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Transdermal hormone delivery system: compositions and methods

Inactive Publication Date: 2007-03-22
AGILE THERAPEUTICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0027] Other features and advantages of the invention will be understood by reference to the detailed description and examples that follow.

Problems solved by technology

Though the combination of synthetic progestin and estrogen effectively suppresses ovulation, certain undesirable side effects are associated with this type of oral contraceptive.
Further, the risk increases sharply in women over 35 years of age.
Contraceptive use has also been associated with increased evidence of benign liver tumors and an increased risk of gallbladder disease.
Additionally, fetal abnormalities may result if a woman continues to take the pill after becoming pregnant.
The above described transdermal delivery systems are deficient in their ability to deliver sufficient quantities of progestin, particularly levonorgestrel, either alone or in proper balance with a selected estrogen, for one or more of a variety of reasons.
The dosage unit described in U.S. Pat. No. 5,762,956 is purportedly smaller, but the amount of progestin delivered is not robust.

Method used

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  • Transdermal hormone delivery system: compositions and methods

Examples

Experimental program
Comparison scheme
Effect test

example 1

Fabrication of THDS Dosage Units for Use in Contraception

[0082]

Materials:mgwt %Humectant PVP / VA-S630:9.661.25Skin permeation enhancers:DMSO73.779.51Lauryl lactate (Ceraphyl ® 31)24.593.10Ethyl lactate24.593.10Capric Acid18.542.39Adhesive polymer: Duro Tak 87-4098617.5979.65Hormones:Levonorgestrel4.480.58Ethinyl estradiol2.200.28Backing layer - Scotchpak ® 973216 sheets—(3M Company)Release liner - Scotchpak ® 102216 sheets—(3M Company)TOTAL775.41 mg100.00%

[0083] Process:

[0084] Hormones were dissolved and dispersed in a solution comprising PVP / vinyl acetate and the combination of skin permeation enhancers. Duro-Tak 87-4098 (33% solid content) adhesive polymer solution was added, and the container was sealed. The solution was stirred using a magnetic stirring bar at approximately 200 rpm at room temperature for 3 hours, to form a homogeneous solution. The stirred solution was deaerated by allowing it to stand without stirring for one hour or until all air bubbles had disappeared. The...

example 2

Quantitative Analysis of Dried Adhesive Polymer Matrix

[0085] The THDS dosage units fabricated as described in Example 1 were subjected to quantitative analysis to determine the post-fabrication amounts of each component. Amounts of levonorgestrel (LNG) and ethinyl estradiol (EE) were measured as follows. A dosage unit was taken from its foil pouch and the release liner was removed. The dosage unit was folded together on the adhesive side and placed into an extraction container, to which 100 ml of methanol was added. The container was shaken vigorously by hand, then placed on an orbital shaker for at least 12 hours, until all adhesive on the dosage units was dissolved. Twenty-one ml of the extracted solution was placed into a centrifuge tube, and 9 ml of HPLC-grade water was added, to yield an aqueous methanol solution composed of 70% methanol. The sample was centrifuged and the supernatant filtered through a 0.45 μm (nylon or Teflon) filter paper into an HPLC vial. The filtrate was...

example 3

Effects of Process Parameters on Final Composition of Skin Permeation Enhancers in the Adhesive Polymer Matrix

[0089] The effect of THDS fabrication parameters on the final composition of skin permeation enhancers in the adhesive polymer matrix was tested. Four process parameters were varied: drying temperature, drying time, initial coating thickness and the weight percent of total enhancers in the initial formulation. Results are shown in the table below. Each value represents an average of four patches. Values are given in mg / g of adhesive polymer matrix.

TABLE 1Enhancer Composition in Patches Subjected to Varying Process ParametersDryingDryingCoatingInitialTemp.TimeThicknessEnhancerEthylLaurylGrp#(° C.)(min)(mm)(Wt %)LactateDMSOCapric AcidLactate1401560020.7735.28 ± 1.17224.84 ± 6.54 76.24 ± 1.12 99.78 ± 6.482501560020.7725.10 ± 0.74158.04 ± 6.33 84.27 ± 2.56115.57 ± 3.843601560020.7717.74 ± 0.92111.12 ± 3.19 90.07 ± 1.52124.79 ± 1.604701560020.7711.31 ± 0.7853.32 ± 4.4791.88 ± ...

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Abstract

A transdermal hormone delivery system (THDS) is disclosed. The THDS is useful for control of fertility and as therapy for a variety of diseases and conditions treatable by robust delivery of progestin and estrogen hormones, particularly the progestin, levonorgestrel. The THDS comprises a backing layer, an adjoining adhesive polymer matrix comprising an effective amount of at least a progestin hormone, delivery of which is enhanced by one or more skin permeation enhancing agents present in pre-determined amounts. The THDS is capable of providing effective daily doses of progestin and estrogen hormones from a small surface area in contact with the skin, e.g., less than 20 square centimeters. Methods of fertility control and various types of hormone replacement therapy utilizing the THDS are also disclosed.

Description

COMPOSITIONS AND METHODS [0001] This application is a continuation-in-part of U.S. application Ser. No. 10 / 130,913, filed May 23, 2002, which is a U.S. National Application of International Application No. PCT / US00 / 32043, filed Nov. 22, 2000, which claims benefit of U.S. Provisional Application 60 / 167,535, filed Nov. 24, 1999, the entire contents of each of which are incorporated by reference herein.FIELD OF THE INVENTION [0002] The present invention relates to hormone treatment for control of fertility and as therapy for a variety of diseases and conditions. Specifically, the invention provides formulations and methods of use in connection with a transdermal hormone delivery system for robust delivery of steroid hormones. BACKGROUND OF THE INVENTION [0003] Various scientific articles and patent publications are referenced herein to describe the state of the art to which this invention pertains. Each of these publications is incorporated by reference herein in its entirety. [0004] H...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/22A61F13/00A61K9/00A61K31/565A61K31/57A61K47/12A61K47/14A61K47/20
CPCA61K9/0014A61K9/7061A61K31/565A61K31/57A61K47/12A61K9/7038A61K47/20A61K47/14A61K2300/00A61P15/00A61P15/08A61P15/10A61P15/12A61P15/14A61P15/18A61P17/10A61P43/00A61P5/24A61P5/26A61P5/30A61P5/34A61K9/70A61K31/56
Inventor CHIEN, TE-YEN
Owner AGILE THERAPEUTICS
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