Abstract: Provided is an injectable sustained release pharmaceutical formulation, including 3-acyl-naltrexone or a pharmaceutically acceptable salt thereof, a biocompatible organic solvent, and optionally a biocompatible polymeric material. Also provided is a method for treating opioid use disorder or alcoholism, including administering the injectable sustained release pharmaceutical formulation to a subject in need thereof. The pharmaceutical formulation provides a sustained release profile after one single injection, and the plasma levels of naltrexone in minipigs could provide a sustained release for 2 months.

Abstract: Provided are pamoate salts of ketamine having a stoichiometry of 2:1 of ketamine to pamoate, including R, S-ketamine pamoate, S-ketamine pamoate, or R-ketamine pamoate, and crystalline or amorphous forms of the pamoate salts, and having excellent safety and properties for pharmaceutical applications. Also provided are pharmaceutical compositions including the pamoate salts of ketamine and their uses in treating a CNS disease or serving as an anesthetic.

Abstract: Provided are sustained-release pharmaceutical compositions including a ketamine pamoate salt and a pharmaceutically acceptable carrier thereof. The compositions include aqueous suspension, solution and matrix delivery system, which can provide sustained release for anesthesia, analgesia or treatment of central nervous system and anti-inflammatory diseases.

Abstract: This disclosure relates to crystalline forms of 3-acyl-buprenorphine derivatives and sustained release injectable pharmaceutical compositions for treatment of opioid dependence, pain or depression, including an aqueous suspension of crystalline 3-acyl-buprenoprhine, or a pharmaceutically acceptable salt thereof, wherein the composition does not include an organic solvent, a polylactide polymer, a polyglycolide polymer, or a copolymer of polylactide and polyglycolide. This disclosure also includes 3-acyl-buprenoprhine or a pharmaceutically acceptable salt thereof prepared in a controlled release matrix, including poly(lactide-co-glycolide), sucrose acetoisobutyrate, lecithin, diolein and a combination of two or more thereof.

Abstract: An injectable pharmaceutical composition includes a solution of 3-acyl-buprenorphine, or a pharmaceutically acceptable salt thereof, in a biocompatible organic solvent, wherein the injectable pharmaceutical composition exhibits a steady release profile lasting over one week when injected into a patient. The acyl group is an alkylcarbonyl group, and an alkyl portion of the alkylcarbonyl group is a straight-chain, branched-chain, having 1-20 carbon atoms. The biocompatible organic solvent is N-methyl-2-pyrrolidone, ethyl acetate, ethanol, butanol, 2-butanol, isobutanol, ispropanol, glycerin, benzyl benzoate, dimethyl sulfoxide, N,N-dimethylacetamide, propylene glycol, dimethyl glycol, benzyl alcohol, or a combination of two or more thereof.

Abstract: An injectable pharmaceutical composition includes a solution of 3-acyl-buprenorphine, or a pharmaceutically acceptable salt thereof, in a biocompatible organic solvent, wherein the injectable pharmaceutical composition exhibits a steady release profile lasting over one week when injected into a patient. The acyl group is an alkylcarbonyl group, and an alkyl portion of the alkylcarbonyl group is a straight-chain, branched-chain, having 1-20 carbon atoms. The biocompatible organic solvent is N-methyl-2-pyrrolidone, ethyl acetate, ethanol, butanol, 2-butanol, isobutanol, ispropanol, glycerin, benzyl benzoate, dimethyl sulfoxide, N,N-dimethylacetamide, propylene glycol, dimethyl glycol, benzyl alcohol, or a combination of two or more thereof.