Phospholipid depot
AssigneeDr. Reddy's Laboratories, Inc.
InventorsHailiang Chen, Andrew Xian Chen, Dushyanth Surakanti, Franklin Okumu
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Abstract
The present invention provides a clear depot comprising at least one hydrophilic water-soluble pharmaceutically active agent selected from the group consisting of vancomycin, gentamicin, a pharmaceutically acceptable salt thereof and a mixture thereof, water, a phospholipid, an oil, optionally a pH adjusting agent, and a viscosity modifying agent selected from the group consisting of ethanol, isopropanol, and a mixture thereof, wherein the water present in the depot is no more than about 4 wt % relative to the total weight of the depot and the depot has a pH of between about 3 and about 6, method of making and administering same.
Claims51
A method for making a depot comprising:
- (1) forming an oil-in-water emulsion including a phospholipid, an oil, at least one hydrophilic water-soluble pharmaceutically active agent selected from the group consisting of vancomycin, gentamicin, a pharmaceutically acceptable salt thereof or a mixture thereof and water;
- (2) homogenizing the emulsion to obtain a primary emulsion;
- (3) microfluidizing the primary emulsion to obtain a monophasic solution;
- (4) ensuring the pH of the primary emulsion and/or the monophasic solution is between about 3 to about 6 by adjusting the pH as necessary,
- (5) lyophilizing the monophasic solution of desired pH to obtain a dry paste,
- (6) adding a viscosity modifying agent to the dry paste in an amount of about 25 wt % or more of the total weight of a resulting viscosity modified solution,
- (7) removing at least some of the viscosity modifying agent to obtain a depot having from about 1 wt % to about 20 wt % of the viscosity modifying agent relative to the total weight of the depot, and
- (8) sterilizing the depot.
A method for making a depot comprising:
- (1) forming an oil-in-water emulsion including a phospholipid, an oil, at least one hydrophilic water-soluble pharmaceutically active agent selected from the group consisting of vancomycin, gentamicin, a pharmaceutically acceptable salt thereof and a mixture thereof and water;
- (2) converting the emulsion to a monophasic solution having a pH of between about 3 to about 6;
- (3) lyophilizing the monophasic solution to obtain a dry paste,
- (4) adding a viscosity modifying agent to the dry paste in an amount sufficient to obtain a viscosity modified solution,
- (5) removing at least some of the viscosity modifying agent to obtain a depot, and
- (6) sterilizing the depot, wherein the depot is clear.
A depot comprising at least one hydrophilic water-soluble pharmaceutically active agent selected from the group consisting of vancomycin, gentamicin, a pharmaceutically acceptable salt thereof and a mixture thereof, water, a phospholipid, an oil, optionally a pH adjusting agent, and a viscosity modifying agent selected from the group consisting of ethanol, isopropanol, and a mixture thereof, wherein the water present in the depot is no more than about 4 wt % relative to the total weight of the depot and the depot has a pH of between about 3 and about 6.
A clear depot comprising vancomycin hydrochloride and gentamicin sulfate, water, a phospholipid, an oil, optionally a pH adjusting agent, and ethanol, wherein the water present in the depot is no more than about 4 wt % relative to the total weight of the depot and the depot has a pH of between about 3 and about 6.
Dependencies are inferred from the claim text.