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Transdermal delivery of hormones without the need of penetration enhancers

A transdermal and estrogen technology, applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, drug combinations, etc. Irritated skin, etc.

Active Publication Date: 2010-05-26
LUYE PHARMA SWITZERLAND AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] Unfortunately, penetration enhancers can have adverse effects on the skin such as skin irritation, which to some extent makes transdermal systems unacceptable to users
Additionally, penetration enhancers are known to negatively impact the stability of active substances, leading to long-term storage issues
Also, it was recognized that the addition of penetration enhancers reduces the viscosity, leading to the risk of dark circles along the patch edges

Method used

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  • Transdermal delivery of hormones without the need of penetration enhancers
  • Transdermal delivery of hormones without the need of penetration enhancers
  • Transdermal delivery of hormones without the need of penetration enhancers

Examples

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Embodiment Construction

[0033] The present invention provides compositions for the transdermal delivery of hormones (transdermal therapeutic systems) which, when applied topically to the skin or mucous membranes, give the hormones A therapeutically effective amount such as a contraceptive effective amount.

[0034] The term "topical" or "locally" as used herein means that the composition comes into direct contact with surface areas of a mammal, including the skin and mucous membranes.

[0035] The term "mucosal membrane" refers to any surface membrane of a mammal that is not skin, such as those found in the oral cavity, vagina, rectum, nose or eyes. Thus, the mucosa may be oral, vaginal, rectal, nasal, or ocular.

[0036] The compositions of the present invention can be designed in a variety of different forms of administration, as long as the composition comprises a drug-containing layer suitable for placement close to or in direct contact with the skin or mucous membranes when the composition is a...

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PUM

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Abstract

The present invention relates to a patch comprising a drug-containing layer with low content of hormones, such as gestodene, and optionally an estrogen (e.g. ethinyl estradiol). Upon administering thepatch to a woman, plasma levels of at least 1.0 ng / ml of Gestodene is achieved at steady state conditions without the need of incorporating penetration enhancers or permeation enhancers in the drug-containing layer. Satisfactorily plasma levels of the hormones is also achieved throughout a period of at least 1 week, making the patch applicable for being used in female contraception with the concept of administering the patch ones weekly.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical compositions. The present invention provides a low-dose pharmaceutical composition for the transdermal delivery of at least one hormone, preferably a progestin such as gestodene and optionally estrogen, to achieve ovulation-inhibiting effective plasma concentrations in women. hormone. Background technique [0002] Transdermal delivery of estrogens and progestins for contraception is a known concept (Sitruk-Ware, Transdermal application of steroid hormones for contraception, J Steroid Biochem Molecul Biol, Volume 53, p 247-251). However, estrogens and progestins generally have difficulty penetrating the skin, so substances that enhance skin penetration are often added to transdermal systems. [0003] The following literature describes transdermal systems where a number of progestogens and estrogens are present in the adhesive layer and where the need for penetration enhancers is emphasized...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/32A61K31/565A61K9/70A61K47/44A61K47/38A61F13/00A61P15/18A61K31/56
CPCA61K9/7053A61K9/7061A61K31/565A61K31/56A61K9/7076A61K31/567A61K31/57A61P15/18A61K2300/00A61K9/70A61K47/32
Inventor 斯特凡·布拉赫特米夏埃尔·迪特根彼得拉·胡贝尔托马斯·朗古特迪尔克·申克
Owner LUYE PHARMA SWITZERLAND AG