Abstract: Various embodiments of a method of preparing sustained release microparticles are described. In one embodiment, the method includes the steps of forming a dispersed phase of an active agent in a polymer and combining the dispersed phase with a continuous phase to form a microparticle dispersion. The method further includes the step of adding a measured amount of a dilution composition to the microparticle dispersion. It has been found herein that the various embodiments for preparing sustained release microparticles using various amounts of the dilution composition alters the release rate of the sustained microparticle for the specific active agent.

Abstract: A method of making a sustained release microsphere formulation, wherein the release rate of a bioactive ingredient is manipulated by controlling the crystallinity of said bioactive ingredient, includes the steps of combining the active ingredient and an encapsulating polymer in at least one solvent, or mixtures thereof, to form a dispersed phase and processing the dispersed phase without filtering, filtering the combined dispersed phase with a hydrophobic or a hydrophilic filter, or filtering the active ingredient and encapsulating polymer individually with a hydrophobic or hydrophilic filter before combining them to form the dispersed phase. The dispersed phase is then combined with a continuous phase to form the microsphere formulation.

Abstract: A sustained release microsphere formulation with a high drug load may be formed by a continuous oil-in-water emulsion process by combining an organic dispersed phase with an aqueous continuous phase. The dispersed phase may include an encapsulating polymer, a primary solvent, such as dichloromethane, a pharmaceutically effective amount of an active agent having a solubility relative to the dispersed phase, and a co-solvent, such as benzyl alcohol, which is capable of increasing the solubility of the active agent relative to the dispersed phase. The continuous phase may include an aqueous solution of polyvinyl alcohol and water.

Abstract: A sustained release microsphere formulation with a high drug load may be formed by a continuous oil-in-water emulsion process by combining an organic dispersed phase with an aqueous continuous phase. The dispersed phase may include an encapsulating polymer, a primary solvent, such as dichloromethane, a pharmaceutically effective amount of an active agent having a solubility relative to the dispersed phase, and a co-solvent, such as benzyl alcohol, which is capable of increasing the solubility of the active agent relative to the dispersed phase. The continuous phase may include an aqueous solution of polyvinyl alcohol and water.

Abstract: A sustained release microsphere formulation with a high drug load may be formed by a continuous oil-in-water emulsion process by combining an organic dispersed phase with an aqueous continuous phase. The dispersed phase may include an encapsulating polymer, a primary solvent, such as dichloromethane, a pharmaceutically effective amount of an active agent having a solubility relative to the dispersed phase, and a co-solvent, such as benzyl alcohol, which is capable of increasing the solubility of the active agent relative to the dispersed phase. The continuous phase may include an aqueous solution of polyvinyl alcohol and water.

Abstract: A method of making a sustained release microsphere formulation, wherein the release rate of a bioactive ingredient is manipulated by controlling the crystallinity of said bioactive ingredient, includes the steps of combining the active ingredient and an encapsulating polymer in at least one solvent, or mixtures thereof, to form a dispersed phase and processing the dispersed phase without filtering, filtering the combined dispersed phase with a hydrophobic or a hydrophilic filter, or filtering the active ingredient and encapsulating polymer individually with a hydrophobic or hydrophilic filter before combining them to form the dispersed phase. The dispersed phase is then combined with a continuous phase to form the microsphere formulation.

Abstract: A sustained release microsphere formulation with a high drug load may be formed by a continuous oil-in-water emulsion process by combining an organic dispersed phase with an aqueous continuous phase. The dispersed phase may include an encapsulating polymer, a primary solvent, such as dichloromethane, a pharmaceutically effective amount of an active agent having a solubility relative to the dispersed phase, and a co-solvent, such as benzyl alcohol, which is capable of increasing the solubility of the active agent relative to the dispersed phase. The continuous phase may include an aqueous solution of polyvinyl alcohol and water.

Abstract: This disclosure features a system for processing microspheres. A vessel contains a suspension of solidified microspheres comprising polymer and an active agent. A hydrocyclone has a fluid inlet, a first fluid outlet and a second fluid outlet. The fluid inlet is in fluid communication with the vessel and receives the suspension. The second fluid outlet contains a flow of the suspension having concentrated microspheres. The first fluid outlet contains a flow of a relatively large amount of liquid compared to the flow from the second fluid outlet. Also featured is a method of processing the microspheres using the hydrocyclone.

Abstract: This disclosure features a system for processing microspheres. A vessel contains a suspension of solidified microspheres comprising polymer and an active agent. A hydrocyclone has a fluid inlet, a first fluid outlet and a second fluid outlet. The fluid inlet is in fluid communication with the vessel and receives the suspension. The second fluid outlet contains a flow of the suspension having concentrated microspheres. The first fluid outlet contains a flow of a relatively large amount of liquid compared to the flow from the second fluid outlet. Also featured is a method of processing the microspheres using the hydrocyclone.

Abstract: This disclosure features microspheres and a method of making them. The microspheres are for sustained release of an octreotide compound with a low initial burst, comprising a poly(D,L-lactide-co-glycolide) polymer matrix and an octreotide compound dispersed in the polymer matrix. The microspheres release less than 1% of a total amount of the octreotide compound within 1 hour at 37° C. and pH 7.4.

Abstract: Various embodiments of a method of preparing sustained release microparticles are described. In one embodiment, the method includes the steps of forming a dispersed phase of an active agent in a polymer and combining the dispersed phase with a continuous phase to form a microparticle dispersion. The method further includes the step of adding a measured amount of a dilution composition to the microparticle dispersion. It has been found herein that the various embodiments for preparing sustained release microparticles using various amounts of the dilution composition alters the release rate of the sustained microparticle for the specific active agent.

Abstract: This disclosure features microspheres and a method of making them. The microspheres are for sustained release of an octreotide compound with a low initial burst, comprising a poly(D,L-lactide-co-glycolide) polymer matrix and an octreotide compound dispersed in the polymer matrix. The microspheres release less than 1% of a total amount of the octreotide compound within 1 hour at 37° C. and pH 7.4.

Abstract: Microspheres for releasing an octreotide compound without an initial time lag include a poly(D,L-lactide-co-glycolide) polymer (PLGA polymer) matrix having a ratio of lactide to glycolide ranging from 80:20 to 90:10 mol %. The polymer has a molecular weight ranging from about 6000 to 16000. The octreotide compound is dispersed in the polymer matrix. The microspheres can be made by forming a dispersed phase by combining the above polymer, dichloromethane, the octreotide compound, methanol and acetic acid. A target loading of the octreotide compound in the dispersed phase ranges from 7 to 12% by weight. Polyvinyl alcohol is dissolved in water to form a continuous phase. The dispersed phase is mixed in the continuous phase to form a microsphere suspension. The dichloromethane, acetic acid, methanol and polyvinyl alcohol are removed from the microsphere suspension. Residual dichloromethane and methanol are removed from the microspheres by washing.

Abstract: A process and apparatus for making and formulating microcapsules and microspheres which can easily be maintained aseptic throughout all stages of the production process.

Abstract: A process and apparatus for making and formulating microcapsules and microspheres which can easily be maintained aseptic throughout all stages of the production process.

Abstract: A continuous process for producing microspheres wherein small particle sizes can be obtained without the problem of foaming. A drug and polymer containing dispersed phase is continuously introduced into a high intensity emulsification vessel along with a continuous phase. An emulsion of the dispersed phase is formed in the continuous phase by high intensity mixing effective to quickly solidify the dispersed phase polymer without having to take steps to address foaming.