TRANSDERMAL THERAPEUTIC SYSTEMS

• US 20010009673A1
• Filed: 02/11/1999
• Published: 07/26/2001
• Est. Priority Date: 07/11/1996
• Status: Abandoned Application

• Current Assignee: Schering Ag (Merck & Co., Inc.)
• Original Assignee: Schering Ag (Merck & Co., Inc.)
• Inventors: LIPP, RALPH, GUNTHER, CLEMENS
• Application Number:
  US09/214,601
• Publication Number:
  US 20010009673A1
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/569 substituted in position 17 alpha, e.g. ethisterone
• CPC Class Codes: A61K 31/575 substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61K 9/7061 Polyacrylates

Abstract

Transderml therapeutic systems are disclosed for the controlled administration of second and third generation gestagenes, and possibly of oestrogens, at least partially dissolved in a matrix. The disclosed systems are characterised in that their matrix contains a copolymer of one or several esters or amides which contain vinyl groups and have the general formula (I), as well as an N-vinyl lactam of general formula (II). In the general formula (I), X symbolises a -COO- group, a -CONH- group or an -OCO- group; R₁ stands for a hydrogen atom or an alkyl group with maximum 4 carbon atoms; and R₂ stands for a hydrogen atom or an alkyl group with maximum 12 carbon atoms. In the general formula (II), n is a digit from 3 to 5.

Claims

1. Transdermal therapeutic systems for the controlled release of gestagens of the second and third generations, which are at least partially dissolved in a matrix and are optionally of estrogens, characterized in that their matrix is a copolymer of one or more vinyl group-containing esters or amides of general formula (I),

in which

X symbolizes a —

COO group, a —

CONH group or an —

OCO group,

R₁ means a hydrogen atom or an alkyl group with a maximum of 4 carbon atoms, and

R₂ represents a hydrogen atom, or an alkyl group with a maximum of 12 carbon atoms, and an N-vinyllactam of general formula II,

in which

n means a number from 3 to 5, whereby the steroidal active ingredients that are dissolved in the matrix essentially do not crystallize out over a prolonged period.

2. Transdermal therapeutic system according to

claim 1

, whose matrix is a copolymer, which per mol of N-vinyllactone of general formula II contains 0.5 to 2.5 mol of one or more vinyl group-containing esters or amides of general formula I.

3. Transdermal therapeutic system according to

claim 1

, whose matrix is a copolymer, which per mol of N-vinyllactone of general formula II contains 0.75 to 1.5 mol of one or more vinyl group-containing esters or amides of general formula I.