition. Also, disclosed is a composition particularly useful for preparing an aqueous suspension.

NSADI delivery employing a powdered hydrocolloid gum obtainable from

Pharmaceutical compositions for orally delivering a therapeutically effective amount of a drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition are described. The composition is a unit dosage in the form of a tablet that comprises about 0.01% by weight to about 10% by weight of the drug that is useful in treating a colonic disorder or that is absorbed from the colon; about 40% by weight to about 98% by weight of a hydrocolloid gum obtainable from higher plants; and about 2% by weight to about 50% by weight of a pharmaceutically acceptable binder. The compositions are useful for treating lower GI disorders in human subjects by administering a suitable amount to a subject in need thereof. A particularly preferred aspect is the process for preparing such composition in the form of a tablet.

Delivery of drugs to the lower GI tract

Pharmaceutical compositions for orally delivering a therapeutically effective amount of a drug to the colon without significant release of the drug in the upper GI tract after oral administration of the composition are described. The composition comprises about 0.5% by weight to about 10% by weight of the drug that is useful in treating a colonic disorder or that is absorbed from the colon; about 40% by weight to about 80% by weight of a hydrocolloid gum obtainable from higher plants; and about 10% by weight to about 50% by weight of a pharmaceutically acceptable binder. The compositions are useful for treating colon disorders in human subjects by administering a suitable amount to a subject in need thereof. A particularly preferred aspect is the process for preparing such composition in the form of a tablet.

Colonic delivery of drugs

Skin permeation enhancer compositions are provided which increase the permeability of skin to transdermally administered pharmacologically active agents. The compositions contain a lower aliphatic ester of a lower aliphatic carboxylic acid such as ethyl acetate and a lower alkanol such as propylene glycol. Methods and transdermal drug delivery systems for using the compositions are also provided.

Skin permeation enhancer compositions

Microencapsulating lubricating fluids and additives and a method of preparing microencapsulated lubricants including the steps of preparing an emulsification medium, adding a lubricant to the emulsification medium, emulsifying the emulsification medium and lubricant to form an emulsion, adding a first solution including resorcinol and dimethylol urea to the emulsion, acidifying the first solution and emulsion, adding a second solution consisting of resorcinol and dimethylol urea to the acidified first solution and emulsion while vigorously stirring it to form a microcapsule suspension, adjusting the pH to be basic, filtering and washing the microcapsule suspension to separate the microcapsules from the solution, and drying the microcapsules.

Microencapsulated lubricating fluids and additives and method of making

A method of preparing microencapsulated basic solutions including the steps of preparing a polymer which is hydrophobic at high pH values, preparing a basic solution, dissolving the polymer in an organic solvent, adding a surfactant to the polymer solution, adding the basic solution to the dissolved polymer, emulsifying the basic solution and dissolved polymer and spray drying the emulsion while stirring the emulsion.

Growing community of inventors

Menlo Park, CA, United States of America

David R Friend