Back to results
US 2003/0165566 A1Published application
Sedative non-benzodiazepine formulations
OwnerEdel O'Toole, Siobhan Fogartyinventors
Life of this patent
Estimating the term…
Abstract
The invention provides for an enhanced absorption pharmaceutical composition comprising a plurality of microparticles, each microparticle comprising at least one sedative non-benzodiazepine, at least one spheronization aid and at least one solubility enhancer. The microparticles of the invention are further incorporated into an oral fast-dispersing dosage form.
Claims77
An enhanced absorption pharmaceutical composition comprising a plurality of microparticles, each microparticle comprising an effective amount of at least one sedative non-benzodiazepine, at least one spheronization aid and at least one solubility enhancer.
An enhanced absorption pharmaceutical composition comprising a plurality of microparticles, each microparticle comprising an effective amount of zolpidem, distilled monoglycerides and a macrogol fatty acid ester.
An oral fast-dispersing dosage form comprising:
- (a) microparticles comprising an effective amount of at least one sedative non-benzodiazepine, at least one spheronization aid and at least one solubility enhancer, said microparticles coated with at least one taste-masking coating and adapted for enhanced absorption of the non-benzodiazepine;
- and
- (b) a matrix having enhanced self-binding characteristics;
- wherein said coated microparticles are dispersed within said matrix and said dosage form adapted to rapidly dissolve in the mouth of a patient.
1 more element
An oral fast-dispersing dosage form comprising:
- (a) microparticles comprising an effective amount of zolpidem, distilled monoglycerides and a macrogol fatty acid ester, wherein said zolpidem is present in an amount of about 4% by weight of the dosage form, said distilled monoglycerides is present in an amount of about 13.33% by weight of the dosage form and said macrogol fatty acid ester is present in an amount of about 9.33% by weight of the dosage form, said microparticles coated with at least one taste-masking coating and adapted for enhanced absorption of zolpidem into the blood stream of a human;
- and
- (b) a shearform matrix having enhanced self binding characteristics and consisting essentially of at least one saccharide carrier and at least two sugar alcohols, comprising sorbitol and about 0.5% to about 25% by weight of xylitol which matrix has been treated with at least one crystallization modifier, wherein said coated microparticles are dispersed within said shearform matrix and said dosage form is adapted to rapidly dissolve in the mouth of a patient, said dosage form when administered in the evening to a patient in need of such administration exhibits a blood absorption profile such that after about 0.25 hours at least about 10% of the zolpidem is absorbed, after about 0.5 hours at least about 25% of the zolpidem is absorbed;
- after about 0.75 hours at least about 35% of the zolpidem is absorbed;
- after about 1 hour at least about 40% of the zolpidem is absorbed, after about 1.5 hours at least about 50% of the zolpidem is absorbed, after about 1.75 hours at least 55% of the zolpidem is absorbed, after about 2 hours at least about 60% of the zolpidem is absorbed, after about 4 hours at least about 75% of the zolpidem is absorbed, and after about 6 hours more than about 90% of the zolpidem is absorbed, into the blood stream of the patient in the fed state.
2 more elements
An oral fast-dispersing dosage form comprising:
- (a) microparticles comprising an effective amount of zolpidem, distilled monoglycerides and a macrogol fatty acid ester, wherein said zolpidem is present in an amount of about 4% by weight of the dosage form, said distilled monoglycerides is present in an amount of about 13.33% by weight of the dosage form and said macrogol fatty acid ester is present in an amount of about 9.33% by weight of the dosage form, said microparticles coated with at least one taste-masking coating and adapted for enhanced absorption of zolpidem into the blood stream of a human;
- and
- (b) a shearform matrix having enhanced self binding characteristics and consisting essentially of at least one saccharide carrier and at least two sugar alcohols, comprising sorbitol and about 0.5% to about 25% by weight of xylitol which matrix has been treated with at least one crystallization modifier, wherein said coated microparticles are dispersed within said shearform matrix and said dosage form is adapted to rapidly dissolve in the mouth of a patient, said dosage form when administered in the evening to a patient in need of such administration exhibits a blood absorption profile such after about 0.25 hours at least about 5% of the zolpidem is absorbed, after about 0.5 hours at least about 55% of the zolpidem is absorbed, after about 0.75 hours at least about 75% of the zolpidem is absorbed, after about 1 hour at least about 80% of the zolpidem is absorbed, after about 1.5 hours at least about 85% of the zolpidem is absorbed, after about 2 hours at least about 90% of the zolpidem is absorbed, and after about 4 hours at least about 97% of the zolpidem is absorbed, into the blood stream of the patient in the fasted state.
An oral fast-dispersing dosage form comprising:
- (a) microparticles comprising an effective amount of zolpidem, distilled monoglycerides and a macrogol fatty acid ester, wherein said zolpidem is present in an amount of about 4% by weight of the dosage form, said distilled monoglycerides is present in an amount of about 13.33% by weight of the dosage form and said macrogol fatty acid ester is present in an amount of about 9.33% by weight of the dosage form, said microparticles coated with at least one taste-masking coating and adapted for enhanced absorption of zolpidem into the blood stream of a human;
- and
- (b) a shearform matrix having enhanced self binding characteristics and consisting essentially of at least one saccharide carrier and at least two sugar alcohols, comprising sorbitol and about 0.5% to about 25% by weight of xylitol which matrix has been treated with at least one crystallization modifier, wherein said coated microparticles are dispersed within said shearform matrix and said dosage form is adapted to rapidly dissolve in the mouth of a patient, said dosage form when administered in the evening to a patient in need of such administration provides a Tmax from about 0.5 hours to about 6 hours, a Cmax of about 42 ng/ml to about 141 ng/ml zolpidem and an AUC(0-t) of about 216 ng.hr/ml to about 1352 ng.hr/ml in the blood after administration of the dosage form to the patient in the fed state.
An oral fast-dispersing dosage form comprising:
- (a) microparticles comprising an effective amount of zolpidem, distilled monoglycerides and a macrogol fatty acid ester, wherein said zolpidem is present in an amount of about 4% by weight of the dosage form, said distilled monoglycerides is present in an amount of about 13.33% by weight of the dosage form and said macrogol fatty acid ester is present in an amount of about 9.33% by weight of the dosage form, said microparticles coated with at least one taste-masking coating and adapted for enhanced absorption of zolpidem into the blood stream of a human;
- and
- (b) a shearform matrix having enhanced self binding characteristics and consisting essentially of at least one saccharide carrier and at least two sugar alcohols, comprising sorbitol and about 0.5% to about 25% by weight of xylitol which matrix has been treated with at least one crystallization modifier, wherein said coated microparticles are dispersed within said shearform matrix and said dosage form is adapted to rapidly dissolve in the mouth of a patient, said dosage form when administered in the evening to a patient in need of such administration provides a Tmax from about 0.5 hours to about 4 hours, a Cmax of about 48 ng/ml to about 189 ng/ml zolpidem and an AUC(0-t) of about 167 ng.hr/ml to about 1764 ng.hr/ml in the blood after administration of the dosage form to the patient in the fasted state.
An oral fast-dispersing dosage form comprising:
- (a) microparticles comprising an effective amount of zolpidem, distilled monoglycerides and a macrogol fatty acid ester, wherein said zolpidem is present in an amount of about 4% by weight of the dosage form, said distilled monoglycerides is present in an amount of about 13.33% by weight of the dosage form and said macrogol fatty acid ester is present in an amount of about 9.33% by weight of the dosage form, said microparticles coated with at least one taste-masking coating and adapted for enhanced absorption of zolpidem into the blood stream of a human;
- and
- (b) a shearform matrix having enhanced self binding characteristics and consisting essentially of at least one saccharide carrier and at least two sugar alcohols, comprising sorbitol and about 0.5% to about 25% by weight of xylitol which matrix has been treated with at least one crystallization modifier, wherein said coated microparticles are dispersed within said shearform matrix and said dosage form is adapted to rapidly dissolve in the mouth of a patient, said dosage form when administered in the evening to a patient in need of such administration provides a mean Tmax from about 2.8 hours, a mean Cmax of about 82.4 ng/ml zolpidem and a mean AUC(0-t) of about 633 ng.hr/ml in the blood after administration of the dosage form to the patient in the fed state.
An oral fast-dispersing dosage form comprising:
- (a) microparticles comprising an effective amount of zolpidem, distilled monoglycerides and a macrogol fatty acid ester, wherein said zolpidem is present in an amount of about 4% by weight of the dosage form, said distilled monoglycerides is present in an amount of about 13.33% by weight of the dosage form and said macrogol fatty acid ester is present in an amount of about 9.33% by weight of the dosage form, said microparticles coated with at least one taste-masking coating and adapted for enhanced absorption of zolpidem into the blood stream of a human;
- and
- (b) a shearform matrix having enhanced self binding characteristics and consisting essentially of at least one saccharide carrier and at least two sugar alcohols, comprising sorbitol and about 0.5% to about 25% by weight of xylitol which matrix has been treated with at least one crystallization modifier, wherein said coated microparticles are dispersed within said shearform matrix and said dosage form is adapted to rapidly dissolve in the mouth of a patient, said dosage form when administered in the evening to a patient in need of such administration provides a mean Tmax from about 1.6 hours, a mean Cmax of about112.7 ng/ml to about 189 ng/ml zolpidem and a mean AUC(0-t) of about 688 ng.hr/ml in the blood after administration of the dosage form to the patient in the fasted state.
Dependencies are inferred from the claim text.