Macrolide particulates, methods for preparation, and medical devices associated therewith
First Claim
1. An implantable or insertable medical device comprising a macrolide particulate, the macrolide particulate comprising macrolide therapeutic agent in an amount of 95% or greater of the weight of the particulate, a component selected from the group consisting of poly(alkyleneimines), alkylated quaternary ammonium salts, and alkyl-substituted chromanols, and having a spherical or substantially spherical shape and a diameter in the range 0.1 μ
- m to 10 μ
m.
1 Assignment
0 Petitions
Accused Products
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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Citations
17 Claims
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1. An implantable or insertable medical device comprising a macrolide particulate, the macrolide particulate comprising macrolide therapeutic agent in an amount of 95% or greater of the weight of the particulate, a component selected from the group consisting of poly(alkyleneimines), alkylated quaternary ammonium salts, and alkyl-substituted chromanols, and having a spherical or substantially spherical shape and a diameter in the range 0.1 μ
- m to 10 μ
m. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9)
- m to 10 μ
-
10. A balloon catheter comprising a drug delivery coating composition comprising
macrolide particulates comprising macrolide therapeutic agent in an amount of 95% or greater of the weight of the particulate and having a size of less than 1 um, wherein the macrolide particulates have a thin coating, a shell, or are encapsulated to promote release of macrolide from the coating composition, the thin coating, shell, or encapsulating material having a thickness that is less than the diameter of the macrolide particulates, wherein the coating composition comprises lipid.
Specification