Macromed Incorporated

Sarcos Lc

Protherics Salt Lake City, Inc.

Novartis Ag

Sarcos Corp.

Aesica Pharmaceuticals Limited

Protherics Medicines Development Limited

Chung Shih

Gaylen M. Zentner

Gaylen M Zentner

Stephen C Jacobsen

Feng Liu

Jong-Seok Bark

Ramesh C Rathi

Ai-Zhi Piao

Byeongmoon Jeong

Mark S Williams

James C McRea

Norman T Smith

Catriona A Oare

Kirk Dee Fowers

Stephen J Martin

Steve J Martin

James C Mcrea

An improved drug delivery composition and method of use is disclosed. The composition comprises one or more biodegradable block copolymer drug carriers; and a reconstitution enhancing and enabling agent comprising polyethylene glycol (PEG), a PEG derivative or a mixture of PEG and a PEG derivative. The composition can be administered as is or after being be dissolved or rapidly reconstituted in an aqueous vehicle to afford a homogeneous solution or uniform colloidal systems.

Biodegradable block copolymeric compositions for drug delivery

The invention relates to drug substance preparations, pharmaceutical compositions and dosage forms containing (R)-(&#x2212;)-2-(2-fluoro-4-biphenylyl) propionic acid as the active pharmaceutical ingredient, and limited amounts of specific product-related and process-related impurities.

Drug substance preparations, pharmaceutical compositions and dosage forms

A polymer blend is prepared by dissolving chitosan and a second polymer in an acidic aqueous solution to form an aqueous polymer blend, dehydrating said aqueous polymer blend, and recovering said polymer blend. The second polymer may be selected from the group consisting of polyether glycols including polyethylene glycols; cellulose esters including cellulose acetate; poloxamers; polysaccharides including dextran and guar; polyvinylpyrrolidones; polyvinyl alcohols; and mixtures or copolymers thereof. These polymer blends swell in an acidic environment and deswell in a more neutral or basic environment. This technology is valuable for the dispensing of biologically active material or drugs into a surrounding environment, especially the environment as is found in the gastrointestinal tract. Since the various polymer blends of the present invention are not covalently or ionically crosslinked, but are physically combined, each polymer in the physical blend maintains its original chemical structure, and therefore, is safe for oral administration.

Polymer blends that swell in an acidic environment and deswell in a basic environment

The present invention relates to compositions and methods for the modulated release of one or more proteins or peptides. The composition is comprised of a biocompatible polymeric matrix, a protein and/or peptide, and a sparingly water-soluble or essentially insoluble particle. The protein is deposited by adsorption or some other mechanism onto the sparingly water-soluble biocompatible particle wherein the protein-particle combination is dispersed within the polymeric matrix. The deposition of the protein onto the particle acts to modulate the release of the protein or peptide from dosage forms including long-acting dosage systems.

Proteins deposited onto sparingly soluble biocompatible particles for controlled protein release into a biological environment from a polymer matrix

Polymeric compositions having improved capability of solubilizing a drug in a hydrophilic environment to form a solution, comprising: a biodegradable polyester oligomer; and biodegradable AB-type, ABA-type, or BAB-type block copolymers are disclosed. The copolymers are comprised of about 50.1 to 65% by weight of a biodegradable, hydrophobic A polymer block comprising a biodegradable polyester, and about 35 to 49.9% by weight of a hydrophilic B polymer block comprising a polyethylene glycol (PEG), and wherein the block copolymer has a weight averaged molecular weight of between 2400 to 4999. The biodegradable polyester oligomer of said composition is within a range of 0.01% to 30% by weight of the total polymer mixture, and the content of the biodegradable AB-type, ABA-type, or BAB-type block copolymer is within a range of 70% to 99.99% by weight of the total polymer mixture.

PLA/PLGA oligomers combined with block copolymers for enhancing solubility of a drug in water

A composition and method for releasing a bio-active agent or a drug within a biological environment in a controlled manner is disclosed. The composition is a dual phase polymeric agent&mdash;delivery composition comprising a continuous biocompatible gel phase, a discontinuous particulate phase comprising defined microparticles and an agent to be delivered. A microparticle containing a bio-active agent is releasably entrained within a biocompatible polymeric gel matrix. The bioactive agent release may be contained in the microparticle phase alone or in both the microparticles and the gel matrix. The release of the agent is prolonged over a period of time, and the delivery may be modulated and/or controlled. In addition, a second agent may be loaded in some of the microparticles and/or the gel matrix.

Bioactive agent delivering system comprised of microparticles within a biodegradable to improve release profiles

A composition and method for releasing a bio-active agent or a drug within a biological environment in a controlled manner is disclosed. The composition is a dual phase polymeric agent-delivery composition comprising a continuous biocompatible gel phase, a discontinuous particulate phase comprising defined microparticles and an agent to be delivered. A microparticle containing a bio-active agent is releasably entrained within a biocompatible polymeric gel matrix. The bio-active agent release may be contained in the microparticle phase alone or in both the microparticles and the gel matrix. The release of the agent is prolonged over a period of time, and the delivery may be modulated and/or controlled. In addition, a second agent may be loaded in some of the microparticles and/or the gel matrix.

Agent delivering system comprised of microparticle and biodegradable gel with an improved releasing profile and methods of use thereof

A water soluble, biodegradable ABA- or BAB-type tri-block polymer is disclosed that is made up of a major amount of a hydrophobic A polymer block made of a biodegradable polyester and a minor amount of a hydrophilic polyethylene glycol(PEG) B polymer block, having an overall average molecular weight of between about 2000 and 4990, and that possesses reverse thermal gelation properties. Effective concentrations of the tri-block polymer and a drug may be uniformly contained in an aqueous phase to form a drug delivery composition. At temperatures below the gelation temperature of the tri-block polymer the composition is a liquid and at temperatures at or above the gelation temperature the composition is a gel or semi-solid. The composition may be administered to a warm-blooded animal as a liquid by parenteral, ocular, topical, inhalation, transdermal, vaginal, transurethral, rectal, nasal, oral, pulmonary or aural delivery means and is a gel at body temperature. The composition may also be administered as a gel. The drug is released at a controlled rate from the gel which biodegrades into non-toxic products. The release rate of the drug may be adjusted by changing various parameters such as hydrophobic/hydrophilic component content, polymer concentration, molecular weight and polydispersity of the tri-block polymer. Because the tri-block polymer is amphiphilic, it functions to increase the solubility and/or stability of drugs in the composition.

Biodegradable low molecular weight triblock poly(lactide-co- glycolide) polyethylene glycol copolymers having reverse thermal gelation properties

A water soluble biodegradable ABA- or BAB-type triblock polymer is disclosed that is made up of a major amount of a hydrophobic polymer made of a poly(lactide-co-glycolide) copolymer or poly(lactide) polymer as the A-blocks and a minor amount of a hydrophilic polyethylene glycol polymer B-block, having an overall weight average molecular weight of between about 2000 and 4990, and that possesses reverse thermal gelation properties. Effective concentrations of the triblock polymer and a drug may be uniformly contained in an aqueous phase to form a drug delivery composition. At temperatures below the gelation temperature of the triblock polymer the composition is a liquid and at temperatures at or above the gelation temperature the composition is a gel or semi-solid. The composition may be administered to a warm-blooded animal as a liquid by parenteral, ocular, topical, inhalation, transdermal, vaginal, transurethral, rectal, nasal, oral, pulmonary or aural delivery means and is a gel at body temperature. The composition may also be administered as a gel. The drug is released at a controlled rate from the gel which biodegrades into non-toxic products. The release rate of the drug may be adjusted by changing various parameters such as hydrophobic/hydrophilic componenet content, polymer concentration, molecular weight and polydispersity of the triblock polymer. Because the triblock polymer is amphiphilic, it functions to increase the solubility and/or stability of drugs in the composition.

Biodegradable low molecular weight triblock poly (lactide-co-glycolide)

The method for automatic dosing of drugs utilizes a microdelivery device which may be implanted in or otherwise administered to an animal or human. A microdelivery device is configured to have at least one compartment containing at least one drug so that a plurality of doses of the drug(s) are held within the device. In accordance with the present invention, the microdelivery device selectively actuates a compartment to selectively release doses of the drug(s) to provide an efficacious dosing pattern. One primary function of the present invention is to release two or more pesticides in such a pattern that parasites are effectively controlled while preventing the development of tolerance to the drugs within the parasites. Preferably, the microdelivery device is programmable to effectuate the release of the drug(s) at a desired time to maintain efficacious levels of the drug while minimizing the amount of drug which must be used.

Method for automatic dosing of drugs

The apparatus for automatic administration and dosing of one or more drugs comprises a microdelivery device which may be implanted in or otherwise administered to an animal or human. The microdelivery device is configured to have at least one compartment containing at least one drug so that a plurality of doses of the drug(s) are held within the device. In accordance with the present invention, the microdelivery device selectively actuates a compartment to selectively release doses of the drug(s) to provide an efficacious dosing pattern. The microdelivery device employs a microprocessor, such as an application specific integrated circuit (ASIC), preprogrammed with a desired dosing regimen and a timing circuit, such as a quartz oscillator, in order to administer the drug(s) according to the dosing regimen. Thus, the microdelivery device is programmable to effectuate the release of the drug(s) at a desired time to maintain efficacious levels of the drug while minimizing the amount of drug which must be used.

Growing community of inventors

Salt Lake City, UT, United States of America

Gaylen M Zentner