GAMMA RADIATION STERILIZED NANOPARTICULATE DOCETAXEL COMPOSITIONS AND METHODS OF MAKING SAME
First Claim
Patent Images
1. A sterile composition comprising:
- (a) particles comprising at least one active agent selected from the group consisting of docetaxel, salts of docetaxel, derivatives of docetaxel, conjugates of docetaxel and analogues of docetaxel, wherein the particles have an effective average particle size of less than about 2000 nm; and
(b) at least one surface stabilizer adsorbed on a surface of the particles, wherein the composition is sterilized by exposure to gamma radiation.
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Accused Products
Abstract
Nanoparticulate compositions comprising docetaxel or a salt, derivative, conjugate or analogue thereof, wherein the compositions are terminally sterilized via gamma radiation, are described, as well as methods of making and using such compositions.
117 Citations
43 Claims
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1. A sterile composition comprising:
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(a) particles comprising at least one active agent selected from the group consisting of docetaxel, salts of docetaxel, derivatives of docetaxel, conjugates of docetaxel and analogues of docetaxel, wherein the particles have an effective average particle size of less than about 2000 nm; and (b) at least one surface stabilizer adsorbed on a surface of the particles, wherein the composition is sterilized by exposure to gamma radiation. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 28, 29)
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26. A dry composition comprising about 18.87% docetaxel, about 4.72% povidone, about 0.94% sodium deoxycholate, about 56.60% sucrose, and about 18.87% mannitol.
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27. A dry composition comprising about 18.87% docetaxel, about 4.72% povidone, about 0.94% sodium deoxycholate, about 37.74% sucrose, and about 37.74% mannitol.
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30. A method for making a sterilized nanoparticulate composition comprising the steps of:
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lyophilizing an aqueous dispersion comprising at least one active agent selected from the group consisting of docetaxel, salts of docetaxel, derivatives of docetaxel, conjugates of docetaxel and analogues of docetaxel, wherein the particles have an effective average particle size of less than about 2000 nm, and at least one surface stabilizer adsorbed on a surface of the particles, to form a lyo; and sterilizing the lyo to produce a sterilized composition. - View Dependent Claims (31, 32, 33, 34, 35, 36, 37)
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39. A terminally sterilized lyophilization composition made from the steps comprising:
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milling at least one active agent selected from the group consisting of docetaxel, salts of docetaxel, derivatives of docetaxel, conjugates of docetaxel and analogues of docetaxel, an excipient selected from the group consisting of a bulking agent, a crystal growth inhibitor, a free radical scavenger agent, a redispersion agent, and at least one surface stabilizer, with milling media in an aqueous medium for a period of time and under conditions sufficient to provide a dispersion of particles of the at least one active agent having an effective average particle size of less than about 2000 nm, and the at least one surface stabilizer adsorbed on the surface of the particles; removing the milling media from the dispersion; lyophilizing the dispersion to form a lyo; and sterilizing the lyo to produce a sterilized composition. - View Dependent Claims (40)
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41. A method of treating a subject in need of docetaxel or a salt, derivative, conjugate or analogue thereof comprising administering to the subject an effective amount of a composition comprising:
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(a) particles comprising docetaxel, a salt, derivative, conjugate or analogue thereof, wherein the particles have an effective average particle size of less than about 2000 nm; and (b) at least one surface stabilizer adsorbed on a surface of the particles, wherein the composition is sterilized by exposure to gamma radiation. - View Dependent Claims (42)
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43. A sterile liquid dosage form of docetaxel for intravenous administration comprising:
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(a) about 5% by weight particles of at least one active agent selected from the group consisting of docetaxel, salts of docetaxel, derivatives of docetaxel, conjugates of docetaxel and analogues of docetaxel, the particles having an effective average particle size of less than about 2000 nm; (b) two surface stabilizers, one or both of the surface stabilizers is adsorbed on a surface of particles; (c) sucrose; and (d) mannitol, wherein the composition is sterilized by exposure to gamma radiation, and wherein the composition is administered to a patient at a dosage amount selected from the group consisting of about 100, 200, 300, 400, 500, 600, 700, 800, 900 and 1000 mg/m2.
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Specification