Abstract: Methods of forming compositions for the sustained release of water soluble active agents, including biologically active polypeptides and products produced by the process are described. Improved product characteristics and ease of scale-up can be achieved using a novel coacervation process wherein at least one coacervation agent is added to the mixture comprising the active agent and the polymer in at least two distinct stages.
Type:
Application
Filed:
December 22, 2011
Publication date:
October 11, 2012
Applicant:
Alkermes, Inc.
Inventors:
Rajesh Kumar, Gregory Troiano, J. Michael Ramstack, Paul Herbert, Michael Figa
Abstract: The present invention relates to a pharmaceutical composition comprising sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs.
Type:
Application
Filed:
March 19, 2012
Publication date:
September 20, 2012
Applicant:
ALKERMES, INC.
Inventors:
Jason M. PERRY, Daniel R. DEAVER, Magall B. HICKEY, Julius F. REMENAR, Jennifer VANDIVER
Abstract: The present invention relates to the discovery of a novel opioid modulator effective in reducing pharmacologically induced weight gain associated with atypical antipsychotic use. The present invention provides methods of reducing antipsychotic induced weight gain, methods for suppressing food intake and reducing ghrelin levels induced by atypical antipsychotic medications in a patient.
Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
Type:
Application
Filed:
June 24, 2011
Publication date:
December 29, 2011
Applicant:
Alkermes, Inc.
Inventors:
Laura Cook Blumberg, Julius F. Remenar, Örn Almarsson, Tarek A. Zeidan
Abstract: The inventions described herein arose from unexpected discoveries made during clinical trials with a long acting formulation of naltrexone. As such, the invention includes a method for treating an individual in need of naltrexone comprising the step of parenterally administering a long acting formulation comprising naltrexone and to the use of naltrexone in the manufacture of medicaments for use in such methods.
Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.
Type:
Application
Filed:
December 23, 2010
Publication date:
July 21, 2011
Applicant:
Alkermes, Inc.
Inventors:
Orn Almarsson, Laura Cook Blumberg, Julius F. Remenar
Abstract: Compounds of Formula I and Formula II and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed.
Abstract: Compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia and manic or mixed episodes associated with bipolar I disorder with or without psychotic features is disclosed: wherein R1-R8, G, N and A? are as defined in the written description.
Abstract: In one aspect, the invention is related to a method of treating a patient with Parkinson's disease, the method including administering to the respiratory tract of the patient particles that include more than about 90 weight percent (wt %) of levodopa. The particles are delivered to the patient's pulmonary system, preferably to the alveoli or the deep lung.
Type:
Application
Filed:
December 20, 2010
Publication date:
June 23, 2011
Applicant:
Alkermes, Inc.
Inventors:
Blair Jackson, David J. Bennett, Raymond T. Bartus, Dwaine F. Emerich
Abstract: The present invention is based, in part, on the unexpected discovery that particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that comprise a phospholipid and a sufficient amount of leucine can produce sustained effect of the agent. Specifically, particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that contain a phospholipid or combination of phospholipids, wherein the phospholipid or combination of phospholipids is present in the particles in an amount of about 1 to 46 weight percent; and leucine, wherein leucine is present in the particles in an amount of at least 46 weight percent, can contribute to sustained effect of the agent. Particles that comprise at least 46 weight percent leucine but that do not contain phospholipids do not exhibit these same sustained effect properties.
Type:
Application
Filed:
October 19, 2010
Publication date:
May 26, 2011
Applicant:
Alkermes, Inc.
Inventors:
Sujit K. Basu, Giovanni Caponetti, Robert Clarke, Katharina J. Elbert
Abstract: Methods for preparing microparticles having reduced residual solvent levels. Microparticles are contacted with a non-aqueous washing system to reduce the level of residual solvent in the microparticles. Preferred non-aqueous washing systems include 100% ethanol and a blend of ethanol and heptane. A solvent blend of a hardening solvent and a washing solvent can be used to harden and wash microparticles in a single step, thereby eliminating the need for a post-hardening wash step.
Type:
Application
Filed:
December 14, 2010
Publication date:
April 14, 2011
Applicant:
Alkermes, Inc.
Inventors:
Michael E. Rickey, J. Michael Ramstack, Rajesh Kumar
Abstract: The inventions described herein arose from unexpected discoveries made during clinical trials with a long acting formulation of naltrexone. As such, the invention includes a method for treating an individual in need of naltrexone comprising the step of parenterally administering a long acting formulation comprising naltrexone and to the use of naltrexone in the manufacture of medicaments for use in such methods.
Abstract: In one aspect, the invention is related to a method of treating a patient with Parkinson's disease, the method including administering to the respiratory tract of the patient particles that include more than about 90 weight percent (wt %) of levodopa. The particles are delivered to the patient's pulmonary system, preferably to the alveoli or the deep lung.
Type:
Grant
Filed:
March 19, 2003
Date of Patent:
February 1, 2011
Assignee:
Alkermes, Inc.
Inventors:
Blair Jackson, David J. Bennett, Raymond T. Bartus, Dwaine F. Emerich
Abstract: Methods for preparing microparticles having reduced residual solvent levels. Microparticles are contacted with a non-aqueous washing system to reduce the level of residual solvent in the microparticles. Preferred non-aqueous washing systems include 100% ethanol and a blend of ethanol and heptane. A solvent blend of a hardening solvent and a washing solvent can be used to harden and wash microparticles in a single step, thereby eliminating the need for a post-hardening wash step.
Type:
Grant
Filed:
March 20, 2009
Date of Patent:
January 25, 2011
Assignee:
Alkermes, Inc.
Inventors:
Michael E. Rickey, J. Michael Ramstack, Rajesh Kumar
Abstract: The invention is directed to a complex of trospium and saccharin. In one embodiment, the complex is a crystalline form. In another embodiment, the complex is a monohydrate form. The invention also encompasses methods of preparing the the saccharin complex of trospium and to pharmaceutical compositions thereof.
Type:
Application
Filed:
July 23, 2009
Publication date:
October 28, 2010
Applicant:
Alkermes,Inc.
Inventors:
David S. Scher, Rachel A. Ryznal, Charles D. Blizzard
Abstract: Particles having a tap density less than about 0.4 g/cm3 are formed by spray drying from a colloidal solution including a carboxylic acid or salt thereof, a phospholipid, a divalent salt and a solvent such as an aqueous-organic solvent. The colloidal solution can also include a therapeutic, prophylactic or diagnostic agent. Preferred carboxylic acids include at least two carboxyl groups. Preferred phospholipids include phosphatidylcholines, phosphatidylethanolamines, phosphatidylglycerols, phophstidylserines, phosphatidylinositols and combinations thereof. The particles are suitable for pulmonary delivery.
Type:
Grant
Filed:
October 4, 2007
Date of Patent:
October 5, 2010
Assignee:
Alkermes, Inc.
Inventors:
Michael M. Lipp, Richard P. Batycky, Giovanni Caponetti