Modulation of release from dry powder formulations
First Claim
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1. Particles for modulation of drug release comprising:
- (a) a bioactive agent; and
(b) a combination of phospholipids at least two of said phospholipids being miscible in one another, said particles having a matrix transition temperature corresponding to a targeted release rate of the biologically active agent from the particles and a tap density of less than about 0.4 g/cm3.
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Abstract
Particles which include a bioactive agent are prepared to have a desired matrix transition temperature. Delivery of the particles via the pulmonary system results in modulation of drug release from the particles. Sustained release and/or sustained pharmacologic action of the drug can be obtained by forming particles which include a combination of phospholipids that are miscible in one another and have a high matrix transition temperature.
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Citations
41 Claims
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1. Particles for modulation of drug release comprising:
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(a) a bioactive agent; and
(b) a combination of phospholipids at least two of said phospholipids being miscible in one another, said particles having a matrix transition temperature corresponding to a targeted release rate of the biologically active agent from the particles and a tap density of less than about 0.4 g/cm3. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)
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18. A method for delivery via the pulmonary system comprising administering to the respiratory tract of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles having a selected release rate of a bioactive agent, said particles comprising:
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(a) the bioactive agent; and
(b) a combination of phospholipids, at least two of said phospholipids being miscible in one another;
wherein the particles have a matrix transition temperature corresponding to a targeted release rate of the therapeutic, prophylactic or diagnostic agent from the particles and a tap density of less than about 0.4 g/cm3. - View Dependent Claims (19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38)
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39. A method for delivery via the pulmonary system particles having a release rate from the particles of a therapeutic, prophylactic or diagnostic agent comprising:
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administering to the respiratory system of a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising;
(a) the therapeutic, prophylactic or diagnostic agent, or combinations thereof; and
(b) a combination of phospholipids, at least two of said phospholipids being miscible in one another and said combination of phospholipids resulting in a matrix transition temperature such that the particles have the release rate;
wherein the particles have a tap density less than about 0.4 g/cm3.
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40. A method for increasing a release time of a therapeutic, prophylactic or diagnostic agent comprising administering to a patient in need of treatment, prophylaxis or diagnosis an effective amount of particles comprising:
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(a) a therapeutic, prophylactic or diagnostic agent; and
(b) a combination of phospholipids, at least two of said phospholipids being miscible in one another;
wherein the particles have a matrix transition temperature higher than the physiological temperature of the patient and a tap density of less than about 0.4 g/cm3.
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41. Particles for modulation of drug release having a tap density of less than about 0.4 g/Cm3 comprising:
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(a) a therapeutic, prophylactic or diagnostic agent; and
(b) a combination of phospholipids, at least two of said phospholipids being miscible in one another and said combination of phospholipids having a transition temperature higher than the body temperature of a human or veterinary subject.
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Specification