Mixed solvent mutually enhanced transdermal therapeutic system
First Claim
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1. A transdermal drug delivery system comprising(i) an occlusive, impermeable polymeric backing layer;
- (ii) a drug depot on one side thereof;
(iii) a removable, occlusive covering layer over said drug depot; and
(iv) an adhesive means by which said delivery system, absent said removable covering layer may be affixed to an intended patient;
said drug depot containing a drug formulation comprising a transdermally administrable pharmaceutically acceptable pharmaceutically active agent or a precursor thereof, water and ethanol said active agent or precursor thereof being present in a pharmaceutically effective amount;
said ethanol and said water being present in a volume;
volume ratio of from 30;
70 up to less than 95;
5 such that said ethanol, water and drug are delivered to a patient'"'"'s skin, which patient has applied said system absent said removable covering layer to said patient'"'"'s skin, in amounts that said drug is delivered in a transdermally administrable efficacious amount, said water has an activity at said patients skin of about 0.4 to about 0.95 and said ethanol, at said patient'"'"'s skin, has an activity of 0.3 to about 0.9, and wherein, once applied to said patient'"'"'s skin, said ethanol has a flux from said system to said skin of at least 1500 mcg/cm2 /hr and through said skin of at least 1500 mcg/cm2 /hr.
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Abstract
The invention relates to the art of transdermal administration of drug substances, particularly those drug substances having a greater solubility in ethanol than in water and those drug substances having cationic or anionic substituent groups. It is especially useful for the administration of nitroglycerin.
136 Citations
11 Claims
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1. A transdermal drug delivery system comprising
(i) an occlusive, impermeable polymeric backing layer; -
(ii) a drug depot on one side thereof; (iii) a removable, occlusive covering layer over said drug depot; and (iv) an adhesive means by which said delivery system, absent said removable covering layer may be affixed to an intended patient;
said drug depot containing a drug formulation comprising a transdermally administrable pharmaceutically acceptable pharmaceutically active agent or a precursor thereof, water and ethanol said active agent or precursor thereof being present in a pharmaceutically effective amount;
said ethanol and said water being present in a volume;
volume ratio of from 30;
70 up to less than 95;
5 such that said ethanol, water and drug are delivered to a patient'"'"'s skin, which patient has applied said system absent said removable covering layer to said patient'"'"'s skin, in amounts that said drug is delivered in a transdermally administrable efficacious amount, said water has an activity at said patients skin of about 0.4 to about 0.95 and said ethanol, at said patient'"'"'s skin, has an activity of 0.3 to about 0.9, and wherein, once applied to said patient'"'"'s skin, said ethanol has a flux from said system to said skin of at least 1500 mcg/cm2 /hr and through said skin of at least 1500 mcg/cm2 /hr. - View Dependent Claims (2, 3, 4, 5, 6)
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7. A dosage form for transdermally administering a pharmaceutically active agent which dosage form comprises
a) an impermeable backing, b) a rate-controlling membrane of polyurethane or ethylene/vinylacetate of greater than 20% vinyl acetate and from 0.5 to 10.0 mils thick, c) a silicone-based or acrylic-based pressure-sensitive adhesive on said rate controlling membrane distal from said backing, d) a reservoir formed by a and b, e) an aqueous pharmaceutically acceptable lower alkanol reservoir composition having a volume fraction of said ethanol of from 0.35 to 0.9 calculated based on said ethanol alkanol and water only, and f) said pharmaceutically active agent.
Specification