Transdermal therapeutic systems with crystallization-inhibiting protective film (release liner)

30-04-2013 дата публикации
Номер:
AP0201306787A0
Принадлежит:
Контакты:
Номер заявки: 78-06-20137
Дата заявки: 02-09-2011

[1]

Patents Granted (Contd.)

[2]

{51} International Classification: Α61Κ 3/71) (2006.Μ)

[3]

{54} Title

[4]

Tonsdermal therapeutic systems with cr)Steift?.a4i»rHhhifc>il,rtg protective Rim

[5]

(release liner)

[6]

{57} Abstract

[7]

The invention relates to pharmaceutical ΐοΐτηυℓ3ℓΐοη3,ΐη particular to trsnsdenrrsl therapeutic systems, which are., characterized m that no active ingredient

[8]

crystallites out at the interface between removable protective film frelease liner)

[9]

and artiva-ingtedtent coritainirtg matrix

[10]

(56) Documents Cited : WO 2005 058287 Α2

[11]

WO 2∞4 85824? Α1

[12]

IP 154113? Α2

[13]

WO 201004215!. A?

[14]

WO $960908 Α1

[15]

B>0285553 Ai

[16]

FORM 25 (Χ2) PATENT {19} ΑΡ

[17]

(U) Patent No ; ΑΡ 3586 {73} Applicants}

[18]

8ΑΥ6Α XNTEUSCTUAi. PROPERTY GMBH, Alfred-NebshStrasss 10, 40783

[19]

(21) Application No AP/P/20 0/00678? Honheifn, Germany

[20]

(22} Filing Dote ; 02,09.20Π

[21]

(24) {45} Date of Grant & Publit.af.iori ; 10/02/2016

[22]

{30} Priority Data {72) Inventors

[23]

(33) Country <3i) Kamfrer (32) Date LANSSUYH Ttienias, Germany

[24]

06 102OKSO40mO 06,03,2010 T£ft£B6Si ftJBw, Gtsnwny

[25]

BRACHT Stefan, Germany

[26]

(84) Designated States: (74) Representative

[27]

ΚΕ FBHSt COfiMACK & BOTHA, Msfcw



[28]

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 claim 1 , wherein the limited amount of amorphous or crystalline particles which are present have an average diameter of not more than 200 μm.

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 claim 4 , wherein the release liner is selected from the group Perlasic LF75, Loparex 78CC, Scotchpack 9741, Primeliner FL PET 2000 Type 78JR, Primeliner FL PET Type 78 GY and Silex PET liner μ siliconized.

6. Solid transdermal therapeutic system according to claim 1 , 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 1% of the area of the system.

7. Solid transdermal therapeutic system of claim 6 , wherein the limited amount of amorphous or crystalline particles which are present have an average diameter of not more than 100 μm.

8. Solid transdermal therapeutic system according to claim 1 , wherein the system comprises, in order: a backing layer, an adhesive layer, a separation layer, the at least one active-ingredient-containing matrix layer and the removable protective film.

9. Solid transdermal therapeutic system according to claim 8 , wherein the adhesive layer comprises a UV absorber.

10. Solid transdermal therapeutic system according to claim 9 , wherein the UV absorber is Tinosorb S.

11. Solid transdermal therapeutic system according to claim 1 , wherein the system has gestodene present in an amount of 2.1 mg and ethinylestradiol present in an amount of 0.55 mg.

12. Solid transdermal therapeutic system according to claim 11 which has an area of 11 cm2.

13. Solid transdermal therapeutic system (TTS) according to claim 1 , wherein the TTS is in the form of a patch.

14. Solid transdermal therapeutic system according to claim 13 which is suitable for continuous application the skin of a patient over a period of 7 days.

15. Kit comprising 1 to 52, 1 to 26, or 1 to 13 patches as defined in claim 13 for continuous application over a period of 52, 26 or 13 weeks, respectively, in each case plus 7 days without patch.



IPC - классификация

AA6A61A61KA61K9A61K9/A61K9/7A61K9/70