Abstract: A polymer and a method for its preparation are provided. The polymer comprises poly(lactide), poly(lactide/glycolide) or poly(lactic acid/glycolic acid) segments bonded by ester linkages to both ends of an alkanediol core unit. The polymer is for use in a controlled release formulation for a medicament, preferably leuprolide acetate. The controlled release formulation is administered to a patient as a subcutaneous depot of a flowable composition comprising the polymer, a biocompatible solvent, and the medicament. Controlled release formulations comprising the polymer release leuprolide for treatment of prostate cancer patients over periods of 3-6 months.

Abstract: The invention provides methods of extracting a biodegradable polyester with a supercritical fluid effective to obtain a purified biodegradable polyester, such as a purified biodegradable poly(lactide-glycolide) (PLG). The supercritical fluid can be carbon dioxide at an elevated pressure, or can be carbon dioxide with one or more cosolvents. Methods for carrying out stepwise purification of the biodegradable polyester at multiple pressures or multiple temperatures, or both, are also provided. When the polyester is PLG, a purified PLG copolymer is obtained having a narrowed molecular weight distribution with respect to the unpurified polyester. The purified PLG copolymer can have a polydispersity index of less than about 1.7, less than about 2% monomers, and less than about 10% oligomers. The purified PLG copolymer can exhibit a reduced initial burst effect when incorporated into a controlled release formulation such as a flowable implant adapted to be injected into body tissues.

Abstract: The invention provides a controlled release biodegradable polymer formulation adapted for administering bioactive agents such as therapeutic proteins to a patient through implantation of a bolus that forms a depot within the patient's body tissues. The formulation includes a dehydrated inclusion complex of the bioactive agent within a hydrogel, wherein the hydrogel can comprise a polymerized polyalkyleneglycolyl diacrylate, and, optionally, polyalkyleneglycolyl monoacrylates, including methacrylates. Alternatively, the hydrogel can comprise hyaluronic acid, chitosan, agarose, polyvinylacetate, polyvinylpyrrolide, or polyvinylalcohol nanoparticles. The bioactive agent can be a macromolecular material, such as a protein. A method of forming the inventive formulation is also provided, as well as a method for using the formulation in the treatment of a malcondition in a patient in need thereof.

Abstract: A PLG copolymer material, termed a PLG(p) copolymer material, adapted for use in a controlled release formulation for a bioactive material is provided, wherein the formulation exhibits a reduced “initial burst” effect when introduced into the tissue of a patient in need thereof. A method of preparation of the PLG copolymer material is also provided, as are methods of use.

Abstract: The present invention relates to a risperidone sustained release delivery system for treatment of medical conditions relating delusional psychosis, schizophrenia, bipolar disorder, psychotic depression, obsessive-compulsion disorder, Tourette syndrome, and autistic spectrum disorders. The sustained release delivery system includes a flowable composition containing risperidone, a metabolite, or a prodrug thereof and an implant containing risperidone, a metabolite, or a prodrug thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid, and risperidone, a metabolite, or a prodrug thereof.

Abstract: The present invention is directed to a flowable composition that is suitable for use as a controlled release implant. The flowable composition includes a biodegradable thermoplastic polyester that is at least substantially insoluble in aqueous medium or body fluid. The flowable composition also includes a biocompatible polar aprotic solvent. The biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid. The flowable composition also includes leuprolide acetate.

Abstract: The present invention is directed to a flowable composition that is suitable for use as a controlled release implant. The flowable composition includes a biodegradable thermoplastic polyester that is at least substantially insoluble in aqueous medium or body fluid. The flowable composition also includes a biocompatible polar aprotic solvent. The biocompatible polar aprotic solvent is miscible to dispersible in aqueous medium or body fluid. The flowable composition also includes leuprolide acetate.

Abstract: The present invention provides a constant release copolymer composition adapted for use in a controlled release formulation for a bioactive agent, such as a formulation adapted for implantation within a patient's body tissues as a depot to release the agent over a period of time, wherein the copolymer provides a substantially constant rate of release of the bioactive agent over the time period for which the depot persists in the body tissues. The copolymer includes a PLG copolymer and a PLG oligomer of about 5-10 kDa average molecular weight, which can lack free carboxylic acid groups. When the PLG copolymer is a low burst copolymer, the constant release copolymer composition is a low burst, constant release copolymer composition adapted for implantation in the body tissues of a mammal, wherein a substantially constant rate of release of the bioactive agent is achieved.

Abstract: The invention provides methods of extracting a biodegradable polyester with a supercritical fluid effective to obtain a purified biodegradable polyester, such as a purified biodegradable poly(lactide-glycolide) (PLG). The supercritical fluid can be carbon dioxide at an elevated pressure, or can be carbon dioxide with one or more cosolvents. Methods for carrying out stepwise purification of the biodegradable polyester at multiple pressures or multiple temperatures, or both, are also provided. When the polyester is PLG, a purified PLG copolymer is obtained having a narrowed molecular weight distribution with respect to the unpurified polyester. The purified PLG copolymer can have a polydispersity index of less than about 1.7, less than about 2% monomers, and less than about 10% oligomers. The purified PLG copolymer can exhibit a reduced initial burst effect when incorporated into a controlled release formulation such as a flowable implant adapted to be injected into body tissues.

Abstract: A process for lyophilizing a solution of an active agent in a container is provided. Solution of active agent is deposited into a container, the container is covered with a covering plate and placed inside a lyophilizing apparatus. Lyophilization can be conducted to dryness by radiation, convection or both. Also provided is a device made by this process, an active agent-plastic administration device (e.g., a syringe), containing an active agent in the form of lyophilized cake, and an array of such administration devices.

Abstract: The present invention provides bioerodible, water-soluble pharmaceutical carriers for ocular (e.g., transconjunctival or transcorneal) delivery of pharmaceuticals for either systemic or local therapy.

Abstract: A process for lyophilizing a solution of an active agent in a container is provided. Solution of active agent is deposited into a container, the container is covered with a covering plate and placed inside a lyophilizing apparatus. Lyophilization can be conducted to dryness by radiation, convection or both. Also provided is a device made by this process, an active agent-plastic administration device (e.g., a syringe), containing an active agent in the form of lyophilized cake, and an array of such administration devices.

Abstract: The present invention provides a method for protecting against UV radiation-induced skin damage. Specifically, compositions including dapsone are administered to provide UV protection. The dapsone compositions may be administered orally, or by other parenteral routes, such as topically, transdermally, by inhalation, and the like.

Abstract: The present invention relates to a rapamycin sustained release delivery system for treatment of diseases responsive to rapamycin. The sustained release delivery system of the invention includes a flowable composition containing rapamycin or a rapamycin derivative, which is capable of providing an implant containing the rapamycin or derivative thereof. The flowable composition may be injected into tissue whereupon it coagulates to become the solid or gel, monolithic implant. The flowable composition includes a biodegradable, thermoplastic polymer, an organic liquid and rapamycin or a rapamycin derivative.

Abstract: The present invention is directed to a mucoadhesive delivery system for the local or systemic administration of a pharmaceutical agent. The delivery system of the invention effectively and facilely enables transport of the pharmaceutical agent through mucosal membranes and into the vasculattire of the mucosa. The delivery system includes an at least partially water soluble bioadhesive layer and an at least partially water soluble backing layer. Incorporated within either or both of these layers are the pharmaceutical agent and a mucosal penetration enhancing agent. The mucosal penetration enhancing agent displays localized tissue irritation properties. The mucoadhesive delivery system may be in the form of a gel, film, disc or patch. It may be applied to any mucosal membrane of a patient including but not limited to those of the buccal and nasal cavities, throat, eye, vagina, alimentary tract and peritoneum.

Abstract: The present invention provides for a topical composition that includes a topical carrier and an adenosine deaminase inhibitor. Suitable specific adenosine deaminase inhibitors include, e.g., deoxycoformycin (dCF), deoxyadenosine (dAdo), cladrabine (CdA), fludarabine (F-Ara-A), cytrabine (Ara-C), and thioguanine. The present invention also provides for a method to treat lymphocyte mediated skin diseases and to alleviate symptoms associated with such skin diseases. The method includes topically administering the composition to a mammal in need of such treatment. The present invention also provides for kits and syringe systems that include the adenosine deaminase inhibitor.

Abstract: The invention is provides a composition for sustained delivery of a biologically active agent comprising a biologically active mixture and a controlled release formulation. The composition protects the biologically active agent from being destroyed by the controlled release composition. The biologically active mixture includes the biologically active agent and a pharmaceutically acceptable protective carrier. The controlled release formulation includes a pharmaceutically acceptable, biodegradable, matrix forming material that is substantially insoluble in aqueous or body fluids and a pharmaceutically acceptable organic solvent. The biologically active mixture is combined with the controlled release formulation to form an emulsion, the delivery composition, which is then administered to a patient. The protective carrier can be an aqueous substance, a non-aqueous substance or a combination of both. The matrix forming material can be a polymeric material, a non-polymeric material or a combination of both.

Abstract: A process for lyophilizing a solution of an active agent in a container is provided. Solution of active agent is deposited into a container, the container is covered with a covering plate and placed inside a lyophilizing apparatus. Lyophilization can be conducted to dryness by radiation, convection or both. Also provided is a device made by this process, an active agent-plastic administration device (e.g., a syringe), containing an active agent in the form of lyophilized cake, and an array of such administration devices.