Sustained release microparticulate caffeine formulation
First Claim
1. A sustained release stimulant composition of microparticles comprising:
- a stimulant of xanthine or a xanthine derivative; and
substantially spherical solid cores of pharmaceutically acceptable organic material, having;
a) a first layer substantially surrounding the core which comprises a biodegradable matrix of a water soluble binding agent, a water insoluble release retarding agent, and between about 55-95% by weight of the total amount of stimulant present in the particle, wherein;
i) the binding agent binds the stimulant to the microparticle;
ii) the release retarding agent retards the release of the stimulant from the matrix; and
iii) the stimulant is uniformly distributed in the matrix;
b) a second layer substantially surrounding the first layer which comprises a water insoluble material for further delaying the release of the stimulant from the first layer; and
c) a third layer substantially surrounding the second layer which comprises a biodegradable matrix of a water soluble binding agent, a water insoluble release retarding agent and between about 5-45% by weight of the total amount of the stimulant present in the particle, wherein;
i) the binding agent binds the stimulant to the microparticle;
ii) the release retarding agent retards the release of the stimulant from the matrix; and
iii) the stimulant is uniformly distributed in the matrix,and further wherein;
A) at least about 20-50% by weight of the total amount of the stimulant present in the composition is capable of being released within about 2 hours following oral administration; and
B) the balance of the stimulant is capable of being released within about 8-10 hours following oral administration.
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Accused Products
Abstract
The present invention relates to compositions and methods for increasing the alertness of an individual through the administration of a stimulant such as xanthine or an xanthine derivative and preferably caffeine. A particular composition has one or more layers containing the stimulant arranged about the cores of microparticles. This allows the composition to release a significant portion of the stimulant within about two hours after administration so that a level of alertness can be readily achieved. Thereafter, the balance of the composition is released within about 6 to 10 hours, so that the stimulant can provide alertness during that time, but then can dissipate to levels which would not affect the individual'"'"'s ability to sleep. Also, the formulation is carefully designed so that the stimulant does not accumulate in the individual'"'"'s system.
51 Citations
14 Claims
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1. A sustained release stimulant composition of microparticles comprising:
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a stimulant of xanthine or a xanthine derivative; and substantially spherical solid cores of pharmaceutically acceptable organic material, having; a) a first layer substantially surrounding the core which comprises a biodegradable matrix of a water soluble binding agent, a water insoluble release retarding agent, and between about 55-95% by weight of the total amount of stimulant present in the particle, wherein; i) the binding agent binds the stimulant to the microparticle; ii) the release retarding agent retards the release of the stimulant from the matrix; and iii) the stimulant is uniformly distributed in the matrix; b) a second layer substantially surrounding the first layer which comprises a water insoluble material for further delaying the release of the stimulant from the first layer; and c) a third layer substantially surrounding the second layer which comprises a biodegradable matrix of a water soluble binding agent, a water insoluble release retarding agent and between about 5-45% by weight of the total amount of the stimulant present in the particle, wherein; i) the binding agent binds the stimulant to the microparticle; ii) the release retarding agent retards the release of the stimulant from the matrix; and iii) the stimulant is uniformly distributed in the matrix, and further wherein; A) at least about 20-50% by weight of the total amount of the stimulant present in the composition is capable of being released within about 2 hours following oral administration; and B) the balance of the stimulant is capable of being released within about 8-10 hours following oral administration. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
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14. A sustained release stimulant composition of microparticles consisting essentially of:
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a stimulant of xanthine or a xanthine derivative; and substantially spherical solid cores of pharmaceutically acceptable organic material, having; a) a first layer substantially surrounding the core which consists essentially of a biodegradable matrix of a water soluble binding agent, a water insoluble release retarding agent, and between about 55-95% by weight of the total amount of stimulant present in the particle, wherein; i) the binding agent binds the stimulant to the microparticle; ii) the release retarding agent retards the release of the stimulant from the matrix; and iii) the stimulant is uniformly distributed in the matrix; b) a second layer substantially surrounding the first layer which consists essentially of a water insoluble material for further delaying the release of the stimulant from the first layer; and c) a third layer substantially surrounding the second layer which consists essentially of a biodegradable matrix of a water soluble binding agent, a water insoluble release retarding agent and between about 5-45% by weight of the total amount of the stimulant present in the particle, wherein; i) the binding agent binds the stimulant to the microparticle; ii) the release retarding agent retards the release of the stimulant from the matrix; and iii) the stimulant is uniformly distributed in the matrix, and further wherein; A) at least about 20-50% by weight of the total amount of the stimulant present in the composition is capable of being released within about 2 hours following oral administration; and B) the balance of the stimulant is capable of being released within about 8-10 hours following oral administration.
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Specification