Method of Drug Formulation Based on Increasing the Affinity of Crystalline Microparticle Surfaces for Active Agents
First Claim
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1. A microparticle comprising a diketopiperazine and polysorbate 80.
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Abstract
Methods are provided for coating crystalline microparticles with an active agent by altering the surface properties of the microparticles in order to facilitate favorable association on the microparticle by the active agent. Type of surface properties that are altered by the disclosed methods include by electrostatic properties, hydrophobic properties and hydrogen bonding properties.
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Citations
18 Claims
- 1. A microparticle comprising a diketopiperazine and polysorbate 80.
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14. A method of preparing diketopiperazine particles comprising:
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a. obtaining a solution of a diketopiperazine with limited solubility at low pH, b. adding polysorbate 80 to the solution, and c. precipitating diketopiperazine particles comprising polysorbate 80 by a step comprising adding an acid to the solution. - View Dependent Claims (15, 16, 17)
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18. A method for coating a preformed crystalline microparticle with an active agent in a suspension, said method comprising the steps in the sequence set forth of:
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i) obtaining a preformed crystalline microparticle wherein said preformed crystalline microparticle does not comprise an active agent; ii) providing a suspension comprising said preformed crystalline microparticle, said active agent, and a solvent; iii) then altering suspension conditions in said provided suspension to modify an energetic interaction between said active agent and said preformed crystalline microparticle wherein said altering suspension conditions is selected from the group consisting of altering the pH of the solvent, adding monovalent or multivalent ions, altering the polarity, and adding hydrogen bond donors or acceptors to modify a surface property of said preformed crystalline microparticle wherein said altering step does not include a step of removing said solvent from said suspension; and iv) adsorbing said active agent onto a surface of said preformed crystalline microparticle to provide a coating of said active agent on said crystalline microparticle without removing solvent from said suspension;
wherein said altering step causes said adsorbing of said active agent onto a surface of said preformed crystalline microparticle.
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Specification