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Details for Patent: 5,302,395

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Details for Patent: 5,302,395

Title: Method and systems for administering nitroglycerin transdermally at enhanced transdermal fluxes
Abstract:Transdermal delivery systems for delivery of nitroglycerin are disclosed which deliver the drug at enhanced transdermal fluxes. The systems include, in addition to nitroglycerin, a permeation enhancer which is either a sorbitan ester, a C.sub.8 -C.sub.22 aliphatic alcohol, or a mixture thereof. Methods for administering nitroglycerin using such permeation enhancers are also disclosed.
Inventor(s): Ebert; Charles D. (Salt Lake City, UT), Patel; Dinesh (Murray, UT), Heiber; Sonia (Salt Lake City, UT)
Assignee: TheraTech, Inc. (Salt Lake City, UT)
Filing Date:Jul 24, 1992
Application Number:07/919,296
Claims:1. A laminated composite for administering nitroglycerin transdermally through a predetermined area of skin over a sustained time period, comprising:

(a) a backing layer that is substantially impermeable to nitroglycerin,

(b) a reservoir layer comprising an adhesive polymer the basal surface of the reservoir layer being adapted to be adhered to the skin, and

(c) contained in the reservoir layer,

(i) nitroglycerin, and

(ii) a permeation enhancer consisting essentially of

a sorbitan ester having the structural formula ##STR3## wherein R.sub.1 has the structure --O(CO)R', where R' is selected from the group consisting of saturated, mono-unsaturated, di-unsaturated, or tri-unsaturated aliphatic hydrocarbon substituents of 7 to 21 carbon atoms optionally containing 1 to 3 hydroxyl groups, and R.sub.2 and R.sub.3 are selected from the group consisting of hydroxyl and --O(CO)R'; and

an alcohol R--OH, wherein R is a saturated or mono-unsaturated aliphatic hydrocarbon substituent of 8 to 22 carbon atoms and may be either unsubstituted or substituted with one to three additional hydroxyl groups,

wherein the nitroglycerin and the permeation enhancer are present in the reservoir in an amount sufficient to enable transdermal administration of the nitroglycerin at a flux of at least about 50% higher than that obtained in the absence of said enhancer.

2. The laminated composite of claim 1 wherein the sustained time period is about 12 to about 24 hours.

3. The laminated composite of claim 1 wherein the predetermined area of skin is less than about 25 cm.sup.2.

4. The laminated composite of claim 1 wherein the predetermined area of skin is less than about 10 cm.sup.2.

5. The laminated composite of claim 1 wherein the reservoir comprises a crosslinked acrylic adhesive.

6. The laminated composite of claim 1 wherein R.sub.2 and R.sub.3 are both hydroxyl.

7. The laminated composite of claim 6 wherein the enhancer is sorbitan monooleate or sorbitan monolaurate.

8. The laminated composite of claim 7 wherein the enhancer is sorbitan monooleate.

9. The laminated composite of claim 1 wherein the enhancer is oleyl alcohol.

10. The laminated composite of claim 1 wherein the enhancer is lauryl alcohol.

11. The laminated composite of claim 1 wherein the reservoir is about 2-4 mils in thickness.

12. The laminated composite of claim 1, further comprising a strippable protective release liner laminated to the basal surface of the reservoir.

13. The laminated composite of claim 12, wherein said release liner comprises a first strippable protective sheet partially overlapping a second strippable protective sheet, and wherein the area of overlap gives rise to an extending tab which enables ready removal of the first strippable sheet from the reservoir layer.

14. A laminated composite for the transdermal administration of nitroglycerin through a predetermined area of skin over a sustained time period, comprising;

(a) a backing layer that is substantially impermeable to nitroglycerin, and

(b) a reservoir layer, the basal surface of which is adapted to be adhered to the skin, comprising:

(i) approximately 35 wt. % to 67.5 wt. % adhesive;

(ii) approximately 30 wt. % to 45 wt. % nitroglycerin; and

(iii) approximately 2.5 wt. % to 20 wt. % permeation enhancer consisting essentially of

a sorbitan ester having the structural formula ##STR4## wherein R.sub.1 has the structure --O(CO)R', where R' is selected from the group consisting of saturated, mono-unsaturated, di-unsaturated, or ti-unsaturated aliphatic hydrocarbon substituents of 7 to 21 carbon atoms optionally containing 1 to 3 hydroxyl groups, and R.sub.2 and R.sub.3 are selected from the group consisting of hydroxyl and --O(CO)R'; and

an alcohol R--OH, wherein R is a saturated or mono-unsaturated aliphatic hydrocarbon substituent of 8 to 22 carbon atoms and may be either unsubstituted or substituted with one to three additional hydroxyl groups.
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