Controlled-Release of an active substance into a high fat environment
First Claim
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1. A method for the controlled-release of an active substance into a use environment, comprising:
- a. preparing a controlled-release delivery composition comprising an active-substance-containing core and an asymmetric polymeric coating thereon, wherein the polymer used to form said asymmetric polymeric coating is one which, when tested by soaking for at least 16 hours in an aqueous solution comprising 0.5 wt % dietary fat, gains less than about 15 wt %; and
b. administering said composition to said use environment, said use environment comprising at least about 0.5 wt % of dietary fat.
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Abstract
A controlled release delivery composition which can be administered to a high fat use environment such as the human gastrointestinal tract following a high fat meal. The delivery composition is embodied as a core surrounded by an asymmetric polymeric membrane. In a preferred embodiment, the asymmetric polymeric membrane is cellulose acetate.
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Citations
22 Claims
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1. A method for the controlled-release of an active substance into a use environment, comprising:
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a. preparing a controlled-release delivery composition comprising an active-substance-containing core and an asymmetric polymeric coating thereon, wherein the polymer used to form said asymmetric polymeric coating is one which, when tested by soaking for at least 16 hours in an aqueous solution comprising 0.5 wt % dietary fat, gains less than about 15 wt %; and
b. administering said composition to said use environment, said use environment comprising at least about 0.5 wt % of dietary fat. - View Dependent Claims (9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22)
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2. A method for the controlled-release of an active substance into a use environment, comprising:
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a. preparing a controlled-release delivery composition comprising an active-substance-containing core and an asymmetric polymeric coating thereon, wherein the time to release 50% of said active substance from said composition into said use environment is at least 0.5-fold, but less than 2.0-fold the time required for said composition to release 50% of said active substance into a control use environment comprising less than about 0.1% of dietary fat, and b. administering said composition to said use environment, said use environment comprising at least about 0.5 wt % of dietary fat.
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3. A method for the controlled-release of an active substance into a use environment, comprising:
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a. preparing a controlled-release delivery composition comprising an active-substance-containing core and an asymmetric polymeric coating thereon, wherein the amount of drug released from said composition at any time between the 2nd and 10th hour following introduction of said composition to said use environment is at least 0.5-fold, but less than 2.0-fold the amount of said drug released at the same time between the 2nd and 10th hour by said composition into a control use environment comprising less than about 0.1% of dietary fat, and b. administering said composition to said use environment, said use environment comprising at least about 0.5 wt % of dietary fat.
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4. A method for the controlled-release of an active substance into a use environment, comprising:
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a. preparing a controlled-release delivery composition comprising an active-substance-containing core and an asymmetric polymeric coating thereon, wherein the average rate of drug release from said composition between the 2nd and 10th hour after introduction into said use environment is at least 0.5-fold, but less than 2.0-fold the average rate of drug release provided by said composition in a control use environment comprising less than about 0.1% of dietary fat, and b. administering said composition to said use environment, said use environment comprising at least about 0.5 wt % of dietary fat.
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5. A method for the controlled-release of an active substance into a use environment, comprising:
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a. preparing a controlled-release delivery composition comprising an active-substance-containing core and an asymmetric polymeric coating thereon, wherein the composition provides a maximum concentration of said active substance in said use environment that is at least 0.5-fold, but less than 2.0-fold the maximum concentration provided by said composition in a control use environment comprising less than about 0.1% of dietary fat, and b. administering said composition to said use environment, said use environment comprising at least about 0.5 wt % of dietary fat.
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6. A method for the controlled-release of an active substance into a use environment, comprising:
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a. preparing a controlled-release delivery composition comprising an active-substance-containing core and an asymmetric polymeric coating thereon, wherein the composition provides an area under the active substance concentration versus time curve (AUC) for any period of at least 90 minutes between the time of introduction to said use environment and about 270 minutes following introduction to said use environment that is at least 0.5-fold, but less than 2.0-fold the AUC provided by said composition in a control use environment comprising less than about 0.1% of dietary fat, and b. administering said composition to said use environment, said use environment comprising at least about 0.5 wt % of dietary fat.
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7. A method for the controlled-release of an active substance into a use environment, comprising:
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a. preparing a controlled-release delivery composition comprising an active-substance-containing core and an asymmetric polymeric coating thereon, wherein the composition provides a relative bioavailability in said use environment that is at least 0.5-fold, but less than 2.0-fold the relative bioavailability provided by said composition in a control use environment comprising less than about 0.1 % of dietary fat, and b. administering said composition to said use environment, said use environment comprising at least about 0.5 wt % of dietary fat.
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8. A therapeutic package, comprising:
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a container, a controlled-release delivery composition for the controlled release of an active substance into a use environment, comprising an active-substance-containing core and an asymmetric polymeric coating thereon, wherein said delivery composition satisfies any one or more of the following conditions (i) through (vii);
(i) the polymer used to form said polymeric coating is one which, when tested by soaking for at least 16 hours in an aqueous solution comprising 0.5 wt % dietary fat, gains less than about 15 wt %;
(ii) the time to release 50% of said active substance from said composition into said use environment is at least 0.5-fold, but less than 2.0-fold the time required for said composition to release 50% of said active substance into a control use environment comprising less than about 0.1 % of dietary fat;
(iii) the amount of drug released from said composition at any time between the 2nd and 10th hour following introduction of said composition to said use environment is at least 0.5-fold, but less than 2.0-fold the amount of said drug released at the same time between the 2nd and 10th hour by said composition into a control use environment comprising less than about 0.1% of dietary fat;
(iv) the average rate of drug release from said composition between the 2nd and 10th hour after introduction into said use environment is at least 0.5-fold, but less than 2.0-fold the average rate of drug release provided by said composition in a control use environment comprising less than about 0.1% of dietary fat;
(v) the composition provides a maximum concentration of said active substance in said use environment that is at least 0.5-fold, but less than 2.0-fold the maximum concentration provided by said composition in a control use environment comprising less than about 0.1% of dietary fat;
(vi) the composition provides an area under the active substance concentration versus time curve (AUC) for any period of at least 90 minutes between the time of introduction to said use environment and about 270 minutes following introduction to said use environment that is at least 0.5-fold, but less than 2.0-fold the AUC provided by said composition in a control use environment comprising less than about 0.1% of dietary fat;
or(vii) the composition provides a relative bioavailability in said use environment that is at least 0.5-fold, but less than 2.0-fold the relative bioavailability provided by said composition in a control use environment comprising less than about 0.1% of dietary fat, and, associated with said package, written matter non-limited as to whether the dosage form can be taken with or without food.
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Specification