Pharmaceutical nanosuspensions for medicament administration as systems with increased saturation solubility and rate of solution
First Claim
1. Drug carrier comprising particles of at least one therapeutically active compound which is insoluble, only sparingly soluble or moderately soluble in water, aqueous media and/or organic solvents, wherein said active ingredient is solid at room temperature and has an average diameter, determined by photon correlation spectroscopy (PCS) of 10 nm to 1,000 nm, the proportion of particles larger than 5 μ
- m in the total population being less than 0.1% (number distribution determined with a Coulter counter), and, when introduced into water, aqueous media and/or organic solvents, the active compound has an increased saturation solubility and an increased rate of dissolution compared with powders of the active compound prepared using an ultrasonic probe, a ball mill or a pearl mill, the solid particles having been comminuted, without prior conversion into a melt, by using a piston-gap homogenizer.
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Abstract
Provided is a drug carrier comprising particles of at least one pure active compound which is insoluble, only sparingly soluble or moderately soluble in water, aqueous media and/or organic solvents, wherein said active ingredient is solid at room temperature and has an average diameter, determined by photon correlation spectroscopy (PCS) of 10 nm to 1,000 nm, the proportion of particles larger than 5 μm in the total population being less than 0.1% (number distribution determined with a Coulter counter), and, when introduced into water, aqueous media and/or organic solvents, the active compound has an increased saturation solubility and an increased rate of dissolution compared with powders of the active compound prepared using an ultrasonic probe, a ball mill or a pearl mill, the solid particles having been comminuted, without prior conversion into a melt, by using cavitation or shearing and impact forces with introduction of a high amount of energy.
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Citations
57 Claims
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1. Drug carrier comprising particles of at least one therapeutically active compound which is insoluble, only sparingly soluble or moderately soluble in water, aqueous media and/or organic solvents, wherein said active ingredient is solid at room temperature and has an average diameter, determined by photon correlation spectroscopy (PCS) of 10 nm to 1,000 nm, the proportion of particles larger than 5 μ
- m in the total population being less than 0.1% (number distribution determined with a Coulter counter), and, when introduced into water, aqueous media and/or organic solvents, the active compound has an increased saturation solubility and an increased rate of dissolution compared with powders of the active compound prepared using an ultrasonic probe, a ball mill or a pearl mill, the solid particles having been comminuted, without prior conversion into a melt, by using a piston-gap homogenizer.
- 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, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36)
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37. Drug carrier comprising particles of at least one therapeutically active compound which is insoluble, only sparingly soluble or moderately soluble in water, aqueous media and/or organic solvents, wherein said active ingredient is solid at room temperature and has an average diameter, determined by photon correlation spectroscopy (PCS) of 40 nm to 100 nm, the proportion of particles larger than 5 μ
- m in the total population being less than 0.1% (number distribution determined with a Coulter counter), the solid particles having been comminuted, without prior conversion into a melt, by using a piston-gap homogenizer.
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38. A method of making a drug carrier comprising the steps of:
subjecting at least one solid therapeutically active compound dispersed in a solvent to high pressure homogenization in a piston-gap homogenizer to form particles having an average diameter, determined by photon correlation spectroscopy (PCS) of 40 nm to 100 nm, the proportion of particles larger than 5 μ
m in the total population being less than 0.1% (number distribution determined with a Coulter counter), without prior conversion into a melt, wherein said active compound is solid at room temperature and is insoluble, only sparingly soluble or moderately soluble in water, aqueous media and/or organic solvents.
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39. Drug carrier comprising particles of at least one therapeutically active compound which is insoluble, only sparingly soluble or moderately soluble in water, aqueous media and/or organic solvents, wherein said active ingredient is solid at room temperature and has an average diameter, determined by photon correlation spectroscopy (PCS) of 10 nm to 1,000 nm, the proportion of particles larger than 5 μ
- m in the total population being less than 0.1% (number distribution determined with a Coulter counter), and, when introduced into water, aqueous media and/or organic solvents, the active compound has an increased saturation solubility and an increased rate of dissolution compared with powders of the active compound prepared using an ultrasonic probe, a ball mill or a pearl mill, the solid particles having been comminuted, without prior conversion into a melt, by using cavitation or shearing and impact forces with introduction of a high amount of energy, and wherein said active compound comprises at least one compound selected from the group consisting of;
analgesics, anaesthetics, antirheumatics, antiallergics, antibiotics, antiepileptics, antimycotics, calcium metabolism regulators, chemotherapeutics, corticoids, cytokines, cytostatics, dermatics, hypnotics, immunotherapeutics, local anesthetics, metastasis inhibitors, migraine agents, ophthalmics, parathyroid hormones, psychotropics, sedatives, and sex hormones. - View Dependent Claims (40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56)
- m in the total population being less than 0.1% (number distribution determined with a Coulter counter), and, when introduced into water, aqueous media and/or organic solvents, the active compound has an increased saturation solubility and an increased rate of dissolution compared with powders of the active compound prepared using an ultrasonic probe, a ball mill or a pearl mill, the solid particles having been comminuted, without prior conversion into a melt, by using cavitation or shearing and impact forces with introduction of a high amount of energy, and wherein said active compound comprises at least one compound selected from the group consisting of;
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57. A method of making a drug carrier comprising the steps of:
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subjecting at least one solid therapeutically active compound dispersed in a solvent to high pressure homogenization in a piston-gap homogenizer to form particles having an average diameter, determined by photon correlation spectroscopy (PCS) of 40 nm to 100 nm, the proportion of particles larger than 5 μ
m in the total population being less than 0.1% (number distribution determined with a Coulter counter), without prior conversion into a melt, wherein said active compound is solid at room temperature and is insoluble, only sparingly soluble or moderately soluble in water, aqueous media and/or organic solvents, wherein said active compound comprises at least one compound selected from the group consisting of;analgesics, anaesthetics, antirheumatics, antiallergics, antibiotics, antiepileptics, antimycotics, calcium metabolism regulators, chemotherapeutics, corticoids, cytokines, cytostatics, dermatics, hypnotics, immunotherapeutics, local anesthetics, metastasis inhibitors, migraine agents, ophthalmics, parathyroid hormones, psychotropics, sedatives, and sex hormones.
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Specification