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|Title:||Transdermal therapeutic systems having improved stability and their production|
|Abstract:||This invention provides for, inter alia, a transdermal therapeutic system comprising at least one therapeutically active substance, which is oxidizable by hydroperoxides, wherein the amount of oxidative degradation of said active substances(s) and the corresponding formation of oxidative degradation products is reduced, which comprises one or more constituents of said transdermal therapeutic system being in contact with said active substance(s), wherein the sum of the peroxide number(s) (PON) of each of said constituents related to their percentage of the whole amount of said constituents as expressed by the formula ##EQU1## where N is the percentage content of the whole amount of said constituents in the TTS, n is the number of said constituents in the TTS, i is the running number PON is the peroxide number of each of the constituents, is not greater than 20.|
|Inventor(s):||Muller; Walter (Neuwied, DE)|
|Assignee:||LTS Lohmann Therapie-Systeme AG (Andernach, DE)|
1. A transdermal therapeutic system ("TTS") comprising, as constituents, a) at least one therapeutically active substance, which contains at least one secondary or tertiary
amino group, one double bond, one C--H bond in allyl position, one C--H bond in benzyl position, one tertiary C--H bond or one sulfide group which are oxidizable by hydroperoxides; and b) a single-layer or multilayer matrix system, wherein the matrix
system contains the active substance and comprises at least one member selected from the group consisting of hydrocarbon resins, polyvinylpyrrolidone and copolymers of vinylpyrrolidone with acrylic acids, acrylic acid derivatives, ethylene or vinyl
acetate, whereby, the sum of the peroxide number(s) (PON) of each of said constituents related to their percentage of the whole amount of said constituents, as expressed by the formula ##EQU3## where N is the percentage content of the whole amount of
said constituents in the TTS, n is the number of said constituents in the TTS, i is the running number PON is the peroxide number of each of the constituent(s), is not greater than 20 which is obtained by a process comprises: a) if the sum of the
peroxide number of the formulation constituents is greater than 20, treating the constituents with a reducing substance and continue with step c); b) if the sum of the peroxide number(s) is less than or equal to 20, continuing with step c); c)
preparing the transdermal therapeutic system by combining the therapeutic substance(s) with the formulation constituent(s).
2. The transdermal therapeutic system according to claim 1, wherein said sum of peroxide numbers is not greater than 10.
3. The transdernal therapeutic system according to claim 1, wherein said sum of peroxide numbers is not greater than 5.
4. The transdermal therapeutic system according to claim 1, wherein at least one of the constituents comprises one or more self-adhesive containing layers, which comprise the active substance(s) and tackifying resins based on rosin derivatives and/or polyterpenes.
5. The transdernal therapeutic system according to claim 1, wherein said constituents comprise permeation enhancers and/or crystallization inhibitors.
6. The transdermal therapeutic system according to claim 1, which is a reservoir system and wherein the oxidizable active substance is dissolved in a solvent or solvent mixture possessing at least one ether oxygen, tertiary carbon atom or C--H group in allyl position.
7. The transdermal therapeutic system according to claim 5, wherein the permeation enhancer(s) is selected from the group consisting of terpenes, terpene derivatives, unsaturated fatty acids and their derivatives, fatty alcohols and their derivatives, and diethylene glycol and its derivatives.
8. The transdermic therapeutic system according to claim 1, wherein the reducing substance is a sodium sulfite or sodium hydrogen sulfite in an aqueous lower-alkanoic solution.
9. The transdermic therapeutic system according to claim 5, wherein the aqueous lower-alkanoic solution is a methanolic or an ethanolic solution.
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