Macrolide particulates, methods for preparation, and medical devices associated therewith
First Claim
1. A method for producing macrolide particulates, comprising steps ofproviding a first composition comprising a non-antibiotic macrolide therapeutic agent dissolved in a liquid selected from the group consisting of C1-C4 alcohols,forming a mixture by adding to the first composition a second composition that is a non-solvent for the macrolide therapeutic and comprises a component selected from the group consisting of poly(ethyleneimines) and alkylated quaternary ammonium salts, where mixing comprises agitating the mixture to cause the formation of macrolide particulates.
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Abstract
The disclosure provides macrolide particulates including a macrolide therapeutic agent such as rapamycin at high concentration in the particulate. In one method the particulates are made by adding a composition containing an polyoxyethylene sorbitan n-acyl ester, poly(ethyleneimine), or alkylated quaternary ammonium salt to a composition including macrolide dissolved in an alcohol such as ethanol. In another method the particulates are made by adding a non-solvent composition to a composition including macrolide and an alkyl-substituted chromanol dissolved in an alcohol such as ethanol. The formed macrolide particulates have one or more desirable properties including sizes in the range of 0.1 μm to 10 μm, spherical or near spherical shapes, low polydispersity, and/or stability. The macrolide particulates can be used for therapeutic compositions, or in association with an implantable or insertable medical device, such as associated with a polymeric coating on a device.
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17 Claims
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1. A method for producing macrolide particulates, comprising steps of
providing a first composition comprising a non-antibiotic macrolide therapeutic agent dissolved in a liquid selected from the group consisting of C1-C4 alcohols, forming a mixture by adding to the first composition a second composition that is a non-solvent for the macrolide therapeutic and comprises a component selected from the group consisting of poly(ethyleneimines) and alkylated quaternary ammonium salts, where mixing comprises agitating the mixture to cause the formation of macrolide particulates.
Specification