Transdermal therapeutic systems with crystallization-inhibiting protective film (release liner)
Patents Granted (Contd.) {51} International Classification: Α61Κ 3/71) (2006.Μ) {54} Title Tonsdermal therapeutic systems with cr)Steift?.a4i»rHhhifc>il,rtg protective Rim (release liner) {57} Abstract The invention relates to pharmaceutical ΐοΐτηυℓ3ℓΐοη3,ΐη particular to trsnsdenrrsl therapeutic systems, which are., characterized m that no active ingredient crystallites out at the interface between removable protective film frelease liner) and artiva-ingtedtent coritainirtg matrix (56) Documents Cited : WO 2005 058287 Α2 WO 2∞4 85824? Α1 IP 154113? Α2 WO 201004215!. A? WO $960908 Α1 B>0285553 Ai FORM 25 (Χ2) PATENT {19} ΑΡ (U) Patent No ; ΑΡ 3586 {73} Applicants} 8ΑΥ6Α XNTEUSCTUAi. PROPERTY GMBH, Alfred-NebshStrasss 10, 40783 (21) Application No AP/P/20 0/00678? Honheifn, Germany (22} Filing Dote ; 02,09.20Π (24) {45} Date of Grant & Publit.af.iori ; 10/02/2016 {30} Priority Data {72) Inventors (33) Country <3i) Kamfrer (32) Date LANSSUYH Ttienias, Germany 06 102OKSO40mO 06,03,2010 T£ft£B6Si ftJBw, Gtsnwny BRACHT Stefan, Germany (84) Designated States: (74) Representative ΚΕ FBHSt COfiMACK The invention relates to pharmaceutical formulations, in particular to transdermal therapeutic systems, which are characterized in that little or no active ingredient crystallizes out at the interface between the removable protective film (release liner) and the active-ingredient-containing matrix. 1. Solid transdermal therapeutic system with at least one active-ingredient containing matrix layer which comprises a polymer matrix supersaturated with gestodene or a gestodene ester, and optionally comprising ethinylestradiol, and a removable protective film directly adjacent to the matrix,
wherein the fraction of gestodene or gestodene ester in the form of amorphous or crystalline particles at the interface between the removable protective film and the active-ingredient-containing matrix or in the active-ingredient-containing matrix is on less than 2% of the area of the system, and wherein the matrix is free from solubility promoters, crystallization inhibitors and dispersants. 2. Solid transdermal therapeutic system of 3. Solid transdermal therapeutic system with at least one active-ingredient containing matrix layer which comprises a polymer matrix supersaturated with gestodene or a gestodene ester, and optionally comprising ethinylestradiol, and a removable protective film directly adjacent to the matrix,
wherein the active-ingredient-containing matrix is protected by a siliconized or fluorine-coated polyester removable film (release liner). 4. Solid transdermal therapeutic system with at least one active-ingredient containing matrix layer which comprises a matrix polymer supersaturated with gestodene or a gestodene ester, optionally comprising ethinylestradiol, and a removable protective film directly adjacent to the active-ingredient-containing matrix,
wherein FL 2000 75 μm PET 1s (78CC), FL 2000 75 μm PET 1s (RT149), FL 2000 75 μm PET 1s (RT404), Perlasic LF75, Scotchpak 9744, Scotchpak 9741, Silphan S50 M030, Akrosil Release Liner, 490si Release Liner, Primeliner FL PET 2000 Type 78JR, Primeliner FL PET Type 78 GY or Silex PET liner μ siliconized is used as protective film. 5. Solid transdermal therapeutic system according to 6. Solid transdermal therapeutic system according to the fraction of gestodene or gestodene ester in the form of amorphous or crystalline particles at the interface between the removable protective film and the active-ingredient-containing matrix or in the active-ingredient-containing matrix is on less than 1% of the area of the system. 7. Solid transdermal therapeutic system of 8. Solid transdermal therapeutic system according to 9. Solid transdermal therapeutic system according to 10. Solid transdermal therapeutic system according to 11. Solid transdermal therapeutic system according to 12. Solid transdermal therapeutic system according to 13. Solid transdermal therapeutic system (TTS) according to 14. Solid transdermal therapeutic system according to 15. Kit comprising 1 to 52, 1 to 26, or 1 to 13 patches as defined in