Port Systems, L.l.c.

Other

University of Michigan

Tsrl, Inc.

Merck + Co., Inc.

Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.

Sinevir Therapeutics LLC

Gordon L Amidon

John R Crison

Glen D Leesman

Arthur H Goldberg

Ramachandran Chandrasekharan

Lizbeth B Sherman

Jennifer B Dressman

Beverly L Davidson

Takeru Higuchi

Ivan Alferiev

Gershon Golomb

Patrick J Sinko

Eli Breuer

John Hilfinger

James H Meyer

Naama El-Hanany Rozen

Aviva Friedman-Ezra

John M Hilfinger

Steven J Beer

A new class of neuramidase inhibitor prodrugs is provided characterized by a prodrug moiety of a carboxyl group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide or a carbonyl ethoxy tripeptide, a guanidine group modified to form a carbonyl ethoxy amino acid, a carbonyl ethoxy dipeptide, a carbonyl ethoxy tripeptide; a primary alcohol modified to form an esterified single amino acid, dipeptide or tripeptide of zanavimir of the unaltered therapeutic agent. Exemplary therapeutic agents so modified to form prodrugs include zanavimir, oseltamivir and peramivir. The prodrug has increased oral bioavailability relative to the unaltered neuraminidase inhibitor and is effective in the inhibition of viral infections involving neuraminidase in the viral reproductive cycle.

Prodrugs of neuraminidase inhibitors

A device for controlled release of pharmaceutical agents and a method for use of the device. The drug delivery device comprises a covered container with an aperture and an aperture cover, containing a pharmaceutical agent and an excipient formulation.

Controlled release of drugs

A method for treating patients having calcium related disorders includes using di- or tripeptide derivatives of bisphosphonates to enhance oral bioavailability of such compounds.

Phosphonates, biphosphonates and pharmaceutical compositions containing them

A drug delivery system (,) includes a first capsule half (,) having an inner chamber (,) containing a drug (,) therein. A plug (,) is disposed in a passageway (,) of the capsule half (,) for plugging the opening (,) thereof. The plug (,) is releasable from the passageway opening (,) upon the application of pressure from within the inner chamber (,). A pump mechanism, reactive with the external environment of the capsule half (,), causes an increase in pressure within the inner chamber (,) and forces the plug (,) out of the passageway (,) to release the drug (,) from the inner chamber (,) and out of the passageway (,). Thusly, after initial release of drug from a second capsule half (,) releasably mounted on the first capsule half (,), the first capsule half (,) provides a second pulse of drug release at a predetermined time after initial ingestion of the capsule. The invention further provides a method of manufacturing the drug delivery system (,) and method by which the drug delivery system (,) provides the drug to a body.

Multi-stage drug delivery system

Enhancing the bioavailability of proteolytically labile therapeutic

A controlled release delivery system includes a functional gene vector in a biodegradable polymeric microsphere encapsulating the vector. The present invention further provides a method of making a controlled release delivery system by encapsulating the functional gene vector in a biologically degradable polymeric microsphere.

Microsphere encapsulation of gene transfer vectors

A self-microemulsifying excipient formulation for increasing the bioavailability of a drug which includes an emulsion including an oil or other lipid material, a surfactant, and a hydrophilic co-surfactant. A method for making a drug delivery system for increasing the bioavailability of a drug by emulsifying at least one drug with a self-microemulsifying excipient comprising an oil or other lipid material, a surfactant, and a hydrophilic co-surfactant and drugs formulated thereby.

Method and formulation for increasing the bioavailability of poorly

A drug delivery system (10) includes a first capsule half (12) having an inner chamber (16) for containing a drug (18) therein. A plug (28) is disposed in a passageway (26) of the capsule half (12) for plugging the opening (24) thereof. The plug (28) is releasable from the passageway opening (24) upon the application of pressure from within the inner chamber (16). A pump mechanism, reactive with the external environment of the capsule half (12), causes an increase in pressure within the inner chamber (16) and forces the plug (28) out of the passageway (26) to release the drug (18) from the inner chamber (16) and out of the passageway (26). Thusly, after initial release of drug from a second capsule half (14) releasably mounted on the first capsule half (12), the first capsule half (12) provides a second pulse of drug release at a predetermined time after initial ingestion of the capsule. The invention further provides a method of manufacturing the drug delivery system (10) and method by which the drug delivery system (10) provides the drug to a body.

Method for making a multi-stage drug delivery system

A method of making a pharmaceutical composition is disclosed. The method includes the steps of contacting at least one pharmaceutical ingredient with a mixture consisting essentially of gelatin and lecithin to increase the dissolution rate of water-insoluble pharmaceutical ingredients. A pharmaceutical excipient coating for increasing the dissolution rate of water-insoluble pharmaceutical ingredients is also disclosed. The coating consists essentially of gelatin and lecithin.

Water soluble pharmaceutical coating and method for producing coated

A method of making a drug delivery system (10) includes the steps of filling a first water permeable capsule half with a drug and an osmotic agent and plugging an open-end (24) of the capsule (12). The method further includes the steps of disposing a water permeable film (30) over the capsule (12) and plug (28), filling a second capsule half (14) with a drug (18), and releasably mounting an open end (34) of the second capsule half (14) over the plugged end (24) of the first capsule half (12).

A pharmaceutical formulation comprising a polymeric resin having bile acid binding properties in combination with at least one bile acid binding material which enhances the bile acid binding affinity and/or capacity of the formulation, methods for preparing the formulations and methods for using the formulations.

Pharmaceutical formulation having enhanced bile acid binding affinity

An improved bioactive agent delivery composition and method of application are described. The composition comprises a bioactive agent, a hydrophilic polymer in an incompletely hydrated state and a substantially water-miscible solvent system. The agent and polymer are essentially dissolved in the solvent system to form a sprayable composition having a viscosity of less than 350 cP. Upon dilution with water, the viscosity of the composition increases to in excess of 1000 cP to produce a retentive coating at the site of application which provides enhanced bioavailability of the agent.

Bioactive composition

A drug delivery system includes a first capsule half having an inner chamber for containing a drug therein. A plug is disposed in a passageway of the capsule half for plugging the opening thereof. The plug is releasable from the passageway opening upon the application of pressure from within the inner chamber. A pump mechanism causes an increase in pressure within the inner chamber and forces the plug out of the passageway to release the drug from the inner chamber and out of the passageway thereby providing a second pulse of drug release at a predetermined time after initial ingestion of the capsule. The invention further provides a method of manufacturing the drug delivery system and method by which the drug delivery system provides the drug to the body.

Growing community of inventors

Ann Arbor, MI, United States of America

Gordon L Amidon