Donepezil transdermal delivery system
AssigneeCorium, Inc.
InventorsEun Soo Lee, Amit K. Jain, Parminder Singh
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Abstract
A transdermal delivery system for systemic delivery of donepezil is described, where the system comprises an adhesive matrix drug reservoir layer comprised of a copolymer of acrylic acid/vinyl acetate, triethyl citrate, and donepezil base generated in situ by reaction of donepezil HCl and an alkaline salt. The system is provided for treatment of Alzheimer's disease, and achieves transdermal delivery of the therapeutic agent at steady state that is bioequivalent to administration of the therapeutic agent orally.
Claims14
A composition, comprising:
- a drug reservoir comprising (i) donepezil base generated in situ in the drug reservoir by reaction of donepezil HCl and a pharmaceutically acceptable alkaline salt selected from sodium bicarbonate and potassium bicarbonate, said donepezil HCl and said alkaline salt present in the drug reservoir in an equimolar or less than equimolar ratio of alkaline salt to donepezil HCl;
- (ii) glycerine;
- and (iii) an acrylate copolymer, wherein the donepezil base is generated for a period of between about 3-10 days in an amount that provides a therapeutically effective dose of donepezil base to a human for the period.
A composition, comprising:
- a drug reservoir consisting essentially of donepezil base generated in situ in the drug reservoir by reaction of a molar amount of donepezil HCl and an equimolar or less than equimolar amount of sodium bicarbonate;
- a solvent composition comprising one or more of triethyl citrate, lauryl lactate, sorbitan monolaurate, and glycerin;
- crosslinked polyvinylpyrrolidone and an acrylate copolymer, wherein donepezil base is generated for a period of between about 3-10 days in an amount that provides a therapeutically effective dose of donepezil base to a human for the period.
A composition, comprising:
- a drug reservoir consisting essentially of:
- (a) donepezil base generated in situ for a period of between about 3-10 days in the drug reservoir by reaction of between about 5-25 wt % donepezil HCl and between about 1-5 wt % sodium bicarbonate, said donepezil HCl and said sodium bicarbonate present in the drug reservoir in an equimolar or less than equimolar ratio of sodium bicarbonate to donepezil HCl;
- (b) about 0-15 wt % triethyl citrate;
- (c) about 0-5 wt % sorbitan monolaurate
- (d) about 5-15 wt % glycerin;
- (e) about 1-10 wt % lauryl lactate;
- (f) about 5-25 wt % crosslinked polyvinylpyrrolidone;
- and
- (g) about 30-65 wt % acrylate-vinylacetate copolymer.
A composition, comprising:
- a drug reservoir consisting essentially of:
- (a) donepezil base generated in situ for a period of between about 3-10 days in the drug reservoir by reaction of between about 10-18 wt % donepezil HCl and an equimolar or less than equimolar amount of sodium bicarbonate, wherein the weight percent of sodium bicarbonate in the drug reservoir is between about 1-5 wt %;
- (b) about 8-12 wt % triethyl citrate;
- (c) about 1.5-2.5 wt % sorbitan monolaurate
- (d) about 9-11 wt % glycerin;
- (e) about 1-10 wt % lauryl lactate;
- (f) about 13-17 wt % crosslinked polyvinylpyrrolidone;
- and
- (g) about 40-42 wt % acrylate-vinylacetate copolymer.
Dependencies are inferred from the claim text.