Solid formulations of liquid biologically active agents
First Claim
1. A solid product suitable for reconstitution to an essentially clear, stable solution upon addition of an aqueous reconstituting solvent thereto, said solid product comprising an intimate mixture of at least one stabilizing agent, and at least one liquid biologically active agent loaded within said stabilizing agent, in such a manner that said liquid biologically active agent is intimately associated with said stabilizing agent in a substantially solid product;
- whereby upon hydration with a reconstituting aqueous solvent or solution, said solid product forms said essentially clear stable solution in which said at least one biologically active agent is present as stable nanodispersions or micelles loaded with said at least one biologically active agent.
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Accused Products
Abstract
The instant invention relates to a solid product comprising a liquid biologically active agent which is intimately associated to a stabilizing agent; particularly a solid product that can be reconstituted to a clear, stable, stabilized nanodispersion or loaded micelles comprising a polymer as a stabilizing agent and a liquid, preferably water immiscible, biologically active agent. The instant invention is further directed toward a process for the production of the above solid product; particularly to micelles or nanodispersions produced by hydration of a cake or powder of the solid product, produced via an effective treatment of a stabilized solution comprising for example a polymer as a stabilizing agent, such as an amphiphilic block copolymer or a small molecular weight surfactant, loaded with a liquid biologically active agent, such as propofol, an optional additive, and a suitable solvent.
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Citations
38 Claims
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1. A solid product suitable for reconstitution to an essentially clear, stable solution upon addition of an aqueous reconstituting solvent thereto, said solid product comprising an intimate mixture of
at least one stabilizing agent, and at least one liquid biologically active agent loaded within said stabilizing agent, in such a manner that said liquid biologically active agent is intimately associated with said stabilizing agent in a substantially solid product; whereby upon hydration with a reconstituting aqueous solvent or solution, said solid product forms said essentially clear stable solution in which said at least one biologically active agent is present as stable nanodispersions or micelles loaded with said at least one biologically active agent. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 22, 27, 36, 37)
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21. A process for the production of a solid product suitable for reconstitution to a clear stable solution upon addition of an aqueous solution thereto, which comprises forming a first mixture comprising a solution of at least one stabilizing agent and at least one solvent, under conditions to achieve micelle or nanodispersion formation;
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adding at least one liquid biologically active agent to said first mixture in such a manner to load said micelle or nanodispersion therewith and form a second mixture;
treating said second mixture under conditions effective to remove said solvent therefrom while forming a substantially solid product that contains said liquid biologically active agent intimately associated with said stabilizing agent, said solid product upon hydration being capable of forming a clear stable solution in which said at least one biologically active agent is present as nanodispersion or micelle loaded with said at least one biologically active agent. - View Dependent Claims (23, 24, 25, 26, 28, 29, 30, 31, 32, 33, 34, 35)
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38. A device for producing solid formulations of liquid biologically active agents comprising
a container, means for adding at least one stabilizing agent and at least one solvent into said container, mixing means operable with said container to form a first mixture of said stabilizing agent and said solvent under conditions to achieve micelle or nanodispersion therein, means for subsequently adding a liquid biologically active agent to said first mixture and to form a second mixture, means operating said mixing means under conditions to treat said second mixture to load said micelle or nanodispersion with said biologically active agent, and means for treating said loaded micelle or nanodispersion to form a solid product containing said liquid biologically active agent intimately associated with said stabilizing agent and substantiallhy free of said solvent.
Specification